JP7511331B2 - Oral Composition - Google Patents

Description

The present invention relates to an oral composition.

Oral compositions such as dentifrices and gels containing active ingredients such as anti-inflammatory agents and bactericides for use in the prevention and treatment of periodontal diseases such as periodontitis (pyorrhea) and gingivitis are known. Patent Document 1 discloses a toothpaste composition containing a water-soluble pyridinium compound, a quaternary ammonium compound or a biguanide bactericide, a cationized hydroxyethylcellulose having a specific molecular weight and degree of cationization, a specific surfactant, and a specific amount of a non-silica abrasive.

Japanese Patent Application Laid-Open No. 6-239725

In the circumstances described above, the present invention aims to provide an oral composition that has excellent adhesion to the gums or oral mucosa.

As a result of intensive research, the inventors discovered that an oral composition that has high adhesion to the gum surface can be prepared by containing (A) fatty acid dextrin, (B) a polymeric compound and/or an abrasive, and (C) water, and thus arrived at the present invention.

That is, the present invention provides the following oral compositions.
Item 1.
An oral composition comprising (A) a fatty acid dextrin, (B) a polymeric compound and/or an abrasive, and (C) water.
Item 2.
Item 2. The oral composition according to Item 1, wherein the polymer compound and/or the abrasive (B) is a linear polymer compound.
Item 3.
Item 3. The oral composition according to item 1 or 2, wherein the polymer compound and/or abrasive (B) is at least one selected from the group consisting of carboxyvinyl polymers, alginic acid or a salt thereof, pullulan, and cellulose-based polymers.
Item 4.
Item 4. The oral composition according to any one of Items 1 to 3, wherein the total content of the (B) component is 0.01 to 500 parts by mass per part by mass of the total content of the (A) component.
Item 5.
Item 5. The oral composition according to any one of items 1 to 4, further comprising 30% by mass or more of water (C).
Item 6.
Item 6. The oral composition according to any one of Items 1 to 5, wherein the fatty acid dextrin (A) is dextrin palmitate.
Item 7.
The oral composition according to any one of Items 1 to 6, further comprising at least one selected from the group consisting of a bactericide, a tissue repair agent, an anti-inflammatory agent, and a blood circulation promoter.
Item 8.
Item 8. The oral composition according to any one of Items 1 to 7, further comprising a higher alcohol.
Item 9.
Item 9. The oral composition according to any one of items 1 to 8, further comprising a surfactant.
Item 10.
Item 10. The oral composition according to any one of items 1 to 9, further comprising a hydrocarbon.
Item 11.
Item 11. The oral composition according to any one of Items 1 to 10, which is a dentifrice, a liniment, or a mouthwash.

The present invention further provides the following method.
Item 12.
A method for enhancing adhesion of an oral composition to gums, comprising the steps of incorporating (A) a fatty acid dextrin, (B) a polymeric compound and/or an abrasive, and (C) water.

The oral composition of the present invention has enhanced adhesion to oral tissues such as the gums and oral mucosa. As a result, water-soluble and oil-soluble medicinal ingredients can be adhered to oral tissues together with the base, and the medicinal effects of the agent in the oral cavity can be enhanced.

[Oral composition]
The oral composition of the present invention is an oral composition containing (A) a fatty acid dextrin, (B) a polymeric compound and/or an abrasive, and (C) water.

[(A) Fatty acid dextrin]
The fatty acid dextrin refers to an ester compound of dextrin and a fatty acid.

The fatty acid constituting the fatty acid dextrin preferably has 6 to 24 carbon atoms, and examples thereof include palmitic acid, stearic acid, arachic acid, octanoic acid, capric acid, lauric acid, myristic acid, and behenic acid. Among these, palmitic acid is preferred as the fatty acid constituting the fatty acid dextrin, from the viewpoint of more prominently exhibiting the effects of the present invention.

The fatty acid dextrin contained in the oral composition of the present invention may be composed of one or more fatty acids.

The fatty acid dextrin is not particularly limited as long as it is one that is generally used in the fields of pharmaceuticals, quasi-drugs, or cosmetics. For example, commercially available products can be used, such as those under the trade names "Leopearl KL (display name: palmitic acid dextrin)" (manufactured by Chiba Flour Mills Co., Ltd.), "Leopearl KL2 (display name: palmitic acid dextrin)" (manufactured by Chiba Flour Mills Co., Ltd.), "Leopearl TL (display name: palmitic acid dextrin)" (manufactured by Chiba Flour Mills Co., Ltd.), "Leopearl TL2 (display name: palmitic acid dextrin)" (manufactured by Chiba Flour Mills Co., Ltd.), "Leopearl TT (display name: (palmitic acid/octanoic acid) dextrin)" (manufactured by Chiba Flour Mills Co., Ltd.), and "Leopearl TT2 (display name: (palmitic acid/octanoic acid) dextrin" (manufactured by Chiba Flour Mills Co., Ltd.).

The content of component (A) is not particularly limited, but from the viewpoint of improving adhesion to oral tissues, it is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, even more preferably 0.1% by mass or more, and particularly preferably 0.25% by mass or more, based on the total amount of the oral composition.

From the viewpoint of improving usability, the content of component (A) is preferably 2% by mass or less, more preferably 1% by mass or less, and particularly preferably 0.75% by mass or less, based on the total amount of the oral composition.

The content of component (A) is preferably 0.05 to 2 mass%, more preferably 0.1 to 1 mass%, and even more preferably 0.25 to 0.75 mass%, based on the total amount of the oral composition.

[(B) Polymer compound or abrasive]
The polymer compound contained in the oral cavity composition of the present invention may be a naturally occurring substance or a substance obtained by chemical synthesis.

Examples of polymeric compounds include linear polymeric compounds such as carboxyvinyl polymer, sodium polyacrylate, polyvinyl alcohol, polyvinylpyrrolidone, acrylic acid/alkyl methacrylate copolymer, polyethylene glycol, macrogol, (hydroxyethyl acrylate/sodium acryloyldimethyltaurate) copolymer, (ammonium acryloyldimethyltaurate/vinylpyrrolidone) copolymer, polypeptides (gelatin, etc.), and linear polysaccharides (alginic acid or its salt, pullulan, cellulose polymer, pectin, carrageenan, gellan gum, agar, propylene glycol alginate, sodium chondroitin sulfate, hyaluronic acid, sodium hyaluronate, etc.); and branched polymeric compounds such as guar gum, locust bean gum, xanthan gum, gum arabic, karaya gum, thickening anhydrous silicic acid, and bentonite.

The abrasives contained in the oral composition of the present invention are not limited to, but include calcium phosphate-based abrasives such as calcium hydrogen phosphate (calcium phosphate dihydrate or anhydrate, calcium pyrophosphate, calcium triphosphate, hydroxyapatite, and calcium tetraphosphate; silica-based abrasives such as silicic acid anhydride, crystalline silica, amorphous silica, silica gel, precipitated silica, aluminosilicate, and zirconosilicate; zeolite; calcium carbonate-based abrasives; insoluble potassium metaphosphate; aluminum oxide; aluminum hydroxide; alumina; magnesium carbonate; magnesium triphosphate; zinc oxide; and synthetic resin-based abrasives. Among these, calcium phosphate-based abrasives or silica-based abrasives are more preferred, calcium phosphate-based abrasives are even more preferred, and calcium hydrogen phosphate dihydrate or anhydrate is particularly preferred.

These (B) components are not particularly limited as long as they are generally used in the fields of pharmaceuticals, quasi-drugs, or cosmetics, and for example, commercially available products can also be used.

All of these (B) components may be used alone or in any combination of two or more. Although not limited, from the viewpoint of significantly achieving the effects of the present invention and reducing friction with oral tissues, the (B) component is preferably a polymer compound, more preferably a linear polymer, and even more preferably a component selected from the group consisting of carboxyvinyl polymer, alginic acid or a salt thereof, pullulan, and a cellulose-based polymer. In addition, two or more types of (B) components can be combined. When two or more types of (B) components are combined, there is no limitation and the combination is appropriately set depending on the type and content of other blended components, the formulation form, the method of use, etc., but it is preferable to combine two or more types selected from the group consisting of carboxyvinyl polymer, alginic acid or a salt thereof, pullulan, and a cellulose-based polymer.

Carboxyvinyl polymers are vinyl polymers mainly composed of acrylic acid, methacrylic acid, etc., which have carboxyl groups. There are no particular restrictions on their monomer composition or molecular weight, and various commercially available carboxyvinyl polymers can be used without particular restrictions. Examples of these commercially available products include Carbopol 940, Carbopol 941, Carbopol 980, Carbopol 981, Carbopol Ultrez10, and Carbopol ETD2050 sold by Lubrizol Advanced Materials, Hiviswako 103, Hiviswako 104, and Hiviswako 105 sold by Wako Pure Chemical Industries, Sinthalen K and Sinthalen L sold by 3V Sigma, and AQUPEC HV-501, AQUPEC HV-504, and AQUPEC HV-505 sold by Sumitomo Seika Chemicals. HV-505), AQUPEC HV-501E, AQUPEC HV-504E, AQUPEC HV-505E, AQUPEC HV-501ER, AQUPEC HV-505ED, etc.

Alginic acid is a linear polysaccharide composed of two types of uronic acid, namely, D-mannuronic acid (M) and L-guluronic acid (G). Commercially available alginic acid can be used. Examples of alginic acid salts in the present invention include, but are not limited to, sodium salts and potassium salts. Sodium alginate is preferred. Alginic acid or its salts may be used alone or in combination of two or more types. It is more preferred to use alginic acid or its salts in combination with a calcium salt from the viewpoint of suitably adjusting the physical properties of the oral composition of the present invention.

Pullulan is a water-soluble polysaccharide in which maltotriose, which is made up of three glucose molecules each bonded with α-1,4 bonds, is regularly linked with α-1,6 bonds. Commercially available products that can be used include those sold as a food additive by Hayashibara Co., Ltd.

A cellulose-based polymer compound is a cellulose-based polymer compound obtained by replacing the hydroxyl group of cellulose with another functional group. Examples of functional groups that replace the hydroxyl group of cellulose include methoxy, ethoxy, hydroxymethoxy, hydroxyethoxy, hydroxypropoxy, carboxymethoxy, and carboxyethoxy groups. Specific examples of cellulose-based polymer compounds include methyl cellulose, ethyl cellulose, hydroxyethyl methyl cellulose, hydroxyethyl cellulose (HEC), hydroxypropyl cellulose (HPC), hydroxypropyl methyl cellulose (HPMC), carboxymethyl cellulose (CMC) and salts thereof (e.g., carmellose sodium, carmellose calcium, and carmellose ammonium), stearoxy hydroxypropyl methyl cellulose, crystalline cellulose, and O-[2-hydroxy-3-(trimethylammonio)propyl]hydroxyethyl cellulose chloride. These cellulose-based polymers can be used alone or in combination of two or more types. In addition, commercially available cellulose-based polymer compounds can be used, and these compounds can be used alone or in combination of two or more types.

The total content of component (B) is not particularly limited and is set appropriately depending on the type and content of other blended ingredients, the formulation form, the method of use, etc., but from the viewpoint of significantly achieving the effects of the present invention, it is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, even more preferably 0.1% by mass or more, still more preferably 0.25% by mass or more, and particularly preferably 0.5% by mass or more, based on the total amount of the oral composition.

From the viewpoint of achieving a significant effect of the present invention, the total content of component (B) is preferably 50% by mass or less, more preferably 30% by mass or less, even more preferably 20% by mass or less, and particularly preferably 15% by mass or less, based on the total amount of the oral composition.

The total content of component (B) is preferably 0.01 to 50% by mass, more preferably 0.05 to 30% by mass, even more preferably 0.1 to 20% by mass, even more preferably 0.25 to 20% by weight, and particularly preferably 0.5 to 15% by mass, based on the total amount of the oral composition.

When component (B) is a polymeric compound, the total content of the polymeric compound is not particularly limited and is set appropriately depending on the type and content of other blended ingredients, the formulation form, the method of use, etc., but from the viewpoint of significantly achieving the effects of the present invention, it is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, even more preferably 0.5% by mass or more, and particularly preferably 1% by mass or more, based on the total amount of the oral composition.

When component (B) is a polymeric compound, the total content of the polymeric compound is preferably 7.5% by weight or less, more preferably 5% by weight or less, even more preferably 3% by weight or less, particularly preferably 2% by weight or less, and most preferably 1.5% by weight or less, based on the total amount of the oral composition, from the viewpoint of achieving a significant effect of the present invention.

When component (B) is a polymeric compound, the total content of the polymeric compound is preferably 0.05 to 7.5% by mass, more preferably 0.1 to 5% by mass, even more preferably 0.5 to 3% by mass, and particularly preferably 1 to 2% by mass, based on the total amount of the oral composition.

In a preferred embodiment, for example, when a carboxyvinyl polymer is contained as component (B), the content of the carboxyvinyl polymer alone is preferably 0.05 to 7.5% by mass, more preferably 0.1 to 5% by mass, even more preferably 0.5 to 2% by mass, and particularly preferably 1 to 1.5% by mass, based on the total amount of the oral composition, although this is not limited thereto.

In a preferred embodiment, for example, when alginic acid or a salt thereof is contained as component (B), the content of alginic acid or a salt thereof alone is preferably 0.01 to 10% by mass, more preferably 0.05 to 5% by mass, even more preferably 0.1 to 2% by mass, and particularly preferably 0.3 to 1% by mass, based on the total amount of the oral composition, although this is not limited thereto.

When component (B) is an abrasive, the total content of component (B) is not particularly limited and is set appropriately depending on the type and content of other blended components, the formulation form, the method of use, etc., but from the viewpoint of more significantly achieving the effects of the present invention, it is preferably 0.5% by mass or more, more preferably 1% by mass or more, and even more preferably 5% by mass or more, based on the total amount of the oral composition.

When component (B) is an abrasive, the total content of component (B) is preferably 50% by mass or less, more preferably 20% by mass or less, and even more preferably 15% by mass or less, based on the total amount of the oral composition, in order to more significantly exhibit the effects of the present invention.

When component (B) is an abrasive, the total content of the abrasive is preferably 0.5 to 50% by mass, more preferably 1 to 20% by mass, and even more preferably 5 to 15% by mass, based on the total amount of the oral composition.

[Ratio of each component]
The total content of the (B) component per 1 part by mass of the total content of the (A) component in the oral composition of the present invention ((B)/(A)) is not particularly limited, but from the viewpoint of significantly exhibiting the effects of the present invention, it is preferably 0.01 to 500 parts by mass, more preferably 0.05 to 200 parts by mass, even more preferably 0.1 to 100 parts by mass, and particularly preferably 0.5 to 50 parts by mass.

When the (B) component of the present invention is a polymer compound, the total content of the (B) component per 1 part by mass of the total content of the (A) component in the oral composition of the present invention ((B)/(A)) is not particularly limited, but from the viewpoint of significantly exhibiting the effects of the present invention, it is preferably 0.1 to 50 parts by mass, more preferably 0.5 to 20 parts by mass, even more preferably 1 to 10 parts by mass, and particularly preferably 1.3 to 6 parts by mass.

When the component (B) of the present invention is an abrasive, the total content of the component (B) per 1 part by mass of the total content of the component (A) in the oral composition of the present invention ((B)/(A)) is not particularly limited, but from the viewpoint of significantly exhibiting the effects of the present invention, it is preferably 0.1 to 500 parts by mass, more preferably 0.5 to 200 parts by mass, even more preferably 1 to 100 parts by mass, and particularly preferably 5 to 50 parts by mass.

[(C) Water]
The oral composition of the present invention contains water. From the viewpoint of improving the feeling of use, the content of water is preferably 30% by mass or more, more preferably 40% by mass or more, even more preferably 50% by mass or more, and is preferably 80% by mass or less, more preferably 75% by mass or less, even more preferably 70% by mass or less, based on the total amount of the oral composition.

[Medicinal ingredients]
The oral composition of the present invention may contain, as an active ingredient, within a range that does not impair the effects of the present invention, for example, a bactericide (cationic bactericide (cetylpyridinium chloride, benzethonium chloride, chlorhexidine gluconate, chlorhexidine hydrochloride, etc.), amphoteric bactericide (dodecylaminoethylglycine, etc.), nonionic bactericide (isopropylmethylphenol, hinokitiol, triclosan, thymol, 1,8-cineole, etc.), anionic bactericide (sodium lauroyl sarcosine (LSS) etc.)), tissue repair agent (allantoin; β-glycyrrhetinic acid, allantoin dihydroxyaluminum (Aldioxa), allantoin chlorhydroxyaluminum (Alcloxa), allantoin polygalacturonic acid, allantoin ascorbic acid, allantoin acetyl-DL-methionine, allantoin DL-pantothenyl alcohol, salts of allantoin such as sodium DL-pyrrolidone carboxylate, allantoin; panthenol, etc.), anti-inflammatory agents (allantoin or its salts, tranexamic acid, glycyrrhizinic acid or its salts (dipotassium glycyrrhizinate, glycyrrhizinate dipotassium, glycyrrhizinate dibasic acid ... Monoammonium ricyrrhizinate, etc.), β-glycyrrhetinic acid or its derivatives (stearyl glycyrrhetinate, etc.), methyl salicylate, l-menthol, tranexamic acid, ε-aminocaproic acid, Phellodendron bark extract, etc.), bleeding suppressants (carbazochrome, tranexamic acid, ε-aminocaproic acid, etc.), dentin hypersensitivity suppressants (potassium nitrate, strontium chloride, aluminum lactate, etc.), blood circulation promoters (vitamin E (α-tocopherol, β-tocopherol, γ-tocopherol, δ-tocopherol; dl-α-tocopherol acetate, Tocopherol acetate (such as tocopherol acetate, tocopherol nicotinate, tocopherol succinate, etc.), astringents (such as sodium chloride), remineralizing agents (sodium fluoride, sodium monofluorophosphate (MFP), stannous fluoride, etc.), enzymes (lactoferrin, lactoperoxidase, dextranase, lysozyme, protease, amylase, mutanase, etc.), sodium copper chlorophyllin, magnesium L-ascorbyl phosphate, zinc chloride, sodium polyphosphate, sodium pyrophosphate, etc. may be used in combination. These medicinal ingredients may be used alone or in combination of two or more.

The oral composition of the present invention may contain plant-derived medicinal ingredients such as Asarum extract, Phellodendron bark extract, Angelica acutiloba extract, Scutellaria root extract, Chamomile extract, Ratania extract, Myrrh extract, Manuka honey extract, polyphenols, catechins, flavones, and proanthocyanins, either alone or in combination of two or more, within the scope of the invention's effects.

The oral composition of the present invention may contain other medicinal ingredients, such as zinc citrate, sanguinarine, delmopinol, nisin, chitosan, and chlorophyll, either alone or in combination of two or more, as long as the effects of the present invention are not impaired.

From the viewpoint of achieving the effects of the present invention more significantly, the oral composition of the present invention preferably contains, as an active ingredient, at least one selected from the group consisting of bactericides, tissue repair agents, anti-inflammatory agents, and blood circulation promoters, and preferably contains at least one selected from the group consisting of cationic bactericides, allantoin, glycyrrhizinic acid or a salt thereof, β-glycyrrhetinic acid or a derivative thereof, and vitamin E, and more preferably contains at least one selected from the group consisting of cetylpyridinium chloride, allantoin, dipotassium glycyrrhizinate, β-glycyrrhetinic acid, and tocopherol acetate.

The medicinal ingredients used in the oral composition of the present invention, whether water-soluble or water-insoluble, do not inhibit the effects of the present invention, and the effect of the present invention is expected to be enhanced adhesion to the gums. Among these, water-soluble medicinal ingredients are more preferable.

[Surfactant]
The oral cavity composition of the present invention may further contain a surfactant. By containing a surfactant, the effects of the present invention are more significantly exhibited.

As the surfactant, a nonionic surfactant, an amphoteric surfactant, an anionic surfactant, a cationic surfactant, etc. can be used. Among them, from the viewpoint of achieving the effects of the present invention more significantly, it is preferable to include at least one selected from the group consisting of a nonionic surfactant and an amphoteric surfactant.

Examples of nonionic surfactants include sorbitan fatty acid esters such as sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, diglycerol sorbitan penta-2-ethylhexyl acid, and diglycerol sorbitan tetra-2-ethylhexyl acid; polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene (20) sorbitan monolaurate (polysorbate 20), polyoxyethylene (20) sorbitan monostearate (polysorbate 60), polyoxyethylene (20) sorbitan monooleate (polysorbate 80), and polyoxyethylene (20) sorbitan isostearate; polyethylene glycol fatty acid esters such as polyethylene glycol monooleate and polyethylene glycol monolaurate; propylene glycol fatty acid esters such as propylene glycol monostearate; polyoxyethylene sorbitan fatty acid esters such as polyethylene glycol monooleate and polyethylene glycol monolaurate; Hydrogenated castor oil derivatives such as ethylene hydrogenated castor oil 40 (HCO-40), polyoxyethylene hydrogenated castor oil 50 (HCO-50), polyoxyethylene hydrogenated castor oil 60 (HCO-60), and polyoxyethylene hydrogenated castor oil 80; fatty acid alkanolamides such as lauric acid diethanolamide; glycerin alkyl ethers; alkyl glucosides such as lauryl glucoside and decyl glucoside; polyoxyethylene (20) oleyl ether, polyoxyethylene cetyl ether, and other polyoxyalkylene alkyl ethers; polyglycerin fatty acid esters, polyoxyethylene glycerin fatty acid esters, polyoxyalkylene fatty acid esters, glycerin fatty acid esters such as glyceryl monostearate, sugar fatty acid esters such as sucrose fatty acid esters and maltose fatty acid esters; sugar alcohol fatty acid esters such as maltitol fatty acid esters; and polyoxyethylene lauryl alcohol ether.

Examples of amphoteric surfactants include imidazolinium betaines such as 2-alkyl-N-carboxymethyl-N-hydroxyethyl-N-imidazolinium betaine; alkyl sulfobetaines such as lauryl sulfobetaine and lauryl hydroxysulfobetaine; acetate betaines such as lauryl dimethylaminoacetate betaine; coconut oil fatty acid amidoalkyl betaines such as coconut oil fatty acid amidopropyl betaine; and long-chain alkyl imidazoline betaine salts such as sodium N-alkyl-1-hydroxyethyl imidazoline betaine.

Examples of anionic surfactants include alkyl sulfates (sodium lauryl sulfate, etc.), fatty acid monocarboxylates (laurates, palmitates, etc.), polyoxyethylene alkyl ether carboxylates, N-acylsarcosine salts, N-acylamino acid salts (N-acylglutamates, etc.), dialkyl sulfosuccinates, alkanesulfonates (alkyl sulfonates), α-olefin sulfonates, linear alkylbenzene sulfonates, alkyl (branched) benzene sulfonates, N-methyl-N-acyltaurates, polyoxyethylene alkyl ether sulfates, alkyl phosphates, polyoxyethylene alkyl ether phosphates, polyoxyethylene alkyl phenyl ether phosphates, etc.

Examples of cationic surfactants include monoalkylamine salts, dialkylamine salts, trialkylamine salts, alkyltrimethylammonium, dialkyldimethylammonium salts, and alkylbenzalkonium chloride.

Other surfactants include, for example, silicone-based surfactants such as polyoxyethylene-methylpolysiloxane copolymer, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, and PEG-9 polydimethylsiloxyethyl dimethicone.

As the surfactant, from the viewpoint of more significantly exhibiting the effects of the present invention, nonionic surfactants and anionic surfactants are preferred, nonionic surfactants are more preferred, and sorbitan fatty acid esters and polyoxyethylene sorbitan fatty acid esters are even more preferred.
The total content of the surfactant is not particularly limited and is set appropriately depending on the type of surfactant, the type and content of other blended ingredients, formulation form, method of use, etc.; however, from the viewpoint of more prominently exhibiting the effects of the present invention and sufficiently exhibiting cleaning power, it is preferably 0.1 to 20 mass%, more preferably 0.5 to 10 mass%, even more preferably 1 to 7.5 mass%, and particularly preferably 2 to 5 mass%, relative to the total amount of the oral composition.
When the surfactant is a nonionic surfactant, the total content of the nonionic surfactant is preferably 0.1 to 20 mass%, more preferably 0.5 to 10 mass%, even more preferably 1 to 7.5 mass%, and particularly preferably 2 to 5 mass%, relative to the total amount of the oral composition.

[hydrocarbon]
The oral cavity composition of the present invention may further contain a hydrocarbon. By containing a hydrocarbon, the effects of the present invention are more significantly exhibited.

As the hydrocarbon, a paraffinic hydrocarbon or an olefinic hydrocarbon is used, and examples thereof include liquid paraffin, petrolatum, squalane, squalene, ceresin, light liquid paraffin, paraffin wax, beeswax, carnauba wax, pristane, and microcrystalline wax. From the viewpoint of further enhancing the effects of the present invention, liquid paraffin or petrolatum is more preferable, and liquid paraffin is even more preferable.

The total content of hydrocarbons is not particularly limited and is set appropriately depending on the type of hydrocarbon, the type and content of other blended ingredients, the formulation form, the method of use, etc., but from the viewpoint of achieving a significant effect of the present invention and further improving the feeling of use, it is preferably 0.5 to 30 mass%, more preferably 1 to 25 mass%, even more preferably 3 to 20 mass%, and particularly preferably 5.1 to 15 mass% of the total amount of the oral composition.

[Other additives]
The oral cavity composition of the present invention may contain additives such as known higher alcohols, solubilizing agents, humectants, preservatives, chelating agents, pH adjusters, sweeteners, flavorings, and colorants that can be used in medicines, quasi-drugs, cosmetics, foods, etc., within the scope of not impairing the effects of the present invention. Any of these additives may be used alone or in combination of two or more.

The oral composition of the present invention may use a higher alcohol. The higher alcohol refers to an alcohol having 6 or more carbon atoms, and may have either a linear or branched structure. The higher alcohol is preferably, but not limited to, a _C8 to _C24 aliphatic alcohol. Such alcohols include cetanol (cetyl alcohol), stearyl alcohol, cetostearyl alcohol, lauryl alcohol, myristyl alcohol, oleyl alcohol, capryl alcohol, linolyl alcohol, or behenyl alcohol. From the viewpoint of further enhancing the effect of the oral composition of the present invention, preferably, one or more selected from cetanol, stearyl alcohol, and cetostearyl alcohol are used, more preferably, one or more selected from cetanol or stearyl alcohol, and even more preferably, cetanol is used.

Examples of humectants include sugar alcohols such as xylitol, erythritol, maltitol, sorbitol, lactitol, trehalose, and mannitol; and polyhydric alcohols such as ethylene glycol, propylene glycol, butylene glycol, polyethylene glycol, polypropylene glycol, and glycerin.

Suitable examples of solubilizing agents include lower alcohols such as ethanol and propanol.

Examples of preservatives include parabens (methylparaben, ethylparaben, propylparaben, butylparaben, etc.), benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl parahydroxybenzoate, isopropyl parahydroxybenzoate, butyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, benzyl parahydroxybenzoate, methyl parahydroxybenzoate, phenoxyethanol, alkyldiaminoethylglycine hydrochloride, benzalkonium chloride, and benzethonium chloride.

Examples of chelating agents include EDTA disodium salt and EDTA calcium disodium salt.

Examples of pH adjusters include inorganic acids (hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid, etc.), organic acids (lactic acid, citric acid, succinic acid, gluconic acid, maleic acid, adipic acid, succinic acid, etc.), inorganic bases (potassium hydroxide, sodium hydroxide, etc.), organic bases (triethanolamine, diisopropanolamine, triisopropanolamine, etc.), salts (sodium lactate, sodium succinate, sodium citrate, sodium hydrogen citrate, sodium acetate, sodium phosphate, sodium dihydrogen phosphate, sodium carbonate, sodium sesquicarbonate (trisodium dicarbonate), etc.), and basic amino acids (lysine, arginine, etc.).

Sweeteners include, for example, sugars or sugar alcohols (xylitol, palatinose, erythritol, maltitol, arabitol), stevioside, stevia extract, thaumatin, glycyrrhizin, sucralose, acesulfame potassium, saccharin sodium, aspartame, neohesperidyl dihydrochalcone, and perillartine.

[pH]
The pH of the oral composition of the present invention is appropriately set depending on the types of components (A) and (B), the types and contents of other blended components, the formulation, the method of use, etc., and is not limited as long as it is within a physiologically or pharma- ceutically acceptable range. From the viewpoint of improving the feel when used, however, the pH is preferably 3.5 to 9, more preferably 4 to 8, and even more preferably 4.5 to 7.

[Application]
The oral composition of the present invention comes into contact with and adheres to oral tissues such as periodontal tissues, and remains there, thereby allowing the pharmacological components to act sustainably on the oral tissues. Therefore, the composition can be used to improve or prevent periodontal diseases such as gingivitis and alveolar pyorrhea, improve or prevent dental diseases such as caries and hypersensitivity, improve the condition of oral tissues, and the like, but is preferably used for improving or preventing periodontal diseases.

The oral composition of the present invention may be in an embodiment that does not contain an abrasive. In that case, it is expected to have the effect of reducing friction between oral tissues. More specifically, by applying the composition of this embodiment to a toothbrush or the like, it is possible to reduce friction between the gums and the toothbrush when brushing the gums, and therefore it is possible to brush oral tissues such as the gums without damaging them, which is preferable for the above-mentioned uses.

Periodontal disease can be broadly divided into two types, gingivitis (gingivitis) and periodontitis (periodontitis), depending on the progression of the disease. The oral composition of the present invention can be used to improve or prevent either of these.

In this specification, "adheres closely to tissues in the oral cavity" refers to adhering and remaining on the tissues in the oral cavity. Therefore, "adheres closely" or "adherence" can be interpreted as "retention" or "retention", or "adhesion" or "adherence".

As used herein, "prevention" refers to preventing or delaying the onset of a disease or condition, or reducing the risk of onset of a disease or condition.

In addition, in this specification, "improvement" refers to the improvement or alleviation of a disease, symptom, or health condition, the prevention or delay of the deterioration of a disease, symptom, or health condition, or the reversal, prevention, or delay of the progression of a disease or symptom.

[Dosage form]
The properties of the oral composition of the present invention are not particularly limited as long as they are known as pharmaceuticals, quasi-drugs, and cosmetics, and can be liquid, fluid, or semi-solid. The formulation can be, for example, a paste, cream, liquid, emulsion, ointment, gel, suspension, emulsion, lotion, or other formulation. Among them, paste, cream, liquid, emulsion, or ointment are more preferable, paste or cream are even more preferable, and cream is particularly preferable. In addition, when the paste, cream, liquid, emulsion, ointment, etc. contain an oily base and an aqueous base, they may be O/W type or W/O type. However, from the viewpoint of more prominently exhibiting the effects of the present invention, an O/W type emulsion is preferable.

The form of the oral composition of the present invention is not particularly limited as long as it is a known form as a medicine, quasi-drug, cosmetic, or food, but it can be used, for example, as a dentifrice, a liniment, a mouthwash, a beauty serum to be applied to the gums, a mouthwash, etc. Among these, from the viewpoint of evenly distributing the composition to the tissues in the oral cavity and allowing the medicinal and nutritional components to continuously come into contact with and penetrate the tissues, a dentifrice, a liniment, or a mouthwash is preferred, and a dentifrice is even more preferred.

[Production method]
The oral composition of the present invention can be produced by a known method, which may include a sterilization step, if necessary.

[Method for enhancing adhesion to gums]
The method of the present invention for enhancing adhesion to the gums is as follows.
A method for enhancing adhesion of an oral composition to gums, comprising the steps of incorporating (A) a fatty acid dextrin, (B) a polymeric compound and/or an abrasive, and (C) water.

In this method, the types and contents of the components (A), (B) and (C), the types and contents of other components, the formulation form and use of the oral composition, etc. are as explained in [Oral composition].

Next, the present invention will be specifically explained using examples and test examples, but the present invention is not limited to the following examples and test examples.

[Test Example 1. Adhesion test]
Dentifrices having the compositions shown in Table 1 below were prepared in a conventional manner, and the adhesive strength of these was evaluated.
The dentifrices shown in Table 1 (Comparative Examples 1-1, 1-2, Examples 1-1, 1-2) were prepared.
Next, 200 mL of purified water and a 3 cm diameter cross-shaped stirring bar were placed in a 200 mL beaker, and 0.2 g of the formulation was applied to the center of a slide glass (long side 7.6 cm, width 2.6 cm) to a thickness of about 1.4 mm, and the slide glass was placed upright in the beaker with the formulation-coated surface facing downward and immersed. At this time, the coating part was placed about 1.5 cm above the stirring bar.
The knob of a stirrer (KPI, MIGHTY STIRRER, HE-16GX6) was set to 5, and the time (adhesion time) (seconds) until the entire applied preparation floated off the slide glass was measured. Note that a power source of 100 V AC and a frequency of 60 Hz was used.
Next, the adhesive strength improvement rate (%) of each Example relative to the corresponding Comparative Example was calculated using the following formula: The Comparative Example corresponding to Example 1-1 is Comparative Example 1-1, and the Comparative Example corresponding to Example 1-2 is Comparative Example 1-2.
<Improvement rate of adhesion rate (%)>
Adhesion improvement rate (%)
= (adhesion time of example - adhesion time of corresponding comparative example) / adhesion time of corresponding comparative example x 100
Based on the calculated adhesive strength improvement rate (%), evaluation was performed according to the following criteria.
Less than 0%: ×
1% or more but less than 10%: △
10% or more but less than 20%: 〇 20% or more: ◎

As shown in Table 1, it was confirmed that the adhesion rate was significantly improved in Examples 1-1 and 1-2, which further contained dextrin palmitate, compared to Comparative Example 1-1, which contained carboxyvinyl polymer and purified water, and Comparative Example 1-2, which contained sodium alginate and purified water.

The adhesion improvement rates of Examples 1-1 and 1-2 relative to Comparative Examples 1-1 and 1-2 were determined using the same method as above, except that the stirrer knob was set to 10. As a result, the adhesion improvement rates of Examples 1-1 and 1-2 were both 10% or more.

Dextrin palmitate is a gelling agent for fat-soluble components, and is therefore used in W/O compositions, but is not generally used in O/W compositions. However, the compositions of Examples 1-1 and 1-2, in addition to improving the adhesion rate, also had excellent properties in terms of extrusion from the tube, breakage of the formulation during use, and the feel when brushing teeth.

[Test Example 2. Usability test (1)]
Dentifrices having the compositions shown in Table 1 of Test Example 1 above were prepared in a conventional manner, and the sensation of use was evaluated using these.
The dentifrices shown in Table 1 (Comparative Example 1-1, Example 1-1) were prepared.
Three panelists, including the dentifrice developer, were asked to place 0.5 g of each dentifrice on a toothbrush and brush their teeth. They were then asked to evaluate the feeling of the dentifrice on the gums and the level of unpleasant sourness felt one minute after starting to brush, based on the following criteria.
The results are shown in Table 2.
<Evaluation criteria for adhesion to gums>
I feel a strong sense of adhesion: 5
Feels close to skin: 4
I feel some tightness: 3
Almost no adhesion: 2
No feeling of adhesion at all: 1
<Unpleasant sourness evaluation criteria>
I feel an unbearable and unpleasant sour taste: 5
Strong and unpleasant sour taste: 4
A clearly noticeable and unpleasant sour taste: 3
Slightly unpleasant sour taste: 2
Almost no unpleasant sourness: 1

In Example 1-1, it was possible to clearly feel an improvement in adhesion to the gums compared to Comparative Example 1-1. Furthermore, an unpleasant sour taste was felt in Comparative Example 1-1, but in Example 2, which contains dextrin palmitate as component (A) in addition to component (B), no unpleasant sour taste was felt and it was comfortable to use.

[Test Example 3. Usability test (2)]
Dentifrices having the compositions shown in Table 3 below were prepared in a conventional manner, and the sensation of use was evaluated using these.
The dentifrices shown in Table 3 (Comparative Example 2, Example 2) were prepared.
Three panelists, including the dentifrice developer, were asked to place 0.5 g of each dentifrice on a toothbrush and brush their teeth. They were then asked to evaluate which dentifrice they felt more strongly about the feeling of the dentifrice sticking to the gums and the level of unpleasant sourness one minute after starting to brush their teeth.
The results are shown in Table 4.

As in Example 2, when the concentration of each component, such as carboxyvinyl polymer, was changed instead of the formulation example in Table 1, it was confirmed that the effect of improving adhesion to the gums and suppressing unpleasant sourness was obtained compared to when dextrin palmitate was not contained. Also, compared to Comparative Example 2, Example 2 tended to cause less irritation during use.

Therefore, Test Examples 2 and 3 demonstrated that when a polymeric compound is included as component (B), the combination with dextrin palmitate, component (A), improves adhesion to the gums and suppresses unpleasant sourness.

[Formulation example]
Hereinafter, several formulation examples using the oral composition according to the present invention will be described. The following formulation examples can be prepared by a conventional method according to the following formulation. The unit of the content of each component is w/w%.

(Formulation Example 1) Dentifrice Allantoin 0.1
Tocopherol acetate 0.04
Cetylpyridinium chloride hydrate 0.02
Dipotassium glycyrrhizinate 0.2
Peppermint oil 0.3
Lily extract 0.1
Hydrolyzed conchiolin liquid 0.1
Liquid Paraffin 10
White Vaseline 1
Dextrin palmitate 0.5
Sorbitan monostearate 1.5
Carboxyvinyl polymer 1.1
Pullulan 0.1
Polysorbate 60 1.5
Sodium Lauryl Sulfate 1
Concentrated glycerin 5
Paraben: 0.1
Fragrance 0.2
L-arginine (appropriate amount)
Distilled water remaining
Total quantity 100

(Formulation Example 2) Dentifrice Tocopherol acetate 0.04
Isopropyl methylphenol 0.05
Hinokitiol 0.1
Potassium nitrate 5
Sodium chloride 5
Peppermint oil 1
Lily extract 0.05
Liquid Paraffin 6
Dextrin palmitate 0.5
Glyceryl monostearate 1.5
Carboxyvinyl polymer 0.5
Sodium alginate 0.5
Polyoxyethylene cetyl ether 1.5
Sodium Lauroyl Methyl Taurate 1
Propylene glycol 5
Phenoxyethanol 0.3
Fragrance 0.1
L-arginine (appropriate amount)
Distilled water remaining
Total quantity 100

(Formulation Example 3) Dentifrice Benzalkonium chloride 0.01
Sodium monofluorophosphate 0.07
Sodium Lauroyl Sarcosine 0.2
Polyethylene glycol a 5
Menthol 0.3
Hydrolyzed conchiolin liquid 1
Liquid Paraffin 5
White Vaseline 0.1
Dextrin palmitate 0.5
Sorbitan monostearate 1.5
Calcium hydrogen phosphate 10
Polyoxyethylene hydrogenated castor oil 1.5
2-alkyl-N-carboxymethyl-
N-Hydroxyethylimidazolinium betaine 1
1,3-butylene glycol 5
Phenoxyethanol 0.5
Fragrance 0.05
L-arginine (appropriate amount)
Distilled water remaining
Total quantity 100

Claims (10)

An oral composition comprising: (A) a fatty acid dextrin; (B) at least one member selected from the group consisting of a carboxyvinyl polymer, alginic acid, and a salt of alginic acid; and (C) water. The oral composition according to claim 1, in which the total content of the (B) component is 0.01 to 500 parts by mass per 1 part by mass of the total content of the (A) component. The oral composition according to claim 1 or 2, which contains 30% by mass or more of (C) water. The oral composition according to any one of claims 1 to 3, wherein the fatty acid dextrin (A) is palmitic acid dextrin. The oral composition according to any one of claims 1 to 4 further contains at least one selected from the group consisting of bactericides, tissue repair agents, anti-inflammatory agents, and blood circulation promoters. The oral composition according to any one of claims 1 to 5 further contains a higher alcohol having 6 or more carbon atoms. The oral composition according to any one of claims 1 to 6, further comprising a surfactant. The oral composition according to any one of claims 1 to 7, further comprising a hydrocarbon. The oral composition according to any one of claims 1 to 8, which is a dentifrice, a coating agent, or a mouthwash. A method for enhancing adhesion of an oral composition to gums, comprising the steps of: (A) a fatty acid dextrin; (B) at least one selected from the group consisting of a carboxyvinyl polymer, alginic acid , and a salt of alginic acid; and (C) water.