JP6440515B2 - Oral composition - Google Patents

Description

  The present invention relates to an oral composition.

With the aging of society, root caries that develops on dentin exposed by gingival recession has been increasing, and its prevention is desired.
As for the onset mechanism of root caries (dentin caries) that develops in the dentin, first, sugar metabolism occurs by bacteria in the plaque adhering to the dentin surface, and acid is produced. Dentin mineral components are eluted (decalcified) by the produced acid, and the organic (collagen) layer is exposed. Furthermore, the exposed collagen layer is physically and chemically destroyed, resulting in substantial defects at the roots of the teeth.

  Conventionally, methods for preventing demineralization by fluoride and promoting remineralization are known as methods for preventing dentin caries. However, the dentin mineral density is about 50% less than the enamel with a mineral density of about 97%, so it is physically and chemically weak, and the preventive effect of the conventional method was never high. . Thus, in Patent Documents 1 to 11, techniques for suppressing decalcification and promoting remineralization have been proposed.

The dentin caries prevention method disclosed in Patent Document 1 uses an oral composition containing pyrrolidone carboxylic acid, a fluorine compound and casein for the purpose of suppressing dentin demineralization.
The method for preventing dentin caries disclosed in Patent Document 2 is whey or lactoferrin, fluorine compound, nitric acid, phosphoric acid, hydrochloric acid for the purpose of dentin tubule sealing, dentin demineralization inhibiting effect and fluorine stabilization The composition for oral cavity containing K or Na salt of sulfuric acid is used.
The method for preventing dentin caries disclosed in Patent Document 3 includes longan seed extract, fluorine compound and sugar alcohol for the purpose of dentin tubule blockade, dentin demineralization inhibitory effect, fluorine stabilization and formulation stabilization. An oral composition is used.
The method for preventing dentin caries disclosed in Patent Document 4 has an average particle size of hydrolyzed silk and primary particles in the range of 0.04 to 0.5 μm for the purpose of suppressing dentine mineral elution. An oral composition having light calcium carbonate as a component is used.

Patent Document 5 discloses a dental caries preventive agent comprising flavanones and / or glycosides thereof for the purpose of inhibiting collagen degradation and decalcification.
Patent Document 6 discloses a tooth having, as an ingredient, a monomer having a hydroxyl group and a monomer having a phosphorus atom-containing acidic group whose blending amount with respect to the monomer having a hydroxyl group is 5 to 200% by weight for the purpose of promoting remineralization. A quality remineralization promoter is disclosed.
Patent Document 7 discloses an oral composition containing potassium nitrate and reduced palatinose for the purpose of alleviating dentine hypersensitivity and promoting remineralization.
In Patent Document 8, for the purpose of preventing root caries, at least one selected from the group consisting of (A) a zinc compound, (B) an aldehyde compound, a phenol compound and a tea-extracted polyphenol compound, The composition for oral cavity which has as an ingredient is indicated.

Patent Document 9 discloses an oral composition containing a water-soluble aluminum compound, a fluoride, and a water-soluble calcium compound for the purpose of preventing dentin hypersensitivity and preventing root caries.
Patent Document 10 discloses a composition for oral cavity containing a water-soluble aluminum compound and a fluoride for the purpose of preventing dentin hypersensitivity and good usability.
Patent Document 11 discloses a dental composition containing a low-molecular compound that produces a poorly soluble precipitate in water by reacting with a calcium compound for the purpose of suppressing dentin hypersensitivity.

International Publication No. 2013/472826 JP 2012-232937 A JP 2011-168510 A JP 2007-176862 A JP 2009-256341 A JP 2006-8596 A JP 2003-73246 A Japanese Patent Laid-Open No. 11-228368 JP-A-5-155746 JP-A-5-155745 International Publication No. 96/17581

  However, further improvement has been demanded for the effect of inhibiting dentine caries. The subject of this invention aims at providing the composition for oral cavity which exhibits a dentine caries inhibitory effect.

  As a result of intensive studies to solve the above-mentioned problems, by using an oral composition containing a lactam compound, a water-soluble divalent metal salt, and a water-soluble fluorine compound, the amount of fluorine taken up is improved, thereby dentin caries. The knowledge that the suppression effect can be improved was obtained. The present invention is based on such novel findings.

The present invention provides the following [1] to [5].
[1] Component (A): one or more selected from the group consisting of pyrrolidonecarboxylic acid, 6-oxo-2-piperidinecarboxylic acid, 3- (2-oxo-1-azepanyl) propanoic acid, and salts thereof An oral composition containing a lactam compound, (B) component: water-soluble divalent metal salt, and (C) component: water-soluble fluorine compound.
[2] The composition for oral cavity according to [1], wherein the component (A) is pyrrolidonecarboxylic acid and / or a salt thereof.
[3] The composition for oral cavity according to [1] or [2], wherein the component (B) contains one or more water-soluble divalent metal salts selected from the group consisting of magnesium salts, zinc salts, copper salts and strontium salts. object.
[4] The composition for oral cavity according to any one of [1] to [3], wherein the component (C) is sodium fluoride or sodium monofluorophosphate.
[5] The oral cavity according to any one of [1] to [4], which is a dentifrice, a mouthwash, a mouth freshener, an intraoral coating agent, an oral patch, candy, tablet confectionery, or chewing gum. Composition.

  ADVANTAGE OF THE INVENTION According to this invention, the composition for oral cavity which exhibits a dentine caries inhibitory effect and has a favorable usability can be provided.

  The composition for oral cavity of the present invention comprises (A) component: pyrrolidonecarboxylic acid, 6-oxo-2-piperidinecarboxylic acid, 3- (2-oxo-1-azepanyl) propanoic acid, and a group thereof. 1 or more types of lactam compounds chosen, (B) component: water-soluble divalent metal salt, and (C) component: water-soluble fluorine compound.

<(A) component>
The component (A) is a compound having a lactam skeleton and an acidic group, which is pyrrolidone carboxylic acid, 6-oxo-2-piperidinecarboxylic acid, 3- (2-oxo-1-azepanyl) propanoic acid, And one or more lactam compounds selected from the group consisting of salts thereof.

  The salt is not particularly limited as long as it is a pharmacologically acceptable salt. Examples of pharmacologically acceptable salts include acid addition salts, base addition salts, and amino acid salts. Specific examples thereof include inorganic acid salts such as hydrochloride, hydrobromide, sulfate, hydroiodide, nitrate, phosphate; citrate, oxalate, acetate, formate, propion Acid salt, benzoate salt, trifluoroacetate salt, maleate salt, tartrate salt, methanesulfonate salt, benzenesulfonate salt, paratoluenesulfonate salt, etc .; sodium salt, potassium salt, aluminum salt, ammonium salt Inorganic base salts such as salts; organic base salts such as triethylammonium salt, triethanolammonium salt, pyridinium salt, diisopropylammonium salt; amino acid salts such as lysine salt, arginine salt, histidine salt, aspartate, glutamate, etc. . Of these salts, water-soluble salts are preferable, inorganic base salts are preferable, and alkali metal salts are particularly preferable.

A lactam compound may be synthesize | combined according to a well-known scheme, and a commercial item may be used for it.
As a commercially available product of pyrrolidone carboxylic acid, “AJIDEW A-100 (registered trademark)” sold by Ajinomoto Healthy Supply Co., Ltd. may be mentioned. As a commercial item of sodium pyrrolidone carboxylate, Ajinomoto Healthy Supply Co., Ltd. “AJIDEW (registered trademark) N-50, PCA soda (AI = 50% aqueous solution)” can be mentioned.
As a commercially available product of 6-oxo-2-piperidinecarboxylic acid, “(S) -6-Oxo-2-piperidine carboxylic acid (trade name)” sold by Sigma Aldrich Japan Co., Ltd. can be mentioned.
Examples of commercially available 3- (2-oxo-1-azepanyl) propanoic acid include “3- (2-oxoazepan-1-yl) propanoic acid (trade name)” sold by Sigma Aldrich Japan Co., Ltd. be able to.

  The component (A) may be one lactam compound or a combination of two or more lactam compounds, but preferably contains at least one of pyrrolidone carboxylic acid and a salt thereof, More preferred is pyrrolidone carboxylic acid or a salt thereof.

  Although content of (A) component in the composition for oral cavity of this invention is not restrict | limited in particular, from a viewpoint that the stability of (B) component can be improved more and a usability | use_condition (taste) can be improved more. Is preferably 0.1% by mass or more, more preferably 0.5% by mass or more, and further preferably 1% by mass or more with respect to the total amount of the composition for use.

The upper limit of the content of the component (A) is not particularly limited, but even if blended in a large amount, the contribution to the effect of improving the stability of the component (B) and the effect of improving the feeling of use (taste) may be limited. For this reason, the content is preferably 10% by mass or less, more preferably 5% by mass or less, based on the quality of the oral composition.
Therefore, the content of the component (A) is preferably 0.1% by mass to 10% by mass and more preferably 0.5% by mass to 5% by mass with respect to the total amount of the oral composition.

<(B) component>
The component (B) is a water-soluble divalent metal salt, and the “water-soluble divalent metal salt” refers to a divalent metal salt that can be dissolved in 2 g or more in 100 g of water at 20 ° C., for example. Specific examples include alkaline earth metal salts such as magnesium, strontium, and barium, and divalent transition metal salts such as zinc, copper, and iron. These may be used alone or in combination of two or more. Can be used. Of these divalent metal salts, the use of magnesium salts, strontium salts, barium salts and zinc salts is preferred, and the use of magnesium salts and zinc salts is more preferred.

  Specific examples of substances that give divalent metal salts include chlorides such as magnesium chloride, strontium chloride, barium chloride, zinc chloride, copper (II) chloride, iron (II) chloride, magnesium sulfate, zinc sulfate, copper sulfate ( II), sulfates such as iron (II) sulfate, magnesium nitrate, strontium nitrate, barium nitrate, zinc nitrate, copper nitrate (II), nitrates such as iron (II) nitrate, magnesium acetate, magnesium citrate, strontium acetate, Examples include organic acid salts such as zinc acetate, zinc citrate, zinc gluconate, and copper (II) gluconate, but are not limited thereto.

  The content of the component (B) is not necessarily limited, but is preferably 0.01% by mass or more based on the total amount of the oral composition from the viewpoint that the effect of improving the fluorine uptake amount is sufficiently exhibited. More preferably, it is 2% by mass or more.

The upper limit of the component (B) is preferably 5% by mass or less, and more preferably 3% by mass or less, based on the total amount of the oral composition. This is because even if the amount of the component (B) exceeds 5% by mass, the effect of improving the amount of fluorine uptake due to the increased amount may not be obtained.
Therefore, the content of the component (B) is preferably 0.01% by mass to 5% by mass and more preferably 0.2% by mass to 3% by mass with respect to the total amount of the oral composition.

<(C) component>
The “water-soluble fluorine compound” as component (C) refers to a fluorine compound that can be dissolved in 2 g or more in 100 g of water at 20 ° C., for example. As the fluorine compound of component (C), sodium fluoride, potassium fluoride, ammonium fluoride, tin fluoride, amine fluoride, sodium monofluorophosphate, potassium monofluorophosphate, sodium silicon fluoride, calcium calcium fluoride Preferably, sodium fluoride and sodium monofluorophosphate are used.
Component (C) may be a single fluorine compound or a combination of two or more fluorine compounds.

  The compounding amount of the fluorine compound is preferably 0.01 to 0.5% (100 to 5000 ppm) as fluorine, and more preferably 0.05 to 0.3% (500 to 3000 ppm). If the compounding amount of the fluorine compound is less than 0.01% (100 ppm) as fluorine, sufficient dentin caries inhibitory effect may not be obtained, and if it exceeds 0.5% (5000 ppm) as fluorine, fluorine removal In some cases, it is not possible to obtain an improvement effect.

  0.1-100 are preferable and, as for mass ratio (A component / mass of B component) of (A) component and (B) component, 0.3-20 are more preferable. When the mass ratio is less than 0.1, a good feeling of use (unpleasant taste) may not be obtained, and when the mass ratio exceeds 100, sufficient improvement in fluorine uptake may not be obtained. is there.

<Form of oral composition of the present invention>
The dosage form and shape of the composition for oral cavity of the present invention are not particularly limited. For example, liquid (solution, emulsion, suspension, etc.), semi-solid (gel, cream, paste, etc.), solid (tablet, particulate agent) , Capsules, films, kneaded materials, molten solids, waxy solids, elastic solids, etc.). Preferably, it is a liquid or a semi-solid.

  Moreover, the prepared preparations include, for example, dentifrices (toothpaste, liquid dentifrice, liquid dentifrice, powder dentifrice, etc.), mouthwash, mouth freshener, oral application agent, oral patch, food (for example, Chewing gum, tablet confectionery, rice cake, gummi, film, troche, etc.), but not limited to the above as long as it is within the range of oral use. A dentifrice, a mouthwash, a mouth freshener, and a mouth coating are preferable.

<Other optional components>
In the composition for oral cavity of the present invention, if necessary, in addition to the component (A), the component (B) and the component (C), other components are blended within a range not impairing the stability and decalcification inhibiting effect. Can do. Other optional components include, for example, surfactants, abrasives, binders, thickeners, sweeteners, preservatives, fragrances, medicinal ingredients, colorants, brighteners, pH adjusters, solvents such as water, Examples include excipients. Although the specific example of an arbitrary component is shown below, the component which can be mix | blended with the composition for oral cavity of this invention is not restrict | limited to these.

  Examples of surfactants include anionic surfactants such as N-acyl amino acid salts, α-olefin sulfonates, N-acyl sulfonates, alkyl sulfates, sulfates of glycerin fatty acid esters, and polyoxyethylene alkyl ethers. Nonionic surfactants such as polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene hydrogenated castor oil, glycerin ester polyoxyethylene ether, sucrose fatty acid ester, and alkylolamide can be used. These surfactants can be used singly 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. Specifically, in terms of foamability and hard water resistance, sodium lauroyl sarcosine, sodium α-olefin sulfonate having 10 to 16 carbon atoms as the carbon chain length of the alkyl chain, sodium lauryl sulfate, and the like can be used. .

  As the nonionic surfactant, polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, alkylolamide, sorbitan fatty acid ester and the like are preferably used particularly from the viewpoint of versatility. Specifically, polyoxyethylene alkyl ether having an alkyl chain having a carbon chain length of 14 to 18, an ethylene oxide average addition mole number of 15 to 30, and an polyoxyethylene having an ethylene oxide average addition mole number of 40 to 100 Hydrogenated castor oil, alkylol amide having 12 to 14 carbon atoms as 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, average addition mole of ethylene oxide A polyoxyethylene sorbitan fatty acid ester having a number of 10 to 40 can be used.

  Examples of the abrasive include silica-based abrasives such as silicic anhydride, crystalline silica, amorphous silica, silica gel, aluminosilicate, zeolite, calcium hydrogen phosphate anhydrous, calcium hydrogen phosphate dihydrate, Examples thereof include calcium pyrophosphate, calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, tribasic magnesium phosphate, zirconium silicate, tertiary calcium phosphate, hydroxyapatite, tetracalcium phosphate, and a synthetic resin abrasive.

  An abrasive | polishing agent may be used individually by 1 type, and may use 2 or more types together. When mix | blending an abrasive | polishing agent, it is preferable that the compounding quantity is 2-40 mass% of the whole composition in a dentifrice, and it is more preferable that it is 5-20 mass%.

  Examples of the binder include pullulan, gelatin, carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, xanthan gum, gum arabic, guar gum, locust bean gum, polyvinyl alcohol, polyvinylpyrrolidone, sodium polyacrylate, and the like. In general, it can be blended in an amount of 0.01 to 2% based on the whole preparation. A binder may be used individually by 1 type, and may use 2 or more types together.

  Examples of the thickener include propylene glycol, butylene glycol, glycerin, sorbitol, polyethylene glycol, and the like, and can be usually blended in an amount of 1 to 50% with respect to the whole preparation. One type of thickener may be used alone, or two or more types may be used in combination.

  Examples of the sweetening agent include saccharin sodium, stevioside, neohesperidin hydrochalcone, glycyrrhizin, perilartin, p-methoxycinnamic aldehyde, thaumatin, palatinose, maltitol, xylitol, arabitol and the like. A sweetener may be used individually by 1 type and may use 2 or more types together.

  As the preservative, for example, sodium benzoate, paraoxybenzoic acid ester, methyl paraben, ethyl paraben, butyl paraben, ethylenediamine tetraacetate and the like can be blended. A preservative may be used individually by 1 type, and may use 2 or more types together.

  As a fragrance, for example, essential oils such as peppermint and spearmint, fruit-based essences such as lemon and strawberry, 1-menthol, carvone, eugenol, anethole, linalool, limonene, ocimene, cineol, n-decyl alcohol, citronellol, crocodile, Perfume materials such as α-terpineol, methyl salicylate, thymol, rosemary oil, sage oil, perilla oil, lemon oil and orange oil are suitable.

Examples of the fragrances further include natural fragrances, synthetic fragrances (single fragrances), and blended fragrances (oil and fat fragrances (oil-based fragrances), powder fragrances, and the like). A fragrance | flavor may be used individually by 1 type and may use 2 or more types together.
Examples of natural flavors include mastic oil, parsley oil, anise oil, eucalyptus oil, winter green oil, cassia oil, lemon oil, coriander oil, orange oil, mandarin oil, lime oil, lavender oil, laurel oil, chamomile oil. , Cardamom oil, caraway oil, bay oil, lemongrass oil, pine needle oil, neroli oil, rose oil, jasmine oil, iris concrete, peppermint absolute, rose absolute, orange flower, citrus oil, mixed fruit oil, strawberry oil, Cinnamon oil, clove oil, grape oil, clove oil, thyme oil, sage oil, mint oil, rosemary oil, marjoram oil, origanum oil, grapefruit oil, sweetie oil, coconut oil, mango absolute, orange flower absolute Over DOO, capsicum extract, ginger oleoresin, pepper oleoresin, and capsicum oleoresin and the like.
Single flavors include, for example, anethole, methyl salicylate, cinnamaldehyde, linalool, linalyl acetate, limonene, pinene, octylaldehyde, citral, pregon, carbyl acetate, anisaldehyde, ethyl acetate, ethyl butyrate, allylcyclohexane propionate , Methyl anthranilate, ethyl methyl anthranilate, vanillin, undecalactone (γ-undecalactone, δ-undecalactone etc.), hexanal (trans-2-hexenal etc.), ethinone alcohol, propyl alcohol, butanol , Isoamyl alcohol, hexenol (cis-3-hexenol, etc.), dimethylsulfide, cycloten, furfural, trimethylpyrazine, ethyl lactate, ethyl Lurioacetate, cineol (1,8-cineole, etc.), mensofuran, linalool oxide, vanillyl butyl ether, furaneol, ethylcyclopentenolone, 2-methylbutyric acid, propionic acid, decalactone (γ-decalactone, δ-decalactone ), Nonalactone (γ-nonalactone, δ-nonalactone, etc.), hexalactone (γ-hexalactone, δ-hexalactone, etc.), isoamyl acetate, benzaldehyde, hexyl acetate, ethyl-2-methylbutyrate, benzyl alcohol, α -Terpineol, phenylethyl glycidate, phenylethyl alcohol, allyl hexanoate, methyl cinnamate, ethyl β-methylthiopropionate, cis-6-nonenol, Examples include Ron and methyl jasmonate.
The blended fragrance is a fragrance made by blending a single fragrance and / or a natural fragrance. Examples include strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, tropical fruit flavor, butter flavor, milk flavor, yogurt flavor, fruit mix flavor and the like.
The form of the fragrance is not limited, and any of essential oil, extract, solid, and powder obtained by spray-drying any of these may be used.

  Further, as medicinal ingredients, bactericidal or antibacterial agents such as chlorohexidine, triclosan, isopropylmethylphenol, cetylpyridinium chloride, benzethonium chloride and benzalkonium chloride, anticalculus agents such as condensed phosphate and ethane hydroxydiphosphonate, tranexamic acid Anti-inflammatory agents such as glycyrrhizin dipotassium salt, ε-aminocaproic acid, coating agents such as hydroxyethylcellulose dimethyldiallylammonium chloride, enzyme agents such as dextranase and mutanase, astringents such as vitamin C, lysozyme chloride and sodium chloride; Hypersensitivity inhibitors such as potassium nitrate and aluminum lactate can be used within the pharmaceutically acceptable range.

  Examples of the colorant include natural pigments such as safflower red pigment, gardenia yellow pigment, gardenia blue pigment, perilla pigment, red potato pigment, red cabbage pigment, carrot pigment, hibiscus pigment, cacao pigment, spirulina pigment, and coumarindo pigment. Red 3, No. 104, Red No. 105, Red No. 106, Yellow No. 4, Yellow No. 5, Green No. 3, Blue No. 1 and other legal dyes, riboflavin, copper chlorofin sodium, titanium dioxide and the like. . When the oral composition contains a colorant, the content is preferably 0.00001 to 3% by mass with respect to the total amount of the oral composition.

  Examples of the brightener include waxes such as aluminum oxide, titanium oxide, mica titanium, shellac, carnauba wax, and candelilla wax, and calcium stearate. When the oral composition contains a brightener, the content is preferably 0.01 to 5% by mass with respect to the total amount of the oral composition.

  The pH of the composition for oral cavity of the present invention is preferably 7 to 8 from the viewpoint of effectiveness and stability, and can be adjusted with a pH adjuster as necessary. Examples of pH adjusters include phosphoric acid or salts thereof (sodium phosphate, sodium hydrogen phosphate, etc.), citric acid or salts thereof (sodium citrate, etc.), malic acid or salts thereof, gluconic acid or salts thereof, maleic acid or The salt, succinic acid or its salt, glutamic acid or its salt, lactic acid, hydrochloric acid, acetic acid, nitric acid, sodium hydroxide, potassium hydroxide, etc. can be used in the range which does not impair the effect of this invention.

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 quantity of these arbitrary components can be made into the normal dose of the range which does not impair the effect of this invention.

Examples of the solvent include water and lower alcohols having 3 or less carbon atoms such as ethanol and propanol. When oral composition contains water as a solvent, the content can determine an appropriate quantity with the dosage form of oral composition. For example, in the case of toothpaste, it is preferable that it is 20-95 mass% with respect to the composition for oral cavity. When the oral composition contains a lower alcohol as a solvent, the content is preferably 1 to 30% by mass with respect to the total amount of the oral composition. Moreover, in the case of liquid oral compositions such as liquid dentifrices and mouthwashes, it is preferably 30 to 95% by mass with respect to the total amount of the oral composition. When the oral composition contains a lower alcohol as a solvent, the content is preferably 40 to 90% by mass with respect to the total amount of the oral composition.
Examples of the excipient include syrup, glucose, fructose, invert sugar, dextrin, oligosaccharide and the like. When the oral composition is a solid preparation, an excipient is usually added. When the excipient is blended, the blending amount can be appropriately determined within a range not impairing the effects of the present invention.

  EXAMPLES The present invention will be specifically described below with reference to examples, but the present invention is not limited to these examples. In the following, “%” means “mass%” unless otherwise specified.

(Examples 1-24, Comparative Examples 1-3)
(1) Preparation method of dentifrice (dentifrice) In purified water, (A) component, (B) component, (C) component, 70 mass% sorbitol, saccharin sodium and sodium hydroxide are mixed and dissolved at room temperature, solution X Was prepared. Sodium hydroxide was added so that the pH of the solution X was 6.5-8. On the other hand, Y liquid was prepared by dissolving and dispersing propylene glycol and sodium carboxymethylcellulose at room temperature.
Next, after adding and mixing Y liquid in X liquid under stirring, silicic acid anhydride, sodium lauryl sulfate, and a fragrance are mixed at room temperature using a 1.5 L kneader (manufactured by Ishiyama Kogakusho) and reduced in pressure to 4 kPa. After defoaming, 1.0 kg (100 parts by mass) of a dentifrice (oral composition) was obtained. Tables 1 to 3 show the materials used in the examples and the comparative examples and the blending ratios thereof.

Details of the materials used in the preparation of the dentifrice are as follows.
(A) Component pyrrolidone carboxylic acid (γ-lactam compound): AJIDEW A-100 (registered trademark) (Ajinomoto Co., Inc.)
6-oxo-2-piperidinecarboxylic acid (δ-lactam compound): (S) -6-Oxo-2-piperidine carboxylic acid (trade name) (Sigma Aldrich Japan Co., Ltd.)
3- (2-oxo-1-azepanyl) propanoic acid (ε-lactam compound): 3- (2-Oxazepan-1-yl) propanoic acid (trade name) (Sigma Aldrich Japan Co., Ltd.)

Component (B) Magnesium chloride: Magnesium chloride hexahydrate (trade name) (Wako Pure Chemical Industries, Ltd.)
Zinc chloride: Zinc chloride (trade name) (Wako Pure Chemical Industries, Ltd.)
Strontium chloride: Strontium chloride hexahydrate (trade name) (Wako Pure Chemical Industries, Ltd.)

(C) component sodium fluoride: sodium fluoride (trade name) (Stella Chemifa)
Sodium monofluorophosphate: Sodium monofluorophosphate (trade name) (Rhodia Nikka Co., Ltd.)

(Other ingredients)
As the carboxymethyl cellulose, sodium lauryl sulfate, sorbit, anhydrous silicic acid, propylene glycol, sodium saccharin, sodium hydroxide, and purified water, cosmetic raw material standards were used. For sorbit, a dentifrice was prepared using a 70% aqueous solution product (described as 70% sorbitol in the table). The descriptions of the blending amounts in the table are all values converted to a purity of 100%, and the amount of water brought in by sorbit is included in the amount of purified water.

  For the dentifrices of Examples 1 to 24 obtained as described above and the dentifrices of Comparative Examples 1 to 3, an evaluation test of fluorine uptake into ivory and an evaluation test of a feeling of use (disgusting taste) are performed according to the following procedure. went.

(Evaluation test)
(1) Evaluation of Fluorine Uptake into Dentin The dentin of human extracted teeth was cut into a 250 μm-thick section with a microcutter. A 2 mm × 2 mm window was left as a test site, and the other part was coated with nail polish to obtain a human dentin sample. This is a treatment liquid prepared using the dentifrice of each example and the dentifrice of each comparative example (a liquid obtained by diluting each dentifrice 3 times with distilled water assuming that it is diluted with saliva during use). It was immersed for 3 minutes at room temperature and washed lightly to remove the treatment solution. Then, it immersed for 10 minutes in 500 microliters of acid extraction liquids (0.075N hydrochloric acid aqueous solution), and the fluorine taken in by the human dentin sample was extracted. The fluorine concentration in the acid extract was measured with a fluorine ion electrode (9409BN, Orion) and an ion meter (EA920, manufactured by Orion Research). The measurement was performed at n = 5, the average value was calculated, and evaluated according to the following criteria. The evaluation results are shown in Tables 1 to 3.

〔Evaluation criteria〕
A: Fluorine concentration taken into human dentin is 0.4 ppm or more. O: Fluorine concentration taken into human dentin is 0.2 ppm or more and less than 0.4 ppm. Δ: Fluorine concentration taken into human dentin is 0.00. 05 ppm or more and less than 0.2 ppm x: Fluorine concentration incorporated in human dentin is less than 0.05 ppm

(2) Evaluation of feeling of use (unpleasant taste) A questionnaire about feeling of use (disgusting taste) was given to 10 subjects, and points were assigned based on the following criteria (1 to 4 points). (Old taste) was evaluated and the evaluation results are shown in Tables 1 to 3.
[Scoring criteria for feeling of use (disgusting taste)]
4 points: No nasty taste at all 3 points: Somewhat tasty but no problem level 2 points: Nasty taste 1 point: Unusually nasty [evaluation criteria for feeling of use (unusual taste)]
A: Average value of 3.5 points or more
○: Average value of 3.0 points or more and less than 3.5 points Δ: Average value of 2.0 points or more and less than 3.0 points ×: Average value of less than 2.0 points

(Results and discussion)
In the dentifrices of Examples 1 to 24 containing the component (A), the component (B) and the component (C), a favorable result was obtained that the fluorine uptake amount was 0.2 ppm or more (the evaluation result was ◯ or ◎). . On the other hand, in the dentifrice of Comparative Example 1 that does not contain the component (A), the dentifrice of Comparative Example 2 that does not contain the component (B), and the dentifrice of Comparative Example 3 that does not contain the component (C), the fluorine uptake amount is 0. The result that it was less than .2 ppm (the evaluation result is Δ or cannot be evaluated) was obtained.
From this result, one or more lactam compounds selected from the group consisting of pyrrolidonecarboxylic acid, 6-oxo-2-piperidinecarboxylic acid, 3- (2-oxo-1-azepanyl) propanoic acid, and salts thereof [( A) component], a water-soluble divalent metal salt [(B) component], and a water-soluble fluorine compound [(C) component] can be used to improve the amount of fluorine uptake. Thus, it was found that the effect of suppressing dentin caries can be improved.

  Moreover, in the dentifrice (Examples 1-3, Examples 5-10, Examples 12-16, Examples 18-22) whose A / B is 0.3-20, especially the fluorine uptake amount improvement effect is It was found to be excellent (0.4 ppm or more) and preferable.

  In particular, the blending amount of the component (A) is 0.5% by mass to 5% by mass, the blending amount of the component (B) is 0.2% by mass to 3% by mass, and the blending amount of the component (C) is 0. In the dentifrice (Examples 1-3, Examples 6-10, Examples 13-16, Examples 19-22) of 05-0.3%, especially the fluorine uptake amount improvement effect is excellent (0.4 ppm or more). ), It was found to be more preferable because of its excellent usability.

  The other compounding example using the composition for oral cavity of this invention is shown below.

Claims (3)

Component (A): One or more lactams selected from the group consisting of pyrrolidone carboxylic acid, 6-oxo-2-piperidinecarboxylic acid, 3- (2-oxo-1-azepanyl) propanoic acid, and alkali metal salts thereof 0.5 to 10% by mass of the compound,
(B) component: 0.2-3 mass% of 1 or more types of water-soluble divalent metal salt chosen from the group which consists of magnesium salt, zinc salt, copper salt, and strontium salt ,
Component (C): 0.05 to 0.3% by mass of a water-soluble fluorine compound that is at least one of sodium fluoride and sodium monofluorophosphate in terms of fluorine atoms ,
Contain,
The composition for oral cavity whose mass ratio ((A) / (B)) of said (A) component and said (B) component is 0.3-20 . The composition for oral cavity according to claim 1, wherein the component (A) is pyrrolidone carboxylic acid and / or a salt thereof. The composition for oral cavity according to claim 1 or 2 , which is a dentifrice, mouthwash, mouth freshener, oral application, oral patch, candy, tablet confectionery, or chewing gum.