KR101950662B1 - Oral composition - Google Patents

Abstract

It is an object of the present invention to provide a sole component or a combination of two or more components capable of exhibiting a function as an oral composition, such as inhibiting dentin caries, inhibiting or improving dentin hypersensitivity, inhibiting or eliminating stain formation . The present invention relates to a composition containing (A) a compound having at least one lactam skeleton selected from the group consisting of a γ-lactam skeleton, a δ-lactam skeleton and an ε-lactam skeleton and having an acidic group and / To provide an oral composition.

Description

Oral composition {ORAL COMPOSITION}

The present invention relates to an oral composition.

The gums in the mouth are liable to retreat (retract) with periodontal disease or aging of the living body. When the gums retreat, the root of the tooth (齒 根 部), which has not been exposed until then, is exposed. At the root of the tooth, the dentin is present without being covered with enamel. Since dentin has a large number of organic layers mainly composed of collagen as well as having innumerable tubule structure, mineral dentin has a low mineral density of about 50% and physical and chemical properties compared with enamel having a mineral density of about 97% weak. Therefore, when the root portion is exposed in the oral cavity due to the retraction of the gums, caries (dentin dental caries) easily occurs. The dentin caries of the root of the tooth, which is exposed at the root of the tooth root, is called root surface caries.

As a manifestation mechanism of dental caries (hard muscle caries), first, plaque adheres to the surface of dentin exposed in the mouth, metabolism of sugar is caused by bacteria in the plaque, and acid (acid) It is produced. The mineral component of the dentin is eluted (demineralized) by the acid, and the organic (collagen) layer is exposed. Again, the collagen layer is physically and chemically destroyed, and the root of the tooth is virtually defect.

BACKGROUND ART [0002] As a method for preventing dental caries, there have been proposed several techniques for suppressing demineralization and promoting re-deposition (see Patent Documents 1 to 4).

Patent Document 1 discloses that hydrolytic silk and mineral composition dissolution of dentin are inhibited by using an oral composition having hard calcium carbonate as an ingredient having an average primary particle diameter in the range of 0.04 to 0.5 탆.

Patent Document 2 discloses a method for preparing a tooth-shaped toothpaste using a hemorrhagic rehabilitation accelerator having a monomer having a hydroxyl group (a) and a monomer having an acid group (phosphorus atom) in an amount of 5 to 200% by weight based on the component (b) And promoting remineralization.

Patent Document 3 discloses an oral composition comprising (A) a zinc compound and (B) an oral composition having at least one member selected from the group consisting of an aldehyde compound, a phenol compound and a tea extract polyphenol compound, Of dental caries, in particular hardened caries.

Patent Document 4 discloses that collagen degradation and demineralization are inhibited by using a proximal root preventive agent comprising flavanone and / or a glycoside thereof.

Furthermore, it has been pointed out that even when the collagen layer is exposed in the dentin caries (hardened caries), it becomes a footplate of re-crystallization, and calcium ions and phosphate ions in the saliva are consumed to deposit crystals in the exposed collagen layer . Therefore, it can be said that inhibition of degradation of the exposed collagen layer is essential for prevention of dental caries.

BACKGROUND ART As a conventional caries prevention technique, a fluoride sustained-release technique such as a combination technology with metal ions such as calcium (Patent Documents 5 to 7) centered on fluoride is disclosed. They may have a certain effect on enamel caries, but fluoride can not adequately protect the exposed collagen layer when dentin caries (root caries), so collagen breaks down.

On the other hand, as coating techniques, there have been disclosed tooth surface coating techniques (Patent Documents 8 and 9) using phosphate esters or polymers, and hemorrhoid protection techniques using aluminum, fluoride and calcium (Patent Document 10) However, the coating effect of the exposed collagen layer was insufficient.

The polyphenol can be coated on the exposed collagen layer. Polyphenol also has a function of lowering the collagenase enzyme activity, and as a result, it is known as a substance expected to have an effect of inhibiting degradation of the exposed collagen layer. For example, there have been proposed a method of improving the acid resistance of hemorrhoids containing tea polyphenol, fluoride and aluminum salts (patent document 11) and a combination of a dragon eye seed extract, fluoride and sugar alcohol (patent document 12) or Hesperidin (patent document 13) discloses a technique for imparting perspiration acid resistance. However, since polyphenol suffers from the disadvantage that discoloration and turbidity easily occur due to oxidation, pH change, formation of a complex, etc., it is difficult to maintain stability with a formulation such as a skimmed product, a detergent or the like. The polyphenol has other problems such as a decrease in effectiveness after preservation of the preparation and unnecessary coloring of the exposed collagen layer after application of the preparation. Therefore, development of an effective ingredient which can inhibit the decomposition of collagen exposed to the dentin after storage of the preparation, prevents coloring on the exposed collagen layer, and exhibits high formulation stability at the time of formulation is desired.

[Dentin hypersensitivity (sensory hypersensitivity)]

As described above, when the tooth root is exposed and the dentin is exposed, temperature, chemical, and mechanical external stimuli are given to the dentin, resulting in transient very uncomfortable pain known as dentin hypersensitivity.

The cause of dentin hypersensitivity is thought to be caused by nerve stimulation through the dentinal tubules.

Inhibition and improvement (damping) of dentin hypersensitivity by oral hygiene products such as a dentifrice product is a method of blocking ivory tubule with lactic acid aluminum and the like, the nerve being dulled by potassium nitrate, And a method for alleviation.

It has been known that aluminum lactate has an action of blocking the opening of dentinal tubules and improving dentin hypersensitivity (Patent Document 14). However, it takes time to obtain the effect of aluminum lactate, and there is a drawback that it lacks the immediate effect. And the expression of arine and metal tastes peculiar to aluminum lactate is also problematic.

On the other hand, potassium nitrate is widely employed as a nervous system component (Patent Document 15), and although it has an immediate effect, its effect is hard to be sustained. In other words, the effect of potassium nitrate is limited. Potassium nitrate has a bitter taste and may be uncomfortable to use.

[Removal of stain]

Colored staining of teeth is said to be stained or stained pellicle. Polyphenol (tannin, chlorogenic acid, etc.), metal ion, tobacco tar and the like derived from food are deposited and colored in the pellicle adsorbed on the tooth surface of saliva protein It is thought to be. Among these, stain that is most frequently observed is called brown stain and it is said that polyphenol compounds in food such as tannin and chlorogenic acid are involved.

BACKGROUND ART Conventionally, to remove stains adhered to a tooth surface, a technique by mechanical action of an abrasive compounded in an oral composition such as a dressing has been mainly used. On the other hand, a technique of removing stains by chemical action, such as a skirt composition containing pyrophosphate (Patent Document 16) and a composition for inhibiting stain formation (Patent Document 17) containing a sulfo-zapacic acid-based surfactant, (A) a lytic enzyme and / or (B) at least one enzyme selected from the group consisting of lipase, dextranase, glucosidase, 1,3-glucanase and mutanase (Japanese Patent Application Laid-Open No. H11-32532), a stain-removing oral care composition for removing stains (Patent Document 19).

On the other hand, a technique for suppressing the formation of stains in teeth has been proposed. (A) a polyphosphoric acid or a salt thereof, (B) a specific divalent saccharide, and (C) a liquid oral composition containing a polyphosphoric acid or a salt thereof and an acyltaurine salt and exhibiting a predetermined pH (Patent Document 20) It has been proposed that a liquid oral composition containing malic acid, tartaric acid and salts thereof (Patent Document 21) has an effect of preventing the teeth from being colored.

However, when the stain is removed by the mechanical action of the abrasive, there is a risk of tooth damage caused by excessive brushing, stain remaining at a portion where the bristles do not reach the bristles, and the like.

On the other hand, in the case of removal of the stain by a chemical action, there is a problem that the taste derived from the removed component is poor and the feeling of use is lowered. In the removal of stain by enzymatic action, there is a problem that when papain is used, papain is likely to act on the soft tissue in the oral cavity. Even when another enzyme is used, the components of the stain do not necessarily correspond to the decomposition substrate of the enzyme.

All of the above-mentioned stain formation inhibition techniques do not sufficiently overcome the problem of discomfort in the flavor and oral mucous membrane characteristic of the condensed phosphate due to the inclusion of polyphosphoric acid such as sodium tripolyphosphate.

In the above conventional techniques, there has been no technique which sufficiently exerts both the effect of inhibiting stain formation and the effect of removing stain, exhibiting a luster effect, and also exhibiting a feeling of product use.

As described above, suppression of dentin caries (root caries), suppression and improvement of dentin hypersensitivity, and inhibition and elimination of stain have been examined by various conventional methods. Thus, it is currently desired to provide a new means for enabling proper inhibition and improvement of dentin caries (hard muscle caries) and dentin hypersensitivity, and inhibition and removal of stain. Among them, dentin caries (root caries) and dentin hypersensitivity are still increasing with the aging of the population, so their suppression and improvement are urgent.

Background Art Conventionally, pyrrolidone carboxylic acid and / or its salt is known as a component of a gelatinous topical composition which is applied to the skin, scalp, hair, nails and / or mucous membranes for cosmetic treatment (Patent Document 22). However, its use as an ingredient in oral compositions is not known.

Patent Document 1: Japanese Patent Application Laid-Open No. 2007-176862 Patent Document 2: JP-A-2006-8596 Patent Document 3: Japanese Patent Application Laid-Open No. 11-228368 Patent Document 4: JP-A-2009-256341 Patent Document 5: Japanese Patent Laid-Open Publication No. 10-511104 Patent Document 6: Japanese Patent Application Laid-Open No. 11-106322 Patent Document 7: JP-A-2005-112841 Patent Document 8: Japanese Patent Application Laid-Open No. 5-320032 Patent Document 9: Japanese Patent Application Laid-Open No. 2005-200345 Patent Document 10: Japanese Patent Application Laid-Open No. 5-155746 Patent Document 11: Japanese Patent Application Laid-Open No. 6-298632 Patent Document 12: Japanese Patent Application Laid-Open No. 2011-168510 Patent Document 13: JP-A-2009-256341 Patent Document 14: JP-A-2010-222325 Patent Document 15: Japanese Patent Application Laid-Open No. 08-175943 Patent Document 16: Japanese Patent Application Laid-Open No. 10-182389 Patent Document 17: Japanese Patent Application Laid-Open No. 10-17443 Patent Document 18: JP-A-1-503142 Patent Document 19: Japanese Patent Application Laid-Open No. 2001-181163 Patent Document 20: JP-A-2009-051734 Patent Document 21: JP-A-2005-343794 Patent Document 22: Japanese Patent Application Laid-Open No. 9-202708

It is an object of the present invention to provide a composition for oral administration or a composition that exhibits various functions such as inhibition of dentin caries, inhibition or improvement of dentin hypersensitivity, inhibition or elimination of stain formation, and the like. Specifically, the following four examples are given for the purpose of the present invention.

It is a first object of the present invention to provide an oral composition having an effect of inhibiting dentin dental caries, inhibiting or improving dentin hypersensitivity, and inhibiting or eliminating stain.

A second object of the present invention is to provide an oral composition which remarkably inhibits the decomposition and coloring of the exposed collagen layer and exhibits a high formulation stability when formulated.

A third object of the present invention is to provide an oral composition having a good feeling (taste) as well as remarkably alleviating the pain caused by the hypersensitivity. For example, it is possible to block the opening of the dentinal tubules early (early blockade effect of the iv iv tubules), to alleviate pain felt by the patient (pain relief effect), and to prevent argin, metal, (Good taste (good taste)) which is free or almost free from the above-mentioned problems.

A fourth object of the present invention is to provide an oral composition useful for whitening teeth whiteness sufficiently both of a stain removing effect and a stain formation inhibiting effect, exhibiting a gloss effect, and also excellent in feeling of preparation.

A fifth object of the present invention is to provide an oral composition capable of inhibiting collagen pigmentation.

The present invention provides the following [1] to [24].

[1] Component (A): An oral composition comprising a lactam compound having a lactam skeleton of a γ-lactam skeleton, a δ-lactam skeleton, or an ε-lactam skeleton and having an acidic group.

[2] The oral composition according to [1], wherein the component (A) is a pyrrolidone carboxylic acid and / or a salt thereof

[3] The oral composition according to [1] or [2], wherein the content of the component (A) is 0.3 to 10% by mass.

[4] Component (1-B): The oral composition according to [1] or [2], further comprising a fluorine compound.

[5] The oral composition according to [4], wherein the component (B) is at least one selected from sodium fluoride and sodium monofluorophosphate.

[6] The oral composition according to [4] or [5], wherein the mass ratio of the component (A) to the amount of fluorine in the oral composition is 1 to 250.

[7] Component (1-C): In any one of [4] to [6], which further comprises a protein containing 1.0 to 6.0% by mass of a sulfur-containing amino acid residue ≪ / RTI >

[8] The oral composition according to [5], wherein the component (1-C) is casein.

[9] Component (2-B): The oral cavity according to [1] or [2], which further comprises at least one polyphenol compound selected from the group consisting of a seed seed extract, proanthocyanidin, catechin and hesperidin / RTI >

[10] Component (3-B): The oral composition according to [1] or [2], further comprising aluminum lactate.

[11] Component (3-C): The oral composition according to [10], further comprising a monofluorophosphate.

[12] Component (3-D): The oral composition according to [10] or [11], further comprising an inorganic water-soluble potassium salt.

[13] Component (4-B): The oral composition according to [1] or [2], further comprising an inorganic water-soluble potassium salt.

[14] Component (4-C): The oral composition according to [13], further comprising a water-soluble fluorine compound.

[15] Component (5-B): The oral composition according to [1] or [2], further comprising a cationic cellulose.

[16] The oral composition according to [15], wherein the component (5-B) is hydroxyethyl cellulose dimethyldiallylammonium chloride.

[17] Component (6-B): An oral composition according to the above [1] or [2], further comprising a polyphenol compound.

[18] Component (A): A collagen staining inhibitor comprising a lactam compound having a lactam skeleton of any one of γ-lactam skeleton, δ-lactam skeleton, and ε-lactam skeleton and having an acidic group as an active ingredient.

[19] Component (A): A collagen decomposition inhibitor having a lactam skeleton of any one of γ-lactam skeleton, δ-lactam skeleton, or ε-lactam skeleton and having an acidic group as an active ingredient.

[20] Component (A): A dental carotenoid blocking agent comprising as an active ingredient, a lactam compound having a lactam skeleton of any one of a γ-lactam skeleton, a δ-lactam skeleton, and an ε-lactam skeleton and having an acidic group.

[21] Component (A): a dentin hypersensitivity inhibitor or an agent for improving dentin hypersensitivity comprising a lactam skeleton having any one of γ-lactam skeleton, δ-lactam skeleton, or ε-lactam skeleton and having an acidic group as an active ingredient.

[22] Component (A): A stain remover comprising, as an active ingredient, a lactam compound having a lactam skeleton of a γ-lactam skeleton, a δ-lactam skeleton, or an ε-lactam skeleton and having an acidic group.

[23] The agent according to any one of [18] to [22], wherein the component (A) is a pyrrolidone carboxylic acid and / or a salt thereof.

[24] The oral composition according to any one of the above [1], [2] and [9] to [14], wherein the dentin is crustacean and the person is a hypersensitive person.

[Oral composition]

The inventors of the present invention have conducted intensive investigations in order to obtain an oral composition which is superior to the conventional oral composition in suppressing collagen decomposition, inhibiting collagen pigmentation, suppressing or improving dentin hypersensitivity, and removing stain. As a result, a lactam compound having either one lactam skeleton of? -Lactam skeleton,? -Lactam skeleton or? -Lactam skeleton and having an acidic group represented by pyrrolidone carboxylic acid and / It is possible to obtain an excellent effect on inhibition of collagen decomposition, inhibition of collagen coloration, inhibition or improvement of dentin hypersensitivity, and removal of stain.

The present invention provides the following oral compositions [0-1] to [0-4].

[0-1] Component (A): An oral composition comprising a lactam compound having a lactam skeleton of a? -Lactam skeleton, a? -Lactam skeleton, or an? -Lactam skeleton and having an acidic group.

[0-2] The oral composition according to [0-1], wherein the component (A) is a pyrrolidone carboxylic acid and / or a salt thereof.

[0-3] The oral composition according to [0-1] or [0-2], wherein the content of the component (A) is 0.3 to 10% by mass.

[0-4] The dental plaque and the individual, wherein the oral composition according to any one of [0-1] to [0-3] above.

[Oral composition (1)]

The inventors of the present invention have conducted intensive investigations to obtain an oral composition excellent in dentin dental caries prevention effect as compared with the conventional oral composition. In the study, it was confirmed that a lactam compound having either one lactam skeleton of? -Lactam skeleton,? -Lactam skeleton or? -Lactam skeleton and having an acidic group represented by pyrrolidone carboxylic acid and / And a fluorine compound were simultaneously used as a component to prepare an oral composition. This oral composition was used for a caries sample and its dental caries inhibition effect was evaluated by applying Transverse Microradiography (hereinafter abbreviated as TMR).

The TMR method is a method in which a profile of the amount of minerals in teeth is obtained by converting a luminance equivalent to an aluminum thickness to a profile of a tooth using a micro radio graph of a cross section of a thin flake and measuring a depth of cut and a loss of minerals This method is a method in which reliability is publicly recognized as a method of measuring the degree of caries.

As a result of evaluating the dentin dental caries inhibiting effect using the TMR method, it was found that "a lactam compound having a lactam skeleton of any of γ-lactam skeleton, δ-lactam skeleton and ε-lactam skeleton and having an acidic group" and " Fluoride compound "as a component at the same time, the dentin dental caries inhibiting effect above the conventional oral composition is exerted.

The present invention provides the following oral composition (1).

[1-1] Component (A): a lactam compound or a salt thereof having at least one lactam skeleton selected from the group consisting of a γ-lactam skeleton, a δ-lactam skeleton, and an ε-lactam skeleton, (1-B) Component: A composition for oral use characterized by containing a fluorine compound.

[1-2] The oral composition according to the above [1-1], wherein the component (A) is a pyrrolidone carboxylic acid and / or a salt thereof.

[1-3] The oral composition according to the above [1-1] or [1-2], wherein the component (1-B) is at least one selected from sodium fluoride and sodium monofluorophosphate.

[1-4] The oral composition according to any one of [1-1] to [1-3], wherein the mass ratio of the component (A) to the amount of fluorine in the oral composition is 1 to 250.

[1-5] Component (1-C): An oral composition according to any one of [1-1] to [1-4], further comprising a protein containing 1.0 to 6.0% of a sulfated amino acid residue.

[1-6] The oral composition according to the above [1-5], wherein the component (1-C) is casein.

[Oral composition (2)]

DISCLOSURE OF THE INVENTION The inventors of the present invention have conducted intensive studies to achieve the above object and as a result have found that the combination of a predetermined polyphenol compound and a predetermined lactam compound inhibits degradation of the exposed collagen layer Inhibitory effect), and that the effect thereof persisted after storage of the preparation (dentin collagen decomposition inhibitory effect after storage). The above-mentioned lactam compound inhibits the discoloration of the preparation itself after storage of the preparation by the polyphenol compound, has no problems in formulation (formulation stability), and inhibits the coloring by polyphenol in the dentin for a long time Dentin collagen pigmentation inhibitory effect). Thus, the present invention has been accomplished.

The present invention provides the following oral composition (2).

[2-1] Component (A): a compound having at least one lactam skeleton selected from the group consisting of a γ-lactam skeleton, a δ-lactam skeleton and an ε-lactam skeleton and having an acidic group, -B) Ingredient: An oral composition comprising at least one polyphenol compound selected from the group consisting of a seeded seed extract, proanthocyanidin, catechin, and hesperidin.

[2-2] The oral composition according to the above [2-1], wherein the component (A) is a pyrrolidone carboxylic acid and / or a salt thereof.

[Oral composition (3)]

The present invention provides the following oral composition (3).

[3-1] Component (A): a compound having at least one lactam skeleton selected from the group consisting of a γ-lactam skeleton, a δ-lactam skeleton and an ε-lactam skeleton and having an acidic group, -B) Component: An oral composition containing aluminum lactate.

[3-2] The oral composition according to [3-1], wherein the component (A) is a pyrrolidone carboxylic acid and / or a salt thereof.

[3-3] Component (3-C): An oral composition according to [3-1] or [3-2], further comprising a monofluorophosphate.

[3-4] Component (3-D): An oral composition according to any one of [3-1] to [3-3], further comprising an inorganic water-soluble potassium salt.

[3-5] The oral composition according to any one of the above-mentioned [3-1] to [3-4], wherein the dentin is a dentine gum.

[Oral composition (4)]

The present inventors have found that an oral composition containing a specific lactam compound or a salt thereof having an acidic group in combination with an inorganic water-soluble potassium salt significantly reduces the pain caused by the hypersensitivity and has a good feeling (taste) Respectively.

The present invention provides the following oral composition (4).

[4-1] Component (A): a lactam compound or a salt thereof having at least one lactam skeleton selected from the group consisting of a γ-lactam skeleton, a δ-lactam skeleton and an ε-lactam skeleton, 4-B) Component: An oral composition containing an inorganic water-soluble potassium salt.

[4-2] The composition according to [4-2], wherein the component (A) is at least one selected from the group consisting of pyrrolidone carboxylic acid, 6-oxo-2-piperidinecarboxylic acid, 3- (2-oxo- , Wherein the compound is at least one compound selected from the group consisting of:

[4-3] The composition for oral cavity according to [4-1] or [4-2], further comprising a (4-C) water-soluble fluorine compound.

[4-4] The oral composition according to any one of the above-mentioned [4-1] to [4-3], wherein the dentin cortex and the individual are enamored.

[Oral composition (5)]

The present invention provides the following oral composition (5).

[5-1] Component (A): a compound having at least one lactam skeleton selected from the group consisting of a γ-lactam skeleton, a δ-lactam skeleton and an ε-lactam skeleton, -B) Ingredient: Oral composition containing catechinized cellulose.

[5-2] The oral composition according to the above [5-1], wherein the component (A) is a pyrrolidone carboxylic acid and / or a salt thereof.

The oral composition according to the above [5-1] or [5-2], wherein the component [5 - 3] (5-B) is hydroxyethyl cellulose dimethyldiallylammonium chloride.

[Oral composition (6)]

The present invention provides the following oral composition (6).

[6-1] Component (A): a lactam compound having one lactam skeleton of a? -Lactam skeleton, a? -Lactam skeleton, or an? -Lactam skeleton and having an acidic group; and (6-B) A composition for oral use containing a phenolic compound.

[Agent]

The present invention provides the following various agents.

[7-1] Component (A): A collagen coloring inhibitor comprising, as an active ingredient, a lactam compound having one lactam skeleton of a? -Lactam skeleton, a? -Lactam skeleton, or an? -Lactam skeleton and having an acidic group.

[7-2] Component (A): a collagen decomposition inhibitor having a lactam skeleton of any of γ-lactam skeleton, δ-lactam skeleton, or ε-lactam skeleton and having an acidic group as an active ingredient.

[7-3] Component (A): A dental carotenoid blocking agent having a lactam skeleton of any one of a? -Lactam skeleton, a? -Lactam skeleton, and an? -Lactam skeleton and having an acidic group as an active ingredient.

[7-4] Component (A): a dentin antagonist having a lactam skeleton of a γ-lactam skeleton, a δ-lactam skeleton, or an ε-lactam skeleton and having an acidic group as an active ingredient, Improving agent.

[7-5] Component (A): A stain remover comprising, as an active ingredient, a lactam compound having a lactam skeleton of any of γ-lactam skeleton, δ-lactam skeleton, or ε-lactam skeleton and having an acidic group.

[7-6] The agent according to any one of the above-mentioned [7-1] to [7-5], wherein the component (A) is a pyrrolidone carboxylic acid and / or a salt thereof.

INDUSTRIAL APPLICABILITY According to the present invention, there is provided an oral composition and an agent useful for inhibiting dentin caries, inhibiting or improving dentin hypersensitivity, inhibiting or eliminating formation of stain, and the like.

According to the present invention, the oral composition (1) is excellent in dentin dental caries inhibiting effect and excellent in formulation stability. The oral composition (1) is composed of ingredients which are allowed to be absorbed into the body. Therefore, the oral composition (1) can provide an excellent dentin caries prevention effect in a simple form such as a quasi drug, a quasi drug, a quasi drug, a gum, a candy, a food such as a confection .

According to the present invention, there is provided an oral composition (2) capable of remarkably suppressing decomposition of an exposed collagen layer. The effect can be maintained even after storage of the preparation. Oral composition (2) can also inhibit coloring of exposed collagen caused by polyphenol compounds after preservation of the preparation, discoloration and turbidity in the preparation.

According to the present invention, oral compositions (3) and (4) having good feeling (taste) as well as alleviating the pain caused by hypersensitivity are provided. Oral composition (3) is also excellent in ivory tubule blocking effect. Oral compositions (3) and (4) are useful for inhibiting or improving (alleviating) dental hypersensitivity.

According to the present invention, there is provided an oral composition (5) capable of exhibiting a stain removing effect, a stain formation inhibiting effect, a glossing effect, and a good feeling of preparation use.

According to the present invention, an oral composition (6) exhibiting an effect of suppressing collagen coloring is provided.

According to the present invention, there is provided a collagen coloring inhibitor, collagen decomposition inhibitor, dental tubular sequestrant, inhibitor or remedy for perineal hypersensitivity, and a stain remover comprising the component (A) as an active ingredient.

Hereinafter, the present invention will be described in detail. In the following description, "% " represents " mass% "

[Component (A)] [

The component (A) in the present invention is a compound having at least one lactam skeleton selected from the group consisting of a? -Lactam skeleton, a? -Lactam skeleton and an? -Lactam skeleton and having an acidic group (hereinafter referred to as a lactam compound) And / or a salt thereof.

The lactam compound or its salt is not particularly limited as long as it has any one of the above three specific lactam skeletons and is a lactam compound or a salt thereof having an acidic group. The lactone skeleton may have two or more kinds of lactam skeletons in the molecule, two or more kinds of acidic groups, two or more kinds of lactam skeleton and two or more kinds of acidic groups. In a suitable embodiment, the lactam skeleton is a gamma-lactam skeleton.

The acid group of the lactam compound or its salt includes, for example, a phenolic hydroxyl group (hydroxyl group), a carboxyl group, and a sulfonic acid group. Among them, a carboxyl group is preferable as the acidic group.

Examples of the lactam compound having a? -lactam skeleton and having an acidic group include pyrrolidone carboxylic acid, 4- (3-hydroxyphenyl) -4-Aza-tricyclo (5.2.1.0 Dec-8-ene-3,5-dione, 2- (3,5-dioxo-4-Aza-tricyclo (5.2.1.0 And salts thereof, and pyrrolidonecarboxylic acids and salts thereof are preferable.

Examples of the lactam compound having a 隆 -lactam skeleton and having an acidic group include 6-oxo-2-piperidinecarboxylic acid, 4- (2-oxo-1-piperidinyl) -6-oxo-3-piperidinecarboxylic acid, and salts thereof, and 6-oxo-2-piperidinecarboxylic acid is preferable.

Examples of the lactam compound having an ε-lactam skeleton and having an acidic group include 3- (2-oxo-1-azepanyl) propanoic acid, 3- (2-bromo-5-hydroxyphenyl) -Methyl-2-azepanone, and salts thereof, and 3- (2-oxo-1-azepanyl) propanoic acid is preferable.

The salt of the lactam compound may be any pharmacologically acceptable salt, and is not particularly limited. The pharmacologically acceptable salts include, for example, acid addition salts, base addition salts and amino acid salts. Specific examples thereof include inorganic acid salts such as hydrochloride, hydrobromide, sulfate, hydroiodide, nitrate, and phosphate; Organic acid salts such as citrate, oxalate, acetate, formate, propionate, benzoate, trifluoroacetate, maleate, tartrate, methanesulfonate, benzenesulfonate and paratoluenesulfonate; Inorganic bases such as sodium salt, potassium salt, calcium salt, magnesium salt and ammonium salt; Organic base salts such as triethylammonium salt, triethanolammonium salt, pyridinium salt and diisopropylammonium salt; Arginine salts, aspartic acid salts, and glutamic acid salts.

The lactam compound is preferably a pyrrolidone carboxylic acid, 6-oxo-2-piperidinecarboxylic acid or 3- (2-oxo-1-azepanyl) propanoic acid, desirable.

The lactam compound and its salt can be synthesized according to a known scheme. Commercially available lactam compounds and salts thereof may be used.

As a commercially available product of a lactam compound having a γ-lactam skeleton (for example, pyrrolidonecarboxylic acid), for example, "AJIDEW A-100 (registered trademark)", which is commercially available from Ajinomoto Co.,

Examples of commercially available products of a lactam compound having a 隆 -lactam skeleton (e.g., 6-oxo-2-piperidinecarboxylic acid) include "(S) -6-Oxo -2-piperidine carboxylic acid (trade name) ".

Examples of commercially available products of a lactam compound having an ε-lactam skeleton (for example, 3- (2-oxo-1-azepanyl) propanoic acid) include "3- (2 -Oxoazepan-1-yl) propanoic acid (trade name) ".

The kind of the lactam compound as the component (A) in the composition of the present invention may be one type alone, or two or more types.

[Component (1-B)] [

The component (1-B) in the present invention is a fluorine compound. Examples of the fluorine compound include sodium fluoride, potassium fluoride, ammonium fluoride, tin fluoride, amine fluoride, sodium monofluorophosphate, potassium monofluorophosphate, sodium fluoride, and silicon fluoride. Preferred fluorine compounds are sodium fluoride and sodium monofluorophosphate.

Commercially available fluorine compounds may be used. An example of a commercially available sodium fluoride is sodium fluoride, which is available from Sterra Chemipassa. An example of a commercially available product of sodium monofluorophosphate is sodium monofluorophosphate, which is commercially available from Rhodiail.

[Component (1-C)] [

The component (1-C) in the present invention is a protein containing a sulfur-containing amino acid residue in an amount of 1.0 to 6.0% by mass.

Sulfuric amino acid residue means a residue obtained by removing one or more hydrogen from a sulfuric amino acid. Sulfurous amino acid is an amino acid containing sulfur, and examples thereof include methionine and cysteine.

The component (1-C) preferably contains a phosphoric acid group.

In the component (1-C), the number average molecular weight of the protein is preferably from 1,000 to 100,000, more preferably from 10,000 to 100,000. When the number average molecular weight is 1000 or more, the affinity with the dentin can be maintained, the dentin can not be washed away by saliva, and sufficient dentin dental caries inhibiting effect can be exhibited. On the other hand, when the number average molecular weight is 100,000 or less, the adsorptivity to teeth can be maintained, and dentin dental caries inhibiting effect can be sufficiently obtained.

In the component (1-C), the method for measuring the number average molecular weight of the protein is as follows.

As a method for calculating the number average molecular weight, generally, a method of calculating by using gel filtration chromatography (GPC) and a method of calculating by calculation of analytical nitrogen value can be mentioned. The latter method is often used to calculate the number average molecular weight of proteins and polypeptide compounds. The number average molecular weight of the protein of the component (1-C) can also be measured by the latter method.

The number average molecular weight of the component (1-C) can be calculated from the following formula (1-1) based on, for example, the total nitrogen content in the molecule, the amino nitrogen content and the average molecular weight of the constituent amino acid have.

[Equation 1]

In formula (1), the average molecular weight of the constituent amino acids is calculated by multiplying the presence ratio (%) of the constituent amino acids obtained by ordinary amino acid analysis by the molecular weight of each amino acid. The total amount of nitrogen can be measured by the first method of nitrogen determination method or gas chromatography (GC) of the cosmetics raw material standard-general test method. Amino nitrogen content can be measured by the holmium titration method.

Examples of the " protein having an average molecular weight of 1,000 to 100,000 containing 1.0 to 6.0 mass% of a sulfated amino acid residue " include lactoferrin, collagen degradation product and casein.

Lactoferrin is an iron-binding sugar protein with a molecular weight of about 80,000 widely distributed in the animal body. The origin of the lactoferrin, the production method is not limited. For example, there may be mentioned colostrum (milk), transition milk (milk), common milk (milk), terminal milk (milk), and the like of mammals (such as human, Lactoferrin isolated from a lactic acid-treated product (for example, skim milk, fake, etc.) by a routine method (for example, ion exchange chromatography). Lactoferrin prepared by a known method may be used. As lactoferrin, lactoferrin derived from bovine is preferably used.

Commercially available lactoferrin may be used. Examples of commercial products of lactoferrin derived from cattle include "lactoferrin (product name)" (trade name), which is marketed by Wako Pure Chemical Industries, Ltd., "mlF-1", "mlF-EX", which is marketed by Morinaga Kogyo Co., &Quot; lactoferrin ", which is commercially available from Nippon Shokuhin Co., As the component (1-C), one type of lactoferrin may be used, or two or more types of lactoferrin derived from different conditions may be used in combination.

Examples of collagen degradation products include collagen degradation products produced from pig skin, collagen degradation products made from fish scales, and collagen degradation products produced from young ones are preferred. In the component (1-B), the collagen decomposition product may be one kind or a combination of two or more types of collagen decomposition products different in raw materials. As the collagen degradation product, a commercially available product may be used. An example of a commercially available product of collagen degradation product manufactured from a child is the trade name " HACP-U2 ", which is commercially available from JIRAS.

Casein is contained in dairy products such as milk and cheese and accounts for about 80% by mass of milk protein contained in milk. Casein is a protein containing a phosphoryl group, that is, a phosphorylated protein (phosphorylated protein). Most of the serine residues that make up casein bind to phosphoric acid. In the component (1-B), the collagen decomposition product may be one kind or a combination of two or more types of collagen decomposition products different in raw materials. A commercially available casein may be used. An example of a commercial product of casein derived from milk is "casein (derived from milk)" marketed by Wako Pure Chemical Industries, Ltd.

The content of the sulfated amino acid residue of the protein in the component (1-C) is 1.0 to 6.0% by mass per mass of the protein. When the content of the sulfuric amino acid residue is 1.0% or more, the affinity with the dentin can be improved and the dentin dental caries inhibiting effect can be sufficiently obtained. On the other hand, when the content of the sulfuric amino acid residues is 6% or less, the volume of the (1-C) component does not become large enough to cause a steric hindrance with other components, The deterioration of the adsorptivity of the component or other components is effectively prevented, and the dentin dental caries inhibiting effect can be sufficiently obtained.

[Component (2-B)] [

The component (2-B) is at least one polyphenol compound selected from the group consisting of a parent seed extract, proanthocyanidin, catechin and hesperidin.

Euphoria longana (Euphoria longana) is a plant of the oriental tree planted in tropical America and Southeast Asia. The flesh of the dragon is used as a herbal medicine for the purpose of tonic or soothing. Yongan (Ryuugan) is sometimes called Longan.

Rice seed extract is an extract extracted from the seeds of the eye. (2010, 40 (8), p713-721), Identification < RTI ID = 0.0 > and < / RTI > (2005, 53 (5), p1387-1392)).

The extraction method of the seed seed extract from the seeds of the eye is not particularly limited. Examples of the extraction method include a method in which the seeds of the lemon are crushed and the solvent is extracted by a known extraction method. Examples of the solvent include water, lower monohydric alcohols such as methanol, ethanol, and isopropanol, ethylene glycol, polyethylene glycol, propylene glycol, propylene glycol, And polyhydric alcohols such as polypropylene glycol and 1,3-butylene glycol. These may be used singly or in combination of two or more.

As the seed seed extract, a solvent extract may be used as it is, or a concentrate obtained by liquefying and concentrating a solvent may be used. A powder obtained by removing the solvent by drying (for example, freeze-drying or the like) a solvent extract or a concentrate may be used. Alternatively, an excipient or the like may be added. A powder such as a lyophilized product of a solvent extract may be redissolved in a solvent and adjusted to an appropriate concentration. In addition, the yield when extracting the seeds of the seeds of the seeds is not particularly limited.

Commercially available products may be used as the seed seed extract. Commercially available products include, for example, Agitekuto manufactured by Katakura Pharmaceutical Co., Ltd., Longan Seed Extract Powder SD manufactured by the same company, and the like. Agitekuto is an extract of a solution form prepared by dissolving in a solution of 1,3-butylene glycol and water so that an extract concentration of 1.0% is obtained by extracting from the seeds of seeds and freeze-drying after concentration ( Rice seed extract concentration in Agitekuto is 1.0%). Longan seed extract powder SD is a powdery extract prepared by adding dextrin as an excipient to a powder obtained by extraction in the same manner as described above and lyophilization (the concentration of the seed seed extract in longan seed extract powder SD is 83%).

Proanthocyanidin is a kind of polyphenols having a structure in which a plurality of skeletons of catechins are combined. The origin of proanthocyanidin is not particularly limited and may be derived from plants (for example, fruits, pulses, legumes, etc.), or may be artificial synthetic products. Of these, proanthocyanidins derived from plants are preferred, and proanthocyanidins derived from grape seeds are preferred. Grape seeds are rich in proanthocyanidins.

In the case of proanthocyanidins derived from grape seeds, a method for extracting proanthocyanidins from grape seeds is not particularly limited. Examples of the extraction method include a method in which seeds of grapes are disrupted and the solvent is extracted by a known extraction method. Examples of the solvent include water, a monohydric alcohol, a polyhydric alcohol, and mixtures thereof. Examples of the solvent include water, lower monohydric alcohols such as methanol, ethanol and isopropanol, ethylene glycol, polyethylene glycol, propylene glycol, And polyhydric alcohols such as polypropylene glycol and 1,3-butylene glycol. These may be used singly or in combination of two or more.

As the proanthocyanidin, a solvent extract may be used as it is, but a concentrate obtained by concentrating and concentrating the solvent may be used. A powder obtained by removing the solvent by drying (for example, freeze-drying or the like) a solvent extract or a concentrate may be used, or an excipient or the like may be added. It is also possible to use a powder obtained by redissolving a powder such as a lyophilized product in a solvent and adjusting it to an appropriate concentration. The yield of extracting proanthocyanidin is not particularly limited.

As proanthocyanidin, a commercially available product may be used. For example, it is possible to use Guraenol SL manufactured by Kikkoman Co., Ltd. and Guerinol N manufactured by the same company. Guraenol SL is a purest powder of grape seed extract and the main component is proanthocyanidin (concentration of proanthocyanidin in guanol SL is 82%). Guraenol N is likewise an extract of the grape seeds and is a duller brown powder (the concentration of proanthocyanidin in guaniol N is 38%).

Catechin is a generic term for one kind of flavonoid (C ₁₅ H ₁₄ O ₆ ) and its derivatives. Examples of catechins include catechin, epicatechin, gallocatechin, epigallocatechin, epicatechin gallate, gallocatechin gallate, and epigallocatechin gallate. The catechin in the component (2-B) may be one kind of catechin or two or more kinds thereof. The origin of the catechin is not particularly limited and may be derived from a plant (for example, tea), or may be an artificial product. Among them, catechins derived from plants are preferable, catechins derived from tea are more preferable, and catechins derived from tea leaves are more preferable. This is because the tea leaves contain catechins in abundance.

In the case of catechins derived from tea leaves, a method for extracting catechins from tea leaves is not particularly limited. For example, a tea leaf prepared by shredding a tea leaf and extracting it with a solvent by a known extraction method can be used. Examples of the solvent include water, a monohydric alcohol, a polyhydric alcohol, and mixtures thereof. Examples of the solvent include water, lower monohydric alcohols such as methanol, ethanol and isopropanol, ethylene glycol, polyethylene glycol, propylene glycol, And polyhydric alcohols such as polypropylene glycol and 1,3-butylene glycol. These may be used singly or in combination of two or more kinds.

As the catechin, the solvent extract may be used as it is, or a concentrate obtained by concentrating and concentrating the solvent may be used. A powder obtained by removing the solvent by drying (for example, freeze-drying or the like) a solvent extract or a concentrate may be used, or an excipient or the like may be added. It is also possible to use a powder obtained by lyophilizing a powder such as a lyophilized product in a solvent and adjusting it to an appropriate concentration. In addition, the yield when extracting catechins is not particularly limited.

As the catechin, a commercially available product may be used. For example, acid phenol EGCG, acid phenon 90S manufactured by Daiyo Kagaku Co., Ltd., and the like can be used. The acid phenon EGCG is a white to pale gray powder (the concentration of epigallocatechin gallate in the acid phenone EGCG is 95%), which is an extract product of green tea and contains epigallocatechin gallate in a high purity. The acid phenon 90S is also a pale yellow to reddish brown powder (70% of catechin concentration (various concentrations of catechins in acid phenon 90S)).

Hesperidin is a polyphenol, also called vitamin P. The origin of hesperidin is not particularly limited, and it may be derived from a plant (for example citrus fruits such as Onzugi citrus or Hassaku), or may be an artificial product. Among them, hesperidin derived from plants is preferable, hesperidin derived from citrus is preferable, and hesperidin derived from citrus peel (peel) is more preferable. Citrus peels are rich in hesperidin.

In the case of peripherally derived hesperidin, the method of extracting hesperidin from the peripheries is not particularly limited. For example, it is possible to use a preparation prepared by crushing a perilla and extracting it with a solvent by a known extraction method. Examples of the solvent include water, a monohydric alcohol, a polyhydric alcohol, and mixtures thereof. Examples of the solvent include water, lower monohydric alcohols such as methanol, ethanol and isopropanol, ethylene glycol, polyethylene glycol, propylene glycol, And polyhydric alcohols such as polypropylene glycol and 1,3-butylene glycol. These may be used singly or in combination of two or more kinds.

As the hesperidin, the solvent extract may be used in the form of a solution in the form of a solution, but the solvent may be passed through and concentrated to a suitable concentration. They may be dried by lyophilization or the like, and the solvent may be removed to obtain a powdery product. Alternatively, the powdery product may be used as it is, or may be used by adding an excipient or the like. A powdery product such as a lyophilized product may be used which is redissolved in a solvent and adjusted to an appropriate concentration. In addition, the yield when extracting hesperidin is not particularly limited.

As the hesperidin, a commercially available product may be used. For example, hesperidin, manufactured by Wako Pure Chemical Industries, Ltd., methyl hesperidin, manufactured by Tokyo Chemical Industry Co., Ltd., and the like can be used. Hesperidin is a yellow powder (Hesperidin concentration: 92%) obtained by extracting and purifying from perilla crushed material. Methyl hesperidin is a yellowish to reddish yellow powder (methyl hesperidin concentration: 90%) obtained by methylation of hesperidin to dimethyl sulfate and solubilization in water.

The component (2-B) may be one or more of a parent seed extract, at least one proanthocyanidin, at least one catechin, or at least one hesperidin, It is also good. As the component (2-B), a seedling seed extract and / or proanthocyanidin are preferably used, and more preferably a seedling seed extract is used.

[Component (3-B)] [

Component (3-B) in the present invention is aluminum lactate.

As the component (3-B), a commercially available product may be used. For example, as a commercially available product of aluminum lactate, trade name "aluminum lactate" available from Wako Pure Chemical Industries, Ltd. may be mentioned.

In the oral composition (3), because the ingredient (A) is mixed with the ingredient (3-B), the taste of the arine flavor and the flavor of the mouth And the generation of metal taste can be prevented, and the feeling of use (taste) can be improved.

[Component (3-C)] [

(3-C) component is monofluorophosphate.

As the monofluorophosphate, a monofluorophosphate ion is preferably used, and a water-soluble monofluorophosphate is preferable. Examples of the monofluorophosphate include an alkali metal salt of monofluorophosphoric acid, an alkaline earth metal salt of monofluorophosphoric acid, and an ammonium salt of monofluorophosphoric acid. Of these, sodium monofluorophosphate, potassium monofluorophosphate, mono Ammonium fluorophosphate and the like are preferable, and sodium monofluorophosphate is more preferable.

As the component (3-C), a commercially available product may be used. For example, as a commercially available product of monofluorophosphate, there may be mentioned " sodium monofluorophosphate " which is commercially available from Rhodia.

The component (3-C) may be a single monofluorophosphate or a combination of two or more monofluorophosphates.

The monofluorophosphate, which is a component (3-C), mainly contains fluorine in the component. The amount of the total amount of the total amount of the composition contained in the oral composition 3 is preferably 0.01 mass% (100 ppm) or more, more preferably 0.02 mass% (200 ppm) or more, with respect to the total amount of the oral composition 3. The upper limit is preferably 1 mass% (10000 ppm) or less, and more preferably 0.5 mass% (5000 ppm) or less. The amount of fluorine contained in the oral composition (3) of the present invention is preferably 0.01 to 1 mass% (100 to 10000 ppm), more preferably 0.02 to 0.5 mass% (200 to 5000 ppm).

[Component (3-D) and Component (4-B)] [

(3-D) and (4-B) are inorganic water-soluble potassium salts.

In the present invention, the " inorganic water-soluble potassium salt " refers to an inorganic potassium salt which can dissolve 2 g or more in 100 g of water at 20 占 폚.

Examples of the inorganic water-soluble potassium salt include potassium nitrate, potassium chloride, potassium dihydrogenphosphate, potassium sulfate, potassium carbonate, potassium hydrogencarbonate and alum. Among them, potassium nitrate and potassium chloride are preferable from the viewpoint of remarkable alleviation effect and sensation of use (taste) due to hypersensitivity. These inorganic water-soluble potassium salts may be commercially available reagents (available from Wako Pure Chemical Industries, Ltd., etc.).

The (3-D) component and the (4-B) component may be used either singly or in combination of two or more.

The component (4-B) has a problem that the alleviation effect on the pain caused by the hypersensitivity is limited, bitter tastes are produced, and the feeling of use (taste) is poor. Among the components (4-B), potassium nitrate has a certain effect on alleviating pain caused by hypersensitivity, but has a bitter taste and is inferior to a feeling of use (taste). In the oral composition (4), by using the ingredient (A) in combination with the ingredient (4-B), the effect of alleviating the pain caused by the hypersensitivity of the ingredient (4-B) (Taste) is achieved even when potassium nitrate is used, for example, by suppressing the bitter taste derived from the component (4-B).

[Component (4-C)] [

In the present invention, the component (4-C) is a water-soluble fluorine compound. The "water-soluble fluorine compound" refers to a fluorine compound capable of dissolving 2 g or more in 100 g of water at 20 ° C.

The water-soluble fluorine compound is a known component that has been conventionally used in oral compositions as a source of fluoride ions having a re-crystallizing action of teeth, etc. However, the inventors of the present invention have found that such a water- (That is, remarkable improvement in the alleviation effect of the component (B) against pain caused by the hypersensitive hypersensitivity) can be further enhanced.

Examples of the water-soluble fluorine compound which can be suitably used as the component (4-C) include sodium fluoride, potassium fluoride, ammonium fluoride, tin fluoride, amine fluoride, sodium monofluorophosphate, potassium monofluorophosphate, , And calcium fluoride. Among them, sodium fluoride and sodium monofluorophosphate are preferable as the water-soluble fluorine compound from the viewpoint of enhancing the effect of the component (A). These water-soluble fluorine compounds may be used in the form of commercially available reagents (for example, those available from sources such as Sterachemipa, Rhodia, and the like).

[Component (5-B)] [

(5-B) component is cationized cellulose.

As the cationic cellulose, for example, a cellulose derivative to which a cationic group is added may, for example, be mentioned. Examples of the cationizing group include dimethyldiallylammonium, 2-hydroxy-3 (trimethylammonio) propyl, and the like. Examples of the cellulose derivative to which a cationic group is added include hydroxyethyl cellulose dimethyldiallylammonium chloride, O- [2-hydroxy-3- (trimethylammonio) propyl] hydroxyethyl cellulose, derivatives thereof and the like. . The cationic cellulose preferably has a nitrogen content of 0.1 to 3% by mass.

The component (5-B) may be one kind or a combination of two or more kinds.

As the component (5-B), hydroxyethyl cellulose dimethyldiallylammonium chloride can excellently be used because it is excellent in the stain formation inhibiting effect and glossing effect of teeth.

[Component (6-B)] [

(6-B) is a polyphenol compound. Examples of polyphenol compounds include flavonoids, phenylcarboxylic acids, chlorogenic acids, lignans, quercumin, and the above-mentioned (2-B) components.

[Composition or Agent of the Present Invention]

The composition or agent of the present invention comprises a lactam compound (A) and / or a salt thereof. A lactam compound and / or a salt thereof as an active ingredient.

The content of the component (A) in the composition or agent of the present invention is not particularly limited.

When the active ingredient of the composition of the present invention is the component (A) alone, the content of the component (A) is preferably 0.3% by mass or more, more preferably 0.5% by mass or more based on the total amount of the composition. Thereby, the effect of blending the lactam compound can be sufficiently obtained. When the component (A) is a lactam compound having a? -Lactam skeleton and / or an? -Lactam skeleton, the compounding amount is more preferably 1% by mass or more.

When the active ingredient of the composition of the present invention is the component (A) alone, the amount of the component (A) is preferably 10 mass% or less, more preferably 5 mass% or less, with respect to the total amount of the composition. This is because the contribution to the improvement of each effect is limited even when a large amount is added.

The blending amount of the component (A) in the present invention is preferably from 0.3 to 10% by mass, more preferably from 0.5 to 5% by mass, based on the total amount of the composition.

Hereinafter, preferred embodiments in which the composition of the present invention is an oral composition will be described.

[Oral composition (1)]

The oral composition of the present invention may contain the component (A) and the component (1-B). Hereinafter, the oral composition containing the component (A) and the component (B-1) is referred to as an oral composition (1).

[Content of Component (A) in Oral Composition (1)] [

The content of the component (A) in the oral composition (1) is not particularly limited, but is preferably 0.1% by mass or more, more preferably 0.5% by mass or more, It is preferably at least 1% by mass. When the content of the component (A) is 0.1% by mass or more, dentin dental caries inhibitory effect can be sufficiently obtained.

The upper limit of the content of the component (A) in the oral composition (1) is preferably 10% by mass or less, more preferably 5% by mass or less. As a result, the gelation ability of the thickening agent in the oral composition (1) can be maintained, precipitation of the component (A) due to aging can be prevented, and good formulation stability can be maintained. It is possible to maintain the dentin dental caries inhibiting effect.

The content of the component (A) is preferably from 0.1 to 10% by mass, and more preferably from 0.5 to 5% by mass, based on the whole amount of the oral composition (1). When the component (A) is a lactam compound having a? -Lactam skeleton and / or an? -Lactam skeleton, the content of the component (A) is more preferably 1 to 5% by mass.

[Content of (1-B) component in oral composition (1)] [

In the oral composition (1) of the present invention, the action of both of the (1-B) ingredient serving as a source of fluoride ions in the oral cavity and the ingredient (A) Excellent dentin dental caries prevention effect which is not available in the past can be exerted.

Since the effect of the component (1-B) used in the present invention is responsible for the fluorine in the component (1-B), the compounding amount of the component (1-B) It is useful to specify. Therefore, in the following description, the content of the component (1-B) in the oral composition (1) is replaced with the fluorine content in the oral composition (1).

The content of the component (1-B) in the mouth composition (1) is preferably 0.01 mass% (100 ppm) or more, more preferably 0.02 mass% (200 ppm) Or more. Thereby, a sufficient dentin dental caries inhibiting effect can be obtained.

On the other hand, the upper limit of the content of the component (1-B) in the oral composition (1) is preferably 1% by mass (10000 ppm) or less in terms of the fluorine content with respect to the whole amount of the composition for oral cavity % (5000 ppm) or less is more preferable. When the fluorine content is 1 mass% (10000 ppm) or less, the stability of the preparation can be maintained. An example of the stability of the formulation stability is prevention of a decrease in the gelation ability of the thickening agent in the oral composition (1). As another example, when the oral composition (1) is a liquid preparation, prevention of the occurrence of sediment can be mentioned.

The content of the component (1-B) in the oral composition (1) of the present invention is preferably 0.01 to 1 mass% (100 to 10000 ppm) in terms of the fluorine content with respect to the whole amount of the composition for oral cavity , And 0.02 to 0.5 mass% (200 to 5000 ppm) are more preferable.

[Component (A) / (1-B) in Oral Composition (1)] [

In the present invention, the compounding ratio of the component (A) to the component (1-B) has a preferable range. The mass ratio of the component (A) to the component (1-B) in the oral composition (1) can be represented by the mass ratio of the component (A) to the fluorine content [component (A) / fluorine content]. The "component (A) / fluorine content] is preferably 1 or more, more preferably 2 or more. As a result, since the amount of fluoride ions to the component (A) is appropriate, precipitation of fluoride ions on the surface of the dentin is prevented, and sufficient dentin dental caries inhibiting effect can be obtained.

The upper limit of the mass ratio of the component (A) to the fluorine content in the oral composition (1) is preferably 250 or less, more preferably 100 or less. Thereby, since the amount of the fluoride ion relative to the component (A) is within a suitable range, a remarkable dentin dental caries inhibiting effect can be obtained.

The mass ratio of the component (A) to the fluorine content in the oral composition (1) is preferably 1 to 250, more preferably 2 to 100.

The oral composition (1) of the present invention may also contain a component (1-C). This is preferable because the dentin dental caries prevention effect of the oral composition (1) is further increased.

[Content of (1-C) component in oral composition (1)] [

When the oral composition (1) contains the ingredient (1-C), the content of the ingredient (1-C) is not particularly limited, but is preferably 0.1 to 10 mass %, More preferably 0.1 to 5 mass%. When the content is 0.1% by mass or more, dentin dental caries inhibiting effect can be sufficiently obtained. On the other hand, when the content is 10% by mass or less, discoloration can be prevented and deterioration of feeling due to generation of a base odor originating from the component (1-C) can be prevented.

[Component (1-C) / (1-B) in Oral composition (1)] [

When the oral composition 1 contains the component (1-C), the mass ratio of the component (1-C) to the component (1-B) ), That is, the mass / fluorine content of the (1-C) component.

The mass ratio [(1-C) component / fluorine content] of the component (1-C) to the amount of fluorine in the oral composition (1) is preferably 0.3 to 800, more preferably 0.5 to 80. Since the mass ratio is 0.3 or more, the amount of fluoride ions to the component (1-C) is appropriate, so precipitation of fluoride ions on the surface of the dentin can be prevented, and sufficient dentin dental caries inhibiting effect can be obtained. On the other hand, since the mass ratio is 800 or less, a synergistic effect can be obtained on the dentin dental caries inhibiting effect, since the amount of fluoride ions is in a suitable range with respect to the (1-C) component.

[Oral composition (2)]

The oral composition of the present invention may contain the component (A) and the component (2-B). Hereinafter, the oral composition containing the component (A) and the component (B-2) is referred to as an oral composition (2).

[Content of component (A) in Oral composition (2)] [

The content of the component (A) in the oral composition (2) is not particularly limited, but is preferably 0.5% or more, more preferably 1% or more, relative to the total amount of the oral composition (2) of the present invention. Thus, by combining with the component (2-B), the dentin collagen decomposition inhibiting effect after preservation and the dentin collagen discoloration inhibiting effect after preservation can be sufficiently exhibited. The upper limit of the content of the component (A) in the oral composition (2) is preferably 10% or less, more preferably 5% or less. As a result, the stability of the preparation can be sufficiently exerted, and the dentin collagen decomposition inhibiting effect after storage can be sufficiently exhibited. The content of the component (A) is preferably 0.5 to 10%, more preferably 1 to 5%.

[Content of (2-B) component in oral composition (2)] [

The content of the component (2-B) in the oral composition (2) is not particularly limited, but is preferably 0.001% or more, more preferably 0.01% or more, relative to the total amount of the oral composition (2). When the content is 0.001% or more, the dentin collagen decomposition inhibitory effect and the dentin collagen decomposition inhibitory effect after storage can be sufficiently exhibited by the combined use with the component (A). The upper limit of the content of the component (2-B) is preferably 0.5% or less, more preferably 0.2% or less. Thereby, the effect of inhibiting the coloring of dentin collagen after storage and the stability of the preparation can be sufficiently exhibited. The content of the component (2-B) is preferably 0.001 to 0.5%, more preferably 0.01 to 0.2%.

[Component (A) / (2-B) in Oral composition (2)] [

In the oral composition (2), the mass ratio ((A) / (2-B)) relative to the (2-B) component of the component (A) is not particularly limited but is usually 5 or more, to be. Thereby, the dentin collagen coloration inhibiting effect and the preparation stability after preservation can be sufficiently exhibited. The upper limit of the mass ratio of the component (A) to the component (2-B) is usually 3000 or less, preferably 300 or less. As a result, the dentin collagen decomposition inhibiting effect can be sufficiently exhibited even after preservation. The mass ratio ((A) / (2-B)) of the component (A) to the component (2-B) in the oral composition (2) is preferably 5 to 3000, more preferably 10 to 300 Do.

[Oral composition (3)]

The oral composition of the present invention may contain the component (A) and the component (3-B). Hereinafter, the oral composition containing the component (A) and the component (3-B) is referred to as the oral composition (3).

[Content of Component (A) in Oral Composition (3)] [

The content of the component (A) in the oral composition (3) is not particularly limited, but is preferably 0.1% by mass or more, more preferably 0.5% by mass or more based on the total amount of the oral composition (3) . As a result, it is possible to sufficiently obtain an early blocking effect of dentinal tubules and a pain relief effect. When the component (A) is a compound having an? -Lactam skeleton and having an acidic group and / or a compound having an? -Lactam skeleton and having an acidic group, the content is more preferably 1% by mass or more. The upper limit of the content of the component (A) is preferably 10% by mass or less, more preferably 5% by mass or less. If it exceeds 10% by mass, it may be impossible to obtain further improvement of the early blocking effect of iv iv tubules.

The content of the component (A) is preferably 0.1 to 10% by mass, more preferably 0.5 to 5% by mass. When the component (A) is a compound having an acidic group and / or an acidic group having a? -Lactam skeleton and / or an? -Lactam skeleton, the content of the component (A) is preferably 1 to 5% by mass desirable.

[Content of (3-B) component in oral composition (3)] [

The content of the component (3-B) in the oral composition (3) is not particularly limited, but is preferably 0.01% by mass or more, more preferably 0.1% by mass or more, Or more. As a result, it is possible to sufficiently obtain an early blocking effect of dentinal tubules and a pain relief effect. The upper limit of the content of the component (3-B) is preferably 10% by mass or less, and more preferably 5% by mass or less. Thereby, it is possible to keep the feeling of use (taste) satisfactorily and to prevent occurrence of arine taste, metal taste, and the like. The content of the component (3-B) is preferably 0.01 to 10% by mass, and more preferably 0.1 to 5% by mass.

[Component (A) / (3-B) in Oral composition (3)] [

The mass ratio [(A) / (3-B)] of the component (A) to the component (3-B) in the oral composition (3) is preferably 0.1 or more, more preferably 0.5 or more. As a result, the effect of improving the feeling of use (taste) can be sufficiently exhibited. The upper limit is preferably 500 or less, more preferably 45 or less. As a result, the effect of blocking the daphnia of the component (3-B) is sufficiently exerted, and the synergistic effect of the component (A) and the component (3-B) can be remarkably expressed. The mass ratio of the component (A) to the component (3-B) is preferably 0.1 to 500, more preferably 0.5 to 45.

[Content of (3-C) component in oral composition (3)] [

The oral composition (3) may also contain a (3-C) component.

When the oral composition 3 contains the component (3-C), the content of the component (C) in the oral composition (3) is preferably such that the total fluorine content contained in the oral composition (3) The amount of fluorine contained in the composition is preferably 0.01 to 1 mass% (100 to 10000 ppm), more preferably 0.02 to 0.5 mass% (200 to 5000 ppm).

The content of the component (3-C) in the oral composition (3) is preferably 0.076% by mass or more, more preferably 0.15% by mass or more in the case of sodium monofluorophosphate. As a result, it is possible to sufficiently obtain an early blocking effect of dentinal tubules and a pain relief effect. The upper limit of the content of the component (3-C) in the oral composition (3) is preferably 7.6 mass% or less, more preferably 3.8 mass% or less. Thereby, the feeling of use (taste) can be maintained satisfactorily. The content of the component (3-C) is preferably 0.076 to 7.6 mass%, more preferably 0.15 to 3.8 mass%.

[Content of (3-D) component in oral composition (3)] [

The oral composition (3) may further contain a component (3-D).

The content of the component (3-D) in the oral composition (3) is not particularly limited, but is preferably 0.005% by mass or more, more preferably 0.1% by mass or more based on the total amount of the oral composition (3) Do. Thereby, the pain relief effect can be sufficiently obtained. The upper limit is preferably 10 mass%, more preferably 7 mass% or less. Thereby, the feeling of use (taste) can be maintained satisfactorily. The content of the component (3-D) is preferably 0.005 to 10 mass%, more preferably 0.1 to 7 mass%.

[Oral composition (4)]

The composition of the present invention may contain the component (A) and the component (4-B). Hereinafter, the oral composition containing the component (A) and the component (4-B) is referred to as the oral composition (4).

[Content of component (A) in Oral composition (4)] [

The content of the component (A) in the oral composition (4) is preferably 0.1% by mass or more, more preferably 0.5% by mass or more from the viewpoint of a remarkable alleviating effect on the pain caused by the hypersensitivity and a feeling of use Is more preferable. When the? -Lactam compound having an acidic group, the? -Lactam compound having an acidic group, or a salt thereof is used as the component (A), the content of the component (A) in the oral composition is preferably about From the viewpoint of remarkable alleviating effect, it is particularly preferable that the content is 1% by mass or more.

Although the upper limit of the content of the component (A) in the oral composition (4) is not particularly limited, the contribution to the remarkable reduction in the pain relief due to the hypersensitivity is limited, , More preferably 5 mass% or less.

In one embodiment, the content of the component (A) in the oral composition (4) is preferably from 0.1 to 10% by mass, particularly preferably from 0.5 to 5% by mass, based on the whole amount of the oral composition (4) . When a? -Lactam compound having an acidic group or an? -Lactam compound having an acidic group is used as the component (A), the content of the component (A) in the oral composition is particularly preferably from 1 to 5% by mass.

[Content of (4-B) component in oral composition (4)] [

The content of the component (4-B) in the oral composition (4) is preferably not less than 0.1% by mass, more preferably not less than 1.0% by mass from the viewpoint of remarkable relieving effect on pain caused by hypersensitivity.

The content of the component (4-B) in the oral composition (4) is preferably 10% by mass or less, more preferably 7% by mass or less, from the viewpoint of feeling of use (taste).

In one embodiment, the content of the component (4-B) in the oral composition (4) is preferably from 0.1 to 10% by mass, particularly preferably from 1.0 to 7% by mass.

[Component (A) / (4-B) in Oral composition (4)] [

In the oral composition (4), the mass ratio of the component (A) to the component (4-B) is preferably within a preferable range . That is, the mass ratio of the component (A) / (4-B)) to the component (4-B) in the oral composition (4) is preferably 0.02 to 80, More preferably from 0.1 to 10, and still more preferably from 0.1 to 5.

[Content of Component (C) in Oral Composition (4)] [

The oral composition (4) may also contain the component (4-C).

Since the effect of the water-soluble fluorine compound used in the present invention is responsible for the fluorine in the (4-C) component, the content of the (4-C) component is determined in terms of the fluorine content in the oral composition This is useful. Therefore, in the following description, the content of the component (4-C) is replaced with the fluorine content in the oral composition (4).

The content of the component (4-C) in the oral composition (4) is preferably higher than that of the oral composition (4) by further enhancing the effect of the component (A) Is preferably 0.01 mass% (100 ppm) or more, more preferably 0.02 mass% (200 ppm) or more, in terms of the fluorine content with respect to the whole amount of the oral composition (4).

The content of the component (4-C) in the oral composition of the present invention is preferably at most 1 mass% (10000 ppm), more preferably at most 1 mass% , And more preferably 0.5 mass% (5000 ppm) or less.

In one embodiment, the content of the component (4-C) in the oral composition of the present invention is 0.01 to 1% by mass (100 to 10000 ppm) relative to the total amount of the oral composition (4) in terms of the fluorine content , More preferably from 0.02 to 0.5 mass% (200 to 5000 ppm).

[Component (4-C) / (A) in Oral composition (4)] [

The effect of the component (A) is further enhanced to further enhance the effect of alleviating the pain caused by the hypersensitivity of the oral composition (4). The mass ratio of the component (A) . That is, the mass ratio [(4-C) component / (A) component] of the component (4-C) to the component (A) in the oral composition (4) is preferably 0.002 to 5, (Provided that the mass of the component (C) is a fluorine content conversion value).

[Oral composition (5)]

The composition of the present invention may contain the component (A) and the component (5-B). Hereinafter, the oral composition containing the component (A) and the component (5-B) is referred to as an oral composition (5).

[Content of Component (A) in Oral Composition (5)] [

The content of the component (A) in the oral composition (5) is not particularly limited, but is preferably 0.1% by mass or more with respect to the total amount of the oral composition (5) of the present invention. Thereby, the stain removal effect and the stain formation inhibiting effect are sufficiently obtained. The content of the component (A) in the oral composition (5) is preferably 10 mass% or less with respect to the total amount of the oral composition (5) of the present invention. As a result, good solubility and appearance can be obtained, so that discomfort can be suppressed and the feeling of use can be improved. The content of the component (A) in the oral composition (5) is preferably 0.1 to 10% by mass, more preferably 0.5 to 5% by mass with respect to the total amount of the oral composition (5) of the present invention.

[Content of (5-B) component in oral composition (5)] [

The content of the component (5-B) in the oral composition (5) is preferably 0.005 mass% or more with respect to the total amount of the composition for oral cavity (5). Whereby the effect of suppressing stain formation and the effect of luster can be sufficiently exhibited. The content of the component (5-B) in the oral composition (5) is preferably 0.1% by mass or less with respect to the total amount of the oral composition (5). Thereby, it is possible to suppress the uncomfortable feeling derived from the cationic cellulose and maintain a good feeling of use. The content of the component (5-B) in the oral composition (5) is preferably 0.005 to 0.1% by mass relative to the total amount of the oral composition (5) of the present invention, By mass, more preferably 0.01 to 0.05% by mass.

[Component (A) / (5-B) in Oral composition (5)] [

In the oral composition (5), the mass ratio ((A) / (5-B)) of the component (A) and the component (5-B) is not particularly limited, but is usually 3 or more, preferably 15 or more . The mass ratio of the component (A) to the component (5-B) is generally 600 or less, preferably 300 or less. When the ratio is 3 or more, the effect of inhibiting stain formation and the effect of removing stain can be sufficiently exhibited. When it is 600 or less, the stain formation inhibiting effect and the glossing effect can be sufficiently exerted, and a good feeling of use can be maintained. The ratio of the component (A) to the component (5-B) is preferably from 3 to 600, more preferably from 15 to 300.

[Action of Oral composition (5)] [

It is presumed that the oral composition (5) exerts the effect of inhibiting stain formation, the effect of removing stain, the luster effect and the feeling of use of the agent by the action of the component (A) and the component (5-B)

The component (5-B) effectively inhibits adhesion of the stain to the enamel surface and imparts gloss to the teeth. On the other hand, the component (A) functions to soften and dissolve the limestone after adsorption to the stain adhering to the enamel surface or to the stain again calcined after the adhering, Lt; / RTI >

The combination of the component (A) and the component (5-B) makes it possible to strongly inhibit adhesion and lamination of the stain to the tooth surface. Thus, the oral composition (5) The stain formation inhibiting effect and the glossing effect can be combined. (5) is superior to the oral composition (5) because neither the component (A) nor the component (5-B) has any discomfort or taste problems with the oral mucosa of the conventional condensed phosphoric acid, enzyme and surfactant. You can also feel the feeling of preparation.

[Oral composition (6)]

The composition of the present invention may contain the component (A) and the component (6-B). Hereinafter, the oral composition containing the component (A) and the component (6-B) is referred to as an oral composition (6). Since the polyphenol compound contains each compound of the component (3-B), the oral composition (6) can be said to be a superordinate concept of the oral composition (3) Is different in terms of effectiveness.

[Content of component (A) in Oral composition (6)] [

The content of the component (A) in the oral composition (6) is not particularly limited, but is preferably 0.3% by mass or more based on the total amount of the oral composition (6) of the present invention. Thereby, the collagen coloring inhibiting effect by the (6-B) component can be sufficiently obtained. The content of the component (A) in the oral composition (6) is preferably 10% by mass or less with respect to the total amount of the oral composition (6) of the present invention. As a result, good solubility and appearance can be obtained, so that a feeling of discomfort can be suppressed and the feeling of use can be improved. The content of the component (A) in the oral composition (6) is preferably 0.3 to 10% by mass, more preferably 0.5 to 5% by mass, based on the whole amount of the oral composition (6) of the present invention.

[Content of (6-B) component in oral composition (6)] [

The content of the component (6-B) in the oral composition (6) is preferably 0.001% by mass or more with respect to the total amount of the oral composition (6). As a result, the component (6-B) causes coloring of the collagen, and the effect of inhibiting the collagen coloration by the combination of the component (A) and the component (6-B) can be expected. The content of the component (6-B) in the oral composition (6) is preferably 5% by mass or less with respect to the total amount of the oral composition (6). Thereby, the effect of inhibiting the collagen coloring by the component (A) can be sufficiently exhibited. The content of the component (6-B) in the oral composition (6) is preferably 0.001 to 5% by mass, more preferably 0.01 to 1% by mass relative to the total amount of the oral composition (6) Do.

[Component (A) / (6-B) in Oral composition (6)] [

In the oral composition (5), the mass ratio ((A) / (6-B)) of the component (A) and the component (6-B) is not particularly limited, but is usually 0.5 or more, preferably 3 or more . The mass ratio of the component (A) to the component (6-B) is generally 1000 or less, preferably 200 or less. Within this range, the effect of inhibiting the collagen coloring by the component (A) can be sufficiently exhibited. The ratio of the component (A) to the component (6-B) is preferably 0.5 to 200, more preferably 3 to 1000.

In the present invention, the content of each component in the composition is based on the amount of each component (the amount of the component) when the composition is produced.

The dosage form of the composition of the present invention is not particularly limited. For example, oral administration (for example, oral administration, sublingual administration, etc.), parenteral administration (intravenous administration, intramuscular administration, subcutaneous administration, percutaneous administration, ), Parenteral (parenteral) administration, etc.), and the like. Of these, a dosage form having low invasiveness is preferable, and oral administration is more preferable.

The form of the composition of the present invention can be appropriately determined according to the dosage form and the like, and is not particularly limited. Examples of formulations for oral administration include liquid (liquid), syrup (syrup), tablets (tablets, tablets), capsules (capsules), powders (granules, Semi-liquid phase, cream phase, paste phase, and chewing gum can be cited as examples. Of these, granular, capsule, powder, soft capsule, and solid forms are preferable, and granular (tablets) are more preferable. Examples of formulations for transdermal administration include aerosol, cream, lotion, spray, stick, and the like.

When the composition of the present invention is an oral composition, it is preferable that the formulation is a liquid system (liquid, liquid, paste), a solid system (solid, solid, semi-solid, film).

[Pharmacologically acceptable carrier (optional component)]

In the oral composition of the present invention, in addition to the above components, a pharmacologically acceptable carrier (optional component) may be added, if necessary. Examples of optional components include solvents such as surfactants, dyes, thickeners, sweeteners, preservatives, flavors, acidifiers, lubricants, abrasives, colorants, preservatives, polishes, fluidizers, binders, disintegrators, (Solvent) and an excipient within the range that does not impair the stability and demineralization suppressing effect. Specific examples of the optional components are shown below, but the components that can be incorporated into the composition of the present invention are not limited thereto.

Examples of the abrasive include silica-based abrasives such as silicic anhydride, crystalline silica, amorphous silica, silica gel and aluminosilicate, zeolite, calcium hydrogenphosphate anhydrate, calcium hydrogenphosphate dihydrate, calcium pyrophosphate, calcium carbonate , Aluminum hydroxide, alumina, magnesium carbonate, magnesium phosphate, zirconium silicate, calcium phosphate dibasic, hydroxyapatite, calcium phosphate dibasic, synthetic resin abrasive and the like.

The abrasives may be used singly or in combination of two or more. When blending the abrasive, the blending amount of the abrasive is preferably 2 to 40%, more preferably 5 to 20% in the total composition of the composition. In a detergent, it is preferably 0 to 10%, more preferably 0 to 5% of the whole composition.

Examples of the viscous solution include thickening agents such as thickening silica, pullulan, gelatin, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, carboxymethylcellulose sodium, carrageenan, sodium alginate, xanthan gum, sodium polyacrylate, , Guar gum, locust bean gum, polyvinyl alcohol, polyvinyl pyrrolidone, carboxyvinyl polymer and the like. The binder can be used singly or in combination of two or more kinds. When blending is used, the blending amount is usually 0.01 to 3% based on the total amount of the composition.

Examples of the viscosifier (wetting agent) include sorbitol, propylene glycol, butylene glycol, glycerin, polyethylene glycol, and the like. The viscosifiers may be used alone or in combination of two or more. When a gauge is used, its content can be determined within a range that does not disturb the effect of the present invention, and is usually 1 to 60% based on the total amount of the composition.

Examples of the surfactant include anionic surfactants and nonionic surfactants.

Examples of the anionic surfactant include N-acyl amino acid salts,? -Olefinsulfonic acid salts, N-acylsulfonic acid salts, alkylsulfuric acid salts, glycerin fatty acid ester sulfates, POE alkylsulfosuccinate salts, POE alkyl ether sulfate salts, POE alkyl Ether phosphates, and the like. Of these, N-acyl amino acid salts,? -Olefin sulfonic acid salts, alkyl sulfate salts and the like are preferable from the standpoint of general versatility. From the viewpoint of foaming property and inner diameter water resistance, the carbon chain length of the lauroylsalicosin sodium, More preferably sodium alpha-olefinsulfonate having 10 to 16 carbon atoms, sodium lauryl sulfate and the like.

Examples of the nonionic surfactant include polyoxyethylene alkyl ethers, polyoxyethylene-polyoxypropylene block copolymers, polyoxyethylene hardened castor oil, polyoxyethylene ethers of glycerin esters, sucrose fatty acid esters, alkylol amides, Glycerin fatty acid esters and the like. Of these, polyoxyethylene alkyl ethers, polyoxyethylene hardened castor oil, alkylol amides, sorbitan fatty acid esters and the like are suitably used in view of versatility. In the polyoxyethylene alkyl ether, the carbon chain length of the alkyl chain is preferably 14 to 18 carbon atoms. The polyoxyethylene alkyl ether preferably has an average addition mole number of ethylene oxide of 15 to 30. It is preferable that the polyoxyethylene hardened castor oil has an average addition mole number (average addition EO) of ethylene oxide of 20 to 100. The alkylolamide preferably has a carbon chain length of 12 to 14 carbon atoms in the alkyl chain. The sorbitan fatty acid ester preferably has 12 to 18 carbon atoms in the fatty acid. The polyoxyethylene sorbitan fatty acid ester preferably has 16 to 18 carbon atoms in the fatty acid. The polyoxyethylene sorbitan fatty acid ester preferably has an average addition mole number of ethylene oxide of 10 to 40. [

The surfactants may be used singly or in combination of two or more. When a surfactant is used, the content is usually 0 to 10%, preferably 0.01 to 5%, based on the total amount of the composition.

Examples of the sweetening agent include sweeteners such as sodium saccharin, stevioside, neohepyridine dihydrochalcone, glycyrrhizin, perylartin, p-methoxycinnamic aldehyde, tau martin, palatinose, maltitol, xylitol, . The sweetening agents may be used alone or in combination of two or more. When a sweetener is used, the content can be appropriately determined within a range that does not impair the effect of the present invention.

Examples of the preservative include paraoxybenzoic acid esters such as sodium benzoate, methylparaben, ethylparaben and butylparaben, ethylenediamine tetraacetate, and benzalkonium chloride. The preservative can be used singly or in combination of two or more kinds. When a preservative is used, the content can be appropriately determined within a range that does not impair the effect of the present invention.

Examples of the fragrance include natural fragrance, synthetic fragrance (single product fragrance), combined fragrance (preservative fragrance (oily fragrance), powder fragrance and the like). The perfume can be used singly or in combination of two or more kinds.

Examples of natural flavorings include natural flavors such as mastic oil, parsley oil, anise oil, eucalyptus oil, wintergreen oil, cacao oil, menthol oil, spearmint oil, peppermint oil, lemon oil, coriander oil, orange oil, mandarin oil, It is also possible to use it in a variety of ways, including, but not limited to, water, laurel oil, camomile oil, cardamom oil, caraway oil, bayeses, lemongrass oil, pine needle oil, neroli oil, rose oil, jasmine oil, iris concrete, Citrus oil, mix fruity oil, strawberry oil, cinnamon oil, clove oil, grape oil, time oil, sage oil, mint oil, rosemary oil, marjoram oil, olive oil, grapefruit oil, , And ownership.

Examples of the individual product flavorings include carbohydrates, anethole, methyl salicylate, cinnamic aldehyde, linalool, linalool acetate, limonene, menton, mentyl acetate, pinene, octylaldehyde, citral, , Anisaldehyde, ethyl acetate, ethyl butyrate, allyl cyclohexane propionate, methyl anthranilate, ethyl methyl anthranilate, vanillin, undecalactone, hexanal, ethynon alcohol, propyl alcohol, butanol, isoamyl alcohol , Cetanol, ogenol, ocimene, n-decyl alcohol, citronellol, alpha -terpineol, ethyl lactate, ethyl thioacetate, .

Combined flavor is a perfume made by combining a single product flavor and / or a natural flavor. For example, there can be mentioned menthol micron, strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, tropical fruit flavor, butter flavor, milk flavor, yogurt flavor, fruit flavor mix flavor, have.

The form of the perfume is not limited, and may be any of essential oils, extracts, solids, and powder obtained by spray drying any one of them. The perfume material is preferably used in an amount of 0.000001 to 1% in the formulation. It is preferable that the flavorings for inhalation using the perfume materials are used in an amount of 0.1 to 2.0% in the formulation.

Examples of the medicinal component include the following components: condensed phosphate,

Tartaric acid prevention agents such as ethanedioxy diphosphonate; An astringent such as sodium chloride; Strontium chloride, strontium acetate, zinc chloride, and the like. The content of the medicinal component in the case of using the medicinal ingredient can be appropriately set within a range that is pharmaceutically acceptable for each medicinal ingredient.

Examples of the coloring agent include colorants such as a safflower pigment, a gardenia yellow pigment, a gardenia blue pigment, a red pigment, a red pigment, a red cabbage pigment, a carrot pigment, a hibiscus pigment, a cacao pigment, a spilurina blue pigment, It is recommended to use a coloring agent such as Sona, Red No. 3, Red No. 104, Red No. 105, Red No. 106, Yellow No. 4, No. 5 No. 3, No. 3 No. Green No. 3, No. No. No. 1 Blue No. 1, riboflavin, copper chloropyrin sodium, . When a colorant is contained, its content is preferably 0.00001 to 3% with respect to the total amount of the composition.

Examples of the polishing agent include waxes such as shellac, carnauba wax and candelilla wax, and calcium stearate. When a brightener is contained, its content is preferably 0.01 to 5% based on the total amount of the composition.

When the composition of the present invention is an oral composition, the pH (20 ° C) is usually 6 to 10, preferably 7 to 9. Examples of the pH adjusting agent include acetic acid, hydrochloric acid, sulfuric acid, nitric acid, citric acid, phosphoric acid, gluconic acid, maleic acid, succinic acid, glutamic acid, sodium hydroxide, potassium hydroxide, sodium acetate, sodium carbonate, sodium citrate, sodium hydrogen citrate, Sodium and sodium dihydrogenphosphate; acids and alkalis; and buffers. When the pH adjusting agent is contained, the content thereof can be appropriately determined within a range that does not impair the effects of the present invention.

Examples of the solvent include water and lower alcohols having 3 or less carbon atoms such as ethanol and propanol. Solvents are usually contained in liquid-based oral compositions. When water is contained as a solvent, its content is preferably 20 to 95% with respect to the total amount of the composition. When a lower alcohol is contained as a solvent, its content is preferably 1 to 20% based on the total amount of the composition.

Examples of the excipient include starch syrup, glucose, fructose, phosgene, dextrin and oligosaccharides. When the composition for oral use is a food preparation, usually an excipient is contained. When an excipient is contained, its content can be appropriately determined within a range not to impair the effect of the present invention.

The pH (20 캜) of the oral composition of the present invention is usually 5 to 10, preferably 6 to 10, more preferably 6 to 9, further preferably 6 to 8 or 7 to 9 . Examples of the pH adjusting agent include acetic acid, hydrochloric acid, sulfuric acid, nitric acid, citric acid, phosphoric acid, gluconic acid, maleic acid, succinic acid, glutamic acid, sodium hydroxide, potassium hydroxide, sodium acetate, sodium carbonate, sodium citrate, sodium hydrogen citrate, Sodium, sodium dihydrogenphosphate, and the like, alkali, and a buffer. When the pH adjusting agent is contained, the content thereof can be appropriately determined within a range that does not impair the effects of the present invention.

[Formulation of oral composition of the present invention]

The shape and formulation of the oral composition of the present invention are not particularly limited. For example, it can be prepared into various shapes such as a liquid system (liquid, liquid, paste), solid (solid, solid), and the like. Examples of the formulations include dentifrice compositions such as kraft skirts, liquid skirts, liquid skirts and partial skirts, cushioning compositions, coating compositions, mouthwashes, mouthwash compositions, food compositions (for example, , Candy, gumi, film, troch, etc.). In the form of a food, any one of a confection, a candy, a chewing gum, a bean curd, and a film is preferable in terms of simplicity and portability that can be used regardless of time and place.

Examples of the candy include soft candy such as caramel, lucer, etc., hard candy such as drop, tapi, and the like, and although not particularly limited, hard candy is preferable in view of giving a high functional feeling. The hard candy can be produced by a routine method and is not particularly limited. For example, water is added to a raw material other than a functional ingredient and a flavoring agent, followed by pulverization at a high temperature (for example, 140 to 200 ° C) (For example, from 70 to 130 캜), adding a functional ingredient and a flavoring agent, and cooling and molding again. Water is added to the raw materials other than the functional ingredient and the flavoring agent and the mixture is cooled at a high temperature (140 to 200 ° C) and then cooled (for example, to 70 to 100 ° C) , A functional ingredient and a flavoring agent, and further cooling and shaping the mixture.

A chewing gum is a chewy elastic food made from a gum base and saccharides as main ingredients, and may have a sugar coating. It can be manufactured by the glowing black routine method, and is not particularly limited. For example, in the case of a plate-like casting needle, it is possible to manufacture by mixing each component containing the active ingredient in the present invention such as the component (A), and molding. In the case of sugar chewing gum of the present invention, the active ingredient in the present invention such as the component (A) may be contained in either or both of the sugar and the gum base, but is preferably contained in the sugar. Thus, the storage stability of the sugar chewing gum can be improved. The sugar chewing gum of such a sugar can be produced, for example, by mixing each raw material of the main chewing gum and then molding it with a sugar containing the active ingredient in the present invention such as the component (A) have. The content of the active ingredient in the present invention such as the component (A) in the sugar layer in the case of the sugar chewing gum of the sugar is preferably the mass% of each of the above-mentioned components relative to the total amount of the sugar.

As the chewing gum base compounded to the main chewing gum base, those commonly used for chewing gum can be used. The gum base may be a gum base such as a polyvinyl acetate resin having an average degree of polymerization of about 100 to about 1000, natural resins such as chicle, gel tub, sorber, polyisobutylene, polybutene, A plasticizer or softening agent such as a base resin, an emulsifier, calcium carbonate, calcium phosphate, a filler (such as talc), lanolin, stearic acid, sodium stearate, potassium stearate, glyceryl triacetate, glycerin, natural wax, Paraffin, and the like. A commercially available product can be used for the gum base, specifically, a gum base made by Natural Bass Co., Ltd., or a gum base made by Youth Co., Ltd. In addition, the gum base may contain a coloring agent such as natural color or titanium dioxide, such as gardenia, safflower, or red pepper.

The content of the gum base is preferably 10 to 50%, particularly preferably 15 to 30% based on the total amount of the composition.

The chewy gum is made of saccharides as the main raw material and compression-molded by a device such as a tablet machine, and may have sugar chains. The composition can be prepared by a routine method and is not particularly limited. For example, the ingredients can be mixed and compressed by a device such as a tablet machine (for example, under a pressure of 5 to 20 kN) .

When the application amount of the oral composition of the present invention to the human is applied, for example, three times per day, it is possible to appropriately adjust the amount to be used once to 0.5 to 2 g, preferably about 0.5 to 1 g.

The use of the composition of the present invention is not particularly limited, but from the viewpoint of the application site, for example, an oral composition (including a food and drink composition) can be mentioned. Examples of the composition for oral use include a dentifrice composition such as a soft skirt, a liquid skirt, a liquid skirt, and a split skirt, a curing agent composition, a citric acid curing agent composition, and a food and drink composition.

Other examples of the composition of the present invention include collagen coloration inhibiting composition, collagen decomposition inhibiting composition, dentin caries inhibiting composition, dental carotid blocking composition, pain relieving composition due to hypersensitivity, stain formation inhibiting or stain removing composition, .

The subject of application of the composition of the present invention is not particularly limited. For example, although it is not known whether the dentin crust and the dentin, dentin caries, dentin hypersensitivity and dentin caries are not affected or are affected, it is desirable to prevent dentin hypersensitivity and dentin caries And the like.

The composition of the present invention may be any of pharmaceuticals, quasi-drugs, cosmetics, and foods.

[Collagen coloring inhibitor]

The lactam compound or its salt, which is a component (A), is effective as an active ingredient of a collagen coloring inhibitor since it has an effect of suppressing coloration to collagen.

Collagen is present in animal tissues. Human collagen is classified into dozens of types, and the main collagen is type I. The collagen to be treated by the collagen coloring inhibitor of the present invention is not particularly limited, but collagen containing I-type collagen is preferable.

Collagen pigmentation means a change from the original color of the collagen to another color. The collagen coloration to be targeted by the collagen coloring inhibitor is preferably coloration of the collagen produced in the living body, and more preferably coloration of the dentin collagen layer. Examples of collagen coloration include coloring of dentin collagen layer by medicines, foods, and oral bacteria. When the dentin collagen layer is adhered to the dentinous caries, the dentin collagen layer is colored by applying the medicine in the treatment of the dentin dentin or in the treatment of the dentin caries. In addition, the same coloration may be caused by ingestion of food. By applying the collagen decomposition inhibitor of the present invention, the coloring can be suppressed. A major example of a drug that causes collagen pigmentation is polyphenol. Examples of polyphenols include flavonoids, phenylcarboxylic acids, chlorogenic acids, lignans, quercumin, and the respective examples of the component (2-B). In addition, food containing a large amount of polyphenol (for example, tea containing catechin, green tea, coffee containing chlorogenic acid, etc.) may cause coloring.

The dosage form of the collagen staining inhibitor of the present invention is not particularly limited. Examples thereof include oral administration (for example, oral administration, sublingual administration, etc.), parenteral administration (intravenous administration, intramuscular administration, subcutaneous administration, transdermal administration, . Of these, a dosage form having low invasiveness is preferable, and oral administration or transdermal administration is more preferable.

The subject to be ingested by the collagen coloring inhibitor of the present invention includes a subject who has already developed collagen coloration and wants to improve it, and a subject who does not develop collagen coloration but wants to prevent it. The administration timing of the agent of the present invention is not particularly limited.

[Collagen decomposition inhibitor]

The lactam compound or its salt, which is a component (A), is useful as an effective ingredient of a collagen decomposition inhibitor since it has a collagen decomposition inhibiting effect.

The collagen to be treated by the collagen decomposition inhibitor of the present invention is not particularly limited, but collagen containing I-type collagen is preferable.

When the collagen layer of the dentin is exposed and broken by the collagenase in dentin caries, the root of the tooth is substantially deficient. By applying the collagen decomposition inhibitor of the present invention to teeth, collagen decomposition can be suppressed or improved, so that dentin caries can be prevented.

Collagen degradation of periodontal tissue causes periodontal tissue problems such as gingival recession and alveolar bone absorption. Since the collagen decomposition inhibitor of the present invention can inhibit collagen degradation, the problem of periodontal tissue can be prevented.

The mode of administration of the collagen decomposition inhibitor of the present invention is not particularly limited. Examples of the dosage form and preferred examples are the same as the examples and preferred examples of the explanation of the collagen staining inhibitor.

The person to be ingested with the collagen decomposition inhibitor or the improvement agent of the present invention is a person suffering from the collagen degradation inhibitor or the improvement agent which has already developed symptoms of collagen degradation (for example, dental caries progression, periodontal tissue trouble (gingival recession, The person who thinks that he / she wants to, and the person who does not develop such symptoms but wants to prevent it. The administration timing of the agent of the present invention is not particularly limited.

[Antioxidant blocking agents]

The lactam compound and / or its salt as the component (A) is useful as an iv iv tubulin blocking agent because it has an early blocking effect on iv tubules.

The mode of administration of the dental tubular sequestrant of the present invention is not particularly limited. Examples of the dosage form and preferred examples are the same as the preferred and preferred examples among the descriptions of the collagen decomposition inhibitor.

The subject to be ingested with the dental caries blocking agent of the present invention is a person to whom the dentin hypersensitivity has already been developed and the person who wants to block the dental caries can not confirm whether the symptom is not onset or onset, And those who want to leave. The administration timing of the agent of the present invention is not particularly limited.

[Inhibition or improvement agent of dentin hypersensitivity]

The lactam compound and / or salt thereof as component (A) is useful as an agent for suppressing or improving dentin hypersensitivity because it has an early blocking effect on dentinal tubules and a pain relief effect.

The mode of administration of the dentin hypersensitivity suppressing or improving agent of the present invention is not particularly limited. Examples of the dosage form and preferred examples are the same as the preferred and preferred examples among the descriptions of the collagen decomposition inhibitor.

The subjects to whom the dentin hypersensitivity suppressing agent or the improvement agent of the present invention is to be ingested are those who have already developed dentin hypersensitivity and want to improve their symptoms and those who do not develop symptoms but want to prevent the dentin hypersensitivity. The administration timing of the agent of the present invention is not particularly limited.

[Stain remover]

The lactam compound or its salt as the component (A) is effective as an effective ingredient of a stain remover because it has an effect of removing stain which is contamination of a tooth.

A subject to be ingested by the stain remover of the present invention is a subject who thinks that the stain which is the contamination of teeth adheres to the subject and wants to remove the contamination. The administration timing and dosage form of the agent of the present invention are not particularly limited, but may be the same as the administration form of the above-mentioned composition.

Example

Hereinafter, the present invention will be described in detail by way of examples. The following embodiments are for explaining the present invention properly and do not limit the present invention. All percentages in the examples below represent the mass percentages.

Examples 1-1 to 1-30 and Comparative Examples 1-1 to 1-4

[Main raw materials used]

[Component (A)] [

(1) Pyrrolidone carboxylic acid (? -Lactam compound):

AJIDEW A-100 (registered trademark) " manufactured by Ajinomoto Co.,

(2) 6-oxo-2-piperidinecarboxylic acid (? -Lactam compound):

(S) -6-Oxo-2-piperidine carboxylic acid, manufactured by Sigma-Aldrich Japan Co.,

(3) 3- (2-oxo-1-azepanyl) propanoic acid (? -Lactam compound):

3- (2-Oxoazepan-1-yl) propanoic acid "available from Sigma-Aldrich Japan Co.,

[Comparative product of component (A)]

(4) Polyvinylpyrrolidone (lactam compound without acidic group):

Manufactured by Wako Pure Chemical Industries, Ltd., trade name "Polyvinylpyrrolidone K25"

(5) Proline (cyclic amino acid):

Manufactured by Wako Pure Chemical Industries, Ltd., trade name "DL-proline"

[Component (1-B)] [

(6) Sodium Fluoride:

Ltd., trade name " sodium fluoride "

(7) Sodium monofluorophosphate:

Sodium lauryl sulfate, sodium lauryl sulfate,

[Component (1-C)] [

(8) casein:

Quot; Casein (derived from milk) ", product of Wako Pure Chemical Industries, Ltd.

Sulfur content of amino acid (%): 3.0

Average molecular weight: 88000

Phosphate: Yes

(9) Lactoferrin:

Manufactured by Wako Pure Chemical Industries, Ltd., trade name " lactoferrin

Sulfur content of amino acid (%): 5.4

Average molecular weight: 86,000

Phosphorus: None

(10) Hydrolyzed Collagen:

Product name " HACP-U2 "

Sulfur content of amino acid (%): 1.5

Average molecular weight: 1500

Phosphorus: None

(11) Other additives other than the active ingredient:

(Sodium dodecylsulfate), carboxymethylcellulose sodium (dentifrice), anhydrous sodium sulfate (pH adjusting agent), citric acid (pH adjusting agent), sorbitol solution (viscous agent), sodium saccharin (sweetener), propylene glycol Silicate (abrasive), sodium lauryl sulfate (anionic surfactant), perfume

[Preparation of a skirt preparation]

1.0 kg (100 parts by mass) of a skirt preparation was prepared according to the following method of preparing a skirt preparation according to the mass ratio (parts by mass) shown in Tables 1 to 9 described below using the above-mentioned active ingredients.

(Preparation method of skirt preparation)

The following "(i) Active ingredient for phase A" and "(ii) Added ingredient for phase A" were mixed and dissolved in purified water at room temperature to prepare an A-phase. On the other hand, in the propylene glycol, the "(iii) B-phase additive component" was dissolved or dispersed at room temperature to prepare the B phase. Next, the phase B was added to and mixed with the phase A during the stirring to prepare the phase C. Finally, in the C phase, the following "(iv) C-phase additive component" was mixed at room temperature using a 1.5 L kneader (manufactured by Ishiyama Kogyo Co., Ltd.) (100 parts by mass). The content of each component was set as shown in Tables 1 to 9.

(Active ingredients and additives added to A phase, B phase and C phase)

(i) active ingredients for A: pyrrolidone carboxylic acid, 6-oxo-2-piperidinecarboxylic acid, 3- (2-oxo-1-azepanyl) propanoic acid, sodium fluoride, sodium monofluorophosphate , Casein, lactoferrin, hydrolyzed collagen

(Ii) Additives for A: sodium sorbitol, sodium saccharin, citric acid, sodium hydroxide

(Iii) Additive components for phase B: propylene glycol, sodium polyacrylate, sodium carboxymethylcellulose

(Iv) Additive components for C-phase: silicic anhydride, sodium lauryl sulfate, fragrance

Using each of the dentifrices obtained as described above, the dentin dental caries inhibiting effect and the formulation stability were evaluated as follows.

(Evaluation of Dental Caries Inhibitory Effect)

(1) A dentin block with a window on its surface was prepared from the umbrella root and immersed in a demineralized solution of acetic acid (100 mmol / l, pH 4.8) at 37 캜 for 6 hours to obtain a dental caries sample.

(2) Assuming that the skimming agent was diluted with the saliva during use, each skimming agent was diluted three times with distilled water, and each skimming agent treatment solution was obtained. A dental caries sample was immersed in each dental treatment solution for 3 minutes at room temperature, and then the dental treatment solution was lightly removed.

(3) A collagenase derived from Clostridium histolyticum (manufactured by Wako Pure Chemical Industries, Ltd.), 1.0 unit / ml of CaCl ₂ : 1.5 mmol / l, KH ₂ PO ₄ : 5.0 mmol / l, acetic acid 100 mmol / l, NaCl 100 mmol / Type 1A, made by Sig < RTI ID = 0.0 > mA). ≪ / RTI > Each of the cariogenic samples after the treatment of the above (2) was immersed in the remineralization solution under the conditions of 37 DEG C for 18 hours.

(4) Each of the dental caries samples after the treatment of (3) was immersed again in each dental treatment liquid for 3 minutes at room temperature, and the dental treatment liquid was removed lightly. Acetic acid (100 mmol / L) and pH 4.8 at 37 DEG C for 6 hours, and the demineralized solution was gently removed.

(5) The treatments of the above (2) to (4) were repeated once a day for three days in total.

(6) After the above three days of treatment, each of the cariogenic teeth samples was thoroughly rinsed with distilled water, and the sample was rinsed with a microcutter (MC-201 (trade name) The slices were cut out carefully under flowing water.

(7) The sample flakes ejected from the wet state were placed on a soft x-ray film (Kodak, "SO-343 (trade name)") TMR (Transverse Micro Radiography) image of each flake sample was obtained by irradiating soft X-ray (2.8 mA, 18 kVp) for 60 minutes by means of "

(8) Finally, the degree of delignification of each flake sample was confirmed as follows. Mineral profiles of TMR images of each flake sample were prepared from the TMR images of 15 aluminum step wedges taken together with the flake samples using an image analyzer ("PIAS-V (trade name)", manufactured by Pierce) . The mineral loss amount? Z (demineralization amount) was calculated from each obtained mineral profile.

The amount of demineralization of the sample (untreated group) not treated with the treatment liquid for the skimmed material was similarly calculated.

(9) The series of experiment operations were performed for each group (the example, the comparative example, and the non-treatment group) with N = 3, respectively. With respect to each group, the average value (average? Z) of each of the corners constituting the group was obtained, and the average? Z of the untreated group, the average? Z of the example, and the average? Z of the comparative example were obtained. The dentin dental caries inhibition rate was calculated from the "average ΔZ of the example" or "the average ΔZ of the comparative example" by the following equation (1-2), with the "average ΔZ of the untreated group"

[Equation 2]

The dental caries prevention effect of each example and comparative example was evaluated based on the following five criteria. If the following evaluation point is 3 or more, it may be considered that there is a good dentin caries prevention effect.

[Evaluation standard]

5 points: More than 70% dentin caries inhibition rate

4 points: dentin caries inhibition rate is 50% or more and less than 70%

3 points: 30% to less than 50% dentin caries inhibition rate

2 points: dentin dental caries inhibition rate is 10% or more and less than 30%

1 point: Less than 10% inhibition of dental caries

(Evaluation of stability of preparation)

Appearance of each of the examples and comparative examples immediately after the preparation of the skirt preparation was visually evaluated. The flavor immediately after the preparation of each of the examples and comparative examples was evaluated for sensory evaluation. Thereafter, samples stored for one month under an environment of 50 캜 were similarly evaluated.

Evaluation was made according to the following criteria.

[Evaluation standard]

A: No precipitation or sedimentation, no discoloration, no liquid separation, no layer separation. There is no deterioration of flavor.

B: Any or all of precipitation / sedimentation, discoloration, liquid separation, and flavor deterioration is slightly seen, but it is a problem-free level.

C: There is no problem immediately after preparation, but at least one of precipitation, precipitation, discoloration, liquid separation, and flavor deteriorates after storage at 50 캜 for one month.

D: At least one of precipitation / sedimentation, discoloration, liquid separation, and flavor is remarkably worse than immediately after production, which is problematic.

The dentin dental caries inhibiting effect and preparation stability of each of the examples and comparative examples evaluated according to the above evaluation methods and evaluation criteria are shown in Tables 1 to 9 below.

[Table 1]

In Examples 1-1 to 1-5 shown in Table 1, pyrrolidone carboxylic acid was used as the component (A), and (1- B) sodium fluoride is used as the component.

The dentin dental caries inhibiting effect of Examples 1-1 to 1-5 was evaluated to be 3 or more.

It is well known that fluorine compounds are effective for inhibiting caries. However, as shown in Comparative Example 1-1 to be described later, the evaluation of the dentin caries-inhibiting effect by the fluorine compound alone is 2, and the practical application is insufficient.

On the other hand, the evaluation of the dentin dental caries inhibition effect of the oral composition of the Example using the component (A) and the component (1-B) as an active ingredient was 3 or more, 3 is rated 4. Therefore, it can be seen that by using the component (A) and the component (1-B) simultaneously as the active component, a synergistic effect of the components (A) and (1-B) .

[Table 2]

In Examples 1-6 and 1-7 shown in Table 2, sodium fluoride was used as the component (1-B) without adding the component (1-C). In Example 1-6, 6-oxo-2-piperidinecarboxylic acid was used as the component (A), and 3- (2-oxo-1-azepanyl) propane I am using mountains.

The evaluation of the dentin caries inhibitory effect of Examples 1-6 and 1-7 is 3 and is good.

[Table 3]

In Examples 1-8 to 1-11 shown in Table 3, as in Examples 1-1 to 1-5 of Table 1, the components (1-C) were not added, and as the component (A) And sodium fluoride is used as the component (1-B).

The dentin dental caries inhibiting effect of Examples 1-8 to 1-11 was evaluated to be 3 or more, which is preferable. Among them, the evaluation of Examples 1-8 and 1-9 is 4. From this, it can be seen that the synergistic effect of the component (A) and the component (1-B) is obtained.

[Table 4]

In Examples 1-12 to 1-15 shown in Table 4, pyrrolidone carboxylic acid was used as the component (A) without adding the component (1-C). Sodium monofluorophosphate was used as the component (1-B) in Examples 1-12 and 1-13, and sodium fluoride was used in Examples 1-14 and 1-15.

The evaluation of the dentin dental caries inhibiting effect of Examples 1-12 to 1-15 is 3 or more and is good. Among them, in Examples 1-12 and 1-13, evaluation is 4. From this, it can be seen that the synergistic effect of the component (A) and the component (1-B) is obtained.

[Table 5]

In Examples 1-16 to 1-19 shown in Table 5, casein was used as the component (1-C), pyrrolidone carboxylic acid was used as the component (A), and fluorinated Sodium is used.

Evaluation of the dental caries-inhibiting effect of Examples 1-16 to 1-19 was 5. From this, it can be seen that a high dentin dental caries inhibiting effect is obtained by adding the (1-C) component to the component (A) and the component (1-B).

[Table 6]

In Examples 1-20 and 1-21 shown in Table 6, component (1-C) was added. Lactoferrin was used as the component (1-C) in Example 1-20, and hydrolyzed collagen was used as the component (1-C) in Example 1-21. In each of the examples, pyrrolidone carboxylic acid was used as the component (A) and sodium fluoride was used as the component (1-B).

The dentin dental caries inhibiting effect of Examples 1-20 and 1-21 was evaluated to be 5, and by adding the (1-C) component to the components (A) and (1-B) .

[Table 7]

In Examples 1-22 to 1-26 shown in Table 7, plural kinds of compounds are used in combination as an effective ingredient.

In Examples 1-22, pyrrolidonecarboxylic acid (? -Lactam compound) and 6-oxo-2-piperidinecarboxylic acid (? -Lactam compound) are used in combination as the component (A).

In Examples 1-23, pyrrolidone carboxylic acid (? -Lactam compound) and 3- (2-oxo-1-azepanyl) propanoic acid (? -Lactam compound) are used in combination as the component (A).

In Examples 1-24, 6-oxo-2-piperidinecarboxylic acid (隆 -lactam compound) and 3- (2-oxo-1-azepanyl) propanoic acid (竜 -lactam compound ).

In Examples 1-25, pyrrolidone carboxylic acid (? -Lactam compound), 6-oxo-2-piperidinecarboxylic acid (? -Lactam compound) and 3- (2- Oxo-1-azepanyl) propanoic acid (epsilon -lactam compound) are used in combination.

In Examples 1-26, pyrrolidonecarboxylic acid (? -Lactam compound) was used as the component (A), and sodium fluoride and sodium monofluorophosphate were used in combination as the component (1-B).

[Table 8]

In Examples 1-27 to 1-30 shown in Table 8, plural kinds of compounds are used in combination as an active ingredient.

In Examples 1-27, casein and lactoferrin are used together as the component (1-C).

In Examples 1-28, caseine and hydrolyzed collagen are used together as the component (1-C).

In Examples 1-29, lactoferrin and hydrolyzed collagen are used together as the component (1-C).

In Examples 1-30, casein, lactoferrin, and hydrolyzed collagen are used together as the component (1-C).

[Table 9]

In Comparative Example 1-1, sodium fluoride was used as the component (1-B) without using the component (A).

Comparative Examples 1-2 and 1-3 use a lactam compound and a similar lactam compound as comparative products of the component (A). In Comparative Example 1-2, polyvinyl pyrrolidone was used as a comparative product of the component (A). Polyvinylpyrrolidone is a lactam compound having no acidic group. In Comparative Example 1-3, proline was used instead of the comparative product of component (A). Proline is a cyclic amino acid.

In Comparative Examples 1-4, pyrrolidone carboxylic acid was used as the component (A) without using the component (1-B).

In Comparative Example 1-1, sodium fluoride was used as the component (1-B) without using the component (A). It is well known that fluorine compounds are effective for inhibiting caries. However, the evaluation of the dentin caries inhibitory effect by this fluorine compound alone is 2, and the practical use is insufficient.

In Comparative Examples 1-4, the stability of the preparation stability was evaluated as ○, but the evaluation of dentin dental caries inhibition was 1.

As is apparent from the evaluation results of Comparative Examples 1-1 and 1-4 and the evaluation results of the foregoing Examples, by using the component (A) and the component (1-B) simultaneously as an effective component, It is possible to obtain an effect more than the enemy effect.

Hereinafter, two formulations of the oral composition according to the present invention are shown. In this prescription example, dentin dental caries prevention effect similar to that of the oral composition of the above-described embodiment can be obtained.

[Table 10]

[Table 11]

Examples 2-1 to 2-36 and Comparative Examples 2-1 to 2-6

[Main raw materials used]

[Component (A)] [

(1) Pyrrolidone carboxylic acid (? -Lactam compound):

AJIDEW A-100 (registered trademark) " manufactured by Ajinomoto Co.,

(2) 6-oxo-2-piperidinecarboxylic acid (? -Lactam compound):

(S) -6-Oxo-2-piperidine carboxylic acid, manufactured by Sigma-Aldrich Japan Co.,

(3) 3- (2-oxo-1-azepanyl) propanoic acid (? -Lactam compound):

3- (2-Oxoazepan-1-yl) propanoic acid "available from Sigma-Aldrich Japan Co.,

[Comparative product of component (A)]

(4) Polyvinylpyrrolidone:

Manufactured by Wako Pure Chemical Industries, Ltd., trade name "Polyvinylpyrrolidone K25"

[Component (2-B)] [

(5) Rice seed extract (used in Examples and Comparative Examples other than Practical Examples 2-12 and 2-13):

Manufactured by Katakura Chikarin Co., Ltd., trade name "Ajijitekuto"

Rice seed extract content: 1%;

(6) Rice seed extract (used in Examples 12 and 13):

Manufactured by Katakura Chemical Co., Ltd., "Longan Seed Extract Powder SD"

Rice seed extract content: 83%;

(7) Proanthocyanidins:

"Gurinol SL" made by Kikkoman Corporation,

Proanthocyanidin content: 82%

(8) Catechin:

Manufactured by Daiyo Kagaku Co., Ltd., trade name " Sanphenone EGCg "

Catechin content: 95%

(9) Hesperidin:

Manufactured by Tokyo Chemical Industry Co., Ltd., trade name " methyl hesperidin "

Hesperidin content: 90%

[Comparison product of (2-B) component]

(10) Rosemary Extraction:

Manufactured by Maruzen Pharmaceutical Co., Ltd., trade name " RKC-87 "

Rosemary Extract Content: 1.5%

The compounding ratios of the respective polyphenol compounds shown in Tables 12 to 16 are the compounding ratios of the polyphenols contained in the respective commercial products in the raw materials of the respective compositions.

Experimental Example 2-1 Evaluation of inhibitory effect on collagen decomposition of dentin

[Preparation of a skirt preparation]

Each oral composition having the composition shown in Tables 12 to 16 was prepared. The preparation method is as follows. A phase obtained by mixing a water-soluble raw material (lactam compound, polyphenol compound, disodium hydrogenphosphate, sodium saccharin) in purified water containing 70% sorbitol and a B phase obtained by adding sodium alginate, carrageenan and methylparaben to propylene glycol Respectively. To the resultant mixture, anhydrous silicic acid, a flavoring agent and sodium laurylsulfate were mixed at room temperature in a 1.5 L kneader (manufactured by Ishiyama Kogyo Co., Ltd.). Thereafter, the mixture was subjected to degassing at a reduced pressure to 4 ㎪, and mixing was continued again to obtain a composition. The obtained composition was used within one week of preservation at room temperature to carry out the following evaluation.

[Assessment of inhibition of collagen decomposition]

The surface of the right root was polished to a width of about 2 mm for demetallization window to remove the cementum, and then a section of 250 탆 in thickness was cut out by a micro-cutter. Of the portions from which the cementate was removed, about 1.5 mm x 250 m was used for the demetallization window, and the other portions were covered with manicure. The nail polish was dried at room temperature and immersed in 0.1 mol / l of an aqueous acetic acid solution (pH 4.5) for 50 hours to prepare a hardened carious sample in which collagen was exposed in the window portion. This sample was immersed in a three-fold dilution of the composition of each of the examples and the comparative example for 5 minutes at room temperature, washed with distilled water, and incubated at 37 ° C in an artificial saliva (CaCl ₂ : 2.2 mmol / l, KH ₂ PO ₄ : 2.2 (Type 1A, manufactured by Sigma): 1.0 unit / ml, pH 6.5) containing 0.1 mg / m 2 / mol of acetic acid, 0.1 mol / l of acetic acid, and Clostridium histolyticum-derived collagenase. The composition treatment was carried out three times a day as morning, day and night, and the other times were immersed in artificial saliva containing collagenase, and the procedure was repeated for 4 days in total. After completion of the experiment, the hardened carious samples were observed under a microscope, and the depth of exposed collagen was measured at three points per one sample and averaged. The measurement was carried out with n = 3, and an average value was calculated. Collagen degradation inhibition rate was calculated by the following formula and evaluated according to the following criteria. In the following formulas, the examples or comparative groups are groups treated with the composition shown in the examples or comparative examples, and the control group indicates the groups not treated with the compositions shown in the examples and comparative examples. In each of the examples and comparative examples, n = 3 was also evaluated. The results are shown in Tables 12 to 16.

[Equation 3]

[Evaluation criteria for inhibiting collagen decomposition of dentin]

A: 70% to less than 90% inhibition of collagen decomposition in dentin

B: Suppression rate of dentin collagen degradation is 50% or more and less than 70%

C: Suppression rate of dentin collagen degradation is 20% or more and less than 50%

D: 0% to less than 20% inhibition of dentin collagen degradation

Experimental Example 2-2 Evaluation of inhibitory effect on collagen decomposition of dentin after storage (after preservation at 50 ° C for 1 month)

[Preparation of composition]

An oral composition having the compositions shown in Tables 12 to 16 similar to those in Experimental Example 2-1 was prepared and stored for 1 month in a high-temperature bath at 50 占 폚.

[Evaluation of dentin collagen decomposition inhibitory effect after storage]

The dentin collagen decomposition inhibition evaluation after preservation was carried out using the preserved product composition. The evaluation method, the calculation method of dentin collagen decomposition inhibition rate, and the evaluation criteria were all the same as those in Experimental Example 2-1.

EXPERIMENTAL EXAMPLE 2-3 Evaluation of inhibitory effect on dentin collagen staining after storage (after preservation at 50 ° C for 1 month)

[Preparation of a skirt preparation]

An oral composition having the compositions shown in Tables 12 to 16 similar to those in Experimental Example 2-1 was prepared and stored for 1 month in a high-temperature bath at 50 占 폚.

[Evaluation of dentin collagen coloration inhibition after storage]

The right root was cut into a block shape, and the cement material was removed by surface polishing. About 3.5 mm x 3.5 mm of the part from which the cement was removed was used for demineralization window, and the other part was covered with manicure. The nail polish was dried at room temperature and immersed in 0.1 mol / l of an aqueous acetic acid solution (pH 4.5) for 72 hours to prepare a hardened carious sample in which collagen was exposed in the window portion. First, color differences (L * 0, a * 0, b * 0) were measured as initial values. Next, the immersion for 5 minutes at room temperature the sample in each case carried out, and 3 multiple dilutions of the comparative examples of the composition, and then washed with distilled water, artificial saliva of _{37 ℃ (CaCl 2: 2.2m㏖ /} ℓ, KH 2 PO ₄ : 2.2 mmol / l, acetic acid: 0.1 mol / l, and collagenase from Clostridium histolyticum (Type 1A, Sigma): 0.1 unit / ml, pH 6.5). The composition treatment was carried out three times a day as morning, day and night, and the other times were immersed in artificial saliva containing collagenase, and the procedure was repeated for 4 days in total. After the end of the experiment, the color difference (L * 1, a * 1, b * 1) was measured with n = 3 and the average value was calculated. The color difference was measured using a spectroscopic colorimeter (CM-2022, manufactured by Konica Minolta Co., Ltd.), and the coloring inhibition effect was evaluated from the value of? E calculated by the following formula (2-2) And evaluated based on the criteria. The results are shown in Tables 12 to 16.

△ E value = ((L * 1-L * 0) 2 + (a * 1-a * 0) 2 + (b * 1-b * 0) 2) 1/2

[Evaluation standard]

A: 0? DELTA E < 2.0

B: 2.0? DELTA E < 4.0

C: 4.0? DELTA E < 6.0

D: 6.0? DELTA E < 8.0

Experimental Example 2-4 Evaluation of formulation stability (after 1 month storage at 50 ° C)

As in Experimental Example 2-1, a skimming agent having the compositions shown in Tables 12 to 16 was prepared and stored for 1 month in a high-temperature bath at 50 占 폚. The appearance after preservation was visually confirmed, and the preparation stability (discoloration and retention property) was evaluated based on the following evaluation criteria.

[Evaluation standard]

A: Discoloration of the composition extracted from the tube is not recognized, and there is no problem in shape-forming

B: There is almost no problem in discoloration and formation of the composition extracted from the tube

C: There is a slight problem in discoloration and / or formation of the composition extracted from the tube

D: The composition extracted from the tube has considerable problems in discoloration and / or formation of beads.

The results of Experimental Examples 2-1 to 2-4 relating to the oral compositions of Examples and Comparative Examples are shown in Tables 12 to 16.

[Table 12]

[Table 13]

[Table 14]

[Table 15]

[Table 16]

The following can be seen from Tables 12 to 16. (Examples 2-34 to 2-36) using the component (A) (Examples 2-34 to 2-36) retained excellent dentin collagen decomposition inhibitory effects equivalent to those before storage even after storage at 50 ° C for 1 hour. In addition, the dentin collagen decomposition inhibitory effect of the preparation of the oral composition (Examples 2-34 to 2-36) was superior to that of the oral composition using polyvinylpyrrolidone (Comparative Example 2-5). (A) and (2-B), each of the components (A) and (2-B) (Comparative example) using each of the comparative products of the comparative products of the present invention, the dentin collagen degradation inhibitory rate was remarkably high and the dentin collagen degradation inhibitory effect persisted even after the preparation was stored at 50 캜 for 1 month . Further, the oral composition (Example) in which the ingredient (A) was blended or the ingredient (A) and the ingredient (2-B) were blended had remarkable inhibition of coloration to the dentin collagen by the polyphenol component In addition, discoloration after preservation of the preparation is remarkably suppressed. These results indicate that the oral composition of the present invention can sufficiently exhibit a dentin collagen decomposition inhibiting effect, an effect of inhibiting dentin collagen decomposition after storage, an effect of inhibiting dentin collagen coloring after storage, and a formulation stability in a balanced manner. These results also show that the oral composition (2) is remarkably excellent in both dentin collagen decomposition inhibitory effect, dentin collagen decomposition inhibitory effect after storage, dentin collagen coloring inhibitory effect after storage, and formulation stability.

Here are some other prescriptions. Even in such a case, the same effects as those of the above-described embodiment can be obtained.

[Table 17]

[Table 18]

[Table 19]

[Table 20]

[Table 21]

[Table 22]

[Table 23]

[Table 24]

Examples 3-1 to 3-26 and Comparative Examples 3-1 to 3-3

[Main raw materials used]

[Component (A)] [

(1) Pyrrolidone carboxylic acid (? -Lactam compound):

AJIDEW A-100 (registered trademark) &quot; manufactured by Ajinomoto Co.,

(2) 6-oxo-2-piperidinecarboxylic acid (? -Lactam compound):

(S) -6-Oxo-2-piperidine carboxylic acid, manufactured by Sigma-Aldrich Japan Co.,

(3) 3- (2-oxo-1-azepanyl) propanoic acid (? -Lactam compound):

3- (2-Oxoazepan-1-yl) propanoic acid "available from Sigma-Aldrich Japan Co.,

[Comparative product of component (A)]

(4) Polyvinylpyrrolidone:

Manufactured by Wako Pure Chemical Industries, Ltd., trade name "Polyvinylpyrrolidone K25", manufactured by Wako Pure Chemical Industries, Ltd.

(5) Proline:

Manufactured by Wako Pure Chemical Industries, Ltd., trade name "DL-proline"

[Component (3-B)] [

(6) Aluminum lactate:

Manufactured by Wako Pure Chemical Industries, Ltd., trade name "Lactic acid aluminum"

[Component (3-C)] [

(7) Sodium monofluorophosphate:

Purchased from Rhodia Japan, trade name &quot; sodium monofluorophosphate &quot;

[Component (3-D)] [

(8) Potassium nitrate:

Manufactured by Wako Pure Chemical Industries, Ltd., trade name "potassium nitrate"

The following "(i) Active ingredient for A" and "(ii) Added ingredient for A" were mixed and dissolved in purified water at room temperature to prepare an A-phase. On the other hand, in the propylene glycol, the "(iii) B-phase additive component" was dissolved or dispersed at room temperature to prepare the B phase. Next, the phase B was added to and mixed with the phase A during the stirring to prepare the phase C. Finally, in the C phase, the following "(iv) C-phase additive component" was mixed at room temperature using a 1.5 L kneader (manufactured by Ishiyama Kogyo Co., Ltd.) (100 parts by mass). The blending amounts of the respective components were as shown in Tables 25 to 29.

(Active ingredients mixed in phase A, phase B, and phase C and other additives)

(i) active ingredients for A: pyrrolidone carboxylic acid, 6-oxo-2-piperidinecarboxylic acid, 3- (2-oxo-1-azepanyl) propanoic acid, aluminum lactate, sodium monofluorophosphate , Potassium nitrate

(Ii) Additive component for A: 70 mass% Sorbitol, sodium saccharin, sodium hydroxide

(Iii) Additive components for the B-phase: propylene glycol, xanthan gum, carboxymethylcellulose sodium, methylparaben

(Iv) Additive components for C-phase: silicic anhydride, sodium lauryl sulfate, fragrance

Evaluation of early ivory tubule blocking effect, pain relief effect, and feeling of use (taste) of each of the skins obtained as described above was performed according to the following Experimental Examples 3-1 to 3-3.

(Experiment 3-1) Evaluation of early blocking effect of iv

Resins of the dentinal tubules were measured by the modified method of Pashley's method (J. Dent. Res. 57, 187-193, 1978) using the prepared dentifrice, The early blocking effect was evaluated.

A dentin disc having a thickness of 3 mm was cut out from the crown of a human molar and was polished with a domestic abrasive paper # 2000 and further etched with a 37% aqueous phosphoric acid solution to obtain a dentinal tubule As a sample. 20 g of artificial saliva of pH 7.0 containing 10 g of each skirt, 1.5 mM of CaCl ₂ , 2.5 mM of KH ₂ PO ₄ , 0.1 M of equivalent amount of NaCl, 0.1 M of acetic acid and 1.0 unit / ml of acid phosphatase, And mixed to give a 3-fold dilution, which was used as a treatment solution. The reason for the 3-fold dilution is that it was assumed that the skirt was diluted three times by the saliva. The sample was immersed in the treatment solution for 3 minutes, gently rinsed with distilled water to remove the excess treatment solution, and immersed in the artificial saliva solution at 37 캜 for 15 hours. The sample was rinsed well with distilled water, the water was removed, and the sample was immobilized on the apparatus. Distilled water was flown for 5 minutes under a constant pressure, and the amount of distilled water per unit time (5 minutes) passing through the sample was measured. The percent inhibition of passages in the examples and comparative examples was calculated (equation (3-1)). In each of the examples and comparative examples, the evaluation was N = 5, and the average value of the passage inhibition rate of the samples constituting each example was calculated. When the average value was 60% or more, Early blocking effect.

[Equation 4]

Footnote (*) in equation (3-1)

The passing amount means the distilled water amount (쨉 l) passed in 5 minutes.

(Experiment 3-2) Evaluation of pain relief effect

Three subjects with sensory hypersensitivity who had a temporary pain at the time of rinsing the water after the skirt were considered subjects. As in Experimental Example 3-1, the subjects were polished twice a day using the prepared skimming agent. After 2 days, the degree of pain at the time of rinsing the water immediately after brushing was rated based on the following rating criteria (1 to 5 points), and the pain relief effect was evaluated from the average of three scores. In addition, the degree of the pain before the start of the test was one point of the lower grade standard in all the subjects.

[Criteria of pain rating]

5 points: I do not feel pain

4 points: I rarely feel pain

3 points: I feel a little pain but no problem

2 points: I feel a little pain.

1 point: I feel a lot of pain.

[Evaluation criteria for pain relief effect]

A: Average 5 points

B: Average of 4 points or more and less than 5 points

C: Average 3 points or more and less than 4 points

D: Average 2 points or more and less than 3 points

E: less than average 2

(Experiment 3-3) Evaluation of feeling (taste)

For the three subjects in Experiment 3-2, a questionnaire was asked about the feeling of use (taste) which synthesized the arine taste, metal taste, odd taste, etc. of each skirt when evaluating the pain relief effect. In the questionnaire, scores were given based on the following rating criteria (1 to 4 points). The feeling of use (taste) of each skirt was evaluated from the average of scores of three subjects.

[Feeling (taste), based on the rating]

4 points: Good

3 points: slightly better

2 points: Slightly bad

1 point: Bad

[Evaluation criteria for feeling (taste)]

A: Average of 3.5 points or more

B: Average of 3.0 points or more and less than 3.5 points

C: Average of 2.0 points or more and less than 3.0 points

D: Average value less than 2.0

[Table 25]

[Table 26]

[Table 27]

[Table 28]

[Table 29]

From the results of Experimental Examples 3-1 to 3-3 shown in Tables 25 to 29, the following can be seen. (3-B) was used alone, or the component (A) was used alone, or the dentifrice early blocking effect, the pain relief effect and the feeling of use (Comparative Examples 1 to 3) using a comparative product (polyvinylpyrrolidone or proline). The early blocking effect, pain relief effect and feeling on use (taste) of the dentifrice composition of Example 3-1 to 3-25 combined with the component (A) and the component (3-B) (Example 3-26, Comparative Examples 3-1 to 3-3) using the component (A-3) alone or the comparative product (polyvinylpyrrolidone or proline) Lt; / RTI &gt; (3-16) to (3-19) in which the (3-C) component was added in addition to the component (A) and the component (3-B). Further, in the case of the skirt preparation containing the component (D) (Examples 3-24 and 3-25), the pain relief effect was excellent. Alternatively, in the case of the skirt preparation containing the components (3-C) and (3-D) (Examples 3-20 to 3-23), the early blocking effect and the pain relief effect of iv iv tubules were excellent.

These results indicate that the oral composition of the present invention is excellent in an early blocking effect of dentinal tubules, a pain relief effect, and a feeling of use (taste). These results also show that the oral composition (3) of the present invention is remarkably excellent in an early blocking effect on dentinal tubules, a pain relief effect and a feeling of use (taste).

Here are some other prescriptions. In this prescription, the same effects as those of the above-described example can be obtained.

[Table 30]

[Table 31]

[Table 32]

Examples 4-1 to 4-22 and Comparative Example 4-1

[Main raw materials used]

[Component (A)] [

(A-1): pyrrolidone carboxylic acid

AJIDEW A-100 (registered trademark) "made by Ajinomoto Co., Ltd.

(A-2): 6-oxo-2-piperidinecarboxylic acid

(S) -6-Oxo-2-piperidine carboxylic acid, manufactured by Sigma-Aldrich Japan Co.,

(A-3): 3- (2-oxo-1-azepanyl) propanoic acid

3- (2-Oxoazepan-1-yl) propanoic acid "available from Sigma-Aldrich Japan Co.,

[Component (B)] [

(B-1): Potassium nitrate

Made by Wako Pure Chemical Co., Ltd.

[Component (C)] [

(C-1): sodium fluoride

Ltd., trade name &quot; sodium fluoride &quot;

(C-2): Sodium monofluorophosphate

Sodium lauryl sulfate, sodium lauryl sulfate,

[Other components added]

(Viscosity adjuster), sodium carboxymethyl cellulose (dentifrice), sodium hydroxide (pH adjusting agent), sodium saccharin (sweetener) ), Perfume, methylparaben (preservative), purified water (solvent)

Using the above-mentioned components, 1.0 kg (100 parts by mass) of a skirt preparation was prepared according to the blending ratio (parts by mass) shown in Tables 33 to 35 by the following method of preparing a skirt preparation.

(Preparation method of skirt preparation)

The following "I active ingredient for I phase" and "(ii) I phase additive ingredient" were mixed and dissolved in purified water at room temperature to prepare I phase. On the other hand, the following "(iii) II addition component for commercial use" was dissolved or dispersed in propylene glycol at room temperature to prepare phase II. Next, the II phase was added and mixed in the I phase in the stirring to prepare the III phase. Finally, in the phase III, the following "(iv) III added component for commercial use" was mixed at room temperature using a 1.5 L kneader (manufactured by Ishiyama Kogyo Co., Ltd.) (100 parts by mass). The blending amounts of the respective components were as shown in Tables 33 to 35.

(Active ingredient combined with phase I, phase II, and phase III and other additives)

(i) Active ingredient for I-phase: pyrrolidone carboxylic acid, 6-oxo-2-piperidinecarboxylic acid, 3- (2-oxo-1-azepanyl) propanoic acid, potassium nitrate, sodium fluoride

(Ii) Addition ingredients for I-phase: 70% by mass Sorbitol, sodium saccharin, sodium hydroxide

(Iii) Commercial additives: Propylene glycol, carboxymethyl cellulose sodium, methyl paraben

(Iv) III Additives for commercial use: Anhydrous silicic acid, sodium lauryl sulfate, fragrance

With respect to each of the dental preparations obtained as described above, the alleviation effect on the pain caused by the hypersensitivity and the feeling of use (taste) were evaluated as follows.

(Assessment of relief effect on pain caused by sensory irritation)

Of the 23 types of skins prepared as described above, 8 subjects (total of 24 subjects) were selected as one group of three subjects who suffered from sensory hypersensitivity with teeth having a transient pain at the time of rinsing with water after skirt rinsing Quot; Practical Examples 4-1 &quot; to &quot; Practical Examples 4-8 &quot;) were assigned to the respective groups, and the wiping was performed twice a day for three days. After the fourth day, with respect to all the groups, the flaw removal was performed in the same manner twice a day by using the Furacebosomma agent prepared by removing the active ingredient from the I phase. The score of the pain at the time of rinsing with water immediately after the brushing after 1 week after switching to Furazebo was changed according to the following score, and the average value of the scores of the three subjects was calculated for each group.

After the interval of about 3 weeks, eight other kinds of skirts (the skirts of Examples 4 to 9 and 4-16) were assigned to each of the 24 subjects in the total of the 8 groups And the same evaluation test was carried out.

After the interval of 3 weeks was made again, seven kinds of skirts (the "Practical Example 4-17" to "Practical Example 4-22", "Comparative Example 4-1" Were assigned to each group, and similar evaluation tests were conducted.

Based on the average value of the scores calculated for each skimming agent, the mitigation effect on the pain caused by the hypersensitivity was evaluated based on the following evaluation criteria. In addition, the degree of pain before the start of each evaluation test was one point in all the subjects on the basis of the following score.

[Based on the score of the degree of pain]

5 points: I do not feel pain

4 points: I rarely feel pain

3 points: I feel a little pain but no problem

2 points: I feel a little pain.

1 point: I feel a lot of pain.

[Evaluation criteria for relieving pain caused by sensory irritation]

A: Average of 4.5 points or more and 5.0 points or less

B: Average of 4.0 points or more and less than 4.5 points

C: Average 3 points or more and less than 4 points

D: Average 2 points or more and less than 3 points

E: less than average 2

(Evaluation of feeling (taste))

In the evaluation test on the pain relieving effect due to the hypersensitivity, a questionnaire was conducted on the feeling of use (taste) synthesizing the arine taste, metal taste, odd taste, etc. of the skirt preparation for each group of subjects, Scores (1 to 4 points) were attached based on the score criteria, and an average value was calculated. The feeling of use (taste) was evaluated from the average value of the calculated scores on the basis of the following evaluation criteria.

[Feeling (taste) score basis]

4 points: Good

3 points: slightly better

2 points: Slightly bad

1 point: Bad

[Evaluation criteria for feeling (taste)]

A: Average of 3.5 points or more

B: Average of 3.0 points or more and less than 3.5 points

C: Average of 2.0 points or more and less than 3.0 points

D: Average value less than 2.0

The pain relief effects and feelings (taste) of each example and comparative example evaluated according to the above evaluation method and evaluation criteria are described in Tables 33 to 35. &lt; tb &gt; &lt; TABLE &gt;

[Table 33]

[Table 34]

[Table 35]

The rinse agent of Comparative Example 4-1 containing no component (A) but containing the component (4-B) had a tendency to be affected by crustal hypersensitivity at the time of rinsing the water immediately after rinsing after 1 week from conversion to Furazebo The pain relief effect was almost not achieved and the feeling (taste) was poor (Table 35).

The skimmed preparations of Examples 4-22 containing no component (4-B) and containing the component (A) had the same effect as that of Comparative Example 4-1, (Table 35). The results are shown in Table 35. The results are shown in Table 35.

On the other hand, the rinse agents of Examples 4-1 to 4-21 containing the component (A) in combination with the component (4-B), even when rinsing the water immediately after rinsing for one week after the conversion to Furazebo, It has been confirmed that pain caused by hypersensitivity is effectively reduced and a significant reduction effect on pain due to hypersensitivity is obtained (Tables 33 and 34). It was also confirmed that the skirt preparations of Examples 4-1 to 4-21 had a good feeling (taste).

The skim preparations of Examples 4-16 to 4-21 containing the (4-C) component in addition to the component (A) and the component (4-B) (4-C) component, the effect of the component (A) is further enhanced, and the pain caused by the hypersensitivity is reduced. (Compared with Examples 4-11 and 4-16 to 4-19, and Example 4-2 with Examples 4-20 and 4-21) ).

Three formulations of the oral composition according to the present invention are shown below. Even in such a prescription, a remarkable alleviation effect on the pain caused by the hypersensitivity similar to that of the oral composition of the above-described embodiment and a good feeling of use (taste) can be obtained.

[Table 36]

[Table 37]

[Table 38]

Examples 5-1 to 5-14 and Comparative Examples 5-1 to 5-5 (skirt preparation)

A skirt preparation having the compositions shown in Tables 39 to 41 was prepared. That is, an A phase in which a water-soluble component (component (A), component (5-B), sodium fluoride, sodium saccharin, sorbitol, etc.) was mixed and dissolved at room temperature was prepared in purified water. On the other hand, B-phase was prepared by dissolving or dispersing an oil-soluble component such as methylparaben, sodium polyacrylate, sodium alginate, etc. as a binder in propylene glycol at room temperature. Next, the phase B was added to and mixed with the phase A during the stirring to prepare the phase C. In the C phase, perfume, silicic anhydride and other components (sodium laurylsulfate, etc.) were mixed at room temperature using a 1.5 L kneader and subjected to degassing at a reduced pressure of 4 kPa to prepare respective compositions. The units of the blending amounts of the components in Tables 39 to 41 are% by mass.

[Main raw materials used]

[Component (A)] [

(1) Pyrrolidone Carboxylic Acid:

AJIDEW A-100 (registered trademark) &quot; manufactured by Ajinomoto Co.,

(2) 6-Oxo-2-piperidinecarboxylic acid:

(S) -6-Oxo-2-piperidine carboxylic acid, manufactured by Sigma-Aldrich Japan Co.,

(3) 3- (2-oxo-1-azepanyl) propanoic acid (? -Lactam compound):

3- (2-Oxoazepan-1-yl) propanoic acid "available from Sigma-Aldrich Japan Co.,

[Comparative product of component (A)]

(4) Polyvinylpyrrolidone:

Manufactured by Wako Pure Chemical Industries, Ltd., trade name "Polyvinylpyrrolidone K25"

(5) Proline:

Manufactured by Wako Pure Chemical Industries, Ltd., trade name "DL-proline"

[Component (5-B)] [

(6) Hydroxyethyl cellulose Dimethyldiallylammonium chloride:

Japan, a trade name &quot; Cellcoat L-200 &quot;

(7) O- [2-hydroxy-3- (trimethylammonio) propyl] hydroxyethyl cellulose chloride:

Lion Corporation, product name "Leogado GP" (low viscosity product)

(8) O- [2-hydroxy-3- (trimethylammonio) propyl] hydroxyethyl cellulose chloride:

Quot; POISE C-150L &quot; (product of high viscosity) manufactured by Kao Chemical Co.,

[Comparative product of (5-B) component]

(9) Cationic guar gum:

Product name: JAGUAR C-13S

[Other components]

(10) Sodium Fluoride:

Ltd., trade name &quot; sodium fluoride &quot;

The dummies of the examples and comparative examples were provided in Experimental Examples 5-1 to 5-4 described below.

Experimental Example 5-1 Evaluation of Stain Formation Inhibitory Effect

1. Preparation of Green Tea Extract

The green tea extract was prepared by the extraction method described in the food ingredient analysis method. That is, a tea pack containing 3 g of green tea leaves (a 980-car tea of house-grown tea, made by Itoen Co., Ltd.) was added to 100 ml of tap water at about 90 ° C and extracted for 2 minutes.

2. Evaluation of Stain Formation Inhibitory Effect Using Hydroxyapatite (HA) Disk

The color difference (color difference) of the HA of the initial HA of the HA disk (APP-735; manufactured by Pentax KK) polished with the sandpaper # 1500 was measured with a spectroscopic colorimeter (CM2022, manufactured by Konica Minolta Co., Ltd.). Next, six HA discs were mounted on the mouthpiece and fixed on the lingual side of eleven volunteers. The immobilization time was 1 hour, followed by agitation washing in distilled water, and immersion for 5 minutes in green tea extract. The dentifrice of each example was diluted 3 times with distilled water, and the HA discs were centrifuged at the centrifugal supernatant (room temperature, 20 minutes, 10,000 rotations) And immersed for 5 minutes. After that, it was lightly washed with distilled water, and the excess water was sucked into the filter paper. The reason for using a 3-fold dilution solution is that it was assumed that the skirt was diluted by saliva during brushing. The reason for rinsing by the distilled water is that it is presumed that after the use of the skimming agent. Immersed in the oral cavity, immersed in the green tea extract and immersed in the treatment solution twice a day, and immersed in physiological saline for another time. This operation was repeated for 14 days, and the color difference of HA was measured with a spectroscopic colorimetric system, and the degree of coloring was evaluated by the b * value of the L * a * b * colorimetric system. The b * value was calculated by the following formula (5-0).

Equation (5-0):

(? B * value) = b * value after 14 days treatment - initial b * value

[Evaluation criteria for inhibiting stain formation]

A series of experimental manipulations were carried out with n = 3 for each of the examples and comparative examples, and the average value of the respective? B * values was calculated, and the effect of inhibiting stain formation was evaluated by the following evaluation criteria.

A:? B * value is less than 0.5

B:? B * value is 0.5 or more and less than 3.0

C:? B * value is not less than 3.0 and less than 6.0

D:? B * value is less than 6.0

EXPERIMENTAL EXAMPLE 5-2 Evaluation of Stain Removal Effect

1. Preparation of concentrated black tea

Three bags of a tea tea bag (manufactured by Japan Tea Daily Club, manufactured by Mitsui Agriculture & Forestry Co., Ltd.) were added to 200 mL of distilled water, which was then extracted for 10 minutes. Thereafter, the supernatant was filtered through a filter paper (No. 5C, manufactured by Adobantech Touyang Co., Ltd.) to obtain a concentrated black tea extract.

2. Creating a model stain

The surface of the HA (hydroxyapatite) disk (APP-735; manufactured by Hoya Co., Ltd.) was polished by sand blasting and then the HA disk was immersed in a 0.5 mass% albumin solution for 20 minutes, And then immersed in a ferric chloride solution for 20 minutes and a 0.3 mass% ferric chloride solution for 20 minutes in that order. This procedure was repeated 20 times in total to prepare a model stain.

3. Model stain removal test

The L * value of the L * a * b * colorimetric system was measured in the same manner as in Experiment 1, and the L * value of the HA disk before the model stain formation was measured as CM * 0. Next, the chromaticity of the model stain prepared as described above was measured as chromaticity (L * 1) before cleaning.

To the HA disk on which the model stain was formed, 1 ml of a solution in which the skimming agent of each example was diluted by three times with distilled water was impregnated into the head of a toothbrush (Kurinikaharashii 4 columns, manufactured by Lion Corporation) Followed by brushing for a minute (cleaning). After rinsing, the HA disk was rinsed lightly with distilled water, and excess water was sucked through the filter paper. After the HA disk was dried, the chromaticity (L * 2) was measured after the scintillation. From these measured values, the stain removal ratio was obtained by the following formula (5-1).

[Equation 5]

[Evaluation Criteria of Stain Removal Effect]

A series of experimental operations were carried out with n = 3 for each of the examples and comparative examples, and the average value of the respective stain removal rates was calculated. The stain removal effect was evaluated based on the following evaluation criteria.

A: More than 80% stain removal rate

B: Stain removal rate is 60% or more and less than 80%

C: Stain removal rate from 30% to less than 60%

D: Stain removal rate less than 30%

EXPERIMENTAL EXAMPLE 5-3 Evaluation of gloss effect

The skins of each example were diluted 3-fold with distilled water to an HA disk (APP-735; manufactured by Pentax KK) polished with a sandpaper # 3,500 on the surface to be tested, and centrifuged at that time for 20 minutes at 10,000 rpm , And these HA disks were immersed for 5 minutes. After that, it was lightly washed with distilled water, and the excess water was sucked into the filter paper. Then, it was immersed at 37 캜 in artificial saliva (CaCl ₂ : 1.0 mmol / l, KH ₂ PO ₄ : 3.0 mmol / l, acetic acid: 100 mmol / l, NaCl: 100 mmol / l, pH 6.5). This operation was performed three times a day for three consecutive days in total.

[Evaluation criteria of gloss effect]

Three days later, the HA disk was taken out, rinsed well with distilled water, and naturally dried, and the gloss effect was evaluated by five persons on the basis of the rating of the evaluator described below. The experiment was carried out with n = 3 in each of the examples and the comparative examples. Finally, the average value of the rating of the evaluator was calculated and evaluated based on the average value of the gloss effect.

(Based on the rating of the evaluator)

3: Glossy on the front

2: Glossy except for some

1: Some are glossy

0: No gloss (no change)

(Based on the average of the evaluator's ratings)

A: 2.5 points or more

B: 1.6 points or more and less than 2.5 points

C: 0.5 point or more and less than 1.6 point

D: Less than 0.5

EXPERIMENTAL EXAMPLE 5-4.

Each treatment was diluted three times with distilled water, and the treatment solution was applied to five panelists for 30 seconds.

[Evaluation Criteria of Product Use Feeling]

The feeling of feeling of preparation after use of the treatment liquid was evaluated on the basis of the following rating. Finally, the mean value of 5 persons was calculated and evaluated based on the average value of the product use feeling.

(Based on the rating of the evaluator)

3: Good use feeling

2: I feel a little bitter and unpleasant taste

1: Bitter and unpleasant taste is felt

0: I feel strong bitter and unpleasant taste

A: 2.5 points or more

B: 1.6 points or more and less than 2.5 points

C: 0.5 point or more and less than 1.6 point

D: Less than 0.5

[Table 39]

[Table 40]

[Table 41]

The composition of Example 5-14 containing component (A) was excellent in stain removal effect and feeling of preparation use (Table 41). The compositions of Examples 5-1 to 5-13 containing the component (A) and the component (5-B) were well balanced and excellent in the stain formation inhibiting effect, the stain removing effect, the glossing effect, 40). On the other hand, among the compositions of the comparative examples lacking the component (B), none of the above four effects were satisfied (Table 41). This result shows that the oral composition of the present invention contains the ingredient (A) and the ingredient (5-B), thereby exhibiting excellent stain formation inhibitory effect, stain removal effect, gloss effect, and feeling of product use.

Examples 5-15 to 5-17 (remedy)

An example of the three-agent system is shown below.

A specified amount of purified water was added to a container made of stainless steel equipped with a three-one motor and a stirrer having a rotating blade, and water-soluble components such as component (A), component (5-B) And the mixture was added and dissolved while stirring. On the other hand, a prescribed amount of an organic solvent such as ethanol was added to another container made of stainless steel equipped with a three-one motor and a stirrer having a rotating blade, and an oil soluble component such as perfume or methylparaben was added and dissolved while stirring . Again, an oil-soluble component was added to a vessel in which the water-soluble component had been dissolved, and the mixture was stirred for 30 minutes to prepare a homogeneous solution.

[Table 42]

[Table 43]

[Table 44]

Examples 6-1 to 6-14 and Comparative Examples 6-1 to 6-2

In Example 5-1, a skimming agent was prepared in the same manner as in the preparation except that each composition shown in Tables 45 and 46 was used. The dentin collagen coloration inhibition evaluation of each skirt was performed under the following conditions.

[Evaluation of Inhibition of Dentin Collagen Coloring]

The right root was cut into a block shape, and the cement material was removed by surface polishing. About 3.5 mm x 3.5 mm of the part from which the cement was removed was used for demineralization window, and the other part was covered with manicure. The nail polish was dried at room temperature and immersed in 0.1 mol / l of an aqueous acetic acid solution (pH 4.5) for 72 hours to prepare a hardened carious sample in which collagen was exposed in the window portion. First, color differences (L * 0, a * 0, b * 0) were measured as initial values. Next, this sample was immersed in each of Example and Comparative Example 3 3 minutes in the multiple dilution of the composition in the room temperature, washed with distilled water, artificial saliva of _{37 ℃ (CaCl 2: 2.2m㏖ /} ℓ, KH 2 PO (Type 1A, manufactured by Sigma): 0.2 unit / ml, pH 6.5) containing ₁ : ₄ : 2.2 mmol / l of acetic acid and 0.1 mol / l of Clostridium histolyticum. Thereafter, immersion in 0.2% bovine serum albumin at 37 ° C for 20 minutes and immersion in the coloring liquid (1) or (2) at 37 ° C for 20 minutes were repeated five times. After the end of the experiment, the color difference (L * 1, a * 1, b * 1) was measured with n = 3 and the average value was calculated. The color difference was measured using a spectroscopic colorimetric system (CM-2022, manufactured by Konica Minolta Co., Ltd.), and the coloring inhibition effect was evaluated from the value of? E calculated by the following formula (6-1) Respectively. The results are shown in Tables 45 to 46.

Equation (6-1):

△ E value = ((L * 1-L * 0) 2 + (a * 1-a * 0) 2 + (b * 1-b * 0) 2) 1/2

[Coloring solution]

Coloring solution (1): 0.3% aqueous solution of instant tea (Kroger (TM) Instant Tea)

Coloring solution (2): An aqueous solution of 1.5% instant coffee (NESCAFE Excella: Nestle Japan)

[Evaluation standard]

A: 0? DELTA E &lt; 2.0

B: 2.0? DELTA E &lt; 4.0

C: 4.0? DELTA E &lt; 6.0

D: 6.0? DELTA E &lt; 8.0

[Table 45]

[Table 46]

The compositions of Comparative Examples 6-1 to 6-2, which did not contain the component (A), showed no coloring effect on dentin collagen, whereas the compositions of Examples 6-1 to 6-14 containing the component (A) Was superior in dentin collagen coloring inhibitory effect. This result shows that the component (A) is useful as an active ingredient of the dentin collagen stain inhibitor. This result also suggests that the oral composition (6) can exert an effect of suppressing collagen coloring.

Claims (15)

Component (A): at least one member selected from the group consisting of pyrrolidone carboxylic acid, 6-oxo-2-piperidinecarboxylic acid, 3- (2-oxo-1-azepanyl) propanoic acid, (1-B) component selected from the group consisting of sodium fluoride, potassium fluoride, ammonium fluoride, tin fluoride, sodium fluorophosphate, sodium monofluorophosphate, potassium monofluorophosphate, sodium fluoride, and silicon fluoride , And the content of the component (A) is 0.1 to 10% by mass. The method according to claim 1,
Wherein the component (A) is a pyrrolidone carboxylic acid and / or an inorganic base salt thereof. 3. The method according to claim 1 or 2,
Wherein the inorganic base salt as the component (A) is a salt of any one of a sodium salt, a potassium salt, a magnesium salt and an ammonium salt. 3. The method according to claim 1 or 2,
Wherein the component (1-B) is at least one of sodium fluoride and sodium monofluorophosphate. 3. The method according to claim 1 or 2,
Wherein the ratio by mass of the component (A) to the fluorine content in the oral composition ((A) / fluorine content) is 1 to 250. 3. The method according to claim 1 or 2,
Wherein the content of the component (1-B) is 0.01 to 1% by mass as a fluorine content. 3. The method according to claim 1 or 2,
(1-C) component: a composition containing 1.0 to 6.0% by mass of a sulfamic amino acid residue. 8. The method of claim 7,
Wherein the component (1-C) is casein. 8. The method of claim 7,
Wherein the content of the component (1-C) is 0.1 to 10% by mass. 8. The method of claim 7,
(1-C) / (fluorine content) of the (1-C) component relative to the fluorine content in the oral composition is 0.3 to 800. The oral composition according to claim 1, 3. The method according to claim 1 or 2,
Wherein the composition contains 20 to 95% by mass of water and / or 1 to 20% by mass of a lower alcohol. 3. The method according to claim 1 or 2,
Wherein the formulation is a dressing, a mouthwash, an oral coating agent, an oral pasta, or a food form. Component (A): at least one member selected from the group consisting of pyrrolidone carboxylic acid, 6-oxo-2-piperidinecarboxylic acid, 3- (2-oxo-1-azepanyl) propanoic acid, (1-B) component selected from the group consisting of sodium fluoride, potassium fluoride, ammonium fluoride, tin fluoride, sodium fluorophosphate, sodium monofluorophosphate, potassium monofluorophosphate, sodium fluoride, and silicon fluoride , Wherein the content of the component (A) is 0.1 to 10% by mass, and the content of the component (A) is 0.1 to 10% by mass. 14. The method of claim 13,
Wherein the component (A) is a pyrrolidone carboxylic acid and / or an inorganic base salt thereof. The method according to claim 13 or 14,
Wherein the inorganic base salt as the component (A) is a salt of any one of a sodium salt, a potassium salt, a magnesium salt and an ammonium salt.