KR102579556B1 - Oral composition - Google Patents

Abstract

The object is to provide an oral composition that is excellent in the effect of suppressing staining on the dentin surface and below the surface layer, comprising (A) component: at least one of pyrrolidone carboxylic acid and its salt, and (B) component: water-soluble pyrophosphoric acid. and an oral composition containing at least one of its salts.

Description

Oral composition

The present invention relates to compositions for oral use.

Recently, discoloration of tooth root surface dentin exposed due to gum recession due to aging has become a public issue. In the oral cavity, the tooth surface, including root surface dentin, becomes stained due to various reasons. One of the causes is the Maillard reaction, which occurs due to a non-enzymatic reaction between proteins and sugars derived from the pellicle or saliva in the mouth.

Conventionally, oral compositions aimed at preventing discoloration of the enamel surface resulting from the Maillard reaction have been disclosed. For example, Patent Document 1 discloses an oral composition containing a water-soluble polyphosphate for the purpose of removing contamination from the tooth and tongue surfaces. Water-soluble polyphosphates are formulated to enhance the chemical cleaning effect of phenoxyethanol, phenoxypropanol and/or phenoxyisopropanol.

Additionally, oral compositions aimed at providing various effects have also been proposed. Patent Document 2 discloses an oral composition containing pyrrolidone carboxylic acid and/or its salt for the purpose of improving the wetting effect and its sustainability. Patent Document 3 discloses an oral composition containing pyrrolidone carboxylic acid and/or its salt for the purpose of providing warmth without causing irritation in the oral cavity. Patent Document 4 discloses an oral composition containing pyrrolidone carboxylic acid and/or its salt for the purpose of exhibiting excellent formulation stability and a high anti-inflammatory inhibitory effect. Patent Document 5 discloses an oral composition containing pyrrolidone carboxylic acid and/or its salt for the purpose of being excellent in usability and exhibiting an effect of suppressing dental plaque adhesion. No literature discloses that pyrrolidone carboxylic acid and/or its salts exhibit a discoloration prevention effect.

However, the bond of the tooth coloring material derived from the Maillard reaction is significantly stronger in dentin, which is composed of a complex of minerals and organic materials such as collagen, than in enamel, which is composed mostly of inorganic materials. Additionally, the substance that causes the Maillard reaction to stain teeth penetrates into the dentin tissue and causes staining. Therefore, a sufficient staining inhibition effect on dentin is not obtained with conventional staining suppression techniques on enamel.

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

Japanese Patent Publication No. 2002-47161 Japanese Patent Publication No. 2014-189524 Japanese Patent Publication No. 2015-42625 International Publication No. 2014/157547 Japanese 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 material is strongly bound to the tooth root surface due to the interaction between proteins and sugars and organic substances such as collagen that constitutes dentin, thereby damaging the mail of the dentin tissue. The inhibitory effect on staining resulting from the Raad reaction is not sufficient.

The object of the present invention is to provide an oral composition that has an excellent effect of suppressing staining on the surface and under the surface layer of dentin.

The present inventors provide the following [1] to [11].

[1] An oral composition containing (A) component: at least one of pyrrolidone carboxylic acid and its inorganic base salt, and (B) component: at least one of water-soluble pyrophosphoric acid and its salt.

[2] The oral composition according to [1] above, wherein the content of component (A) is 0.1 to 10% by mass.

[3] The oral composition according to [1] or [2] above, wherein the content of component (B) is 0.01 to 5% by mass.

[4] The oral composition according to any one of [1] to [3] above, wherein the mass ratio (A/B) of component (A) and component (B) is 0.1 to 300.

[5] The oral composition according to any one of the above [1] to [4], further comprising (C) component: a fluorine compound.

[6] The oral composition according to [5] above, wherein the content of component (C) is 0.01 to 0.5% by mass in terms of fluorine content.

[7] The oral drug according to any one of the above [1] to [6], further comprising component (D): at least one sugar alcohol selected from the group consisting of xylitol, reduced paratinose, and erythritol. Composition.

[8] The oral composition according to [7] above, wherein the content of component (D) is 0.5 to 50% by mass.

[9] The method of [7] or [8] above, wherein the xylitol content is 0.5 to 10 mass%, the reduced paratinose content is 2 to 50 mass%, and the reduced paratinose content is 2 to 50 mass%. Oral composition.

[10] The oral composition according to any one of [1] to [9] above, which is a dentifrice or oral rinse.

[11] A dentin staining inhibitor containing (A) component: at least one of pyrrolidone carboxylic acid and its inorganic base salt, and (B) component: water-soluble pyrophosphoric acid and at least one of its salts.

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

Hereinafter, the present invention will be described in detail based on its preferred embodiments.

(1) Oral composition of the present invention

The present inventors conducted intensive studies to obtain an oral composition that has an excellent effect of suppressing staining on the surface and under the surface layer of dentin compared to conventional oral compositions. As a result, in addition to suppressing staining of the dentin surface, the oral composition combining at least one of pyrrolidone carboxylic acid and its inorganic base salt and water-soluble pyrophosphoric acid and at least one of its salts I discovered that the coloring below can also be suppressed.

Sodium pyrophosphate is known as a stain removal ingredient (Japanese Patent Application Laid-Open No. 10-182389). However, the effect of sodium pyrophosphate is only described as an effect on contamination adhered and deposited on the tooth surface, and it is not described that it has an inhibitory effect on staining below the surface layer of dentin.

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

<(A) Ingredient>

Component (A) contained in the oral composition of the present invention is at least one of pyrrolidone carboxylic acid and its inorganic base salt.

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

The method for producing pyrrolidone carboxylic acid or its inorganic base salt is not particularly limited. In this manufacturing method, for example, glutamic acid extracted from living organisms such as seaweed and sugar cane, or processed products such as wheat flour, is dehydrated to obtain pyrrolidone carboxylic acid, and metal ions (for example, sodium ions) are added to this. There are ways to combine them.

Examples of the inorganic base salt of pyrrolidone carboxylic acid include monovalent to trivalent inorganic base salts of pyrrolidone carboxylic acid. Examples of 1- to 3-valent inorganic base salts include 1- to 3-valent metal salts. Examples of monovalent to trivalent metal salts include alkali metal salts such as sodium salts and potassium salts; Alkaline earth metal salts such as calcium salts and magnesium salts; Copper salts, zinc salts, aluminum salts, etc. can be mentioned. Among these, sodium salt, potassium salt, calcium salt, magnesium salt, and aluminum salt are preferable, and sodium salt and potassium salt are more preferable.

Pyrrolidone carboxylic acid or its inorganic base salt may be commercially available. Commercially available products of pyrrolidone carboxylic acid include "AJIDEW A-100 (registered trademark)" manufactured by AJINOMOTO HEALTHY SUPPLY CO., INC. Commercially available products of sodium pyrrolidone carboxylate include “AJIDEW-N-50 (registered trademark); PCA soda (AI = 50% aqueous solution)”.

(A) Component may be used individually, or two or more types may be used together.

The content of component (A) in the oral composition of the present invention is preferably 0.1% by mass or more, and more preferably 0.3% by mass or more with respect to the entire oral composition. Accordingly, a sufficient effect of suppressing staining on the dentin surface and below the surface layer can be obtained. The upper limit of the content of component (A) is not particularly limited, but is preferably 10 mass% or less, and more preferably 5 mass% or less, relative to the entire oral composition. Accordingly, by dissolving pyrrolidone carboxylic acid or its salt, a sufficient effect of suppressing staining on the dentin surface and below the surface layer can be obtained, and the stability of the preparation can be maintained.

The content of component (A) in the oral composition of the present invention is preferably 0.1 to 10% by mass, and more preferably 0.3 to 5% by mass, based on the entire oral composition. The lower limit of the content of component (A) is not particularly limited, but if it is less than 0.1% by mass, there is a possibility that the effect of suppressing coloring on the dentin surface and below the surface layer may not be sufficiently obtained. In addition, the upper limit of the content of component (A) is not particularly limited, but if it exceeds 10% by mass, the effect of suppressing coloration of the dentin surface may be poor.

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

<(B) Ingredient>

Component (B) contained in the oral composition of the present invention is at least one of water-soluble pyrophosphoric acid and its salt. In particular, water-soluble pyrophosphate is represented by the formula M ₄ ·P ₂ O ₇ (where 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.

At least one of water-soluble pyrophosphoric acid and its salts includes pyrophosphoric acid; There are alkali metal salts of pyrophosphate such as tetrasodium pyrophosphate, disodium dihydrogen pyrophosphate, disodium dipotassium pyrophosphate, and tetrapotassium pyrophosphate. Suitable specific examples include pyrophosphoric acid, sodium pyrophosphate, potassium pyrophosphate, and disodium dihydrogen pyrophosphate. These compounds may be commercially available products manufactured by TAIHEI CHEMICAL INDUSTRIAL CO., LTD.

(B) Component may be used individually, or two or more types may be used together.

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

The content of component (B) in the oral composition of the present invention is preferably 0.01 to 5% by mass, and more preferably 0.1 to 3% by mass, based on the entire oral composition. The lower limit of the content of component (B) is not particularly limited, but if it is less than 0.01% by mass, there is a possibility that the effect of suppressing discoloration of the dentin surface may not be sufficiently obtained. In addition, the upper limit of the content of component (B) is not particularly limited, but if it exceeds 5% by mass, the effect of suppressing coloration under the dentin surface layer may be poor.

The lower limit of the mass ratio ((A)/(B)) of component (A) and component (B) is preferably 0.1 or more, and more preferably 0.3 or more. Accordingly, a sufficient effect of suppressing staining on the dentin surface and below the surface layer can be obtained. Moreover, the upper limit of the mass ratio ((A)/(B)) of component (A) and component (B) is preferably 300 or less, more preferably 50 or less, and still more preferably 30 or less. Accordingly, the effect of suppressing discoloration of the dentin surface can be sufficiently obtained.

The mass ratio ((A)/(B)) of component (A) and component (B) is preferably 0.1 to 300, more preferably 0.1 to 50, and even more preferably 0.3 to 30. When the mass ratio is less than 0.1, the effect of suppressing staining on the dentin surface and below the surface layer may be poor. On the other hand, when the mass ratio is more than 300, the effect of suppressing coloration of the dentin surface may be poor.

Another embodiment of the oral composition of the present invention includes (A) component: at least one of pyrrolidone carboxylic acid and its inorganic base salt, (B) component: at least one of water-soluble pyrophosphoric acid and its salt, (C) Component: Contains a fluorine compound. By mixing component (C) into an oral composition containing component (A) and component (B), the effect of suppressing staining under the surface layer of dentin can be further improved.

<(C) Ingredient>

Specific examples of fluorine compounds include sodium fluoride, potassium fluoride, ammonium fluoride, tin fluoride, amine fluoride, sodium monofluorophosphate, potassium monofluorophosphate, sodium silicon fluoride, and calcium silicon fluoride. Among them, sodium fluoride and sodium monofluorophosphate are particularly preferred.

The fluorine compound may be a commercially available product. An example of a commercially available product of sodium fluoride is "Sodium Fluoride" commercially available from STELLACHEMIFA CORPORATION. An example of a commercially available product of sodium monofluorophosphate is “Sodium Monofluorophosphate” commercially available from Rhodia Nicca, Ltd. In addition, component (C) may be used individually as one type of fluorine compound, or may be used in combination of two or more types of fluorine compounds.

Fluorine in component (C) is responsible for the effect of component (C) mixed in the oral composition of the present invention. Therefore, it is useful to define the content of component (C) by converting it into the fluorine content in the oral composition. Therefore, in the following description, the content of component (C) is expressed instead of the fluorine content in the oral composition.

The content of component (C) blended in the oral composition of the present invention is preferably 0.01 mass% (100 ppm) or more, and more preferably 0.02 mass% (200 ppm) or more as a fluorine content rate with respect to the entire oral composition. Accordingly, the effect of suppressing staining under the surface layer of dentin can be sufficiently obtained. The upper limit of the content of component (C) is not particularly limited, but is preferably 0.5% by mass (5000ppm) or less, and more preferably 0.4% by mass (4000ppm) or less with respect to the entire oral composition. Accordingly, the stability of the fluorine compound in the preparation prepared using the oral composition is improved, and the effect of improving the inhibition of staining under the dentin surface layer can be sufficiently obtained.

The content of component (C) blended in the oral composition of the present invention is preferably 0.01 to 0.5 mass% (100 to 5000 ppm), and 0.02 to 0.4 mass% (200 to 4000 ppm) in terms of fluorine content relative to the entire oral composition. It is more desirable. If the fluorine content is less than 0.01% by mass (100ppm), the effect of suppressing coloration under the dentin surface layer may not be sufficiently improved. In addition, if it exceeds 0.5% by mass (5000ppm), the stability of the fluorine compound in the preparation prepared using the oral composition may deteriorate, so the effect of improving the inhibition of staining under the dentin surface layer may not be sufficiently obtained.

The lower limit of the mass ratio ((A)/(C)) of component (A) and component (C) is preferably 0.8 or more, more preferably 1 or more, and especially preferably 8 or more. Accordingly, the effect of improving the inhibition of staining under the surface layer of dentin becomes significant. Moreover, the upper limit of the mass ratio ((A)/(C)) of component (A) and component (C) is preferably 250 or less, and more preferably 150 or less. Accordingly, the effect of improving the inhibition of staining under the surface layer of dentin becomes significant.

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

Another embodiment of the oral composition of the present invention includes (A) component: at least one of pyrrolidone carboxylic acid and its salt, (B) component: at least one of water-soluble pyrophosphoric acid and its salt, ( D) Component: Contains at least one type of sugar alcohol selected from the group consisting of xylitol, reduced paratinose, and erythritol. By mixing component (D) into an oral composition containing component (A) and component (B), irritation to the oral mucosa peculiar to condensed phosphoric acid is alleviated, improving usability and further improving the effect of suppressing staining on the dentin surface. It can be.

The composition for oral cavity in another embodiment may contain (C) component, and does not need to contain it. However, since the effect of the oral composition containing component (C) and the effect of the oral composition containing component (D) are not canceled out, the oral composition in another embodiment does not contain component (C). desirable. In this case, the content regarding component (C) may be the same as the content described in <Component (C)> above.

<(D) Ingredient>

(D) Sugar alcohols used as components are xylitol, erythritol, and reduced paratinose. (D) Component may be used individually, or two or more types may be used together.

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

(D) When using xylitol as a component, the content is preferably 0.5 to 10 mass%, and more preferably 3 to 7 mass%.

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

(D) When using reduced paratinose as a component, the content is preferably 2 to 50% by mass, and more preferably 10 to 40% by mass.

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

(D) When using erythritol as a component, the content is preferably 2 to 50 mass%, and more preferably 10 to 40 mass%.

If it is less than the lower limit, the effect of improving usability may not be sufficiently obtained, and the effect of suppressing coloring of the dentin surface may be insufficiently improved. Moreover, when using 2 or more types as (D) component together, it is preferable that the total content of (D) component with respect to the entire oral composition is 50 mass % or less. If the total content of the component (D) exceeds 50% by mass, the stability of the component (D) in the preparation manufactured using the oral composition deteriorates, and the effect of suppressing staining on the dentin surface may be insufficient.

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

<Arbitrary component>

Optional ingredients include, for example, surfactants, abrasives, binders, thickeners, sweeteners, preservatives, fragrances, medicinal ingredients, and water. Arbitrary components can be blended into the oral composition of the present invention within a range that does not impair the effects of the present invention. Specific examples of optional components are shown below, but the optional components that can be blended in the oral composition of the present invention are not limited to these.

Types of surfactants include anionic surfactants, nonionic surfactants, and amphoteric surfactants. Examples of the surfactant include anionic surfactants such as N-acylamino acid salt, α-olefin sulfonate salt, N-acyl sulfonate salt, alkyl sulfate salt, and glycerol fatty acid ester sulfate salt; Nonionic surfactants such as polyoxyethylene alkyl ether, polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene hydrogenated castor oil, polyoxyethylene ether of glycerin ester, sucrose fatty acid ester, sorbitan fatty acid ester, and alkylolamide. ; There are amphoteric surfactants such as fatty acid amide propyl betaine. When the oral composition contains a surfactant, it is usually 0 to 10% by mass, preferably 0.01 to 5% by mass, relative to the total amount of the oral composition. In addition, these surfactants may be used individually, or two or more types may be used in combination.

As anionic surfactants, N-acylamino acid salts, α-olefin sulfonate salts, alkyl sulfate salts, etc. are particularly suitably used because of their versatility. As an anionic surfactant, specifically, sodium lauroyl sarcosine is preferable in terms of foamability and hard water resistance, sodium α-olefinsulfonate having 10 to 16 carbon atoms as the carbon chain of the alkyl chain, sodium lauryl sulfate, etc.

As nonionic surfactants, polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, alkylolamide, sorbitan fatty acid ester, etc. are particularly suitably used in view of their versatility. As a nonionic surfactant, specifically, polyoxyethylene alkyl ether with an alkyl chain carbon number of 14 to 18 carbon atoms and an average added mole number of ethylene oxide of 15 to 30, and polyoxyethylene oxide with an average added mole number of ethylene oxide of 40 to 100. Ethylene hydrogenated castor oil, alkylolamide with a carbon number of 12 to 14 as the carbon chain of the alkyl chain, sorbitan fatty acid ester with a fatty acid carbon number of 12 to 18, fatty acid with a carbon number of 16 to 18, and the average added mole number of ethylene oxide. Polyoxyethylene sorbitan fatty acid esters of 10 to 40 are preferred.

The amphoteric surfactant is preferably of the betaine type. For example, amphoteric surfactants of the alkyl betaine type, fatty acid amide propyl betaine type, and alkylimidazolinium betaine type are suitably used. Specific examples of the amphoteric surfactant include alkyl dimethyl amino acetic acid betaine such as lauryl dimethyl amino acetic acid betaine; Alkylimidazolinium betaine series such as 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine; Fatty acid amide propyl betaine series, such as coconut oil fatty acid amide propyl dimethylaminoacetic acid betaine and coconut oil fatty acid amide propyl betaine, are included. Among them, the amphoteric surfactants are preferably palm oil fatty acid amidepropyl betaine and 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine.

Examples of the abrasive include silica-based abrasives such as silicic anhydride, crystalline silica, amorphous silica, silica gel, and aluminosilicate; Synthetic resins such as zeolite, calcium hydrogen phosphate anhydrous, calcium hydrogen phosphate dihydrate, calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, tribasic magnesium phosphate, zirconium silicate, tricalcium phosphate, hydroxyapatite, and quaternary calcium phosphate. There are abrasives. When mix|blending an abrasive with a composition for oral cavity, in a dentifrice, it is preferable that it is 0-40 mass % of the whole composition, and it is more preferable that it is 5-20 mass %. In liquid preparations such as mouthwash, it is preferably 0 to 10% by mass, and more preferably 0 to 5% by mass of the entire composition.

Examples of binders include pullulan, gelatin, carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, xanthan gum, gum arabic, guar gum, locust bean gum, polyvinyl alcohol, and polyvinyl. These include pyrrolidone, sodium polyacrylate, and thickened silica. When the oral composition contains a binder, its content is usually 0.01 to 10% by mass with respect to the entire preparation manufactured using the oral composition.

Examples of thickening agents include propylene glycol, butylene glycol, glycerin, sorbitol, and polyethylene glycol. When the composition for oral use contains a viscous agent, its content is usually 1 to 50% by mass with respect to the entire preparation manufactured using the composition for oral use.

Sweeteners include, for example, sodium saccharin, stevioside, neohesperidin hydrochalcone, glycyrrhizin, perillartine, p-methoxycinnamic aldehyde, thaumatin, and maltitol. When using a sweetener, the blending amount can be appropriately determined within a range that does not impair the effect of the present invention.

Examples of preservatives include sodium benzoate, paraoxybenzoic acid ester, methylparaben, ethylparaben, butylparaben, ethylenediamine tetraacetate, and benzalkonium chloride. When using a preservative, the mixing amount can be appropriately determined within a range that does not impair the effect of the present invention.

Examples of fragrances include essential oils such as peppermint and spearmint; Fruit essences such as lemon and strawberry; 1-Menthol, carvone, eugenol, anethole, linalol, limonene, ocimene, cineol, n-decyl alcohol, citronellol, vanillin, α-terpineol, methyl salicylate, thymol, rosemary oil. There are fragrance materials such as 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 based on the total amount of the oral composition.

In addition, as medicinal ingredients, sterilizing or antibacterial agents such as chlorhexidine, triclosan, isopropylmethylphenol, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, zinc gluconate, and zinc citrate; Tartar preventive agents such as ethane hydroxydiphosphonate; Anti-inflammatory agents such as tranexamic acid, glycyrrhizin dipotassium salt, and ε-aminocaproic acid; Coating agents such as hydroxyethyl cellulose dimethyl diallyl ammonium chloride; Enzymes such as dextranase and mutanase can be used.

Additionally, from the viewpoint of effectiveness and stability, dentifrices and mouthwashes are preferable as the dosage form, and water, ethanol, etc. can be mixed as a solvent.

In addition, the mixing ratio of these optional components can be set to the usual amount within a range that does not impair the effect exhibited by 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 can be adjusted using a pH adjuster as needed. pH adjusters include phosphoric acid or its salts (sodium phosphate, sodium hydrogen phosphate, etc.), citric acid or its salts (sodium citrate, etc.), malic acid or its salts, gluconic acid or its salts, maleic acid or its salts, succinic acid or its salts, glutamic acid. Alternatively, its salt, lactic acid, hydrochloric acid, acetic acid, nitric acid, sodium hydroxide, potassium hydroxide, etc. can be used within the range that does not impair the effect exhibited by the oral composition of the present invention.

(2) Dentin staining inhibitor of the present invention

When the component (A) and component (B) are used together, coloration of dentin, specifically the surface and subsurface layer of dentin, can be prevented. Therefore, the composition containing component (A) and component (B) is useful as an inhibitor of dentin staining, particularly as an inhibitor of dentin staining due to the Maillard reaction derived from dentin collagen, which is dentin tissue.

The dosage form of the dentin staining inhibitor of the present invention is not particularly limited. For example, it can be administered as a mouthwash, mouth freshener, or dentifrice (liquid dentifrice, gel dentifrice, soft dentifrice, etc.).

There is no particular limitation on the target audience for the dentin staining inhibitor of the present invention. However, because it prevents staining of dentin, it is preferable for the elderly or those in whom gum recession is observed.

Example

Hereinafter, the present invention will be described in detail by examples. The following examples are intended to appropriately illustrate the present invention, but do not limit the present invention. Additionally, “%” means “mass%” unless otherwise specified.

The details of each component used in preparing the oral composition of Examples 1 to 36 and Comparative Examples 1 to 3 are described below.

<(A) Ingredient>

Sodium pyrrolidone carboxylate

Made by Ajinomoto Co., Inc., brand name “AJIDEW N-50 (registered trademark)”

<(B) Ingredient>

Sodium pyrophosphate

Made by TAIHEI CHEMICAL INDUSTRIAL CO., LTD.

<(C) Ingredient>

sodium fluoride

Manufactured by STELLACHEMIFA CORPORATION (purified sodium fluoride (S))

Sodium monofluorophosphate

Made by ICL Japan Ltd.

<(D) Ingredient>

xylitol

Made by Roquette Japan K.K.

reduced paratinose

Made by Mitsui Sugar Co., Ltd.

Erythritol

Made by MITSUBISHI-CHEMICAL FOODS CORPORATION

<Other added ingredients>

Sodium lauryl sulfate (surfactant), sorbitol (thickener), propylene glycol (thickener), sodium saccharin (sweetener), xanthan gum (caking agent), silicic anhydride (abrasive), fragrance, purified water (solvent)

As the above added ingredients, standard cosmetic raw material products were used.

Examples 1 to 36 and Comparative Examples 1 to 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 method according to the compounding prescriptions shown in Tables 1 to 6.

(Method for preparing 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 was added separately. The liquid in which glycol and xanthan gum were dispersed was added and stirred. After that, sodium lauryl sulfate, fragrance, and abrasive were added, and the mixture was further stirred under reduced pressure (pressure 4 kPa) to prepare a dentifrice composition. Additionally, a 1.5L kneader (manufactured by Ishiyama Seisakusho) was used for manufacturing. The prepared dentifrice composition was evaluated for its effect in suppressing staining on the dentin surface and below the surface layer and for usability in accordance with the following procedures. The evaluation results are listed in Tables 1 to 6.

(Evaluation of staining inhibition effect on dentin surface)

1. Preparation of Maillard reaction solution

A Maillard reaction solution was prepared by heating 1% glycine and 1% glucose in an autoclave at 110°C for 1 hour.

2. Formation of the coloring model

The small tooth root was cut into a block shape, and the cement was removed by surface polishing. Of the parts from which the cement was removed, approximately 3.5 mm x 3.5 mm was used as a demineralized window, and the remaining parts were covered with nail polish. After drying the nail polish at room temperature, it was immersed in a 0.1 mol/L aqueous acetic acid solution (pH 4.5) for 50 hours to prepare a tooth root surface dentin sample with collagen exposed in the window portion.

First, the color differences (L ^* 0, a ^* 0, b ^* 0) were measured using a spectrophotometer (CM-2022, manufactured by KONICA MINOLTA, INC.) as initial values. The discharged saliva was centrifuged (10000g, 20 minutes, 20°C), and the root surface dentin sample was immersed in the obtained supernatant for 30 minutes with stirring at 37°C, followed by Examples 1 to 36 and Comparative Examples shown in Tables 1 to 6. The dentifrice compositions 1 to 3 were immersed in a 3-fold water dilution for 3 minutes at room temperature. Afterwards, to form a stained pellicle, it was sequentially immersed in 1% bovine serum albumin, 1% lysozyme chloride, Maillard reaction solution, 1% porcine stomach mucin, and 1% lactoferrin (pH 7.0) at 37°C for 10 minutes each. . The process from the treatment of the salivary supernatant to the pellicle formation operation was repeated 4 times a day for a total of 5 days.

3. Evaluation of the effect of inhibiting staining on the dentin surface

The measurement window was lightly rinsed with distilled water, and excess moisture was absorbed with filter paper. After drying, color difference (L ^* 1, a ^* 1, b ^* 1) was measured three times and the average value was calculated. The coloring suppression effect was evaluated according to 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

[Evaluation criteria for coloring]

A: ΔE＜10

B: 10≤ΔE＜15

C: 15≤ΔE＜20

D: 20≤ΔE＜25

E: 25≤ΔE

(Evaluation of the effect of suppressing staining under the dentin surface layer)

A tooth root surface dentin sample was prepared in the same manner as the preparation method in (Evaluation of the effect of suppressing staining on the dentin surface). After being immersed in a 3-fold water dilution of the discharged saliva and 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 staining from the surface layer of collagen to below the surface layer in the stained pellicle window portion formed was measured using a stereoscopic microscope observation image, and evaluated according to the following evaluation criteria.

[Evaluation criteria for coloration below the surface layer]

A: Coloration below the surface layer from the surface <15㎛

B: 15㎛≤Coloring below the surface layer from the surface＜20㎛

C: 20㎛≤Coloring below the surface layer from the surface＜50㎛

D: 50㎛≤Coloring below the surface layer from the surface＜100㎛

E: Coloration below the surface layer from 100㎛≤surface

Evaluation of usability (no irritation)

The treatment solution obtained by diluting the dentifrice composition of each Example and Comparative Example 3 times with distilled water was made to be held in the mouth by 20 panelists for 30 seconds, and the presence or absence of pain in the oral cavity after discharge was evaluated. The evaluation criteria were set as follows.

[Evaluation standard]

A: Less than 1 person showed pain

B: 2 to 5 people showed pain

C: More than 6 but less than 10 people showed pain

D: More than 10 people showed pain

As can be seen from the results of Comparative Example 1, it can be seen that even when sodium pyrophosphate is used alone, there is almost no effect of suppressing staining on the dentin surface and below the surface layer. In addition, as can be seen from the results of Comparative Example 2, even when sodium pyrrolidone carboxylate, which is known to be capable of suppressing the coloring of polyphenol (pharmacological ingredient) on the root surface dentin surface, is used, the dentin tissue It can be seen that there is almost no inhibitory effect on coloring resulting from the Maillard reaction. In addition, as can be seen from the results of Comparative Example 3, it can be seen that, like sodium pyrophosphate, even if known sodium tripolyphosphate is used as a stain removal component, there is almost no effect of suppressing coloration on the dentin surface and below 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 staining on the dentin surface and below the surface layer.

As can be seen from the results of Examples 14 to 18, (C) a fluorine compound is added to a dentifrice composition containing sodium pyrrolidone carboxylate and sodium pyrophosphate, which has an effect of suppressing staining on the dentin surface and under the surface layer. This further improved the effect of suppressing staining under the surface layer of dentin without losing other effects.

As can be seen from the results of Examples 19 to 24, (D) sugar alcohol is added to a dentifrice composition containing sodium pyrrolidone carboxylate and sodium pyrophosphate, which has an effect of suppressing staining on the dentin surface and under the surface layer. This further improves the effect of suppressing staining on the dentin surface, and the feeling of use is also improved as the formulation is non-irritating.

As can be seen from the results of Examples 25 to 36, (C) a fluorine compound and ( D) When sugar alcohol is added, the effect of suppressing staining on dentin is further improved, and the feeling of use is also improved.

In order to investigate the application range of the oral composition of the present invention, an oral rinse (Example 37), a mouth freshener (Example 38), and a gel-like dentifrice (Example 39) were prepared, and as a result of the above evaluation test, all were The effect of suppressing staining on the dentin surface and the effect of suppressing staining under the dentin surface layer were A, and the evaluation of usability (no irritation) was A. Each composition is shown below.

[Mouthwash]

Furtherance

Ingredient A: Sodium pyrrolidone carboxylate (manufactured by Wako Pure Chemical Corporation): 3%

Ingredient B: Potassium pyrophosphate (manufactured by TAIHEI CHEMICAL INDUSTRIAL CO., LTD.): 1%

Ingredient C: Sodium fluoride (manufactured by STELLACHEMIFA CORPORATION) 0.04% (fluorine content: 0.02%)

Component C: Sodium monofluorophosphate (manufactured by ICL Japan Ltd.) 0.23% (fluorine content: 0.03%)

D Ingredient: Xylitol (manufactured by Roquette Japan K.K.): 5%

Ingredient D: Reduced paratinose (manufactured by Mitsui Sugar Co., Ltd.): 15%

Glycerin: 5%

Ethanol: 8%

Polyoxyethylene hydrogenated castor oil (60E.O.): 0.8%

Sodium citrate: 0.1%

Citric acid: 0.3%

Sodium benzoate: 0.5%

Fragrance: 0.2%

Purified water: remainder

[Mouth freshener]

Furtherance

Ingredient A: Sodium pyrrolidone carboxylate (manufactured by Wako Pure Chemical Corporation): 3%

Ingredient B: Potassium pyrophosphate (manufactured by TAIHEI CHEMICAL INDUSTRIAL CO., LTD.): 1%

Ingredient C: Sodium fluoride (manufactured by STELLACHEMIFA CORPORATION): 0.04% (fluorine content: 0.02%)

D Ingredient: Xylitol (manufactured by Roquette Japan K.K.): 5%

Ingredient D: Reduced paratinose (manufactured by Mitsui Sugar Co., Ltd.): 10%

Ingredient D: Erythritol (manufactured by MITSUBISHI-CHEMICAL FOODS CORPORATION): 10%

Glycerin: 13%

Ethanol: 40%

Polyoxyethylene hydrogenated castor oil (60E.O.): 3%

Sodium citrate: 0.1%

Citric acid: 0.03%

Menthol: 0.3%

Fragrance: 0.4%

Purified water: remainder

[Gel-like dentifrice]

Furtherance

Ingredient A: Sodium pyrrolidone carboxylate (manufactured by Wako Pure Chemical Corporation): 3%

Ingredient B: Potassium pyrophosphate (manufactured by TAIHEI CHEMICAL INDUSTRIAL CO., LTD.): 1%

Ingredient C: Sodium fluoride (manufactured by STELLACHEMIFA CORPORATION): 0.04% (fluorine content: 0.02%)

D Ingredient: Xylitol (manufactured by Roquette Japan K.K.): 5%

Ingredient D: Reduced paratinose (manufactured by Mitsui Sugar Co., Ltd.): 10%

Ingredient D: Erythritol (manufactured by MITSUBISHI-CHEMICAL FOODS CORPORATION): 10%

Thickening silica: 1.5%

Propylene glycol: 3%

Sorbit solution: 55%

Carrageenan: 0.3%

Xanthan gum: 0.3%

Cetylpyridinium chloride: 0.02%

Sodium saccharin: 0.12%

Potassium nitrate: 5%

Coconut oil fatty acid amide propyl betaine solution: 0.3%

Fragrance: 0.4%

Purified water: remainder

Claims (11)

(A) Component: At least one of pyrrolidone carboxylic acid and its inorganic base salt,
(B) Component: An oral composition containing at least one of water-soluble pyrophosphoric acid and its salt,
The inorganic base salt is an oral composition selected from the group consisting of sodium salt, potassium salt, calcium salt, magnesium salt, and aluminum salt. According to claim 1,
(A) An oral composition containing 0.1 to 10% by mass of component. The method of claim 1 or 2,
(B) An oral composition containing 0.01 to 5% by mass of component. The method of claim 1 or 2,
An oral composition in which the mass ratio (A/B) of component (A) and component (B) is 0.1 to 300. The method of claim 1 or 2,
(C) Component: Oral composition further containing a fluorine compound. According to claim 5,
(C) An oral composition in which the content of component is 0.01 to 0.5% by mass in terms of fluorine content. The method of claim 1 or 2,
(D) Component: An oral composition further containing at least one type of sugar alcohol selected from the group consisting of xylitol, reduced paratinose, and erythritol. According to claim 7,
(D) An oral composition containing 0.5 to 50% by mass of component. According to claim 7,
An oral composition containing 0.5 to 10% by mass of xylitol, 2 to 50% by mass of reduced paratinose, and 2 to 50% by mass of reduced paratinose. The method of claim 1 or 2,
An oral composition that is a dentifrice or mouthwash. (A) Component: At least one of pyrrolidone carboxylic acid and its inorganic base salt,
(B) Component: A dentin staining inhibitor containing at least one of water-soluble pyrophosphoric acid and its salt,
The inorganic base salt is a dentin staining inhibitor selected from the group consisting of sodium salt, potassium salt, calcium salt, magnesium salt, and aluminum salt.