WO2019054267A1

WO2019054267A1 - Mucosal irritation- and bitterness-reducing agent, and oral composition

Info

Publication number: WO2019054267A1
Application number: PCT/JP2018/033022
Authority: WO
Inventors: 麻里今崎; 友一小熊; 慶貴大野
Original assignee: ライオン株式会社
Priority date: 2017-09-12
Filing date: 2018-09-06
Publication date: 2019-03-21
Also published as: JP2019052095A; JP7058093B2

Abstract

The present invention addresses the problem of providing a mucosal irritation- and bitterness-reducing agent which is useful for the reduction in mucosal irritations and bitterness and can improve the feeling of use of an oral composition. The present invention provides a mucosal irritation- and bitterness-reducing agent comprising pyrrolidonecarboxylic acid and/or an inorganic basic salt thereof. The mucosal irritation- and bitterness-reducing agent according to the present invention is useful for the reduction in mucosal irritations and bitterness associated with tetradecenesulfonic acid and/or a salt thereof. The present invention also provides an oral composition containing: a component (A) that is an α-olefinsulfonic acid and/or a salt thereof; and a component (B) that is pyrrolidonecarboxylic acid and/or an inorganic basic salt thereof.

Description

Mucous membrane irritation and bitterness inhibitor and composition for oral cavity

The present invention relates to an agent for suppressing mucosal irritation and bitterness and a composition for oral cavity.

If components contained in quasi-drugs, foods, and quasi-drugs exhibit mucous membrane irritation and / or bitter taste, they may cause discomfort upon oral intake or use in the oral cavity, and may impair the feeling of use. For example, α-olefin sulfonate is a component that has a high caries biofilm removal effect and is useful for preventing caries (Patent Document 1), and is expected as a medicinal component in oral compositions. However, since the α-olefin sulfonate has a peculiar bitter taste and feels a pungent sensation on the tongue, it is difficult to increase the content in the preparation in order to exert its effect sufficiently.

Patent Document 2 describes that an oral composition containing an anionic surfactant such as sodium α-olefin sulfonate and an acyl amino acid and / or arginine suppresses the bitterness peculiar to α-olefin sulfonic acid. It is done.

International Publication No. 2015/8823 JP, 2013-151474, A

However, since the composition for oral cavity of patent document 2 adds arginine and an acyl amino acid, depending on a composition, a subject may arise in the point of formulation stability. Therefore, another solution is required.

An object of the present invention is to provide an agent for suppressing mucosal irritation and bitterness, which is useful for mucosal irritation and bitterness suppression and can improve the feeling of use of the composition for oral cavity.

The present inventors provide the following [1] to [8].
[1] An agent for suppressing mucosal irritation and bitter taste comprising pyrrolidone carboxylic acid and / or an inorganic base salt thereof.
[2] The agent according to [1], which suppresses mucosal irritation and bitter taste by α-olefin sulfonic acid and / or a salt thereof.
[3] An oral composition comprising (A) component: α-olefin sulfonic acid and / or a salt thereof, and (B) component: pyrrolidone carboxylic acid and / or an inorganic base salt thereof.
[4] The composition according to [3], wherein the content of the component (A) is 0.1 to 2% by mass relative to the total amount of the composition.
[5] The composition according to [3] or [4], wherein the content of the component (B) is 0.1 to 10% by mass with respect to the total amount of the composition.
[6] Any one of [3] to [5], wherein the mass ratio of the content of the component (B) to the content of the component (A) ((B) / (A)) is 0.05 to 100. The composition as described in a term.
[7] Component (A): A method for suppressing mucous membrane irritation and bitter taste, wherein component (B): pyrrolidone carboxylic acid and / or an inorganic base salt thereof is added to α-olefin sulfonic acid and / or a salt thereof.
[8] The method according to [7], wherein the mass ratio of the content of the component (B) to the content of the component (A) ((B) / (A)) is 0.05 to 100.

The agent for suppressing mucous membrane irritation and bitter taste according to the present invention can be used in an oral composition exhibiting mucous membrane irritation and bitter taste, and the composition can effectively suppress mucous membrane irritation and bitter taste. In addition, the composition for oral cavity of the present invention has suppressed mucous membrane irritation and bitter taste, and has a good feeling of use.

Hereinafter, the present invention will be described in detail in line with its preferred embodiments. In addition, in this invention, content of each component in the composition for oral cavity is based on the preparation amount of each component at the time of preparing a composition.

[1. Mucous membrane irritation and bitter taste inhibitor]
The agent for suppressing mucosal irritation and bitter taste according to the present invention contains pyrrolidone carboxylic acid and / or an inorganic base salt thereof as an active ingredient.

The pyrrolidone carboxylic acid has the following formula (1):

It has a structure represented by Pyrrolidonecarboxylic acid can be produced by dehydrating glutamic acid extracted from seaweed, wheat flour and sugar cane.

Examples of inorganic base salts of pyrrolidone carboxylic acid include sodium salts, potassium salts, calcium salts, magnesium salts, copper salts, zinc salts, aluminum salts and ammonium salts, with sodium salts and potassium salts being preferred. Sodium salt of pyrrolidone carboxylic acid (PCA soda) has good stability (for example, oxidation stability) and is a component of NMF (natural moisturizing factor) which is a water-retaining substance of skin stratum corneum and is safe It is more preferable because it has high sex.

The pyrrolidone carboxylic acid and the inorganic base salt thereof may be one synthesized according to a known scheme or a commercially available product. Examples of commercially available products of pyrrolidone carboxylic acid include “AJIDEW® A-100” (manufactured by Ajinomoto Healthy Supply Co., Ltd.). As an inorganic base salt of pyrrolidone carboxylic acid, for example, “AJIDEW (registered trademark) N-50, PCA soda (AI = 50% aqueous solution)” (manufactured by Ajinomoto Healthy Supply Co., Ltd., sodium pyrrolidone carboxylate) can be mentioned.

The agent for suppressing mucous membrane irritation and bitter taste according to the present invention can be added to a subject that exhibits at least one of irritation to the oral mucosa and bitterness. Such subjects include, for example, preparations for oral administration and preparations for oral cavity. The form and dosage form of the preparation are not particularly limited, and examples thereof include liquid systems (liquid, liquid, paste-like) and solid systems (solid, solid-like). The preparation may be any of pharmaceuticals, quasi drugs and foods, but quasi drugs and foods are preferable. Oral preparations include, for example, dentifrices (eg toothpaste, liquid dentifrices, liquid dentifrices, powder dentifrices), mouthwashes, coatings, oral pasta, mouth fresheners, foods (eg chewing gum, Confectionery, candy, gummi, film, troches).

The component exhibiting at least one of mucous membrane irritation and bitter taste includes, for example, α-olefinsulfonic acid having a hydrocarbon group having 12 to 18 carbon atoms and a salt thereof, and in particular, the α-olefinsulfonic acid and its salt Salt is preferred. Specifically, α-olefin sulfonic acid having a hydrocarbon group having 14 to 16 carbon atoms and a salt thereof are preferably mentioned. Examples of the salt include inorganic base salts such as sodium salt, potassium salt, calcium salt, magnesium salt, copper salt, zinc salt, aluminum salt, ammonium salt, etc .; triethyl ammonium salt, triethanol ammonium salt, pyridinium salt, diisopropyl ammonium salt And organic base salts such as Among these salts, water-soluble salts and alkali metal salts are preferable, and sodium salts and potassium salts are more preferable. As the α-olefin sulfonic acid and its salt, tetradecene sulfonic acid and its salt are preferable.

The use amount of the mucous membrane stimulation and bitter taste inhibitor of the present invention can be appropriately set depending on the type of mucous membrane stimulation and bitter taste components, and is not particularly limited. For example, when the mucous membrane irritation and bitter taste components are α-olefin sulfonic acid and / or a salt thereof, the mucosal irritation and bitter taste inhibitor of the present invention for α-olefin sulfonic acid and / or a salt thereof (pyrrolidone carboxylic acid and / or its salt The amount ratio of the inorganic base salt is preferably 0.05 or more, more preferably 0.25 or more, and still more preferably 1.6 or more. The upper limit is preferably 100 or less, more preferably 25 or less. Such an amount ratio is preferably 0.05 to 100, more preferably 0.25 to 25 and even more preferably 1.6 to 25.

[2. Oral Composition]
The oral composition of the present invention contains (A) component: α-olefin sulfonic acid and / or a salt thereof, and (B) component: pyrrolidone carboxylic acid and / or an inorganic base salt thereof.

[2-1. (A) component]
Component (A) is α-olefin sulfonic acid and / or a salt thereof. As the α-olefin sulfonic acid, tetradecene sulfonic acid is preferable. The composition for oral cavity of this invention can exhibit a biofilm removal effect by containing (A) component. The α-olefin sulfonic acid and the salt thereof are the same as those described in the item “1. Mucous membrane stimulation and bitter taste inhibitor” in the preceding paragraph.

[2-2. (B) component]
Component (B) is pyrrolidone carboxylic acid and / or an inorganic base salt thereof. By containing the (B) component, the composition for oral cavity of the present invention can suppress mucous membrane irritation and / or bitter taste caused by the (A) component. The pyrrolidone carboxylic acid and / or the inorganic base salt thereof are the same as those described in the item of "1.

[2-3. Content and amount ratio]
Although content in particular of (A) component with respect to the composition for oral cavity of this invention is not restrict | limited in particular, 0.1 mass% or more is preferable, 0.2 mass% or more is more preferable. Thereby, the composition for oral cavity of this invention can exhibit a biofilm removal effect efficiently. The upper limit is preferably 2% by mass or less. Thereby, the mucous membrane stimulation and / or bitter taste inhibitory effect can be exhibited. The content of the component (A) is preferably 0.1 to 2% by mass, and more preferably 0.2 to 2% by mass.

The content of the component (B) in the composition for oral cavity of the present invention is not particularly limited, but the lower limit thereof is preferably 0.1% by mass or more with respect to the whole composition for oral cavity, and 0.5% by mass or more preferable. Thereby, the composition for oral cavity can exhibit a mucous membrane irritation | stimulation and bitter taste inhibitory effect efficiently. 10 mass% or less is preferable, 8 mass% or less is more preferable, and 5 mass% or less is still more preferable. Thereby, the viscosity of the composition for oral cavity can be adjusted appropriately, and in the case of a toothpaste, the extrudability may be good. The content of the component (B) is preferably 0.1 to 10% by mass, more preferably 0.5 to 8% by mass, and still more preferably 0.5 to 5% by mass.

0.05 or more are preferable and, as for mass ratio ((B) / (A)) of content of (B) component with respect to content of (A) component in the composition for oral cavity of this invention, 0.25 or more is more preferable Preferably, 1.6 or more is more preferable. Thereby, a mucous membrane irritation | stimulation and bitter taste inhibitory effect can be exhibited efficiently. The upper limit is preferably 100 or less, more preferably 25 or less. Thereby, the viscosity of the composition for oral cavity can be adjusted moderately, and extrudability may become favorable. (B) / (A) is preferably 0.05 to 100, more preferably 0.25 to 25 and even more preferably 1.6 to 25.

[2-4. Optional ingredients]
The composition for oral cavity of the present invention may contain optional components as needed, as long as the effects of the present invention are not impaired. Such additive components may be components that can be used in the composition for oral cavity, for example, surfactants, binders, abrasives, thickeners, thickeners, sweeteners, preservatives, fragrances, medicinal ingredients, solvents, There may be mentioned acidulants, lubricants, colorants, brighteners, fluidizers, binders, disintegrants, pH adjusters, and excipients. Although the specific example of an addition component is shown below, the component which can be mix | blended with the composition for oral cavity of this invention is not restrict | limited to these.

As surfactant, an anionic surfactant, an amphoteric surfactant, a nonionic surfactant etc. are mentioned, for example.

The anionic surfactant may be an anionic surfactant other than the component (A), and examples thereof include N-acyl amino acid salts, alkyl sulfates, N-acyl sulfonates, and sulfates of glycerin fatty acid esters. . Among them, N-acylamino acid salts, alkyl sulfates and the like are preferable in view of versatility, and lauroyl sarcosine sodium, sodium lauryl sulfate and the like are more preferable in view of foamability and hardness resistance. In addition, as the N-acyl amino acid salt, for example, an acyl amino acid having a saturated or unsaturated hydrocarbon group (for example, having 8 to 18 carbon atoms, preferably 12 to 16 carbon atoms; any of linear and branched chains may be used) Methyl taurine salts such as lauroyl methyl taurine salt, coconut oil fatty acid methyl taurine salt, myristoyl methyl taurine salt, etc .; methylalanine salts such as lauroyl methyl alanine salt; lauroyl glutamate; And glutamate such as myristoyl glutamate.

Examples of amphoteric surfactants include alkyl betaine surfactants, amine oxide surfactants, and imidazolinium betaine surfactants, with coconut oil fatty acid amidopropyl betaine being preferred.

Examples of nonionic surfactants include polyoxyethylene alkyl ether, polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene hydrogenated castor oil, polyoxyethylene ether of glycerin ester, sucrose fatty acid ester, alkylolamide Etc.

The surfactants can be used singly or in combination of two or more. When the composition for oral cavity contains a surfactant, the content thereof is usually 10% by mass or less based on the whole composition for oral cavity including the component (A), and 0.01 to 10 mass%. % Is preferred.

Examples of the caking agent include organic caking agents and inorganic caking agents. In addition, a caking additive can be used individually by 1 type or in combination of 2 or more types.

Examples of organic binders include: carboxymethylcellulose, pullulan, gelatin, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, xanthan gum, sodium alginate, carrageenan, polyvinyl alcohol, polyvinylpyrrolidone, sodium polyacrylate, propylene alginate Examples thereof include glycol esters, gum arabic, guar gum, locust bean gum, karaya gum, carboxyvinyl polymer and the like.

Examples of the inorganic binder include anhydrous silicic acid (hereinafter, also referred to as "thickening silica" or "anhydrous silicic acid (thickening)" as silicic anhydride as a caking agent) and bentonite. Among them, thickening silica is preferred. The liquid absorption capacity of the thickening silica is preferably 2.1 mL / g or more, and more preferably 2.1 to 5 mL / g.

In the present specification, the liquid absorption amount is a value measured by the following method. That is, 1 g of a sample is weighed on a glass plate, and while a 42.5 mass% glycerin aqueous solution is dropped using a burette, mixing is performed so that the solution becomes uniform with a spatula. The amount of the aqueous glycerin solution required for 1.0 g of the sample is represented as the amount of liquid absorption (mL / g), where the sample is one lump and the end point is when the sample becomes cleanly separated from the glass plate with a spatula.

The binder may be used alone or in combination of two or more. When the composition for oral cavity contains a caking agent, the content thereof is usually 0.01 to 10% by mass based on the whole composition for oral cavity.

As the sweetening agent, for example, saccharin sodium, stevioside, neohesperidin hydrochalcone, glycyrrhizin, perillaltin, p-methoxycinnamic aldehyde, thaumatin, palatinose, maltitol, xylitol, arabitol, erythritol and the like can be mentioned. The sweetening agent can be used alone or in combination of two or more. When using a sweetener, content can be suitably determined in the range which does not impair the effect of this invention.

Examples of the preservative include sodium benzoate, parahydroxybenzoic acid ester (eg, methylparaben, ethylparaben, butylparaben etc.), ethylenediaminetetraacetic acid salt, benzalkonium chloride and the like. The preservatives can be used singly or in combination of two or more. In the case of using a preservative, the content can be appropriately determined as long as the effects of the present invention are not impaired.

As the flavor, for example, essential oils (eg, peppermint, spearmint), fruit-based (eg, lemon, strawberry) essence, 1-menthol, carvone, eugenol, anethole, linalool, limonene, osimene, cineole, n-decyl alcohol, citronellol And fragrant materials such as allirin, α-terpineol, methyl salicylate, thymol, rosemary oil, sage oil, perilla oil, lemon oil, orange oil and the like. The fragrance may be used singly or in combination of two or more among the aforementioned fragrances.

Medicinal ingredients include, for example, the following ingredients: bactericidal or antibacterial agents such as chlorhexidine, triclosan, isopropylmethylphenol, cetyl pyridinium chloride, zinc gluconate, zinc citrate, etc .; condensed phosphates, ethane hydroxy diphosphonates Anti-calculus agents such as tranexamic acid, glycyrrhizin dipotassium salt, ε-aminocaproic acid, lysozyme chloride, allantoin chlorhydroxy aluminum, anti-inflammatory agents such as oat extract; Coating agents such as hydroxyethyl cellulose dimethyldiallyl ammonium chloride; dextranase, Enzyme agents such as mutanase; astringents such as vitamin C, sodium chloride; various vitamins such as tocopherol acetate; hypersensitivity inhibitors such as aluminum lactate, strontium chloride, potassium nitrate Sodium fluoride, sodium monofluorophosphate, and the like fluoride such as stannous fluoride. The medicinal components can be used singly or in combination of two or more. The content of the medicinal ingredient can be determined within a pharmaceutically acceptable range.

As the abrasive, for example, anhydrous silicic acid (hereinafter, silicic anhydride as the abrasive is also referred to as "abrasive silica" or "anhydrous silicic acid (abrasive)"), crystalline silica, amorphous silica, silica gel Silica-based abrasives such as aluminosilicate, zeolite, calcium hydrogen phosphate anhydrate, calcium hydrogen phosphate dihydrate, calcium pyrophosphate, calcium carbonate, aluminum carbonate, aluminum hydroxide, alumina, magnesium carbonate, tribasic magnesium phosphate, Examples thereof include zirconium silicate, tribasic calcium phosphate, hydroxyapatite, tetrabasic calcium phosphate, and synthetic resin abrasives. The absorption capacity of the abrasive silica is usually 0.5 to 2.0 mL / g, preferably 0.7 to 1.5 mL / g.

The abrasives can be used singly or in combination of two or more. When the abrasive is contained, the content thereof in the dentifrice is preferably 2 to 40% by mass, and more preferably 5 to 20% by mass, based on the entire composition.

As a thickener (wetting agent), for example, sorbitol (Sorbit), propylene glycol, butylene glycol, glycerin, polyethylene glycol and the like can be mentioned. A thickener can be used individually by 1 type or in combination of 2 or more types. When the composition for oral cavity contains a thickener, the content thereof can be determined within a range not to impair the effect of the present invention, and is usually 1 to 60% by mass with respect to the whole composition for oral cavity .

Examples of the acidulant include organic acids such as citric acid, malic acid, succinic acid and tartaric acid. When the acidulant is contained, the content is preferably 0.001 to 5% by mass with respect to the entire composition.

As a lubricant, glycerin fatty acid ester etc. are mentioned.

Examples of coloring agents include natural pigments such as safflower red pigment, gardenia yellow pigment, gardenia blue pigment, persimmon pigment, red cabbage pigment, red cabbage pigment, carrot pigment, hibiscus pigment, cocoa pigment, spirulina blue pigment, tamarind pigment, etc. And legal dyes such as riboflavin, sodium copper chlorophyllin, titanium dioxide, etc., and red 3, red 104, red 105, red 106, yellow 4, yellow 5, green 3, blue 1. When the composition for oral cavity contains a coloring agent, its content is preferably 0.00001 to 3% by mass with respect to the whole composition for oral cavity.

As the brightener, for example, waxes such as shellac, carnauba wax, candelilla wax, calcium stearate can be mentioned. When the composition for oral cavity contains a brightener, its content is preferably 0.01 to 5% by mass with respect to the whole composition for oral cavity.

As a fluidizer, fine particle silicon dioxide etc. are mentioned. When the composition for oral cavity contains a fluidizing agent, its content is preferably 0.01 to 5% by mass with respect to the whole composition for oral cavity.

As the binder, for example, pullulan, gelatin, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxymethylcellulose, gum arabic, guar gum, locust bean gum, polyvinyl alcohol, polyvinylpyrrolidone, karaya gum can be mentioned.

When the binder is contained, the content varies depending on the preparation and can not be defined uniformly. For example, in the case of a film, usually, 0.01 to 90% by mass is preferable based on the whole composition. In the case of films other than the film, 0.01 to 10% by weight is usually preferable based on the whole composition.

Disintegrants include pregelatinized starch, sodium alginate, crospovidone, croscarmellose, sodium carboxymethylcellulose and the like. Disintegrants are often included in confectionery. Moreover, as an example of the binder contained in tablet confectionery, hydroxypropyl cellulose, hydroxymethyl cellulose, karaya gum etc. are mentioned among the above-mentioned. When the disintegrant and / or the binder is contained in the tablet, each content is preferably 0.1 to 10% by mass with respect to the whole composition.

The pH (20 ° C.) of the composition for oral cavity of the present invention is usually 6-9. The oral composition of the present invention may optionally contain a pH adjuster. Examples of pH adjusters include acids, alkalis, and buffers, and more specifically, for example, phosphoric acid and salts thereof (eg, sodium phosphate, sodium dihydrogenphosphate), citric acid and salts thereof (eg, citric acid) Acid, sodium hydrogen citrate), malic acid and its salts, gluconic acid and its salts, maleic acid and its salts, succinic acid and its salts, glutamic acid and its salts, lactic acid and its salts, hydrochloric acid and its salts, acetic acid and Its salts (eg sodium acetate), nitric acid and its salts, sodium hydroxide, potassium hydroxide, sodium carbonate, sulfuric acid and its salts. When the pH adjuster is contained, the content thereof can be appropriately determined as long as the effects of the present invention are not impaired.

Examples of the solvent include water; and lower alcohols having 3 or less carbon atoms such as ethanol and propanol. The solvent is usually contained in a liquid-based oral composition. When the composition for oral cavity contains water as a solvent, its content is preferably 20 to 95% by mass with respect to the whole composition for oral cavity. When the composition for oral cavity contains a lower alcohol as a solvent, its content is usually at most 20% by mass, preferably from 1 to 20% by mass, based on the whole composition for oral cavity.

Excipients include, for example, starch syrup, glucose, fructose, invert sugar, dextrin, and oligosaccharides. When the composition for oral cavity is a food preparation, it usually contains an excipient. When an excipient is contained, the content can be appropriately determined as long as the effects of the present invention are not impaired.

[2-5. Shape, dosage form]
The shape and dosage form of the oral composition of the present invention are not particularly limited. For example, it can be prepared in various shapes such as liquid (liquid, liquid, paste-like), solid (solid, solid) and the like. Examples of dosage forms are toothpaste, liquid dentifrice, liquid dentifrice, dentifrice compositions such as powder dentifrices, mouthwash composition, coating composition, oral pasta, mouth freshener composition, Food forms (chewing gum, tablets, candy, gummi, films, troches, etc.) can be mentioned.

The oral composition of the present invention is preferably a dentifrice composition or a mouthwash composition, and is more preferably a dentifrice composition, since the moisturizing effect in the oral cavity can be further enhanced. When the composition for oral cavity of the present invention is a dentifrice composition, a dentifrice is more preferable.

Hereinafter, the present invention will be described in detail by way of examples. The following examples are intended to illustrate the invention but not to limit it.

Examples 1 to 25 and Comparative Example 1 (toothpaste)
1. Preparation method of formulation:
The formulation was prepared according to the following procedure. After dissolving pyrrolidone carboxylic acid Na (component (B)), sodium saccharin, sorbit solution and the like in purified water, a solution in which a binder such as a polymer was dispersed in propylene glycol was separately added and stirred. Thereafter, a fragrance, an abrasive, tetradecene sulfonic acid (component (A)) and the like were added, and the mixture was further stirred under reduced pressure to obtain a dentifrice composition. For the production, a 1.5 L kneader (manufactured by Ishiyama Works Co., Ltd.) was used.

2. Raw materials used:
Details of each component used for preparation of the dentifrice composition are shown below.
(A) Component: tetradecene sulfonic acid (K Lipolan PJ-400CJ, manufactured by Lion Specialty Chemicals)
(B) Component: Pyrrolidonecarboxylic acid Na (AJIDEW (registered trademark) N-50, manufactured by Ajinomoto Healthy Supply Co.)
Optional ingredients: Silica (abrasive, liquid absorption 1.0 mL / g) (manufactured by Taki Chemical Co., Ltd.), Sorbit liquid (sorbitol) (70% by mass aqueous solution, viscous formulation) (manufactured by Rocket), xanthan gum ( DSP Gokyo Food & Chemical Co., Ltd., caking agent, sodium alginate (Kimica Co., Ltd., caking agent), sodium fluoride (Stella Chemifa Co., Ltd., medicinal ingredient), sodium saccharin ( Aisan Chemical Industry Co., Ltd. (sweetener), purified water.
In addition, as an optional ingredient, one conforming to the quasi-drug raw material standard 2006 was used.

3. Evaluation method:
(1) Oral Mucous Membrane Irritation and Bitter Taste Evaluation The oral mucous membrane irritant and bitter taste of the composition for oral cavity were subjected to sensory evaluation (10 panelists) according to the following scoring criteria. In addition, 1 g of dentifrice was taken on the toothbrush and evaluated by brushing for 3 minutes. Oral mucous membrane irritation and bitter taste were evaluated based on the following evaluation criteria from the average of 10 persons.

<Oral mucosal irritation properties>
(Scoring criteria)
5 points: no stimulation 4 points: almost no stimulation 3 points: slight stimulation but no problem 2 points: stimulation 1 point: strong stimulation (evaluation criteria)
A: Average value is 4 or more and 5 or less B: Average value is 3 or more and less than 4 points C: Average value is 2 or more and less than 3 points D: Average value is 1 or more and less than 2 points

<Bitterness>
(Scoring criteria)
5 points: no bitterness 4 points: little bitterness 3 points: slightly bitterness but no problem 2 points: bitterness 1 point: strong bitterness (evaluation criteria)
A: Average value is 4 or more and 5 or less B: Average value is 3 or more and less than 4 points C: Average value is 2 or more and less than 3 points D: Average value is 1 or more and less than 2 points

(2) Sensory Evaluation of Ease of Pushability Ten test pieces were evaluated for ease of pushability from the degree of finger pressure when the dentifrice composition of each composition was pushed out of a tube using 10 subjects according to the following five-point rating. The evaluation results of 10 persons were averaged and evaluated by the following evaluation criteria.
(Scoring criteria)
3 points: The dentifrice can be easily taken out of the tube with a slight force.
2 points: The dentifrice can be taken out of the tube with a relatively strong force.
1 point: The dentifrice can not come out of the tube unless it is held firmly.
〔Evaluation criteria〕
A: Average value is 2.5 points to 3.0 points B: Average value is 2.0 points to less than 2.5 points C: Average value is 1.5 points to less than 2.0 points D: Average value is Less than 1.5 points

(3) Biofilm removal evaluation <Method for evaluating biofilm removal effect>
(3-1) Model Biofilm Preparation Method A model obtained by treating untreated hydroxyapatite (HA) pellets with a gap of 1 mm wide and 1 mm deep for 4 hours with human unstimulated saliva filtered through a 0.45 μm filter It was installed in the bottom of a 24-hole multiplate (manufactured by Sumitomo Bakelite Co., Ltd.), as a carrier for producing a biofilm. As a culture medium, a baisal medium mucin medium (BMM) ^{* 1} was used.

The strains used to make the model biofilms are: Actinomyces viscosus ATCC 43146, Veyonella parvula ATCC 17745, Fusobacterium nucleatum ATCC 10953, Streptococcus oralis (Actinomyces viscosus) purchased from the American Type Culture Collection oralis) ATCC 10557, Streptococcus mutans ATCC 25175 was used. These five strains were previously inoculated at 1 × 10 ⁷ cfu / mL (cfu: colony forming units) in a Rotating Disk Reactor (culture tank) containing 3,000 mL of BMM, and at 37 ° C. with a saliva-treated HA carrier. The cells were cultured for 24 hours under anaerobic conditions (5 vol% carbon dioxide gas, 95 vol% nitrogen). Then, BMM medium was continuously supplied at the rate of 5 vol% / hr under the same conditions, and culture was carried out for 10 days to form a model biofilm of a mixture of 5 strain species on the HA surface.

* 1 Composition of BMM: Expressed in mass in 1 liter.
Proteose peptone (Becton and Dickinson): 4 g / L
Tryptone (Becton and Dickinson): 2 g / L
Yeast extract (Becton and Dickinson): 2 g / L
Mucin (manufactured by Sigma Co.): 5 g / L
Hemin (manufactured by Sigma Co.): 2.5 mg / L
Vitamin K (Wako Pure Chemical Industries, Ltd.): 0.5 mg / L
KCl (Wako Pure Chemical Industries, Ltd.): 1 g / L
Cysteine (Wako Pure Chemical Industries, Ltd.): 0.2 g / L
Distilled water: Residue (Measured to a total volume of 1 L and autoclaved at 121 ° C for 20 minutes.)

(3-2) Removal Effect of Model Biofilm A white seal is attached to a portion other than the gap of HA before forming the biofilm, and the value of the gap portion measured with a color difference meter is set as L0 as a reference color. After the seal was peeled off and a biofilm was formed by the above method, a white seal was attached again to the portion other than the gap of HA, and the value of the gap portion was measured with a colorimeter to be L1. The seal was removed, and the HA surface was brushed 20 times with a toothbrush loaded with 1 g of the prepared dentifrice, and then lightly washed with running water and dried. Again, a white seal was attached to a portion other than the gap of HA, and the value of the gap measured by a color difference meter was taken as L2. The biofilm removal rate was calculated by the following equation, and the average value of 10 times was evaluated based on the following evaluation criteria, and the biofilm removal effect on the tooth-to-tooth gap was judged from this evaluation result.
[formula]
Biofilm removal rate (%) = [(L1-L2) / (L1-L0)] × 100

Evaluation criteria A: Biofilm removal rate of 80% or more B: Biofilm removal rate of 60% to less than 80% C: Biofilm removal rate of 40% to less than 60% D: Biofilm removal rate of less than 40%

The results are shown in Tables 1 to 3. The numerical values in the table are compounding amounts (% by mass).

Tables 1 to 3 show the following. In Comparative Example 1 which does not contain the component (B) and contains only the component (A), the mucous membrane irritant property is high and the bitter taste is strong, while in the examples containing the components (A) and (B) Was suppressed. Moreover, the dentifrice composition of the Example was also excellent in extrudability and biofilm removal effect. These results show that the composition for oral cavity of the present invention can suppress the mucous membrane irritation and bitter taste of the component (A), can exert the biofilm removing effect inherent to the component (A), and is a dentifrice composition. It shows that extrudability is good and usability is good.

The composition for oral cavity of the present invention is not limited to the toothpaste of the above example, and may be prepared in the form of liquid, liquid, paste or the like. Moreover, it is not limited to the composition of the said Example, It can prepare as dentifrices, such as toothpaste, liquid toothpaste, liquid toothpaste, moist toothpaste, mouthwash etc. of other compositions, and these are prepared by a usual method. be able to.

Claims

An agent for suppressing mucosal irritation and bitter taste, which comprises pyrrolidone carboxylic acid and / or an inorganic base salt thereof.
The agent according to claim 1, which suppresses mucosal irritation and bitter taste by α-olefin sulfonic acid and / or a salt thereof.
An oral composition containing (A) component: α-olefin sulfonic acid and / or a salt thereof, and (B) component: pyrrolidone carboxylic acid and / or an inorganic base salt thereof.
The composition according to claim 3, wherein the content of component (A) is 0.1 to 2% by mass relative to the total amount of the composition.
The composition according to claim 3 or 4, wherein the content of the component (B) is 0.1 to 10% by mass based on the total amount of the composition.
The composition according to any one of claims 3 to 5, wherein the mass ratio ((B) / (A)) of the content of the component (B) to the content of the component (A) is 0.05 to 100. object.