JP6820149B2 - Oral composition - Google Patents

Description

For new oral cavity, which can improve the adhesion of the cationic bactericide to the oral cavity, especially the teeth, tooth surface, oral mucosa, etc., and can dramatically maintain the bactericidal effect of the cationic bactericide in the oral cavity. Regarding the composition.

The oral composition is a composition used for sterilizing, cleaning, coating the tooth or tooth surface, coating the oral mucosa, etc., such as used as a dentifrice or mouthwash. Oral compositions usually contain antibacterial agents, fragrances, solvents and the like, and in particular, cationic bactericides have been used as antibacterial agents. However, the cationic bactericidal agent has a problem that the adhesiveness to the teeth and the tooth surface is low and the antibacterial effect is not maintained. Therefore, in order to improve the adhesion of the cationic bactericide to the tooth and oral mucosa, a technique of using various adhesive-imparting agents in combination, for example, a method of using polyphosphoric acid or polyglycerin fatty acid ester in combination with the cationic bactericide. (Patent Document 1), those using phosphorylated plulan in combination (Patent Document 2), those using a cationic polymer and an organic acid (antioxidant) in combination (Patent Document 3), and the like have been studied.
However, the above-mentioned adhesive-imparting agent has not been able to dramatically improve the adhesiveness of the cationic bactericide to the tooth and oral mucosa. On the other hand, collagen is known as an adsorbent for the active ingredient to allow the active ingredient to act on the affected area in the oral cavity for a long time and accurately (Patent Documents 4 and 5), but collagen alone is sufficient as a cationic bactericide. It could not be attached, and the relationship between the cationic fungicide and collagen was not elucidated.

Japanese Unexamined Patent Publication No. 2006-117574 International Publication No. 2008/010517 Pamphlet Japanese Unexamined Patent Publication No. 2000-34213 Japanese Unexamined Patent Publication No. 2003-119156 Japanese Unexamined Patent Publication No. 2003-119157

A first object of the present invention is to improve the persistence and adsorptivity of a cationic bactericide on teeth and tooth surfaces.
A second object of the present invention is to improve the persistence and adsorptivity of the cationic bactericide on the oral mucosa.
A third object of the present invention is to promote the persistence and adsorptivity of the cationic bactericidal agent on the tooth or tooth surface by using the cationic bactericidal agent in combination with other antibacterial components or adhesive-imparting components. The purpose is to maintain the antibacterial effect of the cationic bactericide for a long period of time.
A fourth object of the present invention is to exert an excellent plaque formation preventing effect and a dental caries preventing effect by using a cationic bactericidal agent in combination with other antibacterial components and adhesive auxiliary components. is there.

As a result of diligent research, the present inventors have conducted two kinds of components, namely, collagen, citric acid, ascorbic acid phosphate, and salts thereof as an adhesive-imparting agent for the cationic fungicide. By using in combination with one or more selected from the group consisting of, and optionally adjusting the pH of the obtained composition to 3.0 to 9.0, the cationic fungicide in the oral cavity, especially the teeth. It has been found that the adhesiveness to the tooth surface and the oral mucosa can be improved, and thus the bactericidal effect in the oral cavity by the cationic bactericide can be dramatically maintained. More specifically, the following can be mentioned as possible aspects of the present invention.

[1]
It is characterized by containing (A) a cationic bactericide, (B) collagen, and (C) one or more selected from the group consisting of citric acid, ascorbic acid phosphate ester and salts thereof. Oral composition.
[2]
The oral composition according to the above [1], wherein the component (C) is one or more selected from the group consisting of ascorbic acid phosphate ester and salts thereof.
[3]
The oral composition according to the above [1] or [2], wherein the component (C) is L-ascorbyl magnesium phosphate.
[4]
The oral composition according to any one of the above [1] to [3], wherein the component (A) is cetylpyridinium chloride.
[5]
The oral composition according to any one of [1] to [4] above, wherein the component (B) is one or more selected from the group consisting of hydrolyzed collagen, succinyl atelocollagen and myristoylation succinyl atelocollagen.
[6]
(A) The oral composition according to any one of [1] to [5] above, wherein the content of the cationic bactericide is 0.0001 to 10% by mass with respect to the mass of the oral composition. ..
[7]
(B) The oral composition according to any one of [1] to [6], wherein the collagen content is 0.0002 to 40% by mass with respect to the mass of the oral composition.
[8]
The component (C) is an ascorbic acid phosphate ester, and the content of the ascorbic acid phosphate ester is 0.001 to 20% by mass with respect to the mass of the oral composition. 7] The oral composition according to any one of.
[9]
The oral composition according to the above [1], wherein the component (C) is citric acid, and the content of the citric acid is 0.001 to 20% by mass with respect to the mass of the oral composition.
[10]
The oral composition according to any one of [1] to [9], wherein the pH of the oral composition is 6.3 to 9.0.
[11] The oral composition according to any one of [1] to [10] above, which is used for sterilizing the tooth surface.

The oral composition of the present invention can improve the persistence and adsorptivity of the cationic bactericide on the tooth or tooth surface.
The oral composition of the present invention can improve the persistence and adsorptivity of the cationic bactericide on the oral mucosa.
The oral composition of the present invention is used in combination with a cationic bactericidal agent and any other antibacterial component or adhesive-imparting component, so that the cationic bactericidal agent is persistent and adsorptive to teeth and tooth surfaces. The antibacterial effect of the cationic bactericidal agent can be maintained for a long period of time.
The oral composition of the present invention exerts an excellent plaque formation preventing effect and a tooth decay preventing effect by using a cationic bactericidal agent in combination with any other antibacterial component or an adhesive auxiliary component. be able to.

[Composition for oral cavity]
The oral composition of the present invention comprises one or more selected from the group consisting of (A) a cationic bactericide, (B) collagen, (C) citric acid, ascorbic acid phosphate and salts thereof. It contains.
Here, the oral composition refers to a composition that is applied to the entire oral cavity of humans or animals or locally, and is particularly applied to a portion where an antibacterial effect needs to be imparted. The oral composition of the present invention can be applied particularly to the tooth surface, tooth surface, tongue, oral mucosa and the like. More specifically, it can suppress the adhesion of bacteria to the surface of teeth and mucous membranes in the oral cavity, and as a result, the formation of plaque and tartar on the surface of teeth can be suppressed, as well as halitosis, periodontal disease, etc. Concerning oral compositions that are useful in preventing bad breath.
Specific aspects of the oral composition include, for example, dentifrices, liquid dentifrices, oral humectants, mouthwashes and the like.
The oral composition of the present invention can be in various shapes, for example, liquid (emulsified form, solubilized form), liquid, gel form, paste form, tablet, effervescent tablet, powder form, granular form and the like. can do.

(A) Cationic bactericidal agent The cationic bactericidal agent of the present invention is used as a bactericidal component for sterilizing the tooth surface, oral mucosa, etc. in the oral cavity. Examples of the cationic disinfectant that can be used in the present invention include a quaternary ammonium salt and a biguanide-based disinfectant. Specific examples of cationic bactericides include cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, decalinium chloride, distearyldimethylammonium chloride, stearyldimethylbenzylammonium chloride, stearyltrimethylammonium chloride, cetyltrimethylammonium chloride, and chloride. Tertiary ammonium salts such as lauryltrimethylammonium and laurylpyridinium chloride; cationic bactericides such as biguanide-based bactericides such as alexidine gluconate, alexidine hydrochloride, alexidine acetate, chlorhexidine hydrochloride, chlorhexidine acetate, chlorhexidine hydrochloride, chlorhexidine gluconate, etc. Can be mentioned. Among them, as the cationic fungicide, cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, decalinium chloride, chlorhexidine hydrochloride and the like are preferably selected. The above cationic fungicide may be used alone or in combination of two or more.
The amount of the cationic bactericidal agent of the present invention is, for example, 0.0001 to 10% by mass, preferably 0.0005 to 5% by mass, more preferably 0.001 to 1% by mass, based on the total mass of the oral composition of the present invention. It is suitable that it is 1% by mass, more preferably 0.005 to 0.5% by mass, and particularly preferably 0.01 to 0.1% by mass. When the cationic bactericidal agent is 0.0001% by mass or more, sufficient bactericidal property can be imparted, and 10% by mass or less is preferable from the viewpoint of stable formulation and usability.

(B) Collagen The collagen of the present invention promotes the persistence and adsorptivity of the above-mentioned component (A) on the tooth or tooth surface, oral mucosa, etc., and prolongs the antibacterial effect of the cationic bactericide. It can be used as an adhesive-imparting ingredient for duration. Examples of collagen that can be used in the present invention include non-denatured collagen, gelatin, atelocollagen, collagen peptide, fibrous collagen, crosslinked collagen, calcified crosslinked collagen, enzyme-treated collagen, alkali-treated collagen, and hydrolyzed collagen. Can be mentioned as collagen. Specific examples of collagen include one or more selected from the group consisting of hydrolyzed collagen, succinyl atelocollagen and myristoylation succinyl atelocollagen. Here, hydrolyzed collagen means one obtained by hydrolyzing or enzymatically treating non-denatured collagen or atelocollagen, and succinyl atelocollagen means succinylated modified atelocollagen, and myristoylation succinyl atelocollagen. Means myristoylated and succinylated modified atelocollagen. Among them, hydrolyzed collagen, succinyl atelocollagen and myristoylation succinyl atelocollagen are preferably selected as collagen. The above collagen may be used alone or in combination of two or more.
The amount of collagen of the present invention is, for example, 0.0002 to 40% by mass, preferably 0.001 to 30% by mass, and more preferably 0.002 to 20% by mass, based on the total mass of the oral composition of the present invention. , More preferably 0.01 to 10% by mass, and particularly preferably 0.1 to 5% by mass. When collagen is 0.0002% by mass or more, it is possible to sufficiently impart and assist the cationic bactericide on the tooth or tooth surface, oral mucosa, etc., and to stably formulate and use it. From the viewpoint of feeling, 40% by mass or less is preferable.
The mass ratio of the component (A) to the component (B) is, for example, 1 / 5000-250 / 1, preferably 1/1000 to 50/1, more preferably 1 in terms of the mass ratio of (A) / (B). It is suitable that it is / 500 to 25/1, more preferably 1/200 to 5/1, and particularly preferably 1/100 to 1/2.

(C) Citric acid, ascorbic acid phosphate The present invention can further add one or more components selected from the group consisting of citric acid, ascorbic acid phosphate and salts thereof. Here, examples of the salt include sodium salt, potassium salt, calcium salt, magnesium salt and the like, and sodium salt and magnesium salt are preferable. More preferably, the component (C) includes citric acid, sodium citrate, L-ascorbyl magnesium phosphate, and a mixture thereof. The component (C) promotes the persistence and adsorptivity of the above-mentioned component (A) on the tooth or tooth surface, oral mucosa, etc., and maintains the antibacterial effect of the cationic bactericide for a long period of time. Can be used as an adhesive-imparting ingredient for Although the present invention is not limited by theory, the component (C) of the present invention has a long antibacterial effect of the cationic bactericide as the component (A) due to the synergistic effect with the collagen which is the component (B). It acts as an adhesive-imparting ingredient for long-lasting. The present inventors have found that citric acid, ascorbic acid phosphate ester, and salts thereof exert the synergistic effect.

The amount of the component (C) of the present invention is, for example, 0.001 to 20% by mass, preferably 0.002 to 10% by mass, more preferably 0.005 to 5% by mass, based on the total mass of the oral composition of the present invention. It is suitable that it is 7% by mass, more preferably 0.007 to 4% by mass, and particularly preferably 0.01 to 2% by mass. When the component (C) is 0.001% by mass or more, the cationic bactericidal agent can sufficiently impart persistence and adsorptivity to the tooth or tooth surface, oral mucosa, etc., and 0.001% by mass. In the above case, the residual property and the adsorptive property can be more sufficiently imparted, and the content is preferably 20% by mass or less from the viewpoint of stable blending and usability.
The mass ratio of the component (A) to the component (C) is, for example, 1/1000 to 50/1, preferably 1/500 to 20/1, more preferably 1 in terms of the mass ratio of (A) / (C). It is suitable that it is / 100 to 10/1, more preferably 1/70 to 7/1, and particularly preferably 1/50 to 5/1.
The mass ratio of the component (B) to the component (C) is, for example, 1/1000 to 1000/1, preferably 1/100 to 500/1, more preferably 1 in terms of the mass ratio of (B) / (C). It is suitable that it is / 10 to 300/1, more preferably 1/5 to 200/1, and particularly preferably 1/2 to 100/1.

(D) Other antibacterial components In addition to the cationic bactericide, various antibacterial components can be used in combination in the present invention. As other antibacterial components that can be used in the present invention, for example, an anionic bactericidal agent, a nonionic bactericidal agent, an amphoteric bactericidal agent and the like can be used. Examples of the anionic fungicide include benzoate, lauroyl sarcosine salt, lauryl sulfate and the like. Examples of the nonionic bactericide include isopropylmethylphenol, triclosan, hinokithiol, phenol, thymol, eugenol, and bisphenol, which are phenolic bactericides. Examples of the amphoteric bactericide include dodecyldiaminoethylglycine and the like. These other antibacterial components may be used alone or in combination of two or more.

The content of the other antibacterial component is, for example, 0.005 to 5% by mass, preferably 0.008 to 2% by mass, and more preferably 0.01 to 0.01 to the total mass of the oral composition of the present invention. It is appropriate that it is 1% by mass.
The mass ratio of the cationic bactericidal agent to the other antibacterial component is, for example, 100: 1 to 1: 100, preferably 50: 1 to 1:50, and more preferably 10: 1 to 1:20. It is appropriate to have.
Further, the content of other antibacterial components in the oral composition of the present invention is, for example, 0.001 to 10% by mass, preferably 0.005 to 5% by mass, based on the total mass of the oral composition. , More preferably 0.01 to 2% by mass.

(E) Other components In addition to the above components (A) to (D), the oral composition of the present invention contains abrasives, wetting agents, solvents, binders, flavors, excipients, sweeteners, and pH. Regulators, preservatives, emulsifiers, solubilizers, foaming agents, lubricants, surfactants, oils, pigments, antioxidants, other agents and the like can be appropriately added. These additives are usually used in pharmaceutical compositions, oral compositions or food formulation designs, can be appropriately selected within a range that does not impair the effects of the present invention, and can be blended in an appropriate blending amount. it can. Examples of such additives include the following.

Examples of the polishing agent include calcium carbonate, calcium phosphate, dicalcium phosphate, calcium pyrophosphate, insoluble calcium metaphosphate, hydrous silicic acid, silicic acid anhydride, titanium dioxide, amorphous silica, crystalline silica, aluminosilicate, and aluminum oxide. , Aluminum hydroxide, resin, hydroxyapatite and the like can be blended alone or in combination of two or more. The blending amount of the abrasive is generally 3 to 60% by mass with respect to the total amount of the oral composition.
As the wetting agent, for example, polyhydric alcohols such as glycerin, sorbitol, polyethylene glycol, propylene glycol, ethylene glycol, 1,3-butylene glycol, polypropylene glycol, xylitol, maltitol, and lactitol are used alone or in combination of two or more. Can be blended. The blending amount of the wetting agent is generally 0.1 to 50% by mass based on the total amount of the oral composition.

As the solvent, an organic solvent such as alcohol or water is preferable, and examples thereof include ethanol, propyl alcohol, isopropyl alcohol and the like, and ethanol is particularly preferable. These alcohols can be blended alone or in combination of two or more. The blending amount of the solvent is generally 99.9% by mass or less, preferably 0.1 to 30% by mass, based on the total amount of the oral composition.
Examples of the binder include cellulosic derivatives such as carrageenan, carboxymethyl cellulose and sodium carboxymethyl cellulose, alkali metal alginate such as sodium alginate, gums such as xanthan gum, tragacant gum and arabic gum, and synthetic viscosity such as polyvinyl alcohol and sodium polyacrylate. Examples thereof include binders, silica gels, aluminum silica gels, and inorganic binders such as bee gum. The blending amount of the binder is generally 0.5 to 10% by mass based on the total amount of the oral composition.

As fragrances, known fragrance materials such as strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mix flavor, tropical fruit flavor and other blended fragrances, terpenoid essential oils, It can be used in combination with phenylpropanoid essential oils and the like. Examples of the phenylpropanoid-based essential oil include clove oil, fennel oil, keihi oil, eugenol, anethole, keihyaldehyde, cinnamaldehyde and the like. Examples of the terpenoid essential oil include peppermint oil, eucalyptus oil, orange oil, televisionn oil, peppermint oil, sparemint oil, citrus oil, sime oil, perilla oil, tea tree oil, lemon oil, sage oil, rosemary oil, l-. Examples include limonene, l-menthol, menthon, α-pinen, citral, cineole, camphor and the like. The blending amount of the fragrance is generally 0.0001 to 10% by mass with respect to the total amount of the oral composition.
Excipients include, for example, sucrose, lactose, starch, glucose, crystalline cellulose, mannitol, sorbitol, xylitol, erythritol, palatinit, palatinose, maltitol, trehalose, lactitol, lactitol, reduced starch sugar, reduced isomaltooligosaccharide. , Coupling sugar, gum base, arabic gum, gelatin, cetylmethylcellulose, light anhydrous silicic acid, magnesium aluminate, calcium aluminometasilicate, sodium hydrogencarbonate, calcium phosphate and the like. The blending amount of the excipient is generally 0.01 to 30% by mass with respect to the total amount of the oral composition.

Examples of the sweetener include palatinit, aspartame, sodium saccharin, potassium acesulfarm, stebioside, neoheseridyldihydrochalcone, glycyrrhizin, perilalmin, taumatin, aspalathylphenylalanylmethyl ester, ρ-methoxycinnamic aldehyde and the like. , These can be blended alone or in combination of two or more. The blending amount of the sweetener is usually 0.01 to 10% by mass, preferably 0.05 to 5% by mass, based on the entire oral composition.
Examples of the pH adjuster include phosphoric acid, pantothenic acid, malic acid, pyrophosphate, lactic acid, tartaric acid, glycerophosphate, acetic acid, nitric acid, or disodium hydrogen phosphate and the like. Examples thereof include sodium oxide, which can be blended alone or in combination of two or more so that the pH of the composition is in an appropriate range. The blending amount of the pH adjuster is usually 0.01 to 2% by mass with respect to the total amount of the oral composition.
Examples of the chelating agent include sodium tripolyphosphate, sodium metaphosphate, EDTA, and the like, and these can be blended alone or in combination of two or more. The blending amount of the chelating agent is usually 0.01 to 10% by mass, preferably 0.05 to 5% by mass, based on the entire oral composition.

Examples of preservatives include paraoxybenzoic acid esters, benzoic acid and its salts, salicylic acid and its salts, sorbic acid and its salts, phenoxyethanol, alkyldiaminoethylglycine hydrochloride and the like. The blending amount of the preservative is generally 0.005 to 5% by mass with respect to the total amount of the oral composition.
Examples of the emulsifier include polyoxyethylene alkyl ether, polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, sorbitan fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, polyoxyethylene hydrogenated castor oil, stearoyl sodium lactate, and soybean. Examples include phospholipids and alkyltrimethylammonium chloride. The blending amount of the emulsifier is generally 0.05 to 30% by mass with respect to the total amount of the oral composition.
Examples of the solubilizer include esters, polyethylene glycol derivatives, polyoxyethylene hydrogenated castor oil, fatty acid esters of sorbitan, and sulfated fatty alcohols. The blending amount of the solubilizer is generally 0.05 to 30% by mass with respect to the total amount of the oral composition.
Examples of the effervescent agent include N-acylamino acid salts such as sodium lauryl sulfate, sodium lauroyl sarcosin, sodium alkylsulfosuccinate, sodium coconut oil fatty acid monoglycerin sulfonate, sodium α-olefin sulfonate, and N-acylglutamate, 2-. Alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine, maltitol fatty acid ester, sucrose fatty acid ester, polyglycerin fatty acid ester, fatty acid diethanolamide, polyoxyethylene sorbitan monostearate, polyoxyethylene hydrogenated castor oil, Examples thereof include polyoxyethylene fatty acid esters, and one or more of these can be used in combination.

Examples of the lubricant include magnesium stearate, sucrose fatty acid ester, talc, and hydrogenated oil.
Examples of the oil include oils other than the above-mentioned essential oil used as an antibacterial component and the above-mentioned oil used as a fragrance, such as coconut oil, olive oil, sesame oil, peanut oil, parsley oil, parsley seed oil, and red flower oil.
Examples of the surfactant include sodium lauryl sulfate, sodium α-olefin sulfonate, sodium dodecylbenzene sulfonate, sodium lauryl sulfoacetate, sodium N-lauroyl sarcosinate, N-acylglutamate, sucrose fatty acid ester, and polyoxy. Ethylene-hardened castor oil, polyoxyethylene polyoxypropylene block copolymer, alkyl glycosides, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, alkyldimethylamine oxide, lauryl ethanol amide, sodium cocoyl sarcosinate, N-lauroyl methyl taurine Examples include sodium solution. The blending amount of the surfactant is generally 0 to 30% by mass with respect to the total amount of the oral composition.
In addition to the above-mentioned components, for example, pigments such as Blue No. 1, pigments such as titanium dioxide, antioxidants such as dibutylhydroxytoluene, and chelating agents other than the component (D) such as edetate, It may contain a tea extract, a dry distillate of tea, a flavoring agent such as monosodium glutamate, and the like.

The oral composition of the present invention can also contain medicinal ingredients such as moisturizers, anti-inflammatory agents, fluorides, vitamins, and crude drug extracts. These medicinal ingredients can be appropriately selected from those that can be used in pharmaceuticals, foods, and cosmetics.
Examples of moisturizers include amino acids or salts thereof, pyrrolidone carboxylic acid, mucin, hyaluronic acid or salts thereof, mucopolysaccharides such as chondroitin sulfate, sodium lactate, urea, pantenol, aloe extract, rosemary extract, thyme extract, cha extract. Examples include natural extract components such as (cha dry distillate extract) and so-called extracellular matrix such as collagen and elastin. One or a combination of two or more of these may be appropriately selected.

Examples of the anti-inflammatory agent include lysozyme chloride, ε-aminocaproic acid, aluminum hydroxyl allantoin, glycyrrhetinic acid, glycyrrhizates, guaizulene sulfonic acid, dl-α-tocopherol acetate and the like.
Examples of the fluoride include sodium fluoride, potassium fluoride, sodium monofluorophosphate, and stannous fluoride.
Examples of vitamin preparations include vitamin As such as retinoic acid and β-carotene, pantothenic acid or its salts, vitamin Bs such as niacin and biotin, ascorbic acid or its salts, vitamin Cs such as derivatives, α-tocopherol, etc. Examples include vitamin Es and folic acid.
Examples of raw medicine extracts include chamomile extract, kanokosou extract, nut extract, hop extract, ramender extract, linden extract, karin extract, goldfish extract, kumazasa extract, gummy extract, chowji extract, densitin gin extract, salvia extract, mukuroji extract, etc. Can be mentioned.
The concentration of the moisturizer, anti-inflammatory agent, fluoride, vitamin agent, crude drug extract and other medicinal ingredients is generally in the range of 0.001 to 5.0% by mass, more preferably 0. It is in the range of 0.01 to 1.0% by mass.

[Adjustment of pH]
The pH of the oral composition of the present invention is adjusted to, for example, 3.0 to 9.5, preferably 6.3 to 9.0, and more preferably 6.5 to 8.0. The pH adjuster described above can be used to adjust the pH. In the oral composition of the present invention, by adjusting the pH of the composition to 3.0 to 9.5, the persistence and adhesion of the cationic bactericide to the tooth surface are dramatically improved, and by extension, the adhesiveness to the tooth surface is dramatically improved. The bactericidal effect on oral bacteria can be dramatically increased.

[Oral sterilization method]
The present invention also relates to a method of suppressing bacteria in the oral cavity by applying the above-mentioned oral composition to a predetermined place in the oral cavity. Specifically, by applying the above oral composition to the tooth surface, tooth surface, oral mucosa, tongue, etc., or by applying the above oral composition by brushing, mouthwashing, washing, applying, etc. Bacteria adhering to the surface or the like can be suppressed, reduced, or removed. The amount of the oral composition applied is, for example, 0.01 to ² g, preferably 0.05 to 1.5 g, more preferably 0.1 to 1 g per 1 cm ^{2 of the} surface. ..
Hereinafter, specific examples of the oral composition of the present invention will be described, but it should be clearly stated that the examples are not intended to limit the scope of the present invention. In the following examples, the unit of the blending amount is mass% unless otherwise specified.

<Example>
Streptococcus mutans JCM5705 was pre-cultured in SCD medium (Wako Pure Chemical Industries, Ltd.) at 32.5 ° C. for 24 hours to obtain a pre-cultured bacterial solution. The resulting pre-culture solution, bacterial count was obtained by adding the SCD medium to the 10 ⁷ CFU / mL test bacterial liquid.
0.1 g of apatite beads was measured on a 24-well plate. 1 mL of each component of Examples and Comparative Examples shown in Tables 1A to 3C below was added, and the mixture was incubated at 37 ° C. for 1 hour. After incubation, the apatite beads were washed 7 times with 2 mL sterile water to remove non-adherent components. 2 mL of the test bacterial solution was inoculated and incubated at 37 ° C. for 30 minutes. 1 mL of bacterial solution after incubation is LP diluted solution (diluted solution of lectin and polysolvate 80 containing 1 g of casein peptone, 0.7 g of lecithin, 20 g of polysorbate and 8.3 g of purified water per 1 liter of purified water) (Daigo, sum) Serially diluted with 9 ml of Kojunyaku Kogyo Co., Ltd., smear 1 ml of the obtained diluted solution of the bacterial solution on SCDLP agar medium (Wako Pure Chemical Industries, Ltd.), and determine the viable cell count by the pour culture method. I asked. Here, in the pour culture method, the sample solution and the agar medium are mixed and coagulated in a petri dish, cultured at 32.5 ° C. under aerobic conditions, and the number of colonies generated after the culture is visually measured and multiplied. To determine the viable cell count. The details of each raw material used in Examples and Comparative Examples are as follows.
Hydrolyzed Collagen: Promois W-52P manufactured by Seiwa Kasei Co., Ltd.
Succinyl atelocollagen: Pig Atelocollagen SS 2% manufactured by Koken Co., Ltd.
Myristoylation succinyl atelocollagen: Made by Koken Co., Ltd. Pig atelocollagen MS 1%
L-Ascorbyl Magnesium Phosphate: VC-PMG manufactured by Nikko Chemicals Co., Ltd.
Cationic polymer: Marcourt 280 manufactured by Japan Lubrizol Co., Ltd.

Table 1A

Table 1B

Table 2A

Table 3A

Table 3B

Table 3C

As can be understood from the comparison between Examples 1 to 3 and Comparative Examples 1 to 6 and Examples 4 to 6 and Comparative Examples 1 to 5 and 7 described above, the (A) cationic bactericide of the present invention, (B). An oral composition comprising one or more selected from the group consisting of collagen, (C) citric acid, ascorbic acid phosphate and salts thereof is a cationic bactericidal agent on the tooth surface. It promoted the persistence and adsorptivity to collagen, and the bactericidal effect against oral bacteria was dramatically increased. As can be understood from the comparison between Comparative Examples 8 to 10 and the examples of the present invention, it was found that the product of the present invention is more effective than the existing technology. Further, as can be understood from the comparison between Examples 1 and 7 and Comparative Examples 11 to 12, the effect was dramatically increased when the pH of the composition was 6.5 to 8.0. As can be understood from Examples 8 to 11, the content of collagen in the oral composition of the present invention is preferably about 0.002 to 5% by mass.
As can be understood from Examples 12 to 14, the content of citric acid and a salt thereof in the oral composition of the present invention is preferably 0.01 to 2% by mass. As can be understood from Examples 15 to 17, the content of the ascorbic acid phosphate ester and its salt in the oral composition of the present invention is preferably 0.01 to 2% by mass. Examples 4 to 6 and 15 to 17 are reference examples of the present invention.

[Prescription example]
It is characterized by containing one or more selected from the group consisting of (A) cationic fungicide, (B) collagen, (C) citric acid, ascorbic acid phosphate ester and salts thereof. A formulation example of the composition of the present invention prepared by mixing the oral composition with other components is shown. The unit of the compounding amount is mass%.

[Prescription example 1]
<Toothpaste>
Cetylpyridinium chloride 0.05
Hydrolyzed collagen 0.5
Sodium citrate 0.4
Citric acid 0.02
Calcium hydrogen phosphate 40.0
Silicate anhydride 5.0
Glycerin 15.0
Sodium Carboxymethyl Cellulose 2.0
Sorbitol liquid 10.0
Glycerin fatty acid ester 3.0
Fragrance 1.0
Sodium lauryl sulfate 0.1
Paraoxybenzoic acid ester 0.2
Sodium fluoride 0.2
Purified water residue
100% in total

[Prescription example 2]
<Toothpaste>
Cetylpyridinium chloride 0.05
Succinyl atelocollagen 0.01
Sodium citrate 0.8
Citric acid 0.04
Aluminum hydroxide 35.0
Glycerin 15.0
Crystalline cellulose 10.0
Polyethylene glycol 10.0
Hydroxypropyl cellulose 2.0
Fragrance 1.0
Sodium lauryl sulfate 0.1
Butylparaben 0.2
Saccharin sodium 0.1
Dl-α-tocopherol acetate 0.1
Purified water residue
100% in total

[Prescription example 3]
<Toothpaste>
Cetylpyridinium chloride 0.05
Hydrolyzed collagen 0.1
L-Ascorbyl Magnesium Phosphate 2.0
Hinokitiol 0.02
Calcium carbonate 25.0
Sorbitol liquid 15.0
Glycerin 10.0
Silicate anhydride 5.0
Sodium Carboxymethyl Cellulose 2.0
Fragrance 1.0
Sodium lauryl sulfate 0.5
Saccharin sodium 0.05
Purified water residue
100% in total

[Prescription example 4]
<Toothpaste>
Cetylpyridinium chloride 0.05
Succinyl atelocollagen 0.002
L-Ascorbyl Magnesium Phosphate 1.0
Glycerin 25.0
Calcium pyrophosphate 25.0
Silicate anhydride 5.0
Sodium Carboxymethyl Cellulose 1.0
Fragrance 1.0
Sodium lauryl sulfate 0.5
Saccharin sodium 0.05
Purified water residue
100% in total

[Prescription example 5]
<Toothpaste>
Cetylpyridinium chloride 0.01
Hydrolyzed collagen 0.5
Sodium citrate 1.0
Citric acid 0.1
Isopropylmethylphenol 0.1
Silicate anhydride 20.0
70% sorbitol solution 20.0
Glycerin 20.0
Propylene glycol 3.0
Sodium lauryl sulfate 1.7
Polyethylene glycol 1.0
Carrageenan 1.0
Fragrance 1.0
Titanium dioxide 0.5
Methyl paraoxybenzoate 0.2
Purified water residue
100% in total

[Prescription example 6]
<Toothpaste>
Cetylpyridinium chloride 0.05
Succinyl atelocollagen 0.1
Sodium citrate 0.8
Citric acid 0.04
Aluminum hydroxide 30.0
Glycerin 20.0
Sodium chloride 10.0
Silicate anhydride 5.0
Polyoxyethylene hardened castor oil 3.0
Sodium lauryl sulfate 1.8
Sodium Carboxymethyl Cellulose 1.0
Polyethylene glycol 1.0
Fragrance 1.0
Paraoxybenzoic acid ester 0.2
Dl-α-tocopherol acetate 0.1
Purified water residue
100% in total

[Prescription example 7]
<Toothpaste>
Cetylpyridinium chloride 0.05
Hydrolyzed collagen 0.5
Succinyl atelocollagen 0.005
L-Ascorbyl Magnesium Phosphate 0.1
Isopropylmethylphenol 0.1
Calcium pyrophosphate 32.0
Glycerin 20.0
Silicate anhydride 6.0
Sodium Carboxymethyl Cellulose 1.0
Glycyrrhetinic acid 1.0
Polyethylene glycol 1.0
Fragrance 0.1
ε-Aminocaproic acid 0.1
Dl-α-tocopherol acetate 0.1
Purified water residue
100% in total

[Prescription Example 8]
<Toothpaste>
Cetylpyridinium chloride 0.01
Hydrolyzed collagen 0.5
Sodium citrate 0.4
Citric acid 0.02
L-Ascorbyl Magnesium Phosphate 2.0
Glycerin 20.0
Calcium Pyrophosphate 16.0
Silicate anhydride 7.0
Fragrance 1.0
Sodium Carboxymethyl Cellulose 0.8
Sodium lauryl sulfate 0.6
Carrageenan 0.6
Lysozyme chloride 0.4
Stevia extract 0.1
Chlorhexidine gluconate 0.05
Purified water residue
100% in total

[Prescription example 9]
<Oral moisturizer (gel type)>
Cetylpyridinium chloride 0.01
Hydrolyzed collagen 0.5
Sodium citrate 1.0
Citric acid 0.23
Sodium Carboxymethyl Cellulose 3.5
Glycerin 15.0
Propylene glycol 5.0
Sodium benzoate 0.3
Purified water residue
100% in total

[Prescription Example 10]
<Oral moisturizer (gel type)>
Cetylpyridinium chloride 0.01
Succinyl atelocollagen 0.1
Sodium citrate 0.3
Citric acid 0.2
Peppermint oil 0.1
Glycerin 25.0
Carrageenan 0.6
Sodium Carboxymethyl Cellulose 1.4
Sodium benzoate 0.3
Trimethylglycine 0.5
Polyoxyethylene hardened castor oil 0.5
Lactoferrin 0.01
Mucin 0.01
Hyaluronic acid 0.005
Purified water residue
100% in total

[Prescription Example 11]
<Oral moisturizer (gel type)>
Cetylpyridinium chloride 0.01
Hydrolyzed collagen 0.5
Citric acid 0.04
L-Ascorbyl Magnesium Phosphate 0.1
Hinokitiol 0.02
Glycerin 15.0
Carrageenan 0.8
Sodium alginate 1.8
Propylene glycol 10.0
Polyoxyethylene hardened castor oil 3.0
Sodium benzoate 0.5
Disodium hydrogen phosphate 0.1
Disodium edetate 0.2
Ethanol 2.0
Xylitol 5.0
Menthol 0.01
Fragrance 0.1
Hyaluronic acid 0.005
Dipotassium glycyrrhizinate 0.015
Purified water residue
100% in total

The following liquid dentifrices and mouthwash can also be used by being contained in a spray container and sprayed into the oral cavity.
[Prescription Example 12]
<Liquid dentifrice>
Cetylpyridinium chloride 0.05
Hydrolyzed collagen 0.5
Sodium citrate 0.4
Citric acid 0.02
Ethanol 2.0
Agar 1.5
Glycerin fatty acid ester 1.5
Fragrance 0.4
Paraoxybenzoic acid ester 0.1
Saccharin sodium 0.05
Purified water residue
100% in total

[Prescription Example 13]
<Liquid dentifrice>
Cetylpyridinium chloride 0.05
Succinyl atelocollagen 0.01
Sodium citrate 0.8
Citric acid 0.04
Aluminum hydroxide 10.0
Glycerin 10.0
Polyoxyethylene hardened castor oil 0.5
Carrageenan 0.5
Ethanol 0.5
Fragrance 0.4
Paraoxybenzoic acid ester 0.1
Saccharin sodium 0.05
Purified water residue
100% in total

[Prescription Example 14]
<Liquid dentifrice>
Cetylpyridinium chloride 0.05
Hydrolyzed collagen 0.1
L-Ascorbyl Magnesium Phosphate 2.0
Glycerin 15.0
Polyethylene glycol 10.0
Silicate anhydride 3.0
Calcium hydrogen phosphate 2.0
Sodium Carboxymethyl Cellulose 2.0
Polyoxyethylene cured castor oil 1.0
Aluminosilicate 0.5
Fragrance 0.5
Paraben 0.1
Purified water residue
100% in total

[Prescription Example 15]
<Liquid dentifrice>
Cetylpyridinium chloride 0.05
Myristoylation succinyl atelocollagen 0.002
L-Ascorbyl Magnesium Phosphate 1.0
Glycerin 10.0
Aluminum hydroxide 10.0
Agar 1.0
Ethanol 0.5
Polyoxyethylene hardened castor oil 0.5
Carrageenan 0.5
Fragrance 0.4
Paraoxybenzoic acid ester 0.1
Purified water residue
100% in total

[Prescription example 16]
<Liquid dentifrice>
Cetylpyridinium chloride 0.05
Hydrolyzed collagen 0.5
Succinyl atelocollagen 0.1
L-Ascorbyl Magnesium Phosphate 0.1
Glycerin 20.0
Sorbitol liquid 25.0
Xanthan gum 1.0
Sodium Carboxymethyl Cellulose 0.5
Fragrance 0.5
Polyoxyethylene hardened castor oil 0.5
Sodium lauryl sulfate 0.5
Paraoxybenzoic acid ester 0.1
Purified water residue
100% in total

[Prescription example 17]
<Liquid dentifrice>
Cetylpyridinium chloride 0.01
Hydrolyzed collagen 0.5
Sodium citrate 0.4
Citric acid 0.02
L-Ascorbyl Magnesium Phosphate 2.0
70% sorbitol solution 25.0
Silicate anhydride 10.0
Glycerin 10.0
Xanthan gum 1.0
Xylitol 1.0
Fragrance 0.5
Ethyl paraoxybenzoate 0.1
Butyl paraoxybenzoate 0.05
Purified water residue
100% in total

[Prescription Example 18]
<Liquid dentifrice>
Cetylpyridinium chloride 0.05
Succinyl atelocollagen 0.01
Sodium citrate 0.15
Citric acid 0.1
L-Ascorbyl Magnesium Phosphate 2.0
Peppermint oil 0.1
Polyoxyethylene hardened castor oil 5.0
Ethanol 5.0
Xylitol 5.0
Saccharin sodium 0.1
Disodium edetate 0.1
Paraoxybenzoic acid ester 0.1
Fragrance 0.1
Aluminum Chlorhydroxyl Allantoin 0.01
Purified water residue
100% in total

[Prescription Example 19]
<Liquid dentifrice>
Cetylpyridinium chloride 0.01
Hydrolyzed collagen 0.5
Citric acid 0.02
L-Ascorbyl Magnesium Phosphate 2.0
Ethanol 10.0
Polyethylene glycol 2.0
Polyoxyethylene hardened castor oil 2.0
Sodium benzoate 1.0
Fragrance 0.4
Aluminum Chlorhydroxyl Allantoin 0.2
Disodium edetate 0.2
Tea dry distillate 0.1
Stevia extract 0.05
Aluminum lactate 0.01
Purified water residue
100% in total

[Prescription Example 20]
<Liquid dentifrice>
Cetylpyridinium chloride 0.05
Hydrolyzed collagen 0.5
Sodium citrate 0.4
L-Ascorbyl Magnesium Phosphate 2.0
Isopropylmethylphenol 0.1
Hydrous silicic acid 1.0
Silicate anhydride 10.0
Glycerin 25.0
Fragrance 1.0
Carboxymethyl cellulose 1.0
Sorbitol 50.0
Polyoxyethylene hardened castor oil 0.5
Paraoxybenzoic acid ester 0.1
Sodium lauryl sulfate 1.0
Purified water residue
100% in total

[Prescription example 21]
<Mouthwash>
Cetylpyridinium chloride 0.01
Hydrolyzed collagen 0.5
Sodium citrate 0.4
Citric acid 0.02
Peppermint oil 0.2
Ethanol 20.0
Fragrance 1.0
Saccharin sodium 0.05
Chlorhexidine hydrochloride 0.01
Lauryl ethanol amide 0.3
Purified water residue
100% in total

[Prescription example 22]
<Mouthwash>
Cetylpyridinium chloride 0.01
Hydrolyzed collagen 0.5
Sodium citrate 0.12
Citric acid 0.03
L-Ascorbyl Magnesium Phosphate 2.0
Peppermint oil 0.2
Xylitol 2.5
Denatured alcohol No. 56 5.0
Glycerin 5.0
Polyoxyethylene hardened castor oil 0.5
Dipotassium glycyrrhizinate 0.1
Ethyl paraoxybenzoate 0.05
Propyl paraoxybenzoate 0.05
Fragrance 0.1
Purified water residue
100% in total

When the apatite beads were immersed in the compositions of Formulation Examples 1 to 22 described above, the non-adherent components were washed, and then Streptococcus mutans was added, sterilization was successfully performed. The viable cell count was about <10 to 1.0 × 10 ⁴ CFU / ml. It was found that all of the compositions of Formulation Examples 1 to 22 described above suppressed the biofilm viable cell count by 50% or more.

Claims (7)

It contains (A) a cationic bactericide which is cetylpyridinium chloride, (B) collagen which is one or more selected from the group consisting of (B) succinyl atelocollagen and myristyl succinyl atelocollagen , and (C) citric acid or a salt thereof. An oral composition comprising no ascorbic acid phosphate ester or a salt thereof, and having a pH of 3.0 to 9.5. The oral composition according to claim 1, wherein the pH of the oral composition is 3.0 to 9.0. The oral composition according to claim 1 or 2 , wherein the content of the cationic bactericidal agent (A) is 0.0001 to 10% by mass with respect to the mass of the oral composition. (B) The oral composition according to any one of claims 1 to 3 , wherein the content of collagen is 0.0002 to 40% by mass with respect to the mass of the oral composition. The oral cavity according to any one of claims 1 to 4 , wherein the component (C) is citric acid, and the content of the citric acid is 0.001 to 20% by mass with respect to the mass of the oral composition. Composition for. The oral composition according to any one of claims 1 to 5 , wherein the pH of the oral composition is 6.3 to 9.0. The oral composition according to any one of claims 1 to 6 , which is used for sterilizing the tooth surface.