JP2008120753A - Liquid composition for oral cavity - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a liquid composition for an oral cavity excellent in the remaining property of an active ingredient in the oral cavity. <P>SOLUTION: This liquid composition for the oral cavity prepared by blending 0.005 to 0.5 wt.% cetylpyridinium chloride and/or vitamins and 0.01 to 1.0 wt.% non-anionic water soluble polymer, and adjusting the viscosity of the composition so as to become 10 to 500 mPa s is provided with that the non-anionic water soluble polymer in the liquid composition for the oral cavity is hydroxycellulose, and the vitamins are pyridoxines and/or a vitamin E ester. <P>COPYRIGHT: (C)2008,JPO&INPIT

Description

The present invention relates to a liquid oral composition, and more particularly to a liquid oral composition excellent in oral persistence of cetylpyridinium chloride and vitamins.

Dental plaque (plaque) adheres as a cause of caries and periodontitis. Traditionally, oral hygiene has focused on the removal and prevention of adhesion, that is, prevention of plaque adhesion (plaque control). Therefore, securing sufficient blood flow in the gums is said to be important. On the other hand, in addition to food culture changes and unbalanced diets, people who live unfavorably in maintaining good oral hygiene conditions, such as irregular meal times and sustained snacking habits, and reduced resistance With increasing number of elderly people, lifestyle-related diseases, especially diabetic patients, etc., an increasing number of people are worried about the chronicity of periodontal disease. In response to these situations, provision of simple and effective products for the alleviation and prevention of symptoms of oral diseases is desired. Conventionally, as plaque control methods, brushing, a method of mechanically removing plaque with a toothbrush, and a chemical plaque control method of sterilizing oral bacteria by using a bactericidal agent have been generally performed. However, complete removal of plaque with a toothbrush is difficult, and in particular, there are many inadequate cleaning around the back teeth, interdental area, and periodontal pocket. In addition, sterilization using a disinfectant generally uses a liquid oral composition containing these components, but as a method of use, there are many things that are contained in the mouth, and the method However, since there is a limit to the persistence of medicinal ingredients on the tooth surface and gums, it has been difficult to obtain a sufficient bactericidal effect to prevent or alleviate symptoms of oral diseases. For this reason, it is necessary to devise measures such as increasing the concentration of the bactericidal agent and increasing the processing time, but there are not always satisfactory in terms of safety, economic efficiency, sterilization efficiency, etc., and these problems are solved. It was desired to provide products to be used. In response to these demands, in mechanical plaque control, the operability and brushability in the oral cavity are improved by devising the flocking pattern of the toothbrush brush bristles and making the flocking head thin and compact. Although proposals have been made to improve and solve the problem, cleaning of details in the oral cavity and removal of bacteria have been difficult only by physical action. In chemical plaque control, attempts have been made to solve the problem by improving the penetration of sterilization into an aggregate or mass of microorganisms such as plaque in order to improve the sterilizing power. For example, Japanese Patent Application Laid-Open No. 6-321744 proposes that nonionic surfactants and polyhydric alcohols promote the penetration of anthranilic acid anti-inflammatory agents into plaques. When commonly used penetration enhancers, especially nonionic surfactants, are added to cationic fungicides such as urium and chlorhexidine hydrochloride, the fungicides are often incorporated into micelles formed by nonionic surfactants. Therefore, conversely, the bactericidal activity is reduced, and sufficient problems have not been solved. Japanese Patent Publication No. 3-47245 discloses that the inactivation of a bactericidal agent is effectively prevented by incorporating thymol or the like into a composition for oral cavity which is a combination of a cationic bactericidal agent and a nonionic surfactant. In a method for preventing this, Japanese Patent Application Laid-Open No. 7-165546 discloses that when a specific cationic surfactant is added to a nonionic surfactant, mixed micelles are formed in which the micelle surface is controlled to be cationic. A method for preventing the incorporation of cetylpyridinium chloride into micelles by force, and further, by incorporating cyclodextrins in JP-A-8-259428, the reduction of the bactericidal effect of the cationic bactericide by the nonionic surfactant is suppressed. A possible method has been proposed. However, none of the above publications describes any technique for improving plaque control or gum condition by improving the oral residue of cetylpyridinium chloride or vitamins.

JP-A-6-321744 Japanese Patent Publication No. 3-47245 JP-A-7-165546 JP-A-8-259428

In view of the conventional problems as described above, the present invention leaves sufficient cetylpyridinium chloride and vitamins sufficient to exert an effect on the tooth surface and gums, thereby increasing plaque control and increasing blood flow in the gums. And a liquid oral composition for maintaining and improving the oral hygiene environment.

  In order to achieve the above object, the present inventors have made extensive studies in view of such circumstances, and found that cetylpyridinium chloride and / or vitamins 0.005 to 0.5% by weight and a non-anionic water-soluble polymer It has been found that excellent persistence such as cetylpyridinium chloride is obtained in a liquid oral composition prepared by blending 0.01 to 1.0% by weight and adjusting the composition to a viscosity of 10 to 500 mPa · s. Thus, the present invention has been completed.

That is, the present invention
Item 1 A composition containing 0.005 to 0.5% by weight of cetylpyridinium chloride and / or vitamins and 0.01 to 1.0% by weight of a non-anionic water-soluble polymer, and the composition has a viscosity of 10 to 500 mPa · s. A liquid oral composition characterized by the above.
Item 2. The liquid oral composition according to claim 1, wherein the non-anionic water-soluble polymer is hydroxyethyl cellulose. Item 3. The liquid oral composition according to claim 3, wherein the vitamin is pyridoxine and / or vitamin E ester.

The present invention contains cetylpyridinium chloride and / or vitamins in an amount of 0.005 to 0.5% by weight and a non-anionic water-soluble polymer in an amount of 0.01 to 1.0% by weight, and the composition has a viscosity of 10 to 500 mPa.s A liquid oral composition prepared as described above is provided. The non-anionic water-soluble polymer of the present invention is not particularly limited. For example, hydroxyalkyl cellulose such as hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, alkyl cellulose, crystalline cellulose, cellulose powder, pregelatinized starch , Dextrin, polyvinyl alcohol, polyoxyethylene glycol, polyoxypropylene glycol, saponified copolymer of vinyl acetate and alkyl (meth) acrylate, pyrrolidone / dimethylaminoethyl methacrylate copolymer, vinyl caprolactam / vinyl pyrrolidone / dimethyl Examples thereof include aminoethyl methacrylate copolymer. Of these, hydroxyethyl cellulose is preferable.

The amount of the non-anionic water-soluble polymer used in the present invention is 0.01 to 1.0% by weight, preferably 0.1 to 0.5% by weight, based on the entire composition. If the blending amount is less than 0.01% by weight, the persistence effect cannot be obtained sufficiently. If the blending amount exceeds 1.0% by weight, changes such as a decrease in viscosity and precipitation occur with time, which is not preferable.

Hydroxyethyl cellulose used in the present invention is a water-soluble nonionic long-chain polymer derived from cellulose. Properties vary with the average added moles of ethylene oxide per glucose unit in each cellulose molecule. Those having an average added mole number of 1.3 mol or more are water-soluble, and 1.5 mol or more is suitable for the practice of the present invention. The hydroxyethyl cellulose suitable for the present invention is, for example, SE-400, 500, 550, 600, 850, 900 (manufactured by Daicel Chemical Industries, Ltd.) and is commercially available.

The vitamins used in the present invention may be either water-soluble vitamins or oil-soluble vitamins. Examples of water-soluble vitamins include thiamine, thiamine monophosphate, thiamine diphosphate, thiamine triphosphate, and the like. vitamin B ₁ class, riboflavins, pyridoxine and its salts, pyridoxal, pyridoxamine, phosphoric acid ester type at their 5 'position, pyridoxine such as sugar derivatives of pyridoxine hydrochloride and pyridoxine, vitamin B ₁₂ compounds, folic acid, niacin Vitamins such as vitamin A, carotenoids, ergocalciferol and cholecalciferol, vitamins such as tocopherol, tocopherol succinate and tocopherol nicotinate E Esters and other vitamins E, vitamin K and the like.

Of these, pyridoxines and vitamin E esters such as tocopherol succinate and tocopherol nicotinate are preferred, and pyridoxine hydrochloride and tocopherol nicotinate are more preferred.

  The liquid oral composition of the present invention preferably has a viscosity at 25 ° C. of 10 to 500 mPa · s. The viscosity was measured using a BL type viscometer.

In the liquid oral cavity composition of the present invention, conventionally known components can be appropriately blended as long as the effects of the present invention are not impaired. For example, nonionic surfactants include polyoxyethylene hydrogenated castor oil, sucrose fatty acid esters, maltose fatty acid esters, sugar fatty acid esters such as lactose fatty acid esters, fatty acid alkanolamides, sorbitan fatty acid esters, fatty acid monoglycerides, polyoxyethylene addition coefficient Is a polyoxyethylene alkyl ether type having a carbon number of 8 to 10 and an alkyl group of 13 to 15 or a polyoxyethylene alkyl phenyl ether type nonion having a polyoxyethylene addition coefficient of 10 to 18 and a carbon number of an alkyl group of 9 Surfactant etc. are mentioned.

Zwitterionic surfactants include N-alkyldiaminoethylglycine such as N-lauryldiaminoethylglycine and N-myristyldiethylglycine, N-alkyl-N-carboxymethylammonium betaine, sodium 2-alkyl-1hydroxyethylimidazoline betaine It is done. These surfactants can be blended alone or in combination of two or more. The compounding quantity is 0.01 to 30 weight% normally with respect to the composition whole quantity, Preferably it is 0.1 to 5 weight%.

As a flavoring agent, menthol, carboxylic acid, anethole, eugenol, methyl salicylate, limonene, osimene, n-decyl alcohol, citronell, α-terpineol, methyl acetate, citronenyl acetate, methyl eugenol, cineol, linalool, ethyl linalool , Thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, perilla oil, winter green oil, clove oil, eucalyptus oil, pimento oil, etc. A combination of the above can be added at a ratio of 0.01 to 5% by weight, preferably about 0.05 to 1% by weight, based on the total amount of the composition.

In addition, sweeteners such as sodium saccharin, acesulfame potassium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perilartin, thaumatin, asparatylphenylalanyl methyl ester, and ρ-methoxycinnamic aldehyde are added to the total amount of the composition. 0.01 to 1% by weight, preferably 0.05 to 0.5% by weight.

Furthermore, as a wetting agent, sorbit, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, polypropylene glycol, polyethylene glycol, xylit, maltite, lactit and the like can be used alone or in combination of two or more. A compounding quantity is 3 to 70 weight% normally with respect to the composition whole quantity.

In addition, medicinal components other than cetylpyridinium chloride and vitamins can be blended in the liquid oral composition of the present invention. Cationic fungicides such as chlorhexidine hydrochloride and benzethonium chloride, amphoteric fungicides such as dodecyldiaminoethylglycine, nonionic fungicides such as triclosan and isopropylmethylphenol, dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme ( Enzymes such as Litech Enzyme), tranexamic acid and epsilon aminocaproic acid, aluminum chlorohydroxyl allantoin, dihydrocholesterol, glycyrrhizin salts, glycyrrhetinic acid, glycerophosphate, chlorophyll, sodium chloride, caropeptide, etc. can do.

Next, it explains in more detail using an example.

Intraoral persistence test of cetylpyridinium chloride, pyridoxine hydrochloride and tocopherol nicotinate ester The intraoral persistence was measured according to the following method. Using the Examples and Comparative Examples shown in Table 1 as test solutions, and applying 10 ml of each in the oral cavity by a conventional method, cetylpyridinium chloride contained in the exhaled solution was obtained by liquid chromatography. The amount was determined and the remaining amount in the mouth was determined. Pyridoxine hydrochloride and tocopherol nicotinate were similarly tested. The results are shown in Table 1 and FIGS.
(Figure 1)
(Figure 2)
(Figure 3)

As shown in Table 1, the residual properties in Examples 1, 2, and 3 were superior to those of Comparative Examples 1, 2, and 3.

Claims (3)

  Cetylpyridinium chloride and / or vitamins 0.005 to 0.5 wt% and non-anionic water-soluble polymer 0.01 to 1.0 wt% are blended, and the viscosity of the composition is 10 to 500 mPa · s. A liquid oral composition characterized by the above. The liquid oral composition according to claim 1, wherein the non-anionic water-soluble polymer is hydroxyethyl cellulose. The liquid oral composition according to claim 3, wherein the vitamins are pyridoxines and / or vitamin E esters.