JPWO2018043717A1 - Oral composition - Google Patents

Abstract

An object of the present invention is to provide a composition for oral cavity which is excellent in suppressing coloring on the surface and under the surface of dentin, and component (A): at least one of pyrrolidone carboxylic acid and its salt, and component (B): water-soluble pyrophosphate It is an oral composition containing at least one of the salt.

Description

  The present invention relates to an oral composition.

  In recent years, with the aging of the population, the coloring of the exposed root surface dentin has been discussed as the gingival inverts. In the oral cavity, the tooth surface including root surface dentin is colored due to various causes. One of the causes is the Maillard reaction caused by the nonenzymatic reaction of proteins and saccharides derived from pellicle or saliva in the mouth.

  Conventionally, an oral composition intended to prevent the coloring of the enamel surface derived from the Maillard reaction has been disclosed. For example, Patent Document 1 discloses an oral composition which may contain a water-soluble polyphosphate for the purpose of removing stains on tooth surfaces and tongue surfaces. 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 intended to impart 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 wetting effect and its persistence. Patent Document 3 discloses an oral composition containing pyrrolidone carboxylic acid and / or a salt thereof for the purpose of giving a warm feeling without giving irritation in the oral cavity. Patent Document 4 discloses a composition for oral cavity containing pyrrolidone carboxylic acid and / or a salt thereof for the purpose of exhibiting excellent anti-inflammatory effect and excellent preparation stability. Patent Document 5 discloses an oral composition containing pyrrolidone carboxylic acid and / or a salt thereof for the purpose of providing excellent usability and having an effect of suppressing plaque adhesion. In any document, it is not disclosed that pyrrolidone carboxylic acid and / or a salt thereof exhibits the effect of preventing coloration.

  By the way, the bonding of the coloring matter of the tooth derived from the Maillard reaction is remarkably stronger in dentin composed of a complex of an inorganic substance and an organic substance such as collagen than enamel composed of an almost inorganic substance. In addition, the coloring agent causing the Maillard reaction penetrates into the dentin tissue to cause coloring. Therefore, with the conventional coloring suppression technology for enamel, a sufficient coloring suppression effect can not be obtained for dentin.

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

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

  However, when the pyrrolidone carboxylic acid disclosed in Patent Document 6 is used alone, the coloring substance is strongly bound to the root surface due to the interaction between proteins and saccharides and organic substances such as collagen constituting dentin, so ivory The inhibitory effect on the coloration derived from the maillard reaction of the quality tissue is not sufficient.

  An object of the present invention is to provide an oral composition which is excellent in the color suppression effect on the surface and the surface layer of dentin.

The present inventors provide the following [1] to [11].
[1] Component (A): An oral composition containing 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.
The composition for oral cavity as described in said [1] whose content of [2] (A) component is 0.1-10 mass%.
The composition for oral cavity as described in said [1] or [2] whose content of [3] (B) component is 0.01-5 mass%.
The composition for oral cavity in any one of said [1]-[3] whose mass ratio (A / B) of [4] (A) component and (B) component is 0.1-300.
[5] (C) component: The composition for oral cavity in any one of said [1]-[4] which further contains a fluorine compound.
The composition for oral cavity as described in said [5] whose content of (6) (C) component is 0.01-0.5 mass% as a fluorine content.
[7] Component (D): The composition for oral cavity 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 composition for oral cavity as described in [7] above, wherein the content of the (D) component 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 as described in-.
[10] The composition for oral cavity according to any one of the above [1] to [9], which is a dentifrice or a mouthwash.
[11] Component (A): a dentin coloring inhibitor containing at least one of pyrrolidone carboxylic acid and an inorganic base salt thereof, and (B): at least one of water-soluble pyrophosphoric acid and a salt thereof.

  ADVANTAGE OF THE INVENTION According to this invention, the composition for oral cavity which is excellent in the coloring inhibitory effect on the surface of dentin and the surface layer can be provided.

  Hereinafter, the present invention will be described in detail in line with its preferred embodiments.

(1) Oral Composition of the Present Invention The present inventors have intensively studied in order to obtain an oral composition which is superior in suppressing coloring of the surface and subsurface of dentin as compared with the conventional composition for oral cavity. Piled up. As a result, the composition for the oral cavity combining at least one of pyrrolidone carboxylic acid and its inorganic base salt, and at least one of water-soluble pyrophosphate and its salt, in addition to the suppression of the strong coloring of dentin surface, ivory It was found that the coloration 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 only describes the effect on adhesion and deposition on the tooth surface, and it is not described that the suppression effect on coloring under the surface of dentin can be obtained.

  One embodiment of the composition for oral cavity of the present invention comprises (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) component>
The component (A) contained in the composition for oral cavity of the present invention is at least one of pyrrolidone carboxylic acid and its inorganic base salt.

  Pyrrolidonecarboxylic 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 preparation method of pyrrolidone carboxylic acid or its inorganic base salt is not particularly limited. As such a production method, for example, glutamic acid extracted from an organism such as seaweed or sugar cane or from a processed product such as wheat flour is dehydrated to obtain pyrrolidone carboxylic acid, to which a metal ion (for example, sodium ion) is bound. The method is mentioned.
Examples of the inorganic base salt of pyrrolidone carboxylic acid include a monovalent to trivalent inorganic base salt of pyrrolidone carboxylic acid. As a monovalent to trivalent inorganic base salt, for example, there is a mono to trivalent metal salt. Examples of the 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 and the like. Among these, sodium salts, potassium salts, calcium salts, magnesium salts and aluminum salts are preferable, and sodium salts and potassium salts are more preferable.

  The pyrrolidone carboxylic acid and the inorganic base salt thereof may be commercially available products. As a commercial item of pyrrolidone carboxylic acid, "AJIDEW A-100 (registered trademark)" manufactured by Ajinomoto Healthy Supply Co., Ltd. can be mentioned. As a commercial item of pyrrolidone carboxylate sodium, "AJIDEW-N-50 (registered trademark); PCA soda (AI = 50% aqueous solution)" can be mentioned.

  As the component (A), one type may be used alone, or two or more types may be used in combination.

  The content of the component (A) in the composition for oral cavity of the present invention is preferably 0.1% by mass or more, more preferably 0.3% by mass or more, with respect to the whole composition for oral cavity . Thereby, the coloring inhibitory effect of a dentin surface and the subsurface layer can fully be acquired. The upper limit of the content of the component (A) is not particularly limited, but is preferably 10% by mass or less, and more preferably 5% by mass or less, based on the whole composition for oral cavity. Thus, pyrrolidone carboxylic acid or a salt thereof can be dissolved to sufficiently obtain the effect of suppressing coloring on the surface and the surface of dentin, and the stability of the preparation can be maintained.

  The content of the component (A) in the composition for oral cavity of the present invention is preferably 0.1 to 10% by mass, preferably 0.3 to 5% by mass, with respect to the whole composition for oral cavity More preferable. The lower limit of the content of the component (A) is not particularly limited, but if it is less than 0.1% by mass, there is a possibility that the coloration suppressing effect on the dentin surface and the surface layer may not be sufficiently obtained. is there. Further, the upper limit value of the content of the component (A) is not particularly limited, but if it is more than 10% by mass, the effect of suppressing coloring of 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 preparation amount of each component when preparing the composition.

<(B) component>
The component (B) contained in the composition for oral cavity of the present invention is at least one of water-soluble pyrophosphoric acid and a salt thereof. In particular, a water-soluble pyrophosphate is represented by the chemical formula M ₄ · P ₂ O ₇ (wherein M is a hydrogen ion or an alkali metal ion such as sodium or potassium), and is a compound in which phosphoric acid is dehydrated and condensed. It is.

  As at least one of water-soluble pyrophosphates and salts thereof, pyrophosphates; alkali metal salts of pyrophosphates such as tetrasodium pyrophosphate, disodium dihydrogen pyrophosphate, dipotassium disodium pyrophosphate, tetrapotassium pyrophosphate, etc. is there. As preferable examples, pyrophosphate, sodium pyrophosphate, potassium pyrophosphate, and disodium dihydrogen pyrophosphate can be mentioned. These compounds may be commercial products manufactured by Taihei Kagaku Sangyo Co., Ltd.

  As the component (B), one type may be used alone, or two or more types may be used in combination.

  The content of the component (B) in the composition for oral cavity of the present invention is preferably 0.01% by mass or more, more preferably 0.1% by mass or more based on the whole composition for oral cavity . Thereby, the coloring inhibitory effect of a dentin surface can fully be acquired. 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 whole composition for oral cavity. Thereby, the coloring inhibitory effect under the dentine surface layer can fully be acquired.

  The content of the component (B) in the composition for oral cavity of the present invention is preferably 0.01 to 5% by mass, preferably 0.1 to 3% by mass, with respect to the whole composition for oral cavity More preferable. 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 the coloration of the dentin surface may not be sufficiently obtained. Further, the upper limit value of the content of the component (B) is not particularly limited, but in the case of more than 5% by mass, the effect of suppressing coloring under the surface layer of dentin may be inferior.

  The lower limit value 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. Thereby, the coloring inhibitory effect of a dentin surface and the subsurface layer can fully be acquired. The upper limit value 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 preferred. Thereby, the coloring inhibitory effect of a dentin surface can fully be acquired.

  It is preferable that it is 0.1-300, as for mass ratio ((A) / (B)) of (A) component and (B) component, it is more preferable that it is 0.1-50, 0.3- More preferably, it is 30. When the mass ratio is less than 0.1, the effect of suppressing coloring on the surface and the surface of the dentin may be inferior. On the other hand, when the mass ratio is more than 300, the coloring suppression effect of the dentin surface may be inferior.

  Another embodiment of the composition for oral cavity of the present invention comprises (A) component: at least one of pyrrolidone carboxylic acid and its inorganic base salt, and (B) component: at least one of water-soluble pyrophosphate and its salt ( C) Component: containing a fluorine compound. By blending the component (C) with the composition for the oral cavity containing the component (A) and the component (B), the coloring suppression effect under the surface layer of dentin can be further improved.

<(C) component>
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 silicon calcium fluoride. be able to. Among them, sodium fluoride and sodium monofluorophosphate are particularly preferable.

  Commercially available fluorine compounds may be used. As an example of the commercial item of sodium fluoride, "sodium fluoride" sold from Stella Chemifa Co., Ltd. can be mentioned. As an example of the commercial item of monofluorophosphate sodium, "monofluorophosphate sodium" marketed by Rhodia Nikka Co., Ltd. can be mentioned. The component (C) may be used alone as a fluorine compound, or two or more fluorine compounds may be used in combination.

  The effect of the component (C) blended in the composition for oral cavity of the present invention is responsible for the fluorine in the component (C). Therefore, it is more useful to define the content of the component (C) in terms of the fluorine content in the composition for oral cavity. Therefore, in the following description, the content of the component (C) is indicated by substituting the fluorine content in the composition for oral cavity.

  0.01 mass% (100 ppm) or more as a fluorine content rate is preferable with respect to the whole composition for oral cavity, as for content of (C) component mix | blended with the composition for oral cavity of this invention, 0.02 mass% ( 200 ppm or more is more preferable. Thereby, the coloring inhibitory effect under the dentine surface layer can fully be acquired. The upper limit of the content of the component (C) is not particularly limited, but it is preferably 0.5% by mass (5000 ppm) or less, 0.4% by mass (4000 ppm) or less based on the whole composition for oral cavity Is more preferred. Thereby, the stability of the fluorine compound in the preparation manufactured using the composition for oral cavity becomes favorable, and the coloring suppression improvement effect under the dentine surface layer can fully be acquired.

  The content of the component (C) to be added to the composition for oral cavity of the present invention is preferably 0.01 to 0.5% by mass (100 to 5000 ppm) as a fluorine content with respect to the whole composition for oral cavity, 0 More preferably, .02 to 0.4 mass% (200 to 4000 ppm). If the fluorine content is less than 0.01% by mass (100 ppm), the coloring inhibition effect under the surface layer of dentin may not be sufficiently improved. In the case of more than 0.5% by mass (5000 ppm), there is a possibility that the stability and the like of the fluorine compound in the preparation manufactured using the composition for oral cavity may be deteriorated, so the coloration suppression under the dentine surface layer The improvement effect may not be obtained sufficiently.

  The lower limit value 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 preferred. Thereby, the coloring suppression improvement effect under the dentine surface layer becomes remarkable. Moreover, it is preferable that it is 250 or less, and, as for the upper limit of mass ratio ((A) / (C)) of (A) component and (C) component, it is more preferable that it is 150 or less. Thereby, the coloring suppression improvement effect under the dentine surface layer becomes remarkable.

  0.8-250 are preferable, as for mass ratio ((A) / (C)) of (A) component and (C) component, 1-250 are more preferable, and 8-150 are especially preferable.

  Still another embodiment of the composition for oral cavity of the present invention comprises (A) component: at least one of pyrrolidone carboxylic acid and its salt, and (B) component: at least one of water-soluble pyrophosphate and its salt, (D ) Component: at least one sugar alcohol selected from the group consisting of xylitol, reduced palatinose, and erythritol. By blending the component (D) with the composition for oral cavity containing the component (A) and the component (B), the irritation to the oral mucosa peculiar to condensed phosphoric acid is alleviated, and the usability improves. At the same time, the coloring suppression effect of 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 that the composition for oral cavity contains the component (C) and the effect for the composition for oral cavity that contains the component (D) do not offset each other, the composition for oral cavity in still another embodiment contains the component (C) It is preferable to contain. In this case, the contents relating to the component (C) can be said to be the same as the contents described in the above <C).

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

  Although content of (D) component with respect to the whole composition for oral cavity is not specifically limited, It is preferable that it is 0.5-50 mass% as a total. 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 value of the content of xylitol is not particularly limited, but is preferably 10% by mass or less, and more preferably 7% by mass or less.

  When using xylitol as (D) component, it is preferable that it is 0.5-10 mass%, and it is more preferable that it is 3-7 mass%.

  When using reduced palatinose 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 reduced palatinose is not particularly limited, but is preferably 50% by mass or less, and more preferably 40% by mass or less.

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

  When the content is less than the lower limit, the usability improving effect may not be sufficiently obtained, and the improvement of the coloring suppressing effect of the dentin surface may be insufficient. Moreover, when using 2 or more types together as (D) component, it is preferable that content of the sum total of (D) component with respect to the whole composition for oral cavity shall be 50 mass% or less. If the total content of the component (D) is more than 50% by mass, the stability of the component (D) in the preparation produced using the composition for oral cavity worsens, so the coloring inhibition effect of the dentin surface May be inadequate.

  In the composition for oral cavity of the present invention, necessary optional components can be blended in addition to the above components.

<Optional component>
Optional components include, for example, surfactants, abrasives, caking agents, thickeners, sweeteners, preservatives, flavors, medicinal ingredients, water. Optional components can be added to the composition for oral cavity of the present invention as long as the effects of the present invention are not impaired. Although the specific example of an arbitrary component is shown below, the optional component which can be mix | blended with the composition for oral cavity of this invention is not restrict | limited to these.

  Examples of surfactants include anionic surfactants, nonionic surfactants, and amphoteric surfactants. As the surfactant, for example, anionic surfactants such as N-acyl amino acid salt, α-olefin sulfonate, N-acyl sulfonate, alkyl sulfate, sulfate of glycerin fatty acid ester, etc .; polyoxyethylene alkyl ether Nonionic surfactants such as polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene hydrogenated castor oil, polyoxyethylene ether of glycerin ester, sucrose fatty acid ester, sorbitan fatty acid ester, alkylolamide, etc .; fatty acid amidopropyl There are amphoteric surfactants such as betaine. When the composition for oral cavity contains a surfactant, it is usually 0 to 10% by mass, preferably 0.01 to 5% by mass, with respect to the total amount of the composition for oral cavity. 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 in view of versatility in particular. Specific examples of anionic surfactants include sodium lauroyl sarcosine, carbon chains of alkyl chains having 10 to 16 carbon atoms, sodium α-olefin sulfonate, sodium lauryl sulfate and the like in terms of foamability and hard water resistance. Is preferred.

  Particularly as the nonionic surfactant, polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, alkylol amide, sorbitan fatty acid ester, etc. are suitably used in view of versatility. Specific examples of nonionic surfactants include polyoxyethylene alkyl ethers having 14 to 18 carbon atoms and 15 to 30 ethylene oxide average addition moles as the carbon chain length of the alkyl chain, and 40 ethylene oxide average addition moles Hydrogenated castor oil of 100 to 100, alkylol amide having 12 to 14 carbon atoms as the carbon chain length of alkyl chain, sorbitan fatty acid ester having 12 to 18 carbon atoms of fatty acid, 16 to 18 carbon atoms of fatty acid And polyoxyethylene sorbitan fatty acid ester having an average added mole number of ethylene oxide of 10 to 40 is preferable.

  The amphoteric surfactant is preferably a betaine-based one, and for example, an alkylbetaine-based, fatty acid amidopropyl betaine-based or alkylimidazolinium betaine-based amphoteric surfactant is suitably used. Specific examples of amphoteric surfactants include alkyldimethylaminoacetic acid betaines such as lauryl dimethylaminoacetic acid betaine; alkylimidazolinium betaines such as 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine; Examples thereof include fatty acid amidopropyl betaines such as coconut oil fatty acid amidopropyl dimethylaminoacetic acid betaine and coconut oil fatty acid amidopropyl betaine. Among them, the amphoteric surfactant is preferably coconut oil fatty acid amidopropyl betaine or 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, aluminosilicate, etc .; zeolite, calcium hydrogen phosphate anhydrate, calcium hydrogen phosphate dihydrate, There are synthetic resin-based abrasives such as calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, tribasic magnesium phosphate, zirconium silicate, tribasic calcium phosphate, hydroxyapatite, and tetrabasic calcium phosphate. When an abrasive is added to the composition for oral cavity, the dentifrice preferably contains 0 to 40% by mass, more preferably 5 to 20% by mass of the entire composition. In liquid preparations, such as a mouthwash, it is preferable that it is 0-10 mass% of the whole composition, and it is more preferable that it is 0-5 mass%.

  As the caking agent, for example, pullulan, gelatin, carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, xanthan gum, gum arabic, guar gum, locust bean gum, polyvinyl alcohol, polyvinyl pyrrolidone, sodium polyacrylate, thickening property There is silica. When the composition for oral cavity contains a caking agent, the content thereof is generally 0.01 to 10% by mass with respect to the whole preparation manufactured using the composition for oral cavity.

  Examples of the thickener include propylene glycol, butylene glycol, glycerin, sorbitol and polyethylene glycol. When the composition for oral cavity contains a thickener, the content thereof is usually 1 to 50% by mass with respect to the whole preparation produced using the composition for oral cavity.

  Examples of sweetening agents include saccharin sodium, stevioside, neohesperidin hydrochalcone, glycyrrhizin, perillartine, p-methoxycinnamic aldehyde, thaumatin and maltitol. When using a sweetener, the compounding quantity can be suitably determined in the range which does not impair the effect of this invention.

  Examples of preservatives include sodium benzoate, parahydroxybenzoic acid ester, methylparaben, ethylparaben, butylparaben, ethylenediaminetetraacetic acid salt, and benzalkonium chloride. When a preservative is used, the compounding amount can be appropriately determined as long as the effects of the present invention are not impaired.

  Examples of the flavor include essential oils such as peppermint and spearmint; fruit-based essences such as lemon and strawberry; 1-menthol, carvone, eugenol, anethole, linalool, limonene, osmene, cineole, n-decyl alcohol, citronerol, alligator, There are perfume materials such as α-terpineol, methyl salicylate, thymol, rosemary oil, sage oil, perilla oil, lemon oil, orange oil and the like. When the composition for oral cavity contains a spice material, it is preferable that it is 0.000001-1 mass% with respect to the composition for oral cavity whole quantity.

  Furthermore, as medicinal ingredients, bactericidal or antibacterial agents such as chlorhexidine, triclosan, isopropylmethylphenol, cetyl pyridinium chloride, benzalkonium chloride, benzethonium chloride, zinc gluconate, zinc citrate and the like; dental calculus preventing agents such as ethane hydroxy diphosphonate Anti-inflammatory agents such as tranexamic acid, glycyrrhizin dipotassium salt, ε-aminocaproic acid; coating agents such as hydroxyethyl cellulose dimethyl diallyl ammonium chloride; enzyme agents such as dextranase, mutanase etc. can be used.

  Moreover, as a dosage form, a dentifrice, a mouthwash, etc. are preferable from a viewpoint of effectiveness and stability, and water, ethanol, etc. can be mix | blended as a solvent.

  In addition, the compounding ratio of these arbitrary components can be made into the normal dose of the range which does not impair the effect which the composition for oral cavity of this invention show | plays.

  From the viewpoint of stability, the pH of the composition for oral cavity of the present invention is preferably 5 to 9, more preferably 6 or 7 to 8, and the pH is adjusted using a pH adjuster as necessary. be able to. As a pH adjuster, phosphoric acid or a salt thereof (sodium phosphate, sodium hydrogen phosphate 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 Use of a salt thereof, succinic acid or salt thereof, glutamic acid or salt thereof, lactic acid, hydrochloric acid, hydrochloric acid, acetic acid, nitric acid, sodium hydroxide, potassium hydroxide or the like in the range which does not impair the effect of the composition for oral cavity of the present invention it can.

(2) Dentin coloring inhibitor of the present invention The combination of the above-mentioned (A) component and (B) component can prevent coloring of dentin, in particular, the surface and subsurface of dentin. Therefore, the composition containing the (A) component and the (B) component is useful as a dentin coloring inhibitor, in particular, a dentin 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, mouth freshener, or toothpaste (liquid toothpaste, gel-like toothpaste, toothpaste, etc.).

  There are no particular limitations on the person using the dentin coloration inhibitor of the present invention. However, from the viewpoint of preventing the coloring of dentin, elderly people and subjects with gingival regression are 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. Note that "%" means "% by mass" unless otherwise specified.

The detail of each component used for preparation of the composition for oral cavity of Examples 1-36 and Comparative Examples 1-3 is described below.
<(A) component>
Sodium pyrrolidone carboxylate Ajinomoto Co., Ltd., trade name "AJIDEW N-50 (registered trademark)"
<(B) component>
Sodium pyrophosphate manufactured by Taihei Chemical Industry Co., Ltd. <(C) ingredient>
Sodium Fluoride Stella Chemifa Co., Ltd. (purified sodium fluoride (S))
Sodium monofluorophosphate ICL Japan Co., Ltd. <Component (D)>
Xylitol Rotox Japan Co., Ltd. Reduced Palatinose Mitsui Sugar Co., Ltd. Erythritol Mitsubishi Chemical Foods Co., Ltd. <Other Additives>
Sodium lauryl sulfate (surfactant), Sorbit (thickener), propylene glycol (thickener), saccharin sodium (sweetener), xanthan gum (caking agent), anhydrous silica (abrasive), perfume, purified water ( solvent)
As the above-mentioned additive component, a cosmetic material standard standardized product was used.

Examples 1 to 36 and Comparative Examples 1 to 3
The dentifrice compositions of Examples 1 to 36 and Comparative Examples 1 to 3 were prepared by the following preparation method according to the formulation shown in Tables 1 to 6 using the above components.

(Method of preparing dentifrice composition)
After dissolving (component A) sodium pyrrolidonecarboxylate, (component B) sodium pyrophosphate, (component C) fluorine compound, (component D) sugar alcohol, 100 mass% sorbitol, saccharin sodium in purified water, separately A liquid in which glycol and xanthan gum were dispersed was added and stirred. Thereafter, 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. For production, a 1.5 L kneader (manufactured by Ishiyama Kosakusho Co., Ltd.) was used. The prepared dentifrice composition was evaluated for the effect of suppressing the coloration of the dentin surface and the subsurface and the usability was evaluated according to the following procedure. The evaluation results are described together in Tables 1 to 6.

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

2. Formation of a coloring model The bovine tooth root was cut into a block shape, and cement quality was removed by surface grinding. Of the cemented portion, about 3.5 mm × 3.5 mm was used for the decalcification window, and the other part was coated with nail polish. After drying the nail polish at room temperature, it was immersed in an aqueous 0.1 mol / L aqueous acetic acid solution (pH 4.5) for 50 hours to prepare a root surface dentin sample in which the window was exposed to collagen.

First, as an initial value, a color difference (L ^* 0, a ^* 0, b ^* 0) was measured using a spectrocolorimeter (CM-2022 manufactured by Minolta Co., Ltd.). The spouted saliva is centrifuged (10000 g, 20 minutes, 20 ° C.), and the root surface dentin sample is 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 It was immersed in the 3 times water dilution liquid of dentifrice composition of 36 and comparative examples 1-3 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 stomach mucin, 1% lactoferrin (pH 7.0) sequentially at 37 ° C. for 10 minutes. The steps from the treatment of the saliva supernatant fluid to the pellicle formation operation described above were repeated four times a day for a total of five days.

3. Evaluation of the effect of suppressing coloring on dentin surface The measurement window was lightly rinsed with distilled water, and excess moisture was blotted off with filter paper. After drying, color difference (L ^* 1, a ^* 1, b ^* 1) measurement was performed 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 equation.
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 coloring under the surface of dentin)
A root surface dentin sample was prepared in the same manner as the method prepared in (Evaluation of the effect of suppressing coloring on the surface of dentin). After being immersed in a 3-fold water dilution of the exhaled saliva and the dentifrice compositions of Examples 1 to 36 and Comparative Examples 1 to 3 shown in Tables 1 to 6, stain pellicles were formed. The depth of the subsurface coloring from the collagen surface layer in the formed stained pellicle window portion was measured using a stereomicroscopic observation image, and evaluated according to the following evaluation criteria.

[Evaluation Criteria for Subsurface Coloration]
A: Subsurface coloring from the surface <15 μm
B: 15 μm ≦ subsurface coloring from surface <20 μm
C: 20 μm ≦ subsurface coloring from surface <50 μm
D: 50 μm ≦ subsurface coloring from surface <100 μm
E: Subsurface coloring from the surface of 100 μm ≦≦

Evaluation of usability (no irritation) A treatment solution prepared by diluting the dentifrice composition of each Example and Comparative Example by 3 times with distilled water is contained in 20 mouths for 30 seconds by 20 panelists, and the oral cavity after discharge The presence or absence of internal pain was evaluated. Evaluation criteria were set as follows.

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

  As can be seen from the results of Comparative Example 1, even when sodium pyrophosphate is used alone, it can be seen that the effect of suppressing coloring on the surface and subsurface of dentin is scarce. In addition, as can be seen from the result of Comparative Example 2, even when sodium pyrrolidone carboxylate known to be capable of suppressing the coloring of polyphenols (medicinal components) on the surface of root surface dentin is used, Maillard of dentin tissue is It can be seen that there is almost no suppressing effect on the color derived from the reaction. Further, as can be seen from the results of Comparative Example 3, even when sodium tripolyphosphate known as a stain removing component is used as in the case of sodium pyrophosphate, it can be seen that the effect of suppressing coloring on dentin surface and subsurface is scarce. On the other hand, when pyrrolidone carboxylate sodium and sodium pyrophosphate were used in combination as understood from Examples 1 to 13, the effect of suppressing coloring on the dentin surface and the surface was produced.

  As can be seen from the results of Examples 14 to 18, when (C) a fluorine compound is blended in a dentifrice composition containing sodium pyrrolidone carboxylate and sodium pyrophosphate having a coloring inhibiting effect on dentin surface and subsurface. The color suppression effect under the surface of dentin was further improved without losing other effects.

  As can be seen from the results of Examples 19 to 24, when (D) a sugar alcohol is added to a dentifrice composition containing sodium pyrrolidonecarboxylate and sodium pyrophosphate having a coloring inhibiting effect on dentin surface and subsurface. The coloration suppressing effect of the dentin surface was further improved, and further, the preparation was excellent in no irritation and the feeling in use was also improved.

  As can be seen from the results of Examples 25 to 36, (C) a fluorine compound and (D) were added to a dentifrice composition containing sodium pyrrolidonecarboxylate and sodium pyrophosphate having a coloring inhibiting effect on dentin surface and subsurface. When a sugar alcohol is added, the coloration suppressing effect on dentine is further improved, and the feeling in use is also improved.

  In order to investigate the application range of the composition for oral cavity of the present invention, a mouthwash (Example 37), a mouth freshener (Example 38), and a gel toothpaste (Example 39) were produced, and the above-mentioned evaluation test As a result, in each case, the coloring suppression effect of the dentin surface and the coloring suppression effect under the dentine surface layer were A, and the evaluation of usability (a non-stimulation) was A. The respective compositions are shown below.

[Cleaning agent]
Composition A Component: Sodium pyrrolidone carboxylate (manufactured by Wako Pure Chemical Industries, Ltd.): 3%
B component: potassium pyrophosphate (made by Taihei Kagaku Sangyo Co., Ltd.): 1%
Component C: Sodium fluoride (made by Stella Chemifa Co., Ltd.) 0.04% (fluorine content: 0.02%)
Component C: sodium monofluorophosphate (manufactured by ICL Japan Ltd.) 0.23% (fluorine content: 0.03%)
D component: Xylitol (manufactured by Rocket Japan Co., Ltd.): 5%
Component D: reduced palatinose (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%
Perfume: 0.2%
Purified water: balance

[Oral refreshing agent]
Composition A Component: Sodium pyrrolidone carboxylate (manufactured by Wako Pure Chemical Industries, Ltd.): 3%
B component: potassium pyrophosphate (made by Taihei Kagaku Sangyo Co., Ltd.): 1%
Component C: Sodium fluoride (made by Stella Chemifa Co., Ltd.): 0.04% (fluorine content: 0.02%)
D component: Xylitol (manufactured by Rocket Japan Co., Ltd.): 5%
Component D: reduced palatinose (Mitsui Sugar Co., Ltd.): 10%
Component D: erythritol (Mitsubishi Chemical Foods Co., Ltd.): 10%
Glycerin: 13%
Ethanol: 40%
Polyoxyethylene Cured Castor Oil (60E.O.): 3%
Sodium citrate: 0.1%
Citric acid: 0.03%
Menthol: 0.3%
Perfume: 0.4%
Purified water: balance

[Gel-like toothpaste]
Composition A Component: Sodium pyrrolidone carboxylate (manufactured by Wako Pure Chemical Industries, Ltd.): 3%
B component: potassium pyrophosphate (made by Taihei Kagaku Sangyo Co., Ltd.): 1%
Component C: Sodium fluoride (made by Stella Chemifa Co., Ltd.): 0.04% (fluorine content: 0.02%)
D component: Xylitol (manufactured by Rocket Japan Co., Ltd.): 5%
Component D: reduced palatinose (Mitsui Sugar Co., Ltd.): 10%
Component D: erythritol (Mitsubishi Chemical Foods Co., Ltd.): 10%
Thickening silica: 1.5%
Propylene glycol: 3%
Sorbit solution: 55%
Carrageenan: 0.3%
Xanthan gum: 0.3%
Cetyl pyridinium chloride: 0.02%
Saccharin sodium: 0.12%
Potassium nitrate: 5%
Coconut oil fatty acid amidopropyl betaine solution: 0.3%
Perfume: 0.4%
Purified water: balance

Claims (11)

Component (A): at least one of pyrrolidone carboxylic acid and its inorganic base salt,
(B) component: The composition for oral cavity containing water-soluble pyrophosphoric acid and at least any one of its salt.   The composition for oral cavity of Claim 1 whose content of (A) component is 0.1-10 mass%.   The composition for oral cavity of Claim 1 or 2 whose content of (B) component is 0.01-5 mass%.   The composition for oral cavity of any one of Claims 1-3 whose mass ratio (A / B) of (A) component and (B) component is 0.1-300.   (C) component: The composition for oral cavity of any one of Claims 1-4 which further contain a fluorine compound.   The composition for oral cavity according to claim 5, wherein the content of the component (C) is 0.01 to 0.5% by mass as a fluorine content.   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 component (D): xylitol, reduced palatinose, and erythritol.   The composition for oral cavity according to claim 7, wherein the content of the component (D) is 0.5 to 50% by mass.   The composition for oral cavity 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. object.   The oral composition according to any one of claims 1 to 9, which is a dentifrice or a mouthwash. Component (A): at least one of pyrrolidone carboxylic acid and its inorganic base salt,
(B) Component: A dentin coloring inhibitor containing water-soluble pyrophosphoric acid and at least one of its salts.