JP7027315B2 - Oral composition - Google Patents

Description

The present invention relates to an oral composition.

In recent years, coloring of exposed root surface dentin due to involution of the gingiva with aging has been reported. In the oral cavity, the tooth surface including root dentin is colored due to various causes. One of the causes is the Maillard reaction caused by a non-enzymatic reaction between a protein derived from pellicle or saliva in the mouth and a saccharide.

Conventionally, an oral composition for preventing coloring of the enamel surface derived from the Maillard reaction has been disclosed. For example, Patent Document 1 discloses an oral composition to which a water-soluble polyphosphate may be blended for the purpose of removing stains on the tooth surface and the tongue surface. The water-soluble polyphosphate is formulated for the purpose of further enhancing the chemical cleaning effect of phenoxyethanol, phenoxypropanol and / or phenoxyisopropanol.

In addition, oral compositions for the purpose of imparting various effects have also been proposed. Patent Document 2 discloses an oral composition containing pyrrolidone carboxylic acid and / or a salt thereof for the purpose of improving the moisturizing effect and its sustainability. Patent Document 3 discloses an oral composition containing pyrrolidone carboxylic acid and / or a salt thereof for the purpose of imparting a feeling of warmth without giving irritation to the oral cavity. Patent Document 4 discloses an oral composition containing pyrrolidone carboxylic acid and / or a salt thereof for the purpose of exhibiting excellent formulation stability and a high anti-inflammatory effect. Patent Document 5 discloses an oral composition containing pyrrolidone carboxylic acid and / or a salt thereof for the purpose of excellent usability and exerting an effect of suppressing plaque adhesion. Neither document discloses that pyrrolidone carboxylic acid and / or a salt thereof exerts an anticoloring effect.

By the way, the binding of the coloring substance of the tooth derived from the Maillard reaction is remarkably stronger in the dentin composed of the complex of the inorganic substance and the organic substance such as collagen than in the enamel composed of the substantially inorganic substance. In addition, the tooth coloring-causing substance that causes the Maillard reaction penetrates into the dentin tissue and causes coloring. Therefore, the conventional color-suppressing technique for enamel has not sufficiently obtained the color-suppressing effect on dentin.

Patent Document 6 proposes a technique for suppressing the coloring of polyphenol (medicinal ingredient) on the surface of root surface dentin by using pyrrolidone carboxylic acid.

Japanese Unexamined Patent Publication No. 2002-47161 Japanese Unexamined Patent Publication No. 2014-189524 JP-A-2015-42625 International Publication No. 2014/157547 Japanese Unexamined Patent Publication No. 2014-40408 International Publication No. 2013/047826

However, when the pyrrolidone carboxylic acid disclosed in Patent Document 6 is used alone, the coloring substance is firmly bonded to the root surface by the interaction between proteins and sugars and organic substances such as collagen constituting dentin, so that dentin is ivory. The inhibitory effect on coloration derived from the Maillard reaction of the pawnbroker is not sufficient.

An object of the present invention is to provide an oral composition having an excellent effect of suppressing coloration on the surface and under the surface layer of dentin.

The present inventors provide the following [1] to [11].
[1] An oral composition containing at least one of (A) component: pyrrolidone carboxylic acid and an inorganic base salt thereof, and (B) component: at least one of water-soluble pyrophosphoric acid and a salt thereof.
[2] The oral composition according to the above [1], wherein the content of the component (A) is 0.1 to 10% by mass.
[3] The oral composition according to the above [1] or [2], wherein the content of the component (B) is 0.01 to 5% by mass.
[4] The oral composition according to any one of the above [1] to [3], wherein the mass ratio (A / B) of the component (A) to the component (B) is 0.1 to 300.
[5] The oral composition according to any one of the above [1] to [4], which further contains a fluorine compound.
[6] The oral composition according to the above [5], wherein the content of the component (C) is 0.01 to 0.5% by mass as the fluorine content.
[7] The oral composition according to any one of the above [1] to [6], which further contains at least one sugar alcohol selected from the group consisting of xylitol, reduced palatinose, and erythritol.
[8] The oral composition according to the above [7], wherein the content of the component (D) is 0.5 to 50% by mass.
[9] The above [7] or [8], wherein the content of xylitol is 0.5 to 10% by mass, the content of reduced palatinose is 2 to 50% by mass, and the content of reduced palatinose is 2 to 50% by mass. The oral composition according to.
[10] The oral composition according to any one of the above [1] to [9], which is a dentifrice or a mouthwash.
[11] A dentin coloring inhibitor containing at least one of (A) component: pyrrolidone carboxylic acid and an inorganic base salt thereof, and (B) component: at least one of water-soluble pyrophosphate and a salt thereof.

According to the present invention, it is possible to provide an oral composition having an excellent effect of suppressing coloration on the surface of dentin and under the surface layer.

Hereinafter, the present invention will be described in detail according to the preferred embodiment thereof.

(1) Oral composition of the present invention The present inventors have diligently studied to obtain an oral composition having an excellent effect of suppressing coloration on the surface and under the surface of dentin as compared with the conventional oral composition. Was piled up. As a result, an oral composition in which at least one of pyrrolidone carboxylic acid and an inorganic base salt thereof and at least one of a water-soluble pyrophosphoric acid and a salt thereof was added to dentin in addition to suppressing strong coloration of the dentin surface. It was found that coloring under the surface layer can also be suppressed.

Sodium pyrophosphate is known as a stain removing component (Japanese Patent Laid-Open No. 10-182389). However, the effect of sodium pyrophosphate is described only for the effect on the adhered / deposited stains on the tooth surface, and it is not described that the effect of suppressing the coloring under the dentin surface layer is obtained.

One embodiment of the oral composition of the present invention contains (A) component: at least one of pyrrolidone carboxylic acid and an inorganic base salt thereof, and (B) component: at least one of water-soluble pyrophosphoric acid and a salt thereof. do.

<Ingredient (A)>
The component (A) contained in the oral composition of the present invention is at least one of pyrrolidone carboxylic acid and an inorganic base salt thereof.

Pyrrolidone carboxylic acid is produced by dehydrating glutamic acid extracted from seaweed, wheat flour and sugar cane, and has a structure represented by the following formula (1).

The method for producing pyrrolidone carboxylic acid or an inorganic base salt thereof is not particularly limited. As such a production method, for example, glutamic acid extracted from an organism such as seaweed and sugar cane or from a processed product such as wheat flour is dehydrated to obtain pyrrolidone carboxylic acid, and a metal ion (for example, sodium ion) is bound thereto. The method can be mentioned.
Examples of the inorganic base salt of pyrrolidone carboxylic acid include 1 to trivalent inorganic base salts of pyrrolidone carboxylic acid. Examples of the 1- to trivalent inorganic base salt include 1- to trivalent metal salts. Examples of the monovalent to trivalent metal salt include alkali metal salts such as sodium salt and potassium salt; alkaline earth metal salts such as calcium salt and magnesium salt; copper salt, zinc salt, aluminum salt and the like. Among these, sodium salt, potassium salt, calcium salt, magnesium salt and aluminum salt are preferable, and sodium salt and potassium salt are more preferable.

Commercially available products may be used for pyrrolidone carboxylic acid and its inorganic base salt. As a commercially available product of pyrrolidone carboxylic acid, "AJIDEW A-100 (registered trademark)" manufactured by Ajinomoto Healthy Supply Co., Ltd. can be mentioned. Examples of commercially available products of sodium pyrrolidone carboxylate include "AJIDEW-N-50 (registered trademark); PCA soda (AI = 50% aqueous solution)".

The component (A) may be used alone or in combination of two or more.

The content of the component (A) in the oral composition of the present invention is preferably 0.1% by mass or more, more preferably 0.3% by mass or more, based on the entire oral composition. .. This makes it possible to sufficiently obtain the effect of suppressing coloration on the surface of dentin and under the surface layer. The upper limit of the content of the component (A) is not particularly limited, but is preferably 10% by mass or less, more preferably 5% by mass or less, based on the entire oral composition. As a result, pyrrolidone carboxylic acid or a salt thereof can be dissolved to sufficiently obtain the effect of suppressing coloration on the dentin surface and under the surface layer, and the stability of the preparation can be maintained.

The content of the component (A) in the oral composition of the present invention is preferably 0.1 to 10% by mass, preferably 0.3 to 5% by mass, based on the entire oral composition. More preferred. The lower limit of the content of the component (A) is not particularly limited, but if it is less than 0.1% by mass, the effect of suppressing coloration on the dentin surface and under the surface layer may not be sufficiently obtained. be. The upper limit of the content of the component (A) is not particularly limited, but if it exceeds 10% by mass, the effect of suppressing coloration on the dentin surface may be inferior.

In the present invention, the content of each component contained in the oral composition is a value based on the amount of each component charged when preparing the composition.

<Ingredient (B)>
The component (B) contained in the oral composition of the present invention is at least one of water-soluble pyrophosphate and a salt thereof. In particular, the water-soluble pyrophosphate is represented by the chemical formula _{M4 ・ P 2O 7 ( in} the formula, M is a hydrogen ion or an alkali metal ion such as sodium or potassium), and is a compound obtained by dehydration condensation of phosphoric acid. Is.

As at least one of the water-soluble pyrophosphate and its salt, pyrophosphate; an alkali metal salt of pyrophosphate such as tetrasodium pyrophosphate, dihydrogen dihydrogen pyrophosphate, dipotassium pyrophosphate, and tetrapotassium pyrophosphate may be used. be. Suitable specific examples include pyrophosphate, sodium pyrophosphate, potassium pyrophosphate, and disodium dihydrogen pyrophosphate. As these compounds, commercially available products manufactured by Taihei Kagaku Sangyo Co., Ltd. may be used.

The component (B) may be used alone or in combination of two or more.

The content of the component (B) in the oral composition of the present invention is preferably 0.01% by mass or more, more preferably 0.1% by mass or more, based on the entire oral composition. .. Thereby, the effect of suppressing the coloring of the dentin surface can be sufficiently obtained. The upper limit of the content of the component (B) is not particularly limited, but is preferably 5% by mass or less, and more preferably 3% by mass or less, based on the entire oral composition. As a result, the effect of suppressing coloration under the surface layer of dentin can be sufficiently obtained.

The content of the component (B) in the oral composition of the present invention is preferably 0.01 to 5% by mass, preferably 0.1 to 3% by mass, based on the entire oral composition. More preferred. The lower limit of the content of the component (B) is not particularly limited, but if it is less than 0.01% by mass, the effect of suppressing coloration of the dentin surface may not be sufficiently obtained. The upper limit of the content of the component (B) is not particularly limited, but if it exceeds 5% by mass, the effect of suppressing coloring under the surface layer of dentin may be inferior.

The lower limit of the mass ratio ((A) / (B)) of the component (A) to the component (B) is preferably 0.1 or more, and more preferably 0.3 or more. This makes it possible to sufficiently obtain the effect of suppressing coloration on the surface of dentin and under the surface layer. Further, the upper limit of the mass ratio ((A) / (B)) of the component (A) to the component (B) is preferably 300 or less, more preferably 50 or less, and 30 or less. Is more preferable. Thereby, the effect of suppressing the coloring of the dentin surface can be sufficiently obtained.

The mass ratio ((A) / (B)) of the component (A) to the component (B) is preferably 0.1 to 300, more preferably 0.1 to 50, and 0.3 to 0.3. It is more preferably 30. If the mass ratio is less than 0.1, the effect of suppressing coloration on the dentin surface and under the surface layer may be inferior. On the other hand, when the mass ratio exceeds 300, the effect of suppressing coloration on the dentin surface may be inferior.

Other embodiments of the oral composition of the present invention include (A) component: at least one of pyrrolidone carboxylic acid and an inorganic base salt thereof, and (B) component: at least one of water-soluble pyrophosphate and a salt thereof. C) Ingredient: Contains a fluorine compound. By blending the component (C) into the oral composition containing the component (A) and the component (B), the effect of suppressing coloration under the surface layer of dentin can be further improved.

<Ingredient (C)>
Specific examples of the fluorine compound include sodium fluoride, potassium fluoride, ammonium fluoride, tin fluoride, amine fluoride, sodium monofluorophosphate, potassium monofluorophosphate, sodium silicon fluoride, and calcium silicon fluoride. be able to. Of these, sodium fluoride and sodium monofluorophosphate are particularly preferable.

A commercially available product may be used as the fluorine compound. As an example of a commercially available product of sodium fluoride, "sodium fluoride" sold by Stella Chemifa Co., Ltd. can be mentioned. As an example of a commercially available product of sodium monofluorophosphate, "sodium monofluorophosphate" sold by Rhodia Nikka Co., Ltd. can be mentioned. As the component (C), one type of fluorine compound may be used alone, or two or more types of fluorine compounds may be used in combination.

The effect of the component (C) to be blended in the oral composition of the present invention is borne by the fluorine in the component (C). Therefore, it is more useful to specify the content of the component (C) in terms of the fluorine content in the oral composition. Therefore, in the following description, the content of the component (C) is shown by substituting the fluorine content in the oral composition.

The content of the component (C) to be blended in the oral composition of the present invention is preferably 0.01% by mass (100 ppm) or more, preferably 0.02% by mass (100 ppm) or more as the fluorine content with respect to the entire oral composition. 200 ppm) or more is more preferable. As a result, the effect of suppressing coloration under the surface layer of dentin can be sufficiently obtained. The upper limit of the content of the component (C) is not particularly limited, but is preferably 0.5% by mass (5000 ppm) or less, preferably 0.4% by mass (4000 ppm) or less, based on the entire oral composition. Is more preferable. As a result, the stability of the fluorine compound in the pharmaceutical product produced by using the oral composition becomes good, and the effect of improving the color suppression under the dentin surface layer can be sufficiently obtained.

The content of the component (C) to be blended in the oral composition of the present invention is preferably 0.01 to 0.5% by mass (100 to 5000 ppm) as the fluorine content with respect to the entire oral composition, and is 0. 0.02 to 0.4% by mass (200 to 4000 ppm) is more preferable. If the fluorine content is less than 0.01% by mass (100 ppm), the effect of suppressing coloration under the dentin surface layer may not be sufficiently improved. In addition, if it exceeds 0.5% by mass (5000 ppm), the stability of the fluorine compound in the pharmaceutical product produced by using the oral composition may deteriorate, so that the coloration under the dentin surface layer is suppressed. The improvement effect may not be sufficiently obtained.

The lower limit of the mass ratio ((A) / (C)) of the component (A) to the component (C) is preferably 0.8 or more, more preferably 1 or more, and 8 or more. Is particularly preferable. As a result, the effect of improving color suppression under the surface layer of dentin becomes remarkable. Further, the upper limit of the mass ratio ((A) / (C)) of the component (A) to the component (C) is preferably 250 or less, and more preferably 150 or less. As a result, the effect of improving color suppression under the surface layer of dentin becomes remarkable.

The mass ratio ((A) / (C)) of the component (A) to the component (C) is preferably 0.8 to 250, more preferably 1 to 250, and particularly preferably 8 to 150.

Yet another embodiment of the oral composition of the present invention comprises (A) a component: at least one of pyrrolidone carboxylic acid and a salt thereof, and a component (B): at least one of a water-soluble pyrophosphate and a salt thereof, (D). ) Ingredients: Contains at least one sugar alcohol selected from the group consisting of xylitol, reduced palatinose, and erythritol. By blending the component (D) in the oral composition containing the component (A) and the component (B), the irritation to the oral mucosa peculiar to condensed phosphoric acid is alleviated, so that the usability is improved. At the same time, the effect of suppressing coloration on the dentin surface can be further improved.

The oral composition in still another embodiment may or may not contain the component (C). However, since the effect of the oral composition containing the component (C) and the effect of the oral composition containing the component (D) do not cancel each other, the oral composition in still another embodiment contains the component (C). It is preferable to contain it. In this case, it can be said that the content regarding the component (C) is the same as the content described in <(C) component> above.

<(D) component>
The sugar alcohol used as the component (D) is xylitol, erythritol, and reduced palatinose. The component (D) may be used alone or in combination of two or more.

The content of the component (D) with respect to the entire oral composition is not particularly limited, but the total amount is preferably 0.5 to 50% by mass. When xylitol is used as the component (D), its content is preferably 0.5% by mass or more, and more preferably 3% by mass or more. The upper limit of the xylitol content is not particularly limited, but is preferably 10% by mass or less, and more preferably 7% by mass or less.

When xylitol is used as the component (D), its content is preferably 0.5 to 10% by mass, more preferably 3 to 7% by mass.

When reduced palatinose is used as the component (D), the content thereof is preferably 2% by mass or more, more preferably 10% by mass or more. The upper limit of the content of reduced palatinose is not particularly limited, but is preferably 50% by mass or less, and more preferably 40% by mass or less.

When reduced palatinose is used as the component (D), the content thereof is preferably 2 to 50% by mass, more preferably 10 to 40% by mass.

When erythritol is used as the component (D), its content is preferably 2% by mass or more, and more preferably 10% by mass or more. The upper limit of the content of erythritol is not particularly limited, but is preferably 50% by mass or less, and more preferably 40% by mass or less.

When erythritol is used as the component (D), the content thereof is preferably 2 to 50% by mass, more preferably 10 to 40% by mass.

If it is less than the lower limit, the effect of improving usability may not be sufficiently obtained, and the effect of suppressing coloration of the dentin surface may be insufficiently improved. When two or more kinds of the component (D) are used in combination, the total content of the component (D) with respect to the entire oral composition is preferably 50% by mass or less. When the total content of the component (D) exceeds 50% by mass, the stability of the component (D) in the formulation produced by using the oral composition deteriorates, so that the effect of suppressing the coloring of the dentin surface is achieved. May be inadequate.

In addition to each of the above components, the oral composition of the present invention can contain any necessary components.

<Arbitrary ingredient>
Optional ingredients include, for example, surfactants, abrasives, binders, thickeners, sweeteners, preservatives, flavors, medicinal ingredients, and water. The optional component can be blended in the oral composition of the present invention as long as the effect of the present invention is not impaired. Specific examples of the optional components are shown below, but the optional components that can be blended in the oral composition of the present invention are not limited thereto.

Types of surfactants include anionic surfactants, nonionic surfactants, amphoteric surfactants and the like. Examples of the surfactant include anionic surfactants such as N-acyl amino acid salt, α-olefin sulfonate, N-acyl sulfonate, alkyl sulfate, and sulfate of glycerin fatty acid ester; polyoxyethylene alkyl ether. , Polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene hydrogenated castor oil, polyoxyethylene ether of glycerin ester, sucrose fatty acid ester, sorbitan fatty acid ester, nonionic surfactant such as alkyrrole amide; fatty acid amide propyl There are amphoteric surfactants such as betaine. When the oral composition contains a surfactant, it is usually 0 to 10% by mass, preferably 0.01 to 5% by mass, based on the total amount of the oral composition. It should be noted that these surfactants may be used alone or in combination of two or more.

As the anionic surfactant, N-acylamino acid salts, α-olefin sulfonates, alkyl sulfates and the like are preferably used, particularly from the viewpoint of versatility. Specific examples of anionic surfactants include sodium lauroyl sarcosine in terms of foamability and water resistance, sodium α-olefin sulfonate having 10 to 16 carbon atoms as the carbon chain length of an alkyl chain, sodium lauryl sulfate, and the like. Is preferable.

As the nonionic surfactant, polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, alquilolamide, sorbitan fatty acid ester and the like are preferably used, particularly from the viewpoint of versatility. As a nonionic surfactant, specifically, a polyoxyethylene alkyl ether having 14 to 18 carbon atoms as a carbon chain length of an alkyl chain and an average ethylene oxide addition mole number of 15 to 30, and an ethylene oxide average addition mole number of 40. ~ 100 polyoxyethylene oxide hardened castor oil, alkylol amide having 12 to 14 carbon atoms as the carbon chain length of the alkyl chain, sorbitan fatty acid ester having 12 to 18 carbon atoms in the fatty acid, and 16 to 18 carbon atoms in the fatty acid. , Polyoxyethylene sorbitan fatty acid ester having an average number of added moles of ethylene oxide of 10 to 40 is preferable.

As the amphoteric tenside, betaine-based ones are preferable, and for example, alkyl betaine-based, fatty acid amide propyl betaine-based, and alkylimidazolinium betaine-based amphoteric surfactants are preferably used. Specific examples of the amphoteric surfactant include alkyldimethylaminoacetate betaine such as lauryldimethylaminoacetic acid betaine; and alkylimidazolinium betaine such as 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine; Examples thereof include fatty acid amide propyl betaine systems such as coconut oil fatty acid amide propyldimethylaminoacetic acid betaine and coconut oil fatty acid amide propyl betaine. Among them, the amphoteric tenside agent is preferably coconut oil fatty acid amide propyl betaine or 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine.

Examples of the polishing agent include silica-based polishing agents such as silicic acid anhydride, crystalline silica, amorphous silica, silica gel, and aluminosilicate; zeolite, calcium hydrogen phosphate anhydrate, calcium hydrogen phosphate dihydrate, and the like. There are synthetic resin-based abrasives such as calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, magnesium tertiary phosphate, zirconium silicate, calcium tertiary phosphate, hydroxyapatite, and calcium tetraphosphate. When an abrasive is added to the oral composition, the dentifrice is preferably 0 to 40% by mass, more preferably 5 to 20% by mass, based on the total amount of the composition. In a liquid preparation such as a mouthwash, it is preferably 0 to 10% by mass, more preferably 0 to 5% by mass, based on the total composition.

Examples of the binder include pullulan, gelatin, carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, xanthan gum, arabic gum, guar gum, locust bean gum, polyvinyl alcohol, polyvinylpyrrolidone, sodium polyacrylate, and thickening agent. There is silica. When the oral composition contains a binder, the content thereof is usually 0.01 to 10% by mass based on the total amount of the preparation produced by using the oral composition.

Examples of the thickener include propylene glycol, butylene glycol, glycerin, sorbitol, and polyethylene glycol. When the oral composition contains a viscous agent, the content thereof is usually 1 to 50% by mass based on the total amount of the preparation produced by using the oral composition.

Examples of sweeteners include sodium saccharin, stebioside, neohesperidin hydrochalcone, glycyrrhizin, perillartine, p-methoxycinnamic aldehyde, thaumatin, and maltitol. When a sweetener is used, the blending amount can be appropriately determined as long as the effect of the present invention is not impaired.

Examples of preservatives include sodium benzoate, paraoxybenzoic acid ester, methylparaben, ethylparaben, butylparaben, ethylenediamine tetraacetate, and benzalkonium chloride. When a preservative is used, the blending amount can be appropriately determined as long as the effect of the present invention is not impaired.

As fragrances, for example, essential oils such as peppermint and spearmint; fruit-based essences such as lemon and strawberry; 1-menthol, carboxylic, eugenol, anator, linalol, limonene, ossimen, cineol, n-decyl alcohol, citronellol, crocodile, etc. There are fragrance materials such as α-terpineol, methyl salicylate, timol, rosemary oil, sage oil, perilla oil, lemon oil and orange oil. When the oral composition contains a fragrance material, it is preferably 0.000001 to 1% by mass with respect to the total amount of the oral composition.

Further, as medicinal ingredients, bactericidal or antibacterial agents such as chlorhexidine, triclosan, isopropylmethylphenol, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, zinc gluconate, zinc citrate; Anti-inflammatory agents such as tranexamic acid, glycyrrhizin dipotassium salt, ε-aminocaproic acid; coating agents such as hydroxyethyl cellulose dimethyldiallyl ammonium chloride; enzyme agents such as dextranase and mutanase can be used.

Further, as the dosage form, a dentifrice, a mouthwash and the like are preferable from the viewpoint of effectiveness and stability, and water, ethanol and the like can be blended as the solvent.

The blending ratio of these optional components can be set to a normal dose within a range that does not impair the effects of the oral composition of the present invention.

From the viewpoint of stability, the pH of the oral composition of the present invention is preferably 5 to 9, more preferably 6 or 7 to 8, and the pH is adjusted by using a pH adjuster as necessary. be able to. Examples of the pH adjuster include phosphoric acid or a salt thereof (sodium phosphate, sodium hydrogenphosphate, etc.), citric acid or a salt thereof (sodium citrate, etc.), malic acid or a salt thereof, gluconic acid or a salt thereof, maleic acid or The salt, succinic acid or a salt thereof, glutamic acid or a salt thereof, lactic acid, hydrochloric acid, acetic acid, nitrate, sodium hydroxide, potassium hydroxide and the like may be used as long as the effects of the oral composition of the present invention are not impaired. can.

(2) Dentin Coloring Inhibitor of the Present Invention When the above-mentioned components (A) and (B) are used in combination, it is possible to prevent coloring of dentin, in particular, the surface and under the surface of dentin. Therefore, the composition containing the component (A) and the component (B) is useful as an dentin coloring inhibitor, particularly an ivory coloring inhibitor by the Maillard reaction derived from dentin collagen which is a dentin tissue.

The administration form of the dentin coloring inhibitor of the present invention is not particularly limited. For example, it can be administered as a mouthwash, a mouthwash, or a dentifrice (liquid dentifrice, gel-like dentifrice, dentifrice, etc.).

The target person for using the dentin coloring inhibitor of the present invention is not particularly limited. However, from the viewpoint of preventing coloring of dentin, elderly people and subjects in which gingival involution is observed are preferable.

Hereinafter, the present invention will be described in detail with reference to Examples. The following examples are for the purpose of suitably explaining the present invention, and do not limit the present invention. In addition, "%" means "mass%" unless otherwise specified.

Details of each component used in the preparation of the oral compositions of Examples 1 to 36 and Comparative Examples 1 to 3 are described below.
<Ingredient (A)>
Sodium pyrrolidonecarboxylate, manufactured by Ajinomoto Co., Inc., trade name "AJIDEW N-50 (registered trademark)"
<Ingredient (B)>
Sodium pyrophosphate Taihei Kagaku Sangyo Co., Ltd. <(C) component>
Sodium Fluoride Made by Stella Chemipha Co., Ltd. (Purified Sodium Fluoride (S))
Sodium monofluorophosphate manufactured by ICL Japan Co., Ltd. <(D) component>
Xylitol Rocket Japan Co., Ltd. Reduced Palatinose Mitsui Sugar Co., Ltd. Erythritol Mitsubishi Chemical Foods Co., Ltd. <Other additive components>
Sodium lauryl sulfate (surfactant), solvent (viscosing agent), propylene glycol (viscosing agent), sodium saccharin (sweetening agent), xanthan gum (caking agent), silicic acid anhydride (polishing agent), fragrance, purified water ( solvent)
As the above-mentioned additive component, a cosmetic raw material standard standard product was used.

Examples 1-36 and Comparative Examples 1-3
Using the above components, the dentifrice compositions of Examples 1 to 36 and Comparative Examples 1 to 3 were prepared by the following preparation methods according to the formulation shown in Tables 1 to 6.

(Preparation method of dentifrice composition)
After dissolving (component A) sodium pyrrolidone carboxylate, (component B) sodium pyrophosphate, (component C) fluorine compound, (component D) sugar alcohol, 100% by mass sorbitol, and sodium saccharin in purified water, propylene is separately used. A solution in which glycol and xanthan gum were dispersed was added, and the mixture was stirred. Then, sodium lauryl sulfate, a fragrance, and an abrasive were added, and the mixture was further stirred under reduced pressure (pressure 4 kPa) to prepare a dentifrice composition. A 1.5L kneader (manufactured by Ishiyama Kosakusho Co., Ltd.) was used for manufacturing. With respect to the prepared dentifrice composition, the effect of suppressing coloration on the dentin surface and under the surface layer was evaluated and the usability was evaluated according to the following procedure. The evaluation results are also shown in Tables 1-6.

(Evaluation of color suppression effect on dentin surface)
1. 1. Preparation of Maillard reaction solution 1% glycine and 1% glucose were heated at 110 ° C. for 1 hour in an autoclave to prepare a Maillard reaction solution.

2. 2. Formation of coloring model Cow tooth roots were cut into blocks and cementum was removed by surface polishing. Of the parts from which the cementum had been removed, about 3.5 mm × 3.5 mm was used for the decalcification window, and the other parts were covered with nail polish. After drying the manicure at room temperature, a root dentin sample was prepared by immersing the manicure in an aqueous acetic acid solution (pH 4.5) of 0.1 mol / L for 50 hours to expose collagen in the window portion.

First, as initial values, the color difference (L ^* 0, a ^* 0, b ^* 0) was measured using a spectrocolorimeter (CM-2022, manufactured by Minolta Co., Ltd.). The discharged saliva was centrifuged (10000 g, 20 minutes, 20 ° C.), and the root surface dentin sample was stirred and immersed in the obtained supernatant for 30 minutes at 37 ° C., and then Examples 1 to 6 shown in Tables 1 to 6 were used. 36 and Comparative Examples 1 to 3 were immersed in a 3-fold aqueous diluted solution of the dentin composition for 3 minutes at room temperature. Then, in order to form a stained pellicle, it was immersed in 1% bovine serum albumin, 1% lysozyme chloride, Maillard reaction solution, 1% pig gastric mucin, and 1% lactoferrin (pH 7.0) in this order at 37 ° C. for 10 minutes each. The process from the above treatment of saliva supernatant to the operation of pellicle formation was repeated 4 times a day for a total of 5 days.

3. 3. Evaluation of color suppression effect on dentin surface The measurement window was lightly rinsed with distilled water, and excess water was absorbed with filter paper. After drying, the color difference (L ^* 1, a ^* 1, b ^* 1) was measured three times, and the average value was calculated. The coloring suppressing effect was evaluated by the following evaluation criteria using the ΔE value calculated from the following formula.
ΔE value = ((L ^* 1-L ^* 0) ² + (a ^* 1-a ^* 0) ² + (b ^* 1-b ^* 0) ² ) ^1/2

[Coloring evaluation criteria]
A: ΔE <10
B: 10≤ΔE <15
C: 15≤ΔE <20
D: 20≤ΔE <25
E: 25≤ΔE

(Evaluation of color suppression effect under the surface layer of dentin)
A root surface dentin sample was prepared in the same manner as the method prepared in (Evaluation of the effect of suppressing coloration on the dentin surface). After immersing in the discharged saliva and a 3-fold diluted solution of the dentifrice composition of Examples 1 to 36 and Comparative Examples 1 to 3 shown in Tables 1 to 6, a stained pellicle was formed. The depth of subsurface coloring from the collagen surface in the formed stained pellicle window was measured using a stereomicroscopic observation image, and evaluated according to the following evaluation criteria.

[Evaluation criteria for subsurface coloring]
A: Coloring under the surface layer from the surface <15 μm
B: 15 μm ≤ under-surface coloring from the surface <20 μm
C: 20 μm ≤ under-surface coloring from the surface <50 μm
D: 50 μm ≤ under-surface coloring from the surface <100 μm
E: 100 μm ≤ Coloring under the surface layer from the surface

Evaluation of usability (no irritation) Twenty panelists were asked to put a treatment solution obtained by diluting the dentifrice composition of each example / comparative example 3-fold with distilled water in the mouth for 30 seconds, and the oral cavity after discharge. The presence or absence of internal pain was evaluated. The evaluation criteria were set as follows.

〔Evaluation criteria〕
A: 1 or less people who have pain B: 2 or more and 5 or less people who have pain C: 6 or more and less than 10 people who have pain D: 10 or more people who have pain

As can be seen from the results of Comparative Example 1, it can be seen that even if sodium pyrophosphate is used alone, there is almost no effect of suppressing coloration on the dentin surface and under the surface layer. Further, as can be seen from the results of Comparative Example 2, even when sodium pyrrolidone carboxylate known to be able to suppress the coloring of polyphenol (medicinal effect component) on the surface of the root surface dentin is used, Maillard of the dentin tissue is used. It can be seen that there is almost no inhibitory effect on coloring derived from the reaction. Further, as can be seen from the results of Comparative Example 3, it can be seen that even if a known sodium tripolyphosphate is used as a stain removing component as in the case of sodium pyrophosphate, there is almost no effect of suppressing coloration on the dentin surface and under the surface layer. On the other hand, as can be seen from Examples 1 to 13, the combined use of sodium pyrrolidone carboxylate and sodium pyrophosphate produced an effect of suppressing coloration on the dentin surface and under the surface layer.

As can be seen from the results of Examples 14 to 18, when the (C) fluorine compound is added to the dentin composition containing sodium pyrrolidone carboxylate and sodium pyrophosphate having an effect of suppressing coloration on the dentin surface and under the surface layer. , The color-suppressing effect under the dentin surface layer was further improved without losing other effects.

As can be seen from the results of Examples 19 to 24, when (D) sugar alcohol is added to the dentin composition containing sodium pyrolydone carboxylate and sodium pyrophosphate that have an effect of suppressing coloration on the dentin surface and under the surface layer. The effect of suppressing coloration on the surface of dentin was further improved, and the preparation was excellent in non-irritating and the feeling of use was also improved.

As can be seen from the results of Examples 25 to 36, (C) a fluorine compound and (D) a fluorinated compound and (D) were added to the dentifrice composition containing sodium pyrrolidone carboxylate and sodium pyrophosphate having an effect of suppressing coloration on the dentin surface and under the surface layer. ) When sugar alcohol was added, the effect of suppressing coloration on dentin was further improved, and the feeling of use was also improved.

In order to investigate the applicable range of the oral composition of the present invention, a mouthwash (Example 37), a mouthwash (Example 38), and a gel-like dentin (Example 39) were produced, and the above evaluation test was performed. In each case, the effect of suppressing coloration on the surface of dentin and the effect of suppressing coloration under the surface layer of dentin were A, and the evaluation of usability (no irritation) was A. The composition of each is shown below.

[Mouthwash]
Composition A component: sodium pyrrolidone carboxylate (manufactured by Wako Pure Chemical Industries, Ltd.): 3%
Component B: Potassium pyrophosphate (manufactured by Taihei Kagaku Sangyo Co., Ltd.): 1%
C component: Sodium fluoride (manufactured by Stella Chemipha Co., Ltd.) 0.04% (Fluorine content: 0.02%)
C component: Sodium monofluorophosphate (manufactured by ICL Japan Co., Ltd.) 0.23% (Fluorine content: 0.03%)
D component: Xylitol (manufactured by Rocket Japan Co., Ltd.): 5%
Ingredient D: Reduced palatinose (manufactured by Mitsui Sugar Co., Ltd.): 15%
Glycerin: 5%
Ethanol: 8%
Polyoxyethylene hydrogenated castor oil (60EO): 0.8%
Sodium citrate: 0.1%
Citric acid: 0.3%
Sodium benzoate: 0.5%
Fragrance: 0.2%
Purified water: balance

[Mouth refreshing agent]
Composition A component: sodium pyrrolidone carboxylate (manufactured by Wako Pure Chemical Industries, Ltd.): 3%
Component B: Potassium pyrophosphate (manufactured by Taihei Kagaku Sangyo Co., Ltd.): 1%
C component: Sodium fluoride (manufactured by Stella Chemipha Co., Ltd.): 0.04% (Fluorine content: 0.02%)
D component: Xylitol (manufactured by Rocket Japan Co., Ltd.): 5%
Ingredient D: Reduced palatinose (manufactured by Mitsui Sugar Co., Ltd.): 10%
D component: Erythritol (manufactured by Mitsubishi Chemical Foods Co., Ltd.): 10%
Glycerin: 13%
Ethanol: 40%
Polyoxyethylene hydrogenated castor oil (60EO): 3%
Sodium citrate: 0.1%
Citric acid: 0.03%
Menthol: 0.3%
Fragrance: 0.4%
Purified water: balance

[Gel-like toothpaste]
Composition A component: sodium pyrrolidone carboxylate (manufactured by Wako Pure Chemical Industries, Ltd.): 3%
Component B: Potassium pyrophosphate (manufactured by Taihei Kagaku Sangyo Co., Ltd.): 1%
C component: Sodium fluoride (manufactured by Stella Chemipha Co., Ltd.): 0.04% (Fluorine content: 0.02%)
D component: Xylitol (manufactured by Rocket Japan Co., Ltd.): 5%
Ingredient D: Reduced palatinose (manufactured by Mitsui Sugar Co., Ltd.): 10%
D component: Erythritol (manufactured by Mitsubishi Chemical Foods Co., Ltd.): 10%
Viscous silica: 1.5%
Propylene glycol: 3%
Sorbitol solution: 55%
Carrageenan: 0.3%
Xanthan gum: 0.3%
Cetylpyridinium chloride: 0.02%
Saccharin sodium: 0.12%
Potassium nitrate: 5%
Coconut oil fatty acid amide propyl betaine solution: 0.3%
Fragrance: 0.4%
Purified water: balance

Claims (11)

(A) Ingredient: At least one of pyrrolidone carboxylic acid and its inorganic base salt,
(B) Ingredient: Oral composition containing at least one of water-soluble pyrophosphate and a salt thereof (excluding the dentifrice composition containing a zinc salt of pyrrolidonecarboxylic acid, tetrapotassium pyrophosphate and xylitol). .. (A) The oral composition according to claim 1, wherein the content of the component is 0.1 to 10% by mass. (B) The oral composition according to claim 1 or 2, wherein the content of the component is 0.01 to 5% by mass. The oral composition according to any one of claims 1 to 3, wherein the mass ratio (A / B) of the component (A) to the component (B) is 0.1 to 300. (C) The oral composition according to any one of claims 1 to 4, further containing a fluorine compound. The oral composition according to claim 5, wherein the content of the component (C) is 0.01 to 0.5% by mass as the fluorine content. (D) The oral composition according to any one of claims 1 to 6, further comprising at least one sugar alcohol selected from the group consisting of xylitol, reduced palatinose, and erythritol. The oral composition according to claim 7, wherein the content of the component (D) is 0.5 to 50% by mass. The oral composition according to claim 7 or 8, wherein the content of xylitol is 0.5 to 10% by mass, the content of reduced palatinose is 2 to 50% by mass, and the content of reduced palatinose is 2 to 50% by mass. thing. The oral composition according to any one of claims 1 to 9, which is a dentifrice or a mouthwash. (A) Ingredient: At least one of pyrrolidone carboxylic acid and its inorganic base salt,
(B) Ingredient: A dentin coloring inhibitor containing at least one of water-soluble pyrophosphoric acid and a salt thereof.