JP2001158725A - Agent for preventing acid erosion of tooth - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a tooth acid erosion-preventing agent which contains a diphosphonic acid compound as an active ingredient. SOLUTION: This tooth acid erosion-preventing agent contains the diphosphonic acid compound as an active ingredient, and thereby exhibits the long-lasting effect of excellent tooth acid resistance. Thus, the preventing agent can be provided, which is effective not only for acid erosion limited to special persons such as persons working in work sties where large amounts of acid dusts are contained in air, persons regularly using acidic medicines, or persons into whose oral cavities gastric acids easily flow back, but also for acid erosion also spread among general persons, because customs for drinking carbonated drinks, acidic juices or vitamin C for promoting health are recently spread.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an agent for preventing dental erosion.

[0002]

2. Description of the Related Art Tooth erosion has been a problem in the past when people working in workplaces with a lot of acid dust in the air,
It was limited to special people, such as those who regularly use acidic drugs and those whose gastric acid easily flows back into the oral cavity. However, recently, the habit of drinking carbonated beverages, acidic juices, or acidic vitamin C for the purpose of promoting health has been widespread, and more people have dental erosion.

[0003] Dental erosion refers to a condition in which tooth enamel is dissolved by an acid and the thickness of the tooth enamel is reduced in the above cases. Sometimes all of the enamel dissolves,
Erosion may reach the dentin. As a result, not only is the tooth weakened in strength, but it also causes hypersensitivity to dentin and is a serious problem in terms of the aesthetics of the teeth.

Conventionally, dental erosion has been a problem limited to a special person as described above, and thus has not received much attention, and there have been few cases in which a method for preventing it has been widely studied. Generally, it has been limited to passive measures, such as keeping the factors that cause dental erosion as close as possible or less frequent.

[0005] As a drug for preventing dental erosion, a method of neutralizing acid by rinsing with a mouthwash containing baking soda, neutralizing and removing acid by chewing gum to promote secretion of saliva. how to,
Recently, a method of protecting or restoring tooth by mixing calcium or phosphate with gum or carbonated drinking water has been proposed. On the other hand, the use of fluorine dentifrices used in caries prevention has also been suggested.

However, in order to suppress dental erosion,
The method of removing the acid responsible for the gargle and mouth cleaning is an ad-hoc effect, and a sufficient effect cannot be expected in view of the rapid dissolution of enamel. In addition, the acid neutralization method of gargle with baking soda or the like is not decisive because the retention of baking soda is insufficient and the effect is transient. On the other hand, the application of fluorine is not sufficiently effective because the mechanism of dental erosion is not always the same as that of dental caries. That is, among the actions of fluorine in the prevention of dental caries, the acid resistance effect of the tooth is at most pH 4.0.
On the other hand, in the case of dental erosion, the pH may be 2 or less, and the acid resistance effect of fluorine is not sufficient. Further, the effect of promoting remineralization by fluorine is limited to the case of subsurface demineralization, and it is theoretically difficult to repair enamel that has been eroded. Therefore, in order to protect the enamel from demineralization of the dentin by a strong acid that causes dental erosion, a technique for strengthening the enamel so as to be hardly soluble in a strong acid is required.

[0007]

Means for Solving the Problems and Embodiments of the Invention In order to meet the above demands, the present inventors have conducted intensive studies on effective ingredients for effectively preventing tooth erosion. The inventors have found that they have an acid resistance function and have a sustained effect, and have accomplished the present invention.

Conventionally, ethane-1-hydroxy-1,
A diphosphonic acid compound represented by 1-diphosphonic acid is
Formulated in an oral composition, a discoloration inhibitor for hydroxamic acids (Japanese Patent Application Laid-Open No. 62-418), a tartar preventive agent (Japanese Patent Application Laid-Open No. 62-212314, Japanese Patent Application Laid-Open No. 2-501480).
Japanese Patent Application Laid-Open No. 7-165550), a diphosphonic acid compound has a unique effect as an active ingredient for preventing dental erosion. This has been found for the first time by the present inventors.

Hereinafter, the present invention will be described in more detail.
The agent for preventing dental erosion of the present invention comprises a diphosphonic acid compound as an active ingredient.

Here, as the diphosphonic acid compound, compounds represented by the following general formula (1) and salts thereof are used.

[0011]

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In the formula, R is a monovalent hydrocarbon group which may contain an oxygen atom or a nitrogen atom, particularly an alkyl group having 1 to 4 carbon atoms which may contain an oxygen atom or a nitrogen atom.

Examples of the salt include monovalent metal ions such as a sodium salt and a potassium salt.

As the diphosphonic acid compound, one of these compounds represented by the formula (1) and salts thereof may be used alone or in combination of two or more. Among them, ethane-1-hydroxy-1 , 1-Diphosphonic acid (EH
DP) and its salts are preferably used.

The preventive agent for dental erosion of the present invention can be used in combination with various medicinal ingredients, and particularly, medicinal ingredients commonly used in oral compositions such as sodium fluoride, sodium monofluorophosphate, ammonium fluoride and the like. Antibacterial agents such as fluoride, chlorhexidine, triclosan, cetylpyridinium chloride, benzethonium chloride, anti-inflammatory agents such as pyrophosphate, polyphosphate, tranexamic acid, glycyrrhizin dipotassium, enzymes such as dextranase, mutanase, and lysozyme Preparations, vitamins A, C, E,
B6, vitamins such as pantothenate, amino acids such as glycine, lysine, histidine, sodium chloride,
Hypersensitivity agents such as potassium nitrate, sarcosinate,
It can be used in combination with antienzymes such as tannin-like substances. In addition, when used in combination with these medicinal components, particularly fluorides, it is desirable to add a phosphate compound such as sodium phosphate, condensed phosphate or phytic acid in order to enhance the compatibility.

The prophylactic agent for dental erosion of the present invention can be used as a gargle or the like, or in the form of a composition for oral cavity such as dentifrice, mouthwash, paste for application (gel), dental floss, tablet and the like. Can be used as

In this case, the effect of the above-mentioned diphosphonic acid compound on the prevention of dental erosion is significantly reduced when polyvalent metal compounds such as calcium, magnesium, aluminum, zinc, copper, tin, iron and strontium are present. When an oral composition such as dentifrice is prepared by blending the tooth erosion preventive agent of the present invention, it is preferable that the composition does not contain a substance containing a polyvalent metal ion which easily forms a complex with a diphosphonic acid compound.

Therefore, when the prophylactic agent for dental erosion of the present invention is incorporated into toothpaste, mouthwash, etc., as a binder or an organic thickener, carboxymethylcellulose, xanthan gum, hydroxyethylcellulose, guar gum, sodium alginate, pluronic ( Trademark), Gantrez (trademark) (polyvinyl methyl ether / maleic acid copolymer), polyacrylic acid, polyvinyl alcohol, polyvinylpyrrolidone, cyclodextrin, phosphorylated starch, chitin / chitosan and its sulfated or phosphorylated derivatives, casein , Gelatin and the like are used, and the abrasive is selected from substances substantially free of calcium, magnesium and aluminum, such as silica-based abrasives, baking soda, organic particles and clay minerals. In the case of a silica-based material, it is desirable to minimize the influence on enamel in consideration of the amount of the silica-based material and the size of the particles.

As the activator, any of a cationic, anionic, nonionic or amphoteric activator can be used. For example, sodium lauryl sulfate, lauroyl diethanolamide, lauroyl sarcosinate, N
-Sodium acylglutamate, monostearic acid ester, sucrose fatty acid ester, polyoxyethylene hydrogenated castor oil, sorbitan monooleate and the like are used, and as a humectant, polyethylene glycol, propylene glycol, sorbitol, glycerin, xylitol and the like are used. , Other ingredients, alcohol,
Silicone substances such as dimethylsiloxane, preservatives,
Coloring agents, fragrances and the like can also be added.

The amount of the dental erosion preventive agent of the present invention is as follows when it is added to the above oral composition.
0.01-5% of diphosphonic acid compound of the active ingredient
(Percentage by mass, hereinafter the same), and is preferably used daily according to the usual usage of the oral composition.

[0021]

EFFECTS OF THE INVENTION The tooth erosion preventive agent of the present invention exhibits an excellent sustained effect of tooth acid resistance by using a diphosphonic acid compound as an active ingredient. In addition to erosion, which has been limited to special people, such as those who work in workplaces with a lot of acid dust in the air, those who regularly use acidic medicine, and those who have a tendency for stomach acid to flow back into the mouth, The habit of drinking carbonated beverages, acidic juices, or acidic vitamin C for the purpose of promoting health is widespread, and an effective preventive agent can be provided for erosion that is spreading to the general population.

[0022]

The present invention will be described in more detail with reference to the following Examples and Formulation Examples.

[Example] The enamel surface of a human tooth was covered with nail polish except for a certain area (3 × 3 mm).
This surface was treated with an aqueous solution of EHDP for 3 minutes and then lightly washed with distilled water. This was immersed in a hydrochloric acid aqueous solution of pH 3 for 5 minutes, and calcium ions eluted in the hydrochloric acid aqueous solution were measured by an atomic absorption spectrometer. As a control, distilled water containing no EHDP was used. As a result, in the case of the control tooth sample, a high concentration of calcium (0.1 mg) was detected, and the gloss of the enamel surface almost disappeared, whereas when treated with the EHDP aqueous solution, the detected amount of calcium was small. (0.01 mg). The gloss of the enamel surface also maintained its original state.

It is considered that such an acid resistance effect is due to the fact that the diphosphonic acid compound strongly adsorbs to hydroxyapatite which is a mineral component of the tooth, and protects the dissolution of the mineral from the erosive action of a strong acid.

Next, a formulation example in which a diphosphonic acid compound is blended as an active ingredient for preventing dental erosion is shown.

[Formulation Example 1] Dentifrice type baking soda 15.0% Carboxymethylcellulose 1.5 Polyethylene glycol 3.0 Sorbitol 20.0 Sodium lauryl sulfate 1.5 Preservative trace amount Flavor 1.0 Saccharin Trace amount sodium monofluorophosphate 0.8 EHDP 1.0 Purified water Balance meter 100.0%

[Formulation Example 2] Dentifrice type baking soda 20.0% Carboxymethylcellulose 1.5 Polyethylene glycol 3.0 Xylitol 20.0 Sodium lauryl sulfate 1.0 Preservative trace amount of fragrance 1.0 Saccharin Trace amount of sodium fluoride 0. 21 EHDP 1.0 Purified water Balance meter 100.0%

[Formulation Example 3] Dentifrice-type nylon fine particles 10.0% Carboxymethylcellulose 1.5 Polyethylene glycol 3.0 Xylitol 20.0 Sodium lauryl sulfate 1.5 Lauroyl sarcosinate 0.3 Preservative trace amount Perfume 1 0.0 Saccharin Trace amount of sodium fluoride 0.8 EHDP 0.5 Purified water Balance meter 100.0%

[Formulation Example 4] Dentifrice-type plant fiber 10.0% Carboxymethylcellulose 1.5 Polyethylene glycol 3.0 Xylitol 20.0 Sodium lauryl sulfate 1.0 Preservative Trace amount of fragrance 1.0 Saccharin Trace amount of monofluorophosphoric acid Sodium 0.8 Triclosan 0.3 EHDP 0.5 Purified water Balance meter 100.0%

[Formulation Example 5] Dentifrice-type silica 5.0% Smectite 5.0 Carboxymethylcellulose 1.5 Polyethylene glycol 3.0 Sorbitol 20.0 Sodium lauryl sulfate 1.5 Preservative Trace amount of fragrance 1.0 Saccharin Trace amount Mono Sodium fluorophosphate 0.8 EHDP 1.5 Purified water Balance meter 100.0%

[Formulation Example 6] Dentifrice-type silica 5.0% Baking soda 2.0 Carboxymethylcellulose 1.5 Polyethylene glycol 3.0 Xylitol 20.0 Sodium lauryl sulfate 1.0 Preservative Trace amount of fragrance 1.0 Saccharin Trace amount of fluorine Sodium chloride 0.21 EHDP 5.0 Purified water Balance meter 100.0%

[Formulation Example 7] Mouthwash type polyethylene glycol 3.0% sorbitol 10.0 sodium lauryl sulfate 0.3 preservative trace fragrance 1.0 saccharin trace ethanol 5.0 EHDP 1.0 purified water Balance meter 100 0.0%

[Formulation Example 8] Mouthwash type polyethylene glycol 3.0% xylitol 20.0 sodium lauryl sulfate 0.2 preservative trace fragrance 1.0 saccharin trace ethanol 5.0 EHDP 1.0 purified water balance meter 100 0.0%

[Formulation Example 9] Mouthwash type polyethylene glycol 3.0% xylitol 10.0 sodium lauryl sulfate 0.2 ethanol 3.0 preservative trace amount of fragrance 1.0 saccharin trace amount of sodium fluoride 0.05 EHDP 0 Purified water balance meter 100.0%

[Formulation Example 10] Mouthwash type xylitol 10.0% sorbitol 5.0 triclosan 0.3 baking soda 5.0 preservative trace amount sodium fluoride 0.05 EHDP 1.0 purified water balance meter 100.0%

 ────────────────────────────────────────────────── ─── Continuing on the front page (72) Inventor Kumiko Shioki 1-3-7, Honjo, Sumida-ku, Tokyo F-term in Lion Corporation (reference) 4C083 AB052 AB172 AB312 AB442 AB472 AC102 AC132 AC662 AC782 AC812 AC862 AC881 AD042 AD072 AD272 CC41 DD22 DD27 EE32

Claims (1)

[Claims] 1. An agent for preventing dental erosion, which comprises a diphosphonic acid compound as an active ingredient.