JP3329082B2 - Oral composition - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral composition which can effectively suppress the occurrence and progression of gingival tissue inflammation and is effective in preventing and treating periodontal diseases.

[0002]

BACKGROUND OF THE INVENTION Periodontal disease is an inflammatory disease of gingival tissue caused by bacteria present in calculus. For prevention and treatment of this disease, tranexamic acid is used. (Described in JP-B-49-39818),
Glycyrrhetinic acids and glycyrrhizin (JP-A-54-0)
No. 26339, No. 59-227812, No. 61-28
No. 6314, No. 63-0355515, No. 63-198
No. 616) has been reported to be effective.

[0003] However, these drugs can be expected to have considerable preventive and therapeutic effects on periodontal disease when used alone, but in recent years, oral compositions containing drugs that can exhibit higher preventive and therapeutic effects have been developed. Development is desired.

[0004] The present invention has been made to meet the above-mentioned needs, and provides an oral composition which can effectively suppress the occurrence and progress of inflammation of gingival tissue and is effective for the prevention and treatment of periodontal disease. The purpose is to:

[0005]

The present inventors have made intensive studies to achieve the above object, and as a result, when glycyrrhetinic acid or glycyrrhizinate is used in combination with taurine, it will be apparent from experimental examples described later. Surprisingly, the anti-inflammatory effect of glycyrrhetinic acid or glycyrrhizinate is dramatically increased as compared to a single combination of glycyrrhetinic acid or glycyrrhizinate, which can effectively prevent the occurrence and progress of inflammation of gingival tissue. Therefore, the present inventors have found that an oral composition containing these components is extremely effective for prevention and treatment of periodontal disease, and have accomplished the present invention.

Accordingly, the present invention provides an oral composition characterized by using glycyrrhetinic acid or a glycyrrhizinate in combination with taurine.

Hereinafter, the present invention will be described in more detail. The oral composition of the present invention comprises glycyrrhetinic acid or glycyrrhizinate and taurine as active ingredients.
The composition can be prepared and applied to dentifrices such as toothpaste, liquid dentifrice, and lubricating dentifrice, oral paste, ointment, mouthwash, periodontal pocket agent, patch, troche for oral cavity and the like.

The glycyrrhizinate used here includes dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, diammonium glycyrrhizinate,
Disodium glycyrrhizinate, trisodium glycyrrhizinate and the like can be mentioned.

The compounding amount of glycyrrhetinic acid or glycyrrhizinate is 0.001 to 1 with respect to the whole composition.
0% (% by weight, the same applies hereinafter), and particularly preferably 0.05 to 5%. If the amount is less than 0.001%, the anti-inflammatory effect at the gingival region may not be sufficiently exhibited, and 10%
Exceeding the range may adversely affect the usability.

The amount of taurine is preferably 0.001 to 20%, particularly 0.05 to 10%, based on the whole composition. If the amount is less than 0.001%, the enhancing effect may not be sufficiently exhibited, and if it exceeds 20%, the feeling of use may be impaired.

[0011] In addition to the above-mentioned components, the oral composition of the present invention may further contain appropriate components according to the type of the target composition. For example, various medicinal components other than the above essential components, polymer compounds, oils, excipients, surfactants, sweeteners, flavors, stabilizers and the like can be mentioned.

More specifically, antibacterial agents such as chlorhexidine, triclosan, cetylpyridinium chloride, and fluorine compounds such as sodium fluoride, stannous fluoride, and sodium monofluorophosphate as various medicinal components other than the above essential components; Examples include plaque formation inhibitors such as dextranase, mutanase, and protease; gingivitis preventives such as tranexamic acid, azulene, psyllium extract, and sodium chloride; calculus preventives such as polyphosphoric acid; and various vitamins such as tocopherol acetate.

As the high molecular compound, methyl cellulose,
Hydroxypropyl cellulose, sodium carboxymethyl cellulose, hydroxyethyl cellulose, propylene glycol alginate, pullulan, tragacanth gum, xanthan gum, chitosan, polyethylene oxide, polyvinylpyrrolidone, polyacrylic acid and polymethacrylic acid or salts thereof, gelatin,
Peptone, casein, collagen, albumin, xanthan gum, carrageenan, gum arabic, gum karaya,
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, liquid paraffin, paraffin,
Higher alcohols such as cetyl alcohol and stearyl alcohol, and fatty acid esters such as oleic acid and isopropyl myristate can be blended.

As the excipient, aluminum hydroxide, second
Calcium phosphate dihydrate, dicalcium phosphate
Anhydrous, monobasic calcium phosphate, tribasic calcium phosphate, calcium carbonate, calcium pyrophosphate, insoluble sodium metaphosphate, amorphous silica, crystalline silica, aluminosilicate, aluminum oxide, tribasic magnesium phosphate, magnesium carbonate, magnesium sulfate, Titanium oxide, crystalline titanium, 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, and polyoxyethylene sorbitan fatty acid ester. Oxyethylene 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 alkylamines, Fatty acid amide, polyoxyethylene alkylphenyl formaldehyde condensate, single chain length polyoxyethylene alkyl ether, alkyl sulfate of anionic surfactant, polyoxyethylene alkyl sulfate, N-acyl amino acid and its salt, N- Acyl methyl taurate, polyoxyethylene alkyl ether acetate, alkyl sulfocarboxylate, α-olefin sulfonate, alkyl phosphate, polyoxyethylene alkyl ether phosphate, cationic surfactants such as alkyl ammonium, Alkyl benzyl ammonium salts and betaine acetate, imidazolinium betaine, lecithin and the like can be blended as amphoteric surfactants.

As the sweetener, saccharin sodium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartin, p-methoxycinamic aldehyde, aspartame and the like can be blended.

Essential oils such as peppermint and spearmint, l-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 amount of these optional components can be any ordinary amount as long as the effects of the present invention are not impaired.

[0022]

Industrial Applicability The oral composition of the present invention can extremely effectively suppress the occurrence and progress of local inflammation of gingival tissue, and is effective for the prevention and treatment of periodontal disease.

[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] A drug was locally administered to incisor gingivitis in ODU rats (plaque adherent rats) for incisor gingivitis according to the following method, and a verification experiment of the gingivitis ameliorating effect was carried out.

Each group consisted of 10 ODU rats. The rats were weaned at the age of 5 weeks after birth, and MF powder feed (manufactured by Oriental Yeast Co., Ltd.) was freely taken for 3 months to induce gingivitis in the incisor gingiva. Approximately 0.05 g of each drug shown in Table 1 was applied twice daily for 2 weeks to the gingival inflammation area of these rats. The gingival inflammation area before and after the application of the drug was measured under a stereoscopic microscope. The improvement effect of the drug on inflammation was expressed as an inflammation area improvement rate determined by the following formula. Table 2 shows the results.

[0026]

(Equation 1)

[0027]

[Table 1]

[0028]

[Table 2]

From the results shown in Table 2, it was found that when dipotassium β-glycyrrhizinate or β-glycyrrhetinic acid was combined with taurine, a higher inflammation-reducing effect was observed as compared with the case where the drug was formulated alone. Was.

Examples will be described below.

Example 1 Mouse Wash Ethanol 10.0% Glycerin 10.0% O. E. FIG. (60) Hardened castor oil 5.0% Saccharin sodium 0.2% β-glycyrrhizinate dipotassium 0.5% Taurine 0.5% Fragrance 0.2% Purified water Balance 100.0%

[Example 2] Oral pasta Liquid paraffin 15.0% Glycerin 15.0% Sodium benzoate 0.1% Methylparaben 0.2% Cetanol 5.0% Microcrystalline wax 10.0% Paraffin wax 5. 0% Sorbitan monostearate 4.0% β-Glycyrrhizinate dipotassium 1.5% Taurine 1.5% Oat extract 0.5% Fragrance 0.4% Purified water Balance 100.0%

Example 3 Oral Pasta Liquid Paraffin 24.0% Sorbit 14.0% Sodium Benzoate 0.1% Cetanol 5.0% Microcrystalline Wax 10.0% Paraffin Wax 5.0% Hydroxypropylcellulose 1.5% Glycyrrhetinic acid 0.5% Taurine 0.5% Lysozyme chloride 1.0% Fragrance 1.0% Purified water Balance 100.0%

Example 4 Toothpaste Dibasic calcium phosphate 45.0% Carboxymethylcellulose 1.0% Carrageenan 1.0% Glycerin 15.0% Propylene glycol 2.0% Sodium lauryl sulfate 1.0% Diethanolamide laurate 0.5% β-Glycyrrhizinate dipotassium 0.5% Taurine 1.0% Calcium aspartate 0.8% Saccharin sodium 0.1% Triclosan 0.02% Fragrance 1.0% Purified water Balance 100.0%

Example 5 Toothpaste Precipitable silica 20.0% Thickening silica 3.0% 60% Sorbit 25.0% Polyethylene glycol 400 4.0% Sodium carboxymethylcellulose 1.5% Sodium lauryl sulfate 1. 5% sodium saccharin 0.1% glycyrrhetinic acid 0.1% taurine 0.3% chlorhexidine hydrochloride 0.1% sodium hydroxide (50% aqueous solution) 0.3% fragrance 1.0% purified water balance 100.0%

Example 6 Toothpaste Aluminum hydroxide 25.0% Sorbit 25.0% Glycerin 25.0% Polyvinylpyrrolidone 1.0% Lauroyl polyglycerin ester 1.0% O. E. FIG. (60) Sorbitan monolaurate 0.5% Ethyl parahydroxybenzoate 0.1% Sodium saccharin 0.2% Sodium fluoride 0.5% Dipotassium β-glycyrrhizinate 1.0% Taurine 1.0% Flavor 0.8% Purified water balance 100.0%

Example 7 Liquid Dentifrice Precipitable Silica 20.0% Sodium Carboxymethyl Cellulose 1.0% Glycerin 5.0% Propylene Glycol 5.0% Sodium Lauryl Sulfate 1.0% Polyoxyethylene (60 mol) Curing Castor oil 0.5% Glycyrrhetinic acid 1.0% Saccharin sodium 0.2% Flavor 1.0% Tranexamic acid 0.5% Taurine 0.8% Purified water Balance 100.0%

Example 8 Liquid Dentifrice Precipitable Silica 18.0% Propylene Glycol 2.0% 60% Sorbit 30.0% Glycerin 30.0% Sodium Polyacrylate 0.1% Xanthan Gum 0.2% Lauryl Sulfate Sodium 0.8% Polyglycerin fatty acid ester 2.0% Saccharin sodium 0.1% β-glycyrrhizinate dipotassium 1.5% Taurine 0.5% Vitamin C derivative 1.0% Sodium fluoride 0.8% Fragrance 1.0 % Purified water balance 100.0%

Example 9 Toothpaste Precipitable silica 20.0% Thickening silica 3.0% 60% Sorbit 25.0% Polyethylene glycol 400 4.0% Sodium carboxymethyl cellulose 1.5% Sodium lauryl sulfate 1. 5% sodium saccharin 0.1% dipotassium β-glycyrrhizinate 1.0% taurine 0.5% chlorhexidine hydrochloride 0.1% sodium hydroxide (50% aqueous solution) 0.3% hinokitiol 0.2% fragrance 1.0% Purified water balance 100.0%

Example 10 Toothpaste Precipitated silica 25.0% Sorbit 25.0% Glycerin 25.0% Polyvinylpyrrolidone 1.0% Lauroyl polyglycerin ester 1.0% O. E. FIG. (60) Sorbitan monolaurate 0.5% Ethyl paraoxybenzoate 0.1% Saccharin sodium 0.2% Sodium fluoride 0.5% Dipotassium β-glycyrrhizinate 1.0% Taurine 1.0% Vitamin E 0.6 % Perfume 0.8% Purified water Balance 100.0%

Example 11 Mouthwash Sorbit 10.0% Ethanol 5.0% Sucrose monopalmitate 0.2% Polyoxyethylene (60 mol) hydrogenated castor oil 0.1% Methyl parahydroxybenzoate 0. 01% Saccharin sodium 0.2% Dipotassium β-glycyrrhizinate 1.0% Taurine 1.0% Cetylpyridinium chloride 0.2% Fragrance 0.6% Purified water Balance 100.0%

────────────────────────────────────────────────── ─── Continuation of the front page (56) References JP-A-7-165547 (JP, A) JP-A-6-247834 (JP, A) JP-A-5-97639 (JP, A) JP-A-4- 139117 (JP, A) JP-A-5-39213 (JP, A) JP-A-5-962 (JP, A) (58) Fields investigated (Int. Cl. ⁷ , DB name) A61K 7/16

Claims (1)

(57) [Claims] 1. An oral composition comprising a combination of glycyrrhetinic acid or glycyrrhizinate and taurine.