JPWO2019117211A1 - Oral composition - Google Patents

Abstract

An object of the present invention is to provide an oral composition and its use capable of efficiently suppressing the decomposition of the collagen layer inside the dentin when it is exposed. Provided are an oral composition containing A) component: glycerophosphate and / or a salt thereof, and component (B): pyrrolidone carboxylic acid and / or an inorganic base salt thereof; and its use.

Description

The present invention relates to an oral composition.

In the oral cavity, the dentin of the teeth is usually protected by enamel. However, when the gingiva regresses with the onset of periodontal disease, the root portion covered with the gingiva is exposed in the oral cavity. At the root of the tooth, dentin exists without being covered with enamel. This dentin has an innumerable capillary structure and contains a large amount of an organic layer mainly composed of collagen, so that the mineral density is as low as about 50%, which is physical compared to enamel having a mineral density of about 97%. It is physically and chemically vulnerable. Therefore, caries is likely to occur in the exposed tooth root in the oral cavity. Here, "dental caries" refers to a substantial loss of teeth due to decalcification (elution of mineral components) of enamel and dentin by an acid produced by metabolizing sugars by bacteria in the oral cavity. Among caries, dentin caries that occurs at the root of the tooth is called "root surface caries".

The pathogenic mechanism of root caries is as follows. First, plaque adheres to the surface of dentin exposed in the oral cavity, and bacteria in the plaque metabolize sugar to produce acid. Subsequently, the produced acid decalcifies the crystal layer of dentin, exposing the collagen layer existing inside the dentin. Then, the exposed collagen layer is physically and chemically destroyed. As a result, the root surface is substantially defective. On the other hand, it has been pointed out that if the collagen layer remains, it becomes a scaffold for remineralization, and crystals derived from calcium ions and phosphate ions in saliva may be deposited in collagen.

Therefore, it can be said that suppression of decomposition of the exposed collagen layer is effective in preventing root surface caries.

Currently, we are heading toward an aging society, and with the onset of periodontal disease, root caries is on the rise. Therefore, it is currently required to establish a highly effective root caries prevention technique.

Here, as the caries prevention technology, fluoride sustained-release technology such as a technology for using calcium phosphate cement and fluoride in combination (Patent Document 1), an adhesive technology containing metal fluoride (Patent Document 2), and water solubility. Fluoride retention techniques such as a combined technique of calcium salt, other divalent metals, water-soluble phosphate, and water-soluble fluoride (Patent Document 3) are known.

Patent Document 4 describes that a lactam compound such as pyrrolidone carboxylic acid alone or a specific combination containing the same has a collagen decomposition inhibitory effect.

Japanese Unexamined Patent Publication No. 5-23386 Japanese Unexamined Patent Publication No. 2001-322908 Special Table No. 10-511104 International Publication No. 2013/047826

However, the technique using fluoride as disclosed in Patent Documents 1 to 3 described above may exert a certain effect on enamel caries, but in fluoride, root surface caries. Since the exposed collagen of enamel cannot be protected, the decomposition of collagen cannot be suppressed. Therefore, it cannot be expected that these techniques will be effective against dentin caries.

Patent Document 4 shows that pyrrolidone carboxylic acid or a salt thereof alone or a specific combination containing the same exerts a collagen decomposition inhibitory effect, and combines pyrrolidone carboxylic acid or a salt thereof with another compound. Does not provide motivation.

An object of the present invention is to provide an oral composition and its use capable of efficiently suppressing its decomposition when the collagen layer inside the dentin is exposed.

The present inventors have solved the above problems by using the component (A): glycerophosphate and / or a salt thereof and the component (B): pyrrolidonecarboxylic acid and / or an inorganic base salt thereof in combination to solve the above-mentioned problems and expose collagen. We have found that the decomposition of layers can be efficiently suppressed, and have completed the present invention.
That is, the present invention provides the following [1] to [8].
[1] An oral composition containing (A) component: glycerophosphate and / or a salt thereof, and component (B): pyrrolidone carboxylic acid and / or an inorganic base salt thereof.
[2] The oral composition according to [1], wherein the content of the component (A) in the oral composition is 0.005 to 1% by mass.
[3] The oral composition according to [1] or [2], wherein the content of the component (B) in the oral composition is 0.1 to 20% by mass.
[4] The oral cavity according to any one of [1] to [3], wherein the value of the ratio (A / B) of the mass of the component (A) to the mass of the component (B) is 0.001 to 6. Composition for.
[5] The oral composition according to any one of [1] to [4], further containing citric acid and a salt thereof, and one or more selected from the group of phosphoric acid and salts thereof.
[6] The oral composition according to any one of [1] to [5], which is a liquid.
[7] The oral composition according to any one of [1] to [6], which is a liquid toothpaste or mouthwash.
[8] The oral composition according to any one of [1] to [7], which is used for suppressing oral collagen decomposition.

According to the present invention, it is possible to provide an oral composition and its use capable of significantly suppressing the decomposition of the exposed collagen layer and efficiently suppressing the decomposition of the collagen layer inside the dentin caries. it can.

Hereinafter, the present invention will be described in detail according to its preferred embodiment. In the present specification, the content of each component is a value based on the amount of each component charged when preparing the composition.

[1. Oral composition]
The oral composition of the present invention contains the component (A) and the component (B). Furthermore, the oral composition of the present invention may contain an optional component.

<Ingredient (A)>
Ingredient (A) is glycerophosphate and / or a salt thereof.

The glycerophosphate includes α-glycerophosphate and β-glycerophosphate, and α-glycerophosphate is preferable.

Examples of the salt of glycerophosphate include alkali metal salts (for example, sodium salt and potassium salt), alkaline earth metal salts (for example, calcium salt and magnesium salt), copper salt, zinc salt, aluminum salt and ammonium salt. Inorganic base salts; examples include organic base salts such as triethylammonium salt, triethanolammonium salt, pyridinium salt, and diisopropylammonium salt. Among these salts, alkali metal salts and alkaline earth metal salts are preferable, sodium salts, potassium salts and calcium salts are more preferable, and calcium salts are even more preferable.

The component (A) may be glycerophosphate alone or a salt of glycerophosphate alone, a combination of salts of glycerophosphate and glycerophosphate, or a combination of two or more kinds of salts of glycerophosphate.

The glycerophosphate and / or a salt thereof may be commercially available. Examples of commercially available products of α-calcium glycerophosphate include “Ca glycerophosphate (trade name)” manufactured by Iwaki Pharmaceutical Co., Ltd.

The content of the component (A) in the oral composition of the present invention is not particularly limited, but is usually 0.005% by mass or more, preferably 0.01% by mass or more, based on the total amount of the oral composition. As a result, when the collagen layer inside the dentin is exposed, its decomposition can be efficiently suppressed (collagen decomposition suppressing effect). The upper limit is usually 1% by mass or less, preferably 0.5% by mass or less. As a result, the feeling of use can be improved, and the irritation and unpleasant taste derived from the component (A) can be suppressed. In a preferred embodiment, the content of the component (A) is usually 0.005 to 1% by mass, preferably 0.01 to 0.5% by mass.

<Ingredient (B)>
The component (B) is pyrrolidone carboxylic acid and / or an inorganic base salt thereof. Pyrrolidone carboxylic acid is a compound represented by the following formula (1).

The method for producing pyrrolidone carboxylic acid and its inorganic base salt is not particularly limited. As such a production method, for example, a method of dehydrating glutamic acid extracted from an organism such as seaweed or sugar cane or from a processed product such as wheat flour to obtain pyrrolidone carboxylic acid, and binding a metal ion (for example, sodium ion) to the glutamic acid. This allows the production of pyrrolidone carboxylic acid metal salts.

Examples of the inorganic base salt of pyrrolidone carboxylic acid include inorganic base salts of 1 to 3 valent metals. Examples of the inorganic base salts of 1 to 3 valent metals include alkali metal salts such as sodium salt and potassium salt; alkaline earth metal salts such as calcium salt and magnesium salt; copper salt, zinc salt, aluminum salt and ammonium salt. , And alkali metal salts (sodium salt, potassium salt) are preferable. The sodium salt of pyrrolidone carboxylic acid (PCA soda) has good stability (eg, oxidative stability) and is a component and safe of NMF (Natural Moisturizing Factor), which is a water-retaining substance of the stratum corneum of the skin. It is more preferable because it has high properties.

The component (B) may be one kind selected from the group consisting of pyrrolidone carboxylic acid and its inorganic base salt, or a combination of two or more kinds.

The content of the component (B) in the oral composition of the present invention is not particularly limited, but is usually 0.1% by mass or more, preferably 0.3% by mass or more, more preferably 0.% by mass, based on the total amount of the oral composition. It is 5% by mass or more. As a result, the effect of suppressing collagen decomposition can be achieved. The upper limit is usually 20% by mass or less, preferably 10% by mass or less, and more preferably 5% by mass or less. As a result, the usability can be improved. In addition, the off-taste derived from the component (B) can be suppressed. In a preferred embodiment, the content of component (B) is usually 0.1 to 20% by mass, preferably 0.1 to 15% by mass, more preferably 0.3 to 10% by mass, still more preferably 0.5. ~ 5% by mass.

<A / B>
In the oral composition of the present invention, the value of the ratio (A / B) of the mass of the component (A) to the mass of the component (B) is usually 0.001 or more, preferably 0.005 or more, more preferably 0.005 or more. It is 0.01 or more. As a result, the collagen decomposition inhibitory effect can be achieved more efficiently. The upper limit is usually 6 or less, preferably 5 or less, more preferably 2 or less, and particularly preferably 1 or less. As a result, the usability can be improved. In particular, the unpleasant taste can be suppressed. In a preferred embodiment, the value of A / B is usually 0.001 to 6, preferably 0.001 to 5, more preferably 0.005 to 2, and particularly preferably 0.01 to 1.

<Dosage form>
The dosage form of the oral composition is not limited, but it is preferably liquid at normal temperature and pressure (for example, 25 ° C. and 101.325 kPa) from the viewpoint of increasing the possibility of contact with the exposed collagen layer in the oral cavity. .. The liquid oral composition can be prepared and applied as a liquid preparation such as a mouthwash (for example, a mouthwash, a mouthwash), a liquid toothpaste, and a mouthwash. The liquid agent may be a concentrated type. The oral composition may be a pharmaceutical product, a quasi drug, a cosmetic product, or a food product.

<Arbitrary ingredient>
In addition to the above components, any component may be added to the oral composition of the present invention, if necessary. The optional component can be appropriately selected depending on the intended use and dosage form of the oral composition. For example, when the oral composition is a liquid, optional components include surfactants, thickeners, sweeteners, preservatives, flavors, medicinal components, thickeners, wetting agents other than component (A), and pH. Includes regulators, buffers and solvents. When the oral composition is in a dosage form other than a liquid, examples of the components other than the optional components exemplified above include a binder and an abrasive. The content of the optional component is not particularly limited, and can be set to an amount used in a normal oral composition as long as the effect of the present invention is not impaired.

Examples of the surfactant include anionic surfactants, nonionic surfactants, cationic surfactants, and amphoteric surfactants.

Examples of the anionic surfactant include N-acylamino acid salt, α-olefin sulfonate, N-acyl sulfonate, alkyl sulfate, and sulfate of glycerin fatty acid ester.
Examples of the N-acylamino acid salt include acyl amino acids and acyls having a saturated or unsaturated hydrocarbon group (for example, 8 to 18 carbon atoms, preferably 12 to 16; either linear or branched chains). Examples thereof include taurine and salts thereof, and details thereof include, for example, methyl taurine salts such as lauroyl methyl taurine salt, coconut oil fatty acid methyl taurine salt, and myristyl methyl taurine salt; methyl alanine salts such as lauroyl methyl alanine salt; lauroyl glutamic acid, myristol. Examples include glutamates such as glutamates.
Examples of the α-olefin sulfonate include sodium α-olefin sulfonate. The number of carbon atoms of the alkyl group contained in the α-olefin sulfonic acid is, for example, 10 to 16. As the α-olefin sulfonate, tetradecene sulfonate is preferable, and sodium tetradecene sulfonate is more preferable.
Examples of the alkyl sulfate include sodium lauryl sulfate and sodium myristyl sulfate. The number of carbon atoms of the alkyl group contained in the alkyl sulfate is preferably 12 to 14.
Other anionic surfactants include, for example, sodium acylsarcosine such as sodium N-lauroylsarcosine and sodium N-myristylsarcosine; sodium N-methyl-N-acylalanine, sodium dodecylbenzenesulfonate, hydrogenated coconut fatty acid monoglyceride monosulfate. Examples thereof include sodium, sodium lauroyl sulfoacetate, and sodium N-palmitoyl glutarmate. Examples of anionic surfactants having good foamability and / or water resistance include acyl sarcosine sodium (for example, sodium lauroyl sarcosine), α-olefin sulfonate sodium, and alkyl sulfate (for example, sodium lauryl sulfate). , These are preferred.

Examples of the nonionic surfactant include polyoxyethylene alkyl ether, polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene hydrogenated castor oil, glycerin ester polyoxyethylene ether, sucrose fatty acid ester, and alcoholamide. , Sorbitane fatty acid ester, polyglycerin fatty acid ester and the like. As a specific example, a polyoxyethylene alkyl ether having an alkyl chain having a carbon chain length (number of carbon atoms) of 14 to 18 and an ethylene oxide average addition molar number of 15 to 30; an ethylene oxide average addition molar number of 5 to 100 is preferable. Is 50 to 100, more preferably 60 to 100 polyoxyethylene oxide hardened castor oil; alkylolamide having an alkyl chain carbon chain length (carbon atom number) of 12 to 14; sorbitan having a fatty acid carbon atom number of 12 to 18 Fatty acid ester; Polyoxyethylene sorbitan fatty acid ester having 16 to 18 carbon atoms and an average ethylene oxide molar addition of 10 to 40 can be mentioned.

Examples of the cationic surfactant include a quaternary ammonium compound. Examples of the quaternary ammonium compound include an alkylammonium compound and an alkylbenzylammonium compound. Examples of the alkylammonium compound include cetylpyridinium chloride, and examples of the alkylbenzylammonium compound include benzethonium chloride and benzalkonium chloride.

Examples of amphoteric surfactants include alkylamide betaine-type amphoteric surfactants; betaine acetate-type amphoteric surfactants such as alkyldimethylaminoacetic acid betaine and fatty acid amidepropyldimethylaminoacetic acid betaine; N-fatty acid acyl-N-carboxymethyl-. Examples thereof include imidazoline-type amphoteric surfactants such as N-hydroxyethylethylenediamine salt.

Examples of the thickener include propylene glycol, butylene glycol, glycerin, sorbitol, polyethylene glycol, alcohol (for example, ethanol, modified ethanol), and sugar alcohol-reduced starch saccharified product. When the oral composition contains a thickener, the content is usually 0.3 to 50% by mass with respect to the total amount of the oral composition.

Examples of the sweetener include xylitol, saccharin, sodium saccharin, stebioside, neohesperidin hydrochalcone, glycyrrhizin, perillartine, p-methoxycinnamic aldehyde, thaumatin, maltitol, aspartame, erythritol and the like. The sweetener may also serve as a flavor.

Examples of preservatives include paraoxybenzoic acid esters such as methyl paraoxybenzoate and ethyl paraoxybenzoate; sodium benzoate; parabens such as butylparaben, methylparaben and ethylparaben; ethylenediamine tetraacetate; benzalkonium chloride. Be done.

The fragrance is not particularly limited, and examples thereof include natural fragrances, synthetic fragrances (single fragrances), and blended fragrances (fat fragrances (oil fragrances), powder fragrances, etc.). As fragrances, for example, natural essential oils such as peppermint oil, sparemint oil, eucalyptus oil, winter green oil, clove oil, thyme oil, cardamon oil, coriander oil, majorum oil, nutmeg oil, lavender oil, paracress oil, and peppermint oil; Extracts such as extracts, ginger extracts, pepper extracts, sunshaw extracts; fruit-based essences such as lemon and strawberry; l-mentole, carboxylic (l-carboxylic), synamic aldehydes, p-methoxycinnamic Alaldehyde, Methylsalicylate, Eugenol, Anetol, Linarol, Linarol Oxide, Limonen, Osimen, 1,8-cineole, n-decyl alcohol, benzyl alcohol, phenylethyl alcohol, citronellol, varinine, α-terpineol, methyl salicylate, Timor, Menton , Menthylacetate, citral, camphor, borneol, pinen, spiranthol, ethylacetate, ethylbutyrate, ethyl-2-methylbutyrate, isoamylacetate, hexylacetate, linaryl acetate, allylhexanoate, hexanal, hexenal, cis-3 -Hexenal, trans-2-hexenal, decanal, methylanthranilate, ethylmethylphenylglycidate, phenylethylglycidate, benzaldehyde, vanillin, ethyl vanillin, vanillyl butyl ether, flaneol, maltole, ethyl maltor, gamma / deltadecalactone , Gamma / Deltown Decalactone, N-ethyl-p-menthane-3-carboxamide, N-ethyl-2-isopropyl-5-methylcyclohexanecarboxamide, N-[(ethoxycarbonyl) methyl] -p-menthane-3- Carboxamide, N-p-benzene acetonitrile mentan carboxamide, N- (2- (pyridin-2-yl) ethyl) -3-p-menthan carboxamide, menthyl lactate, ethylene glycol-l-menthyl carbonate, methylheptin carbonate, mensoflan , 3-l-Mentixipropane-1,2-diol, Menthylglyceryl ether, Spiranthol, Menthylsuccinate, Isopregol, Ethylcyclopentenolone, 4,5-Dimethyl-3-hydroxy-2 (5H) -Flanone, Cycloten , 2-Methylbutyric acid, Acetic acid , Propionic acid, octanol, methyl cinnamate, yonone, ethyl-β-methylthiopropionate, cis-6-nonenol, 7-methyl-2H-1,5-benzodioxepin-3 (4H) -one , Methyl jasmonate; rosemary oil, sage oil, perilla oil, lemon oil, orange oil, lime oil, mandarin oil, grapefruit oil, anis oil, cassia oil, laurel oil, caraway oil, basil oil, mastic oil, Perfume materials such as neroli oil (orange flower oil), lemongrass oil, jasmine oil, rose oil, iris oil; apple, banana, strawberry, blueberry, melon, peach, pineapple, grape, muscat, wine, cherry, squash, coffee , Brandy, yogurt, vanilla and more selected from blended flavors are preferred.

Medicinal components include, for example: the following components: anti-cariogenic agents such as fluorides (eg, sodium fluoride, sodium monofluorophosphate, stannous fluoride); chlorohexidine, zinc gluconate, zinc citrate, chloride. Tertiary ammonium compounds such as cetylpyridinium, benzethonium chloride, benzalkonium chloride, decalinium chloride; bisguanide compounds such as chlorhexidine gluconate and chlorhexidine hydrochloride; bactericidal or antibacterial agents such as alkyldiaminoethylglycine hydrochloride and isopropylmethylphenol; Toothstone preventive agents such as phosphates and ethane hydroxydiphosphonates; Anti-inflammatory agents such as tranexamic acid, glycyrrhizine dipotassium salt, ε-aminocaproic acid, Oubaku extract; Coating agents such as hydroxyethyl cellulose dimethyldialyl ammonium chloride; Allantin, Allantin chlorhydroxyaluminum, vitamin C, lysozyme chloride, glycyrrhetinic acid and its salts, astringents or vitamins such as sodium chloride; hypersensitivity inhibitors such as strontium chloride, potassium nitrate, aluminum lactate; copper compounds; and plant extracts. The medicinal ingredient may be one kind alone or a combination of two or more kinds.

When the oral composition contains medicinal components, the respective contents may be appropriately set within a pharmaceutically acceptable range.

Examples of the thickener include xanthan gum, carrageenan, hydroxyethyl cellulose, sodium alginate, polyvinyl alcohol, and carboxymethyl cellulose. The content of the thickener when blended is usually 0.01 to 10% by mass with respect to the total amount of the oral composition.

Examples of the wetting agent include sugar alcohols such as sorbitol, maltitol, and lactitol; and polyhydric alcohols such as glycerin, ethylene glycol, polyethylene glycol, and propylene glycol.

Examples of pH adjusters and buffers include citric acid, tartaric acid, malic acid, gluconic acid, maleic acid, succinic acid, glutamate, phosphoric acid, carbonic acid, and their potassium salts, sodium salts, ammonium salts, ribonucleic acid and Examples thereof include salts, lactic acid, hydrochloric acid, acetic acid, nitrate, sodium hydroxide, potassium hydroxide and the like. Above all, the pH of the oral composition at 25 ° C. is stably maintained in the range of 5 to 8.5 by using one or more selected from the group consisting of citric acid and its salt, and phosphoric acid and its salt. can do. As a result, demineralization of tooth enamel can be suppressed. Examples of the salt of citric acid include sodium citrate. Examples of the salt of phosphoric acid include sodium monohydrogen phosphate and sodium dihydrogen phosphate. The pH adjuster and buffer are used in an amount that makes the liquid oral composition the desired pH.

When the oral composition is liquid or the oral composition is liquefied, its pH (25 ° C.) is usually 4.5 to 9, preferably 5 to 8.5, for example 6. ~ 8 or 6 ~ 7.5. As a result, demineralization of tooth enamel can be suppressed, and effectiveness and stability can be maintained. The pH can be measured immediately after preparing the liquid oral composition using a pH meter (model number Hm-30S) manufactured by Toa Denpa Kogyo Co., Ltd. at 25 ° C. after 3 minutes. If necessary for pH adjustment, the oral composition may contain a pH adjuster. When the oral composition contains a pH adjuster, the content thereof may be appropriately determined as necessary (for example, within a range that does not impair the effects of the present invention).

When the oral composition is liquid, it preferably contains a solvent. Examples of the solvent include water, alcohol (for example, lower monohydric alcohol such as ethanol), and propylene glycol. The solvent is preferably a mixed solvent, and more preferably a mixed solvent of ethanol: 0 to 30%, water of 70 to 95%, and propylene glycol of 0 to 10% when the total amount of the solvent is 100% by mass. Propylene glycol also functions as a thickener. When the liquid oral composition contains water, the water content is usually 60% by mass or more based on the total amount of the liquid oral composition. When the liquid oral composition contains a lower monohydric alcohol, the content thereof is usually 30% by mass or less, preferably 20% by mass or less, based on the total amount of the liquid oral composition.

The method of using the oral composition of the present invention is not particularly specified. In the case of a mouthwash and a mouthwash, for example, a method of rinsing the mouth with an appropriate amount in the mouth for 10 to 30 seconds, particularly about 20 seconds can be mentioned. In the case of liquid toothpaste, the teeth are usually brushed after mouthwashing.

<Use>
The oral composition of the present invention is useful in applications for suppressing collagen decomposition. Collagen is not particularly limited, but collagen in the oral cavity is usually collagen containing type I collagen. When the collagen layer of dentin is exposed and decomposed by collagenase in dentin caries, the root of the tooth is substantially lost. By applying the oral composition to teeth, collagen decomposition can be suppressed or improved, so that dentin caries can be prevented.

The subject of ingestion of the oral composition of the present invention is not particularly limited. Subjects who have already developed symptoms caused by collagen degradation (for example, progression of dentin caries, periodontal tissue problems (gingival recession, alveolar bone resorption, etc.)) and want to improve, these symptoms Examples include subjects who have not developed the disease but want to prevent it.

[2. Manufacturing method of oral composition]
The oral composition of the present invention can be produced by mixing the above-mentioned components. The order in which the components are mixed is not particularly limited, but it is preferable to mix them so that they are uniform. A solvent may be used as a dispersion medium in the production. When producing a liquid oral composition, it is preferable to stably maintain the pH of the liquid oral composition at 25 ° C. in the range of 5 to 7 by using citric acid. It is also preferable to stably maintain the pH of the liquid oral composition at 25 ° C. in the range of 6 to 8 by using phosphoric acid instead of this or in combination with citric acid.

Hereinafter, the present invention will be described in detail with reference to Examples. The following examples are for the purpose of preferably explaining the present invention, and do not limit the present invention. In addition, "%" means "mass%" unless otherwise specified. The blending amount of each component shown in Tables 1 and 2 is a value converted into pure content (AI). In addition, the amount of water (balance) includes the amount of water brought in by each component.

[Examples 1 to 14 and Comparative Examples 1 to 3]
By uniformly mixing all the components according to the compositions shown in Tables 1 and 2 (unit of content of each component in Tables 1 and 2: mass%), Examples 1 to 14 and Comparative Examples 1 to 1 3 mouthwashes were prepared. Specifically, the raw materials were sequentially added to the purified water and stirred, and uniformly dissolved using a three-one motor (BL1200, manufactured by HEIDON) to prepare a mouthwash. The pH (25 ° C.) of the prepared mouthwash was 6.2.

Details of each component are described below.
<Ingredient (A)>
Calcium glycerophosphate: α-calcium glycerophosphate (“Ca glycerophosphate (trade name)” manufactured by Iwaki Pharmaceutical Co., Ltd.)
<Ingredient (B)>
Sodium pyrrolidone carboxylate: Ajinomoto Co., Inc. "Ajidew (registered trademark) N-50"
<Arbitrary ingredient>
(Surfactant) Polyoxyethylene hydrogenated castor oil: "Polyoxyethylene (60) cured castor oil" manufactured by Nikko Chemicals Co., Ltd. (number of moles of ethylene oxide added: 60)
(Viscosant) Propylene glycol (manufactured by Asahi Glass Co., Ltd.)
(Viscosant) Glycerin (manufactured by Sakamoto Yakuhin Kogyo Co., Ltd., purity 85%)
(Sweet) Xylitol (manufactured by Rocket Foil)
(PH adjuster) Citric acid (manufactured by Fuso Chemical Industry Co., Ltd.)
(PH adjuster) Sodium citrate (manufactured by Fuso Chemical Industry Co., Ltd.)
(PH adjuster) Sodium monohydrogen phosphate (manufactured by Taihei Kagaku Sangyo Co., Ltd.)
(PH regulator) Sodium dihydrogen phosphate (manufactured by Taihei Kagaku Sangyo Co., Ltd.)
(PH adjuster) Sodium hydroxide (manufactured by Kanto Chemical Co., Inc.)
(Sweet) Saccharin sodium (manufactured by Daito Kagaku Co., Ltd.)
(Fragrance) Perfume compositions AP shown in Tables 3 and 4 to 10 (mixture of high-purity products manufactured by Lion)
(Solvent) water: Commercially available purified water (conforms to the quasi-drug raw material standard 2006)

For each of the mouthwashes in Tables 1 and 2, the collagen decomposition inhibitory effect and usability were evaluated by the following methods and criteria. The results are shown in Tables 1 and 2.

<Evaluation method of collagen decomposition inhibitory effect>
(1) Method for preparing root surface caries sample After polishing the surface of the bovine tooth root with a width of about 2 mm for a decalcification window to remove cementum, a section having a thickness of 250 μm was cut out with a microcutter. Of the cementum-removed part, about 1.5 mm × 250 μm was covered with nail polish so that the decalcification window could be used. A root caries sample was prepared by drying the nail polish at room temperature and then immersing it in a 0.1 mol / L acetic acid aqueous solution (pH 4.5 (25 ° C.)) for 6 hours to expose collagen to the decalcification window. ..

(2) Experimental procedure of collagen decomposition suppression test The root caries sample obtained in (1) above was immersed in the mouthwashes of Examples and Comparative Examples shown in Tables 1 and 2 for 5 minutes at room temperature (washing). Mouthwash treatment), after washing with distilled water, collagenase-containing artificial saliva at 37 ° C (CaCl ₂ : 2.2 mmol / L, KH ₂ PO ₄ : 2.2 mmol / L, acetic acid: 0.1 mol / L, and Clostridium A mixture of collagenase (Type 1A, manufactured by Sigma) derived from Clostridium histolyticum; 1.0 unit / mL, pH 6.5 (25 ° C.)) was immersed. This mouthwash treatment was performed 3 times a day in the morning, noon, and night, and was immersed in collagenase-containing artificial saliva at other times, and repeated for a total of 4 days. At the same time, the same experiment was conducted on the control group treated with purified water instead of the mouthwash of Examples and Comparative Examples.

(3) Calculation of collagen decomposition suppression rate and evaluation of dentin caries preventive effect After the experiment was completed, the root surface caries sample was observed under a microscope, and the decomposition depth of exposed collagen was measured and averaged at 3 points per sample. That is, the measurement was carried out at n = 3, and the average value was calculated. Here, the "decomposition depth" refers to the depth of erosion based on the surface height at the time of forming the decalcification window in the root surface caries sample.
Subsequently, the dentin collagen decomposition inhibition rate (%) was calculated by the following formula, and the calculated dentin collagen decomposition inhibition rate was used to evaluate in four stages according to the following criteria. These results are shown in Tables 1 and 2.
[formula]
Dentin collagen decomposition inhibition rate (%) =
{(Decomposition depth of control group-decomposition depth of example group / comparative example group) / (decomposition depth of control group)} × 100

(Evaluation criteria)
A: Collagen decomposition suppression rate is 80% or more B: Collagen decomposition suppression rate is 70% or more and less than 80% C: Collagen decomposition suppression rate is 50% or more and less than 70% D: Collagen decomposition suppression rate is less than 50%

<Evaluation method of usability (no discomfort and no irritation)>
For each mouthwash in Tables 1 and 2, five judges judged the flavor (feeling of use) after mouthwash. At the time of judgment, each judge first contained 10 mL of each mouthwash in the mouth, circulated in the oral cavity for 30 seconds, and then discharged. Subsequently, each judge graded the feeling of use of the mouthwash on a four-point scale according to the following scoring criteria from the viewpoint of no unpleasant taste and no irritating feeling. As a standard for a mouthwash that does not have an offensive taste or irritation, a mouthwash that does not contain the component (A) and the component (B), that is, the mouthwash that does not contain the component (A) in Comparative Example 1 is used. There was. The average value of the obtained scores was calculated, and the usability of each mouthwash was evaluated according to the following evaluation criteria. The results are shown in Tables 1 and 2.

(1) No taste (scoring standard for no taste after mouthwash)
4 points: No offensive taste 3 points: Almost no offensive taste 2 points: Some offensive taste 1 point: No offensive taste

(Evaluation criteria for no taste after mouthwash)
A: Average score 3.5 points or more and 4.0 points or less B: Average score 3.0 points or more and less than 3.5 points C: Average score 2.0 points or more and less than 3.0 points D: Average score 2.0 points Less than

(2) No irritation (scoring criteria for no irritation after mouthwash)
4 points: No stimulation 3 points: Almost no stimulation 2 points: Slightly stimulated 1 point: There was stimulation

(Evaluation criteria for lack of irritation after mouthwash)
A: Average score 3.5 points or more and 4.0 points or less B: Average score 3.0 points or more and less than 3.5 points C: Average score 2.0 points or more and less than 3.0 points D: Average score 2.0 points Less than

[Consideration]
As shown in Tables 1 and 2, in Comparative Examples 1 to 3, the evaluation result of the collagen decomposition inhibitory effect was "D", whereas in Examples 1 to 14, the evaluation result of the collagen decomposition inhibitory effect was "D". "A" or "B". Therefore, it can be seen that the mouthwashes of Examples 1 to 14 can efficiently suppress the decomposition of collagen existing inside the dentin by containing the component (A) and the component (B). On the other hand, since the mouthwashes of Comparative Examples 1 to 3 contain one of the components (A) and (B) and do not contain the other, they have a collagen decomposition suppressing effect as compared with the mouthwashes of Examples 1 to 14. It is considered inferior. Further, when the component (A) is contained and the component (B) is replaced with a long-chain organic salt (Comparative Example 2), the effect of suppressing collagen decomposition is inferior to that of the mouthwashes of Examples 1 to 14.

Further, as shown in Tables 1 and 2, in Comparative Examples 1 to 3, the evaluation results of usability may be inferior, whereas in Examples 1 to 14, the evaluation results of usability are all excellent. .. Therefore, it can be seen that the mouthwashes of Examples 1 to 14 can improve the usability by containing the component (A) and the component (B).

Further, in Examples 2, 3, 5, 6, 8, 13, and 14, instead of blending 0.2% by mass of the fragrance composition A in the mouthwash, Tables 3 and 4 to 10 (Tables 4 to 10). Unit of content of each component in 3: mass%, unit indicating composition of each component in Tables 4 to 10: parts by mass) A mouthwash containing 0.2% by mass of the fragrance compositions B to P shown in Was manufactured and the same evaluation was performed. As a result, in the mouthwash containing any of the fragrance compositions, the same as in Examples 2, 3, 5, 6, 8, 13 and 14 in which 0.2% by mass of the fragrance composition A was blended. Evaluation result was obtained.

Claims (8)

Ingredient (A): glycerophosphate and / or a salt thereof,
Component (B): Oral composition containing pyrrolidone carboxylic acid and / or an inorganic base salt thereof. The oral composition according to claim 1, wherein the content of the component (A) in the oral composition is 0.005 to 1% by mass. The oral composition according to claim 1 or 2, wherein the content of the component (B) in the oral composition is 0.1 to 20% by mass. The oral composition according to any one of claims 1 to 3, wherein the value of the ratio (A / B) of the mass of the component (A) to the mass of the component (B) is 0.001 to 6. .. The oral composition according to any one of claims 1 to 4, further containing citric acid and a salt thereof, and one or more selected from the group of phosphoric acid and salts thereof. The oral composition according to any one of claims 1 to 5, which is a liquid. The oral composition according to any one of claims 1 to 6, which is a liquid toothpaste or mouthwash. The oral composition according to any one of claims 1 to 7, which is for suppressing the decomposition of collagen in the oral cavity.