JP5842565B2 - Mouthwash composition and method for inhibiting discoloration in mouthwash composition - Google Patents

Description

  TECHNICAL FIELD The present invention relates to a liquid oral composition containing tranexamic acid or ε-aminocaproic acid having a high palatability, in which discoloration with time is suppressed and appearance stability is excellent, and to a method for suppressing discoloration in a liquid oral composition.

  Periodontal disease is an inflammatory disease. Therefore, for the prevention of this periodontal disease, it is effective to alleviate inflammation. For example, the anti-inflammatory action of tranexamic acid (Patent Document 1; described in Japanese Patent Publication No. 49-39818) and the incorporation of ε-aminocaproic acid are very effective. It is known to be effective.

  On the other hand, cinnamic aldehyde is a perfume ingredient indispensable for making a mouthwash with very high palatability. The formulation of the synamic aldehyde into the oral composition is very important both in terms of efficacy and usability.

Japanese Patent Publication No.49-39818

  However, when synamic aldehyde is blended with a liquid oral composition containing tranexamic acid or ε-aminocaproic acid, there is a problem that discoloration occurs over time and appearance stability is poor.

  The present invention was made in order to solve the above-mentioned problems, and has a highly palatable tranexamic acid or ε-aminocaproic acid-containing liquid oral composition having excellent appearance stability that suppresses discoloration of the preparation over time. And it aims at providing the discoloration suppression method in the composition for liquid oral cavity.

As a result of intensive studies to achieve the above-mentioned object, the present inventors have formulated sodium alkyl sulfate in a liquid oral composition containing tranexamic acid or ε-aminocaproic acid and an appropriate amount of cinnamaldehyde. Knowing that blending in an appropriate amount can suppress discoloration over time, improve appearance stability, provide a liquid product with high palatability, and also suppress irritation during use, resulting in a good feeling of use. Thus, the present invention has been made.
In the present invention, in the above liquid preparation, tranexamic acid or ε-aminocaproic acid and cinnamic aldehyde react with each other to prevent discoloration of the preparation over time can be suppressed by blending with sodium alkyl sulfate, giving the above-mentioned special effects. Thus, it is a new finding of the present inventors that sodium alkyl sulfate acts as a discoloration inhibitor in this way.

Therefore, the present invention
[1]
(A) and tranexamic acid or ε- aminocaproic acid, (B) and cinnamic aldehyde, (C) and sodium lauryl sulfate, (A) component from 0.006 to 0.2 mass%, (B) component 0 0002-0.001 mass%, (C) The mouthwash composition characterized by mix | blending so that it may become 0.05-0.12 mass% ,
[2]
(A) and tranexamic acid or ε- aminocaproic acid, (B) and cinnamic aldehyde, (C) and sodium lauryl sulfate, (A) component from 0.006 to 0.2 mass%, (B) component 0 .0002-0.001 mass%, (C) It mix | blends so that a component may be 0.05-0.12 mass% , The said (A), (B), (C) component mix | blended Provided is a method for suppressing discoloration in a prepared mouthwash composition.

  According to the present invention, in a liquid oral composition containing tranexamic acid or ε-aminocaproic acid, the discoloration of the preparation over time due to the formulation of synamic aldehyde is suppressed, and the liquid has high palatability and has excellent appearance stability. A formulation can be provided. Furthermore, there is no irritation at the time of use, and the feeling of use becomes good.

  The present invention will be described in further detail below. The composition for liquid oral cavity of the present invention contains (A) tranexamic acid or ε-aminocaproic acid, (B) cinnamic aldehyde, and (C) sodium alkyl sulfate.

  The component (A) tranexamic acid, ε-aminocaproic acid is an antiplasmin agent, and is an effective component for antiplasmin, bleeding prevention and periodontal disease prevention. As the component (A), tranexamic acid is particularly preferable from the viewpoint of periodontal disease prevention effect.

  Commercial products can be used as tranexamic acid and ε-aminocaproic acid. For example, tranexamic acid includes Japanese Pharmacopoeia tranexamic acid (manufactured by Simic CMO Co., Ltd.), and ε-aminocaproic acid includes ε-amino-n-caproic acid EKD (manufactured by Daiichi Sankyo Co., Ltd.).

  The blending amount of the component (A) is not particularly limited as long as the effect of the present invention is obtained, but is preferably 0.006 to 0.5% (mass%, the same applies hereinafter) of the entire composition, more preferably 0.8. 03 to 0.2%. If it is less than 0.006%, it may be inferior in the periodontal disease prevention effect, and if it exceeds 0.5%, irritation derived from the component may occur or discoloration cannot be suppressed and appearance stability may be inferior.

The component (B), a synthetic aldehyde, is a flavor adjuster. By blending the cinnamic aldehyde, the palatability of the preparation can be increased and the satisfaction of the user can be improved.
As the cinnamaldehyde, for example, commercially available products such as cinnamaldehyde (manufactured by Simrise Co., Ltd.) can be used.

  The compounding quantity of a component (B) is 0.0002 to 0.002% of the whole composition, Preferably it is 0.0003 to 0.001%. If it is less than 0.0002, palatability peculiar to cinnamic aldehyde cannot be obtained, and a blending effect cannot be obtained. If it exceeds 0.002%, the feeling of use is impaired by stimulation, or discoloration cannot be suppressed, resulting in poor appearance stability.

  Component (C) sodium alkyl sulfate is a discoloration inhibitor. In this invention, the discoloration of a formulation by mix | blending a component (B) with the composition for liquid oral cavity containing a component (A) can be suppressed with a component (C).

As sodium alkyl sulfate, those having an alkyl group with 12 to 18 carbon atoms, particularly 12 to 14 carbon atoms, and especially 12 carbon atoms are preferred. For example, sodium lauryl sulfate, sodium myristyl sulfate and the like can be mentioned, and sodium lauryl sulfate is particularly preferable because of its ease of incorporation into the oral composition.
Commercially available products such as sodium lauryl sulfate manufactured by Toho Chemical Industry Co., Ltd. and sodium myristyl sulfate manufactured by Nikko Chemicals Co., Ltd. can be used.

  The compounding quantity of a component (C) is 0.05 to 0.2% of the whole composition, Preferably it is 0.08 to 0.12%. If it is less than 0.05%, a discoloration suppressing effect cannot be obtained.

  The oral composition of the present invention is prepared as a liquid preparation. Here, the composition for liquid oral cavity is a preparation in which a compounding component is solubilized or emulsified. Specifically, it is prepared and applied as a mouthwash of the type that is used as it is, a freshener in the mouth, a mouthwash that is diluted at the time of use in a concentrated type, and a liquid dentifrice that is used by brushing with a toothbrush. In particular, it is suitable as a mouthwash and a liquid dentifrice. In the present invention, particularly when it is prepared into a liquid, the effect of suppressing discoloration is remarkably high, and a liquid preparation without discoloration can be obtained.

  In addition to the above-mentioned components, other known components can be blended in the composition of the present invention as necessary within a range that does not interfere with the effects of the present invention. Specifically, solid components that are not solubilized, such as abrasives, are not usually blended. For example, wetting agents, surfactants, solvents, and if necessary, sweeteners, colorants, fragrances, active ingredients, and the like are blended.

  Examples of the wetting agent include sugar alcohols such as sorbitol, malt, and lactit, and examples of the polyhydric alcohol include glycerin, ethylene glycol, and polyethylene glycol. The blending amount of these wetting agents is preferably 2 to 20% of the total composition.

As the surfactant, known components other than the component (C), for example, nonionic surfactants, cationic surfactants, amphoteric surfactants and the like can be blended.
(C) Nonionic surfactants include, for example, sugar alcohol fatty acid esters such as sucrose fatty acid ester, maltose fatty acid ester, maltitol fatty acid ester, lactol fatty acid ester, alkylol amide, polyoxyethylene sorbitan monostearate and the like Polyoxyethylene fatty acid esters such as oxyethylene sorbitan fatty acid ester, polyoxyethylene hydrogenated castor oil, polyglycerin fatty acid esters such as hexaglyceryl monolaurate, hexaglyceryl monomyristate, decaglyceryl monolaurate, decaglyceryl monomyristate, hexadecyl monocetylate Glyceryl, fatty acid diethanolamides such as monoglyceryl monoglyceryl lauryl mono or diethanolamide, sorbitan fatty acid esters, Polyoxyethylene higher alcohol ethers such as polyoxyethylene lauryl ether, polyoxyethylene polyoxypropylene copolymer, polyoxyethylene polyoxypropylene fatty acid ester, Pluronic, or the like is used.

Examples of the cationic surfactant include alkyl ammonium and alkyl benzyl ammonium salts. Amphoteric surfactants include betaine acetate type amphoteric surfactants such as alkyldimethylaminoacetic acid betaine and fatty acid amidopropyldimethylaminoacetic acid betaine, and imidazoline type such as N-fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine salt. Examples include amphoteric surfactants.
The blending amount of these surfactants is preferably 0.05 to 3% of the entire composition including the component (C).

As a sweetening agent, xylitol, maltitol, saccharin, saccharin sodium, stevioside, aspartame and the like can be blended.
As a colorant, a highly safe water-soluble pigment such as Blue No. 1, Green No. 3, Yellow No. 4, Red No. 105, and the like can be added.

  As the fragrance, other than component (B), for example, peppermint oil, spearmint oil, eucalyptus oil, wintergreen oil, clove oil, thyme oil, sage oil, cardamom oil, rosemary oil, marjoram oil, lemon oil, nutmeg oil , Natural essential oils such as lavender oil and paracres oil, and l-menthol, l-carvone, orange oil, anethole, 1,8-cineole, methyl salicylate, eugenol, thymol, linalool, limonene, menthone, menthyl acetate, citral, camphor Fragrance ingredients contained in the above natural essential oils such as benzene, borneol, pinene, spiranthol, etc., and ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate, ethyl methyl phenyl glycide , Benzaldehyde, vanillin, ethyl vanillin, furaneol, maltol, ethyl maltol, gamma / delta decalactone, gamma / deltown decalactone, N-ethyl-p-menthane-3-carboxamide, menthyl lactate, ethylene glycol-1-menthyl Perfume ingredients such as carbonate, and also a combination of several perfume ingredients and natural essential oils, apple, banana, strawberry, blueberry, melon, peach, pineapple, grape, muscat, wine, cherry, squash, coffee, brandy, One type or two or more types of blended flavors such as yogurt can be added as long as the effects of the present invention are not hindered. The addition amount is usually 0.00001 to 3% in the composition.

  Active ingredients include those other than component (A), for example, bactericides such as isopropylmethylcellulose, enzymes such as dextranase and mutanase, fluorides such as sodium fluoride and sodium monofluorophosphate, aluminum chlorohydroxy allantoin, allantoin Vitamin C such as azulene, lysozyme chloride, ascorbic acid, pyridoxine hydrochloride, tocopherol acetate, dihydrocholesterol, glycyrrhetin salts, glycyrrhetinic acids, glycyrrhizic acid, hydrocholesterol, chlorophyll, copper chlorophyllin sodium, thyme, ogon, clove, hamamelis, etc. Plant extract, copper gluconate, caropeptide, sodium polyphosphate, water-soluble inorganic phosphate compound, polyvinylpyrrolidone, calculus inhibitor, dental plaque inhibitor Potassium nitrate, may be added to aluminum lactate and the like. In addition, the addition amount of these active ingredients can be made into effective amount in the range which does not prevent the effect of this invention.

  As the solvent, water is usually used. The water content is preferably 50% or more of the total composition. You may add about 0-20% of C1-C3 lower monohydric alcohols, such as ethanol.

The composition of the present invention preferably has a viscosity at 25 ° C. of 0 to 50 mPa · s, particularly 0 to 20 mPa · s, measured by the test method described below.
Viscosity measurement method (oral composition);
Weigh 300 g of oral composition in a 300 mL tall beaker. Next, after standing in a constant temperature water bath at 25 ° C. for 1 hour, the viscosity after 1 minute is measured accurately using a BL type viscometer.
Viscometer: manufactured by Tokyo Keiki Co., Ltd. BL viscometer Measurement conditions: Rotor No. 1. 60 rpm

  EXAMPLES Hereinafter, although an experimental example, an Example, and a comparative example are shown and this invention is demonstrated concretely, this invention is not restrict | limited to the following Example. In the following examples, “%” means “% by mass” unless otherwise specified.

[Experimental Example 1]
Mouthwashes having the compositions shown in Tables 1 to 3 were prepared by a conventional method and evaluated as follows using this as a sample. The results are shown in Tables 1-3.

(1) Appearance stability (discoloration)
Fill the sample shown in the table with 80 mL into a clear and transparent 80 mL colorless and transparent PET container (polyethylene terephthalate container, manufactured by Yoshino Kogyo), store for 3 months at room temperature, and visually observe the stability (discoloration) according to the following criteria. Judged. Evaluation was based on colorless and transparent water.
Discoloration criteria A: No color change and colorless and transparent.
○: Slightly yellow discoloration is observed, but at a level that does not cause a problem.
X: Obviously yellow discoloration is recognized.

(2) Stimulation during use After 10 subjects included the sample shown in the table in a 10 mL mouth and rinsed for 20 seconds, the stimulation during mouth washing was evaluated in the following three stages. The average score of 10 people was determined according to the following criteria.
Evaluation criteria for stimulation at the time of use 3: Stimulation was hardly felt.
2: Some irritation was observed.
1: Stimulation was clearly observed.
Stimulation criteria ◎: Average score of 2.5 points or more ○: Average score of 2.0 points or more and less than 2.5 points △: Average score of 1.5 points or more and less than 2.0 points ×: Average score of 1.5 points Less than

Details of the raw materials used are as follows.
Tranexamic acid; Japanese Pharmacopoeia tranexamic acid (manufactured by CMIC CMO)
ε-aminocaproic acid; ε-amino-n-caproic acid EKD (manufactured by Daiichi Sankyo Co., Ltd.)
Cynamic aldehyde; Cynamic aldehyde (manufactured by Simrise Co., Ltd.)
Sodium lauryl sulfate; sodium myristyl sulfate manufactured by Toho Chemical Industry Co., Ltd .; sodium lauroyl sarcosine manufactured by Nikko Chemicals Co., Ltd .; Soypon SLP (manufactured by Kawaken Fine Chemical Co., Ltd.)

  A prescription example is shown below. The following composition for oral cavity has no discoloration, excellent appearance stability, almost no irritation at the time of use, and has a high palatability and a good feeling of use.

[Prescription Example 1] Mouthwash tranexamic acid 0.05
Synamic aldehyde 0.0005
Sodium lauryl sulfate 0.12
Citric acid 0.05
Sodium citrate 0.3
Polyoxyethylene hydrogenated castor oil 0.6
Isopropyl methylphenol 0.05
Allantoin 0.06
Glycerin 6
Propylene glycol 5
Xylit 5
Ethanol 10
Fragrance 0.5
Water balance
Total 100%

[Prescription Example 2] Mouthwash tranexamic acid 0.05
Synamic aldehyde 0.0005
Sodium lauryl sulfate 0.12
Citric acid 0.05
Sodium citrate 0.3
Polyoxyethylene hydrogenated castor oil 0.6
Isopropyl methylphenol 0.05
Allantoin 0.06
Glycerin 6
Propylene glycol 5
Xylit 5
Fragrance 0.5
Water balance
Total 100%

[Prescription Example 3] Mouthwash tranexamic acid 0.05
Synamic aldehyde 0.0005
Sodium lauryl sulfate 0.1
Cetylpyridinium chloride 0.05
Citric acid 0.03
Sodium citrate 0.25
Polyoxyethylene hydrogenated castor oil 0.3
Glycerin 4
Propylene glycol 2
Xylit 5
Ethanol 6
Fragrance 0.5
Water balance
Total 100%

[Prescription Example 4] Mouthwash tranexamic acid 0.05
Synamic aldehyde 0.0005
Sodium lauryl sulfate 0.1
Triclosan 0.02
Citric acid 0.04
Sodium citrate 0.35
Polyoxyethylene hydrogenated castor oil 0.5
Isopropylmethylphenol 0.02
Glycerin 6
Propylene glycol 8
Xylit 6
Ethanol 10
Fragrance 0.5
Water balance
Total 100%

[Prescription Example 5] Mouthwash tranexamic acid 0.05
Synamic aldehyde 0.0005
Sodium lauryl sulfate 0.12
Citric acid 0.05
Sodium citrate 0.3
Polyoxyethylene hydrogenated castor oil 0.6
Isopropyl methylphenol 0.05
Allantoin 0.06
Tocopherol acetate 0.1
Glycerin 6
Propylene glycol 5
Xylit 5
Ethanol 10
Fragrance 0.5
Water balance
Total 100%

[Formulation Example 6] mouthwash tranexamic acid 0.05
Synamic aldehyde 0.0005
Sodium lauryl sulfate 0.12
Citric acid 0.05
Sodium citrate 0.3
Polyoxyethylene hydrogenated castor oil 0.6
Isopropyl methylphenol 0.05
Allantoin 0.06
Dipotassium glycyrrhizinate 0.05
Glycerin 6
Propylene glycol 5
Xylit 5
Ethanol 10
Fragrance 0.5
Water balance
Total 100%

[Prescription Example 7] Mouthwash tranexamic acid 0.05
Synamic aldehyde 0.0005
Sodium lauryl sulfate 0.12
Citric acid 0.05
Sodium citrate 0.3
Polyoxyethylene hydrogenated castor oil 1.0
Isopropyl methylphenol 0.05
Allantoin 0.06
β-glycyrrhetinic acid 0.05
Glycerin 6
Propylene glycol 5
Xylit 5
Ethanol 10
Fragrance 0.5
Water balance
Total 100%

[Prescription Example 8] Mouthwash tranexamic acid 0.05
Synamic aldehyde 0.0005
Sodium lauryl sulfate 0.1
Cetylpyridinium chloride 0.05
Citric acid 0.03
Sodium citrate 0.25
Polyoxyethylene hydrogenated castor oil 0.3
Pyridoxine hydrochloride 0.05
Glycerin 4
Propylene glycol 2
Xylit 5
Ethanol 6
Fragrance 0.5
Water balance
Total 100%

Claims (2)

(A) and tranexamic acid or ε- aminocaproic acid, (B) and cinnamic aldehyde, (C) and sodium lauryl sulfate, (A) component from 0.006 to 0.2 mass%, (B) component 0 0002-0.001 mass%, (C) It mix | blends so that a component may be 0.05-0.12 mass%, The mouthwash composition characterized by the above-mentioned . (A) and tranexamic acid or ε- aminocaproic acid, (B) and cinnamic aldehyde, (C) and sodium lauryl sulfate, (A) component from 0.006 to 0.2 mass%, (B) component 0 .0002-0.001 mass%, (C) It mix | blends so that a component may be 0.05-0.12 mass% , The said (A), (B), (C) component mix | blended The discoloration suppression method in a finished mouthwash composition.