JPH11130644A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject composition having inhibitory actions on alveolar bone absorption, promoting absorption via mucosa of taurine safe in use in an oral cavity for many hours, effective for preventing and treating periodontal disease, having high pharmacodynamic effects, by using both taurine and xylitol. SOLUTION: This composition is obtained formulating (A) 0.001-20 wt.%, especially 0.05-10 wt.% of taurine and (B) xylitol in the weight ratio of xylitol/ taurine of >=0.1, especially >=2 and, if required, adding a polymer, an oil, an excipient or a polishing agent, an alcohol, a surfactant, a sweetener, a spice, a stabilizer, etc., and preparing the mixture into a dosage form such as a dentifrice, e.g. tooth paste, liquid dentifrice, wet dentifrice, etc., paste for oral cavity, ointment, gel agent, mouth wash, periodontal pocket agent, patch, throche for oral cavity, etc.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an oral composition having good transmucosal absorbability of taurine as an active ingredient for alveolar bone resorption and effective for prevention and treatment of periodontal disease.

[0002]

BACKGROUND OF THE INVENTION Periodontal disease is a disease of the periodontal tissue caused by periodontopathic bacteria, and as its symptoms progress, the inflammation of the soft tissue in the periodontal tissue causes the alveolar bone. Is a disease that results in the absorption of bones and eventually leads to tooth loss.

[0003] Conventionally, flurbiprofen (J. Periodont. Res.,
23 , 166-169, 1988), indomethacin (J. Periodont. Res., 17 , 90-1).
00, 1982) are reported to be effective, and JP-A-60-61524 describes that ibuprofen and flurbiprofen have an alveolar bone resorption inhibitory effect. However, use of these drugs for a long time may cause harmful effects on the oral mucosa. For prevention and prevention of alveolar bone resorption caused by periodontal disease which is a chronic disease, it is particularly desirable to use a drug which is safe even when used in the oral cavity for a long period of time. In addition, it was necessary to develop a drug having an excellent alveolar bone resorption inhibiting effect.

[0004] Japanese Patent Application Laid-Open No. 6-247834 describes the effect of taurine on alveolar bone resorption inhibition which is safe even when used in the oral cavity for a long period of time. In addition, taurine is applied to the oral cavity by using a tooth glossing agent (JP-A-49-42838).
Japanese Patent Application Laid-Open No. 63-132820, and Japanese Patent Application Laid-Open No. 8-408 for the purpose of preventing and treating periodontal disease.
No. 58) is known.

[0005] However, for a drug applied to periodontal tissue, efficient drug delivery to a lesion is required to further improve its efficacy. However, taurine is a water-soluble substance, and is generally a water-soluble substance. Percutaneous absorption and transmucosal absorption of water-soluble drugs are by no means high. Therefore, when applying taurine to the oral cavity which is constantly washed away with saliva, it is desired to develop a method and an additive for promoting the transmucosal absorption.

The present invention has been made in view of the above circumstances,
A highly efficacious oral composition that has an alveolar bone resorption inhibitory effect and promotes transmucosal absorption of taurine, which is safe even when used in the oral cavity for a long period of time, and is effective for prevention and treatment of periodontal disease The purpose is to provide.

[0007]

Means for Solving the Problems and Embodiments of the Invention As a result of intensive studies to achieve the above object, the present inventor has found that the combined use of taurine and xylitol increases the transmucosal absorbability of taurine, Therefore, the present inventors have found that a highly efficacious oral composition effective for prevention and treatment of periodontal disease can be obtained, and have accomplished the present invention.

[0008] Xylitol is a pentavalent sugar alcohol which has recently attracted attention as an anti-cariogenic component and has been incorporated in foods, toothpastes, mouthwashes and the like. Examples of agents applied to the oral cavity include JP-A-50-112444 and JP-A-3-48613.
Japanese Patent Application Laid-Open No. H8-175945 and the like disclose the use of xylitol, but do not disclose any use in combination with taurine.

Accordingly, the present invention provides an oral composition characterized by using taurine and xylitol in combination.

Hereinafter, the present invention will be described in more detail. In the oral composition of the present invention, the amount of taurine is 0.001 to 20% (% by weight, hereinafter the same), particularly 0%, based on the whole composition. It is suitable to be 0.05 to 10%. If the amount is less than 0.001%, a sufficient alveolar bone resorption inhibiting effect may not be obtained, and if it exceeds 20%, the feeling of use may be impaired.

The amount of xylitol is preferably 0.1 or more, more preferably 2 or more in weight ratio of xylitol / taurine. If the amount is less than 0.1, a sufficient taurine absorption promoting effect may not be obtained. If the composition ratio of xylitol to the total composition exceeds 50%, the feeling in use may be impaired.

The oral composition of the present invention contains taurine and xylitol as essential components, and includes dentifrices such as toothpaste, liquid dentifrice, and lubricating dentifrice, oral pasta, ointments, gels, and mouthwashes. It can be prepared and applied to dosage forms such as periodontal pockets, patches, and troches for the oral cavity.

[0013] In addition to the above-mentioned components, the oral composition of the present invention may further contain appropriate components in accordance with the purpose and the type of the composition. For example, as a polymer,
Methylcellulose, hydroxypropylcellulose, sodium carboxymethylcellulose, hydroxyethylcellulose, propylene glycol alginate, pullulan, tragacanth gum, xanthan gum, chitosan, polyethylene oxide, polyvinylpyrrolidone,
Polyacrylic acid and polymethacrylic acid and salts thereof, gelatin, peptone, casein, collagen, albumin, xanthan gum, carrageenan, arabic gum, karaya gum, carboxyvinyl polymer, Eudragit (E, L, SR, S, NE), ethyl cellulose , Cellulose acetate, polyvinyl acetal / dimethylaminoacetate, cellulose acetate / dibutylhydroxypropyl ether, and the like.

As the oil, higher alcohols such as liquid paraffin, paraffin, cetyl alcohol and stearyl alcohol, and fatty acid esters such as oleic acid and isopropyl myristate can be blended.

As an excipient or abrasive, aluminum hydroxide, dibasic calcium phosphate dihydrate, dibasic calcium phosphate / anhydride, monobasic calcium phosphate, tribasic calcium phosphate, calcium carbonate, calcium pyrophosphate, insoluble metaphosphate Sodium, amorphous silica, crystalline silica, aluminosilicate, aluminum oxide, tertiary magnesium phosphate, magnesium carbonate, magnesium sulfate, titanium oxide, crystalline cellulose and the like are blended.

As the alcohol, ethanol, propyl alcohol, isopropyl alcohol, butanol,
Lower alcohols such as isobutanol and ethylene glycol, diethylene glycol, propylene glycol,
Polyhydric alcohols such as dipropylene glycol, 1,3-butylene glycol, glycerin, 1,5-pentadiol, sorbite, and polyethylene glycol are blended.

Examples of the surfactant include nonionic surfactants such as sorbitan fatty acid ester, glycerin fatty acid ester, decaglycerin fatty acid ester, polyglycerin fatty acid ester, propylene glycol / pentaerythritol fatty acid ester, polyoxyethylene sorbitan fatty acid ester, Polyoxyethylene glycerin fatty acid ester, polyoxyethylene sorbite fatty acid ester, polyethylene glycol fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene alkyl phenyl ether, polyoxyethylene castor oil / hardened castor oil , Polyoxyethylene lanolin, lanolin alcohol, beeswax derivatives, polyoxyethylene alkylamine Fatty acid amides, polyoxyethylene alkylphenyl formaldehyde condensates, such as a single chain length polyoxyethylene alkyl ethers are used.
Examples of the anionic surfactant include alkyl sulfates, polyoxyethylene alkyl sulfates, N-acyl amino acids and salts thereof, N-acylmethyl taurine and salts thereof, polyoxyethylene alkyl ether acetates, alkyl sulfocarboxylates, α-olefin sulfonates, alkyl phosphates, polyoxyethylene alkyl ether phosphates, and the like, cationic surfactants such as alkyl ammonium and alkyl benzyl ammonium salts; amphoteric surfactants such as betaine acetate; Imidazolinium betaine, lecithin and the like can be blended.

As a sweetener, sodium saccharin,
Stevioside, neohesperidyl dihydrochalcone,
Glycyrrhizin, perillartin, p-methoxycinnamic aldehyde, aspartame and the like can be blended.

As the flavor, essential oils such as peppermint and spearmint, 1-menthol, carvone, eugenol, anethole and the like can be blended.

As the stabilizer, vitamin C, vitamin E, sodium sulfite, sodium pyrosulfite, sodium hydrogen sulfite, butylhydroxytoluene, propyl gallate, butylhydroxyanisole and the like can be blended.

The oral composition of the present invention may contain various medicinal components, for example, antibacterial agents such as chlorhexidine, triclosan, cetylpyridinium chloride, hinokitiol, sodium fluoride, stannous fluoride, Gingivitis such as fluorine compounds such as sodium fluorophosphate, plaque formation inhibitors such as dextranase, mutanase, and protease; tranexamic acid, ε-aminocaproic acid, glycyrrhizic acid, glycyrrhetinic acids, azulene, allantoin, lysozyme chloride, and oak extract A preventive agent, a tartar preventive agent such as polyphosphoric acids, a gum tightening agent such as sodium chloride, various vitamins such as tocopherol acetate, and the like can be added.

[0022]

The oral composition of the present invention has an effect of inhibiting alveolar bone resorption and promotes the transmucosal absorption of taurine, which is safe even when used in the oral cavity for a long period of time. Effective for prevention and treatment.

[0023]

EXAMPLES Hereinafter, the effects of the present invention will be specifically described with reference to experimental examples and examples, but the present invention is not limited to the following examples. In the following examples, all percentages are by weight.

[Experimental Example] The transmucosal absorbability of a drug was compared and studied using a hamster teak pouch mucosa by the following method.

A teak pouch mucosa isolated from a Syrian hamster (male, 6 weeks old) was attached to a Franz cell,
After preincubation at 37 ° C., 100 μl of a sample solution containing taurine and xylitol shown in Table 1 or various polyols as comparative examples was added. After incubating at 37 ° C. for 5 minutes, the mucous membrane was removed from the cell, the surface was washed with water, the portion to which the sample was administered was cut out with a punch having an inner diameter of 7.5 mm, and homogenized with a 10% trichloroacetic acid solution. The mixture was centrifuged, and the supernatant was analyzed by high performance liquid chromatography to measure the amount of taurine absorbed into the mucous membrane (repeating number n = 5). Table 1 shows the results.

From the results shown in Table 1, it was confirmed that the combined use of xylitol promoted the transmucosal absorption of taurine.

[0027]

[Table 1]

Examples will be described below. [Example 1] Toothpaste Aluminum hydroxide 45.0% Gelling silica 5.0% Sorbit 15.0% Sodium carboxymethyl cellulose 1.0% Sucrose monopalmitate 1.0% Sodium lauryl sulfate 1.5% Methyl paraoxybenzoate 0.1% Butyl paraoxybenzoate 0.01% Saccharin sodium 0.05% Xylitol 10.0% Taurine 1.0% Fragrance 0.8% Water balance 100.00%

Example 2 Toothpaste Precipitable silica 40.0% Sorbit 20.0% Glycerin 20.0% Polyvinylpyrrolidone 1.0% Lauroyl polyglycerin ester 1.0% Polyoxyethylene (60 mol) 5% Sorbitan monolaurate Sodium lauryl sulfate 0.5% Sodium saccharin 0.05% Ethyl parahydroxybenzoate 0.1% Tranexamic acid 0.1% Xylitol 9.0% Taurine 0.8% Fragrance 0.8% Water balance 100.00%

Example 3 Liquid Dentifrice Precipitable Silica 18.0% Propylene Glycol 2.0% 60% Sorbit 20.0% Glycerin 24.0% Sodium Polyacrylate 0.1% Xanthan Gum 0.2% Lauryl Sulfate Sodium 1.5% Polyglycerin fatty acid ester 1.6% Methyl parahydroxybenzoate 0.12% Butyl paraoxybenzoate 0.01% Sodium saccharin 0.1% Sodium fluoride 0.5% Xylitol 12.0% Taurine 1.5 % Perfume 1.0% Purified water Balance 100.00%

Example 4 Mouthwash Ethanol 10.0% Sucrose monopalmitate 1.0% Polyoxyethylene (60 mol) hydrogenated castor oil 1.0% Methyl parahydroxybenzoate 0.05% Saccharin sodium 0 0.5% Taurine 1.0% Xylitol 10.0% Fragrance 0.2% Purified water Balance 100.00%

[Example 5] Oral pasta Liquid paraffin 15.0% Glycerin 10.0% Sodium benzoate 0.1% Methyl paraben 0.2% Cetanol 5.0% Microcrystalline wax 10.0% Paraffin wax 5. 0% Sorbitan monostearate 4.0% Xylitol 8.0% Taurine 0.8% Fragrance 0.4% Purified water Balance 100.00%

Example 6 Ointment White petrolatum 10.0% Stearyl alcohol 10.0% Propylene glycol 1.5% Polyethylene glycol # 4000 23.0% Polyethylene glycol # 400 37.0% Taurine 0.5% Xylitol 6.0% ethanol balance 100.00%

Example 7 Gel Preparation Glycerin 13.0% Carbopol 940 1.0% Sodium hydroxide 0.25% Sorbitan monostearate 5.0% Ethanol 7.0% Taurine 1.0% Xylitol 0% purified water balance 100.00%

Claims (1)

[Claims] 1. An oral composition comprising a combination of taurine and xylitol.