JPH1179961A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject composition capable of controlling the formation of dental plaques and effective for preventing oral cavity diseases by including a cationic bactericide, a nonionic compound having one or more phenolic hydroxyl groups, and a polyoxyethylenepolyoxypropylene block copolymer surfactant having a specific clouding point. SOLUTION: This composition for oral cavities contains 0. 0001-5 wt.% of a cationic bactericide (e.g. an alkyl pyridinium salt such as cetylpyridinium chloride), 0.0001-5 wt.% of a nonionic compound having one or more phenolic hydroxyl groups (e.g. 2,4,4'-trichloro-2'-hydroxydiphenyl ether), and 0.01-5 wt.% of a polyoxyethylenepolyoxypropylene block copolymer type surfactant having a clouding point of >=80 deg.C preferably >=100 deg.C, e.g. polyoxyethylene (200) polyoxypropylene (70) glycol of the formula: HO(C2 H4 O)a -(C3 H6 O)b -(C2 H4 )c h [(a), (b), (c) are each an arbitrary integer].

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to an oral composition having an excellent antibacterial and plaque inhibiting effect.

[0002]

2. Description of the Related Art Conventionally, there has been developed a technique for preventing dental caries and periodontal diseases which are two major diseases of dentistry by adding an antibacterial agent to an oral composition such as a dentifrice. And several oral compositions to which an antimicrobial agent has been added have been put on the market. Antibacterial agents are known to reduce the total number of bacteria in the oral cavity due to their effects and suppress plaque formation, which causes disease, but the antibacterial effect in the oral cavity is often a temporary effect There is a need for sustained effects in the oral cavity. To address this problem, several studies have been made to improve the retention of antibacterial agents by adding a polymer compound (JP-A-6-192060, JP-A-7-267840, etc.). It has been reported that the use of a non-cationic bactericide in combination improves the bactericide retention (US Pat. No. 5,236,699). However, in order to maintain the physical properties of the composition in a stable manner, it is necessary to add a surfactant in order to impart an oral cleansing effect at the time of use. It is also known that the bactericide is reduced, and it has been desired to develop a composition for oral cavity that has an excellent bactericide retention in the oral cavity and shows a high antibacterial effect even when a surfactant is added.

[0003] The present invention has been made in view of the above circumstances,
In systems with added surfactants, it improves the retention of antimicrobial agents in the oral cavity, inhibits the attachment and growth of microorganisms on the tooth surface, and contributes to dental caries and periodontal disease as important factors. It is an object of the present invention to provide an oral composition that effectively inhibits scaling.

[0004]

Means for Solving the Problems and Embodiments of the Invention As a result of intensive studies to achieve the above object, the present invention has revealed that a cationic bactericide and a non-anionic compound having a phenolic hydroxyl group are contained. By blending the polyoxyethylene polyoxypropylene block polymerization type surfactant with the oral composition, the retention property on the tooth surface is increased while having the bactericidal activity, and the adhesion of bacteria and bacteria on the tooth surface are improved. For the oral cavity, which suppresses proliferation and exerts an excellent preventive effect on plaque formation, which is an important factor for dental caries and periodontal disease, and is effective in preventing oral diseases (prevention of dental caries and periodontal disease) The inventors have found that a composition can be obtained, and have accomplished the present invention.

Hereinafter, the present invention will be described in more detail. The oral composition of the present invention comprises a cationic bactericide, a non-anionic compound having a phenolic hydroxyl group, and a polyoxyethylene polyoxypropylene block polymerization type surfactant. It contains.

As the cationic bactericide, alkylpyridinium salts, mono-long-chain alkyltri-short-chain alkylammonium salts, mono-long-chain alkyldi-short-chain alkylbenzylammonium salts, alkylphenylethoxyethyldi-short-chain alkylbenzylammonium salts, etc. Is mentioned. Examples of the alkylpyridinium salt include laurylpyridinium salt, myristylpyridinium salt, and cetylpyridinium salt.Examples of the mono-long-chain alkyltri-short-chain alkylammonium salt include lauryltrimethylammonium salt, myristyltrimethylammonium salt, cetyltrimethylammonium salt, and stearyltrimethyl. Examples of the mono-long-chain alkyl di-short-chain alkyl benzyl ammonium salt include lauryl dimethyl benzyl ammonium salt, myristyl dimethyl benzyl ammonium salt (benzalkonium salt), cetyl dimethyl benzyl ammonium salt, and stearyl dimethyl benzyl ammonium salt. Examples of the alkylphenylethoxyethyl di-short-chain alkylbenzylammonium salt include benzethonium Salts can be mentioned, as forms of these salts chlorides, bromides, and the like iodides. These cationic fungicides may be used alone or as a mixture of two or more.

The non-anionic compound having a phenolic hydroxyl group has an electrostatic interaction with a cationic germicide in the pH range of 4 to 9, and includes, for example, triclosan (2,4,4'-trichloro-2'-). Hydroxydiphenyl ether) and the like.

The amount of the cationic bactericide to be added to the oral composition of the present invention is 0.0001 to 5% of the whole composition.
(% By weight, hereinafter the same), particularly 0.001 to 0.5% is preferable, and if it is less than 0.0001%, a sufficient effect may not be obtained. If it exceeds 5%, the viscosity increases, and the composition is mixed. Becomes difficult. The compounding amount of the non-anionic compound having a phenolic hydroxyl group is 0.0% of the whole composition.
001 to 5%, particularly preferably 0.001 to 1%,
If it is less than 0001%, a sufficient effect may not be obtained, and if it exceeds 5%, a problem may occur in solubility.

The mixing ratio of the above-mentioned cationic germicide and the non-anionic compound having a phenolic hydroxyl group is appropriately selected, but 0.5 to 99.5 parts by weight of the cationic germicide,
In particular, 5 to 95 parts by weight, and the non-anionic compound 99.5 to
0.5 parts by weight, particularly preferably 95 to 5 parts by weight.

The oral composition of the present invention preferably does not contain an anionic surfactant such as sodium lauryl sulfate (SDS) and a binder as an anionic polymer such as carrageenan. The germicidal activity of the cationic germicide may be reduced by these formulations.

The polyoxyethylene polyoxypropylene block polymerization type surfactant used in the present invention has the following general formula: HO (C ₂ H ₄ O) _a- (C ₃ H ₆ O) _b- (C ₂ H ₄ O) _c H (where a, b and c are arbitrary integers), and a cloud point of 80
C. or higher, more preferably 100 ° C. or higher. When the cloud point is lower than 80 ° C., the water solubility as a surfactant decreases, and the oral composition of the present invention cannot be dissolved.

Among them, polyoxyethylene (200) polyoxypropylene glycol (70), polyoxyethylene (300) polyoxypropylene glycol (5)
5), polyoxyethylene (200), polyoxypropylene glycol (400), polyoxyethylene (15)
0) Polyoxypropylene glycol (35), polyoxyethylene (160), polyoxypropylene glycol (30) and the like have high effects, and these are used as Pluronic surfactants from Asahi Denka Kogyo KK as Pluronic F-108. , Pluronic F-127, Pluronic F-88, Pluronic F-87, Pluronic F-
It is marketed under 68 trade names.

The blending amount of the polyoxyethylene polyoxypropylene block polymerization type surfactant is 0.1% of the whole composition.
01-5%, particularly preferably 0.1-5%, 0.01%
If it is less than 5%, the dissolving power is insufficient and it is difficult to uniformly mix the composition.

The oral composition of the present invention can be used as a dentifrice such as toothpaste and liquid dentifrice, and a mouthwash, and is particularly suitable as a mouthwash. The oral composition of the present invention may contain, in addition to the above components, appropriate optional components according to the dosage form. Specifically, in the case of toothpastes and mouthwashes, crystalline silica, amorphous silica, other silica-based abrasives, aluminosilicate, aluminum oxide, aluminum hydroxide, insoluble sodium metaphosphate, insoluble metaphosphate are used as abrasives. Potassium, titanium oxide, dicalcium phosphate
Dihydrate, heavy calcium carbonate, light calcium carbonate (usually 3 to 99%), cellulose derivatives such as carboxymethylcellulose, methylcellulose, hydroxymethylcellulose and sodium carboxymethylhydroxymethylcellulose as binders, polyvinyl alcohol, polyvinylpyrrolidone, etc. Inorganic binders (usually 0.5 to 10%) such as synthetic binders, gelling silica, gelling aluminum silica, vegant, and laponite; sorbitol, glycerin, ethylene glycol as a thickener or wetting agent; Propylene glycol, 1,3-butylene glycol, polyethylene glycol, polypropylene glycol, xylit, maltitol, lactit and the like (usually 1-50%) can be blended.

When the oral composition is a mouthwash, the use of xylit as a thickening or wetting agent not only increases the effect of preventing caries, but also has the advantage of improving the liquid stability of the product. . In this case, the preferred amount of xylite is 0.5 to 15%.

Examples of the surfactant include nonionic surfactants such as sucrose fatty acid ester, polyoxyethylene hydrogenated castor oil, polyglycerin fatty acid ester, alkyl glycosides, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, and alkyldimethylamine oxide. Surfactants, betaine acetate-type amphoteric surfactants such as betaine alkyldimethylaminoacetate and fatty acid amidopropyldimethylaminoacetate, and imidazoline-type amphoteric surfactants such as N-fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine salt An agent can be added within a range not to impair the effects of the present invention.

Further optional components include, for example, saccharin sodium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartin, thaumatin, asparatyl phenylalanine methyl ester, p
-Sweeteners such as methoxycinnamic aldehyde, sucrose, fructose, sodium sakuramate, spearmint oil, peppermint oil, wintergreen oil, sassafras oil, clove oil, eucalyptus oil, sage oil, mayonnaise oil,
Flavors such as thyme oil, lemon oil, orange oil, l-menthol, carvone, anethole, methyl salicylate, fungicides, epsilon aminocaproic acid, tranexamic acid, dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme, litech enzyme Enzymes, chlorohexidine salts, hydrocholesterol, glycyrrhetin salts, glycyrrhetinic acid, chlorophyll,
Caropeptides, vitamins, azulene, lysozyme chloride, anti-calculus agents, anti-plaque agents, potassium nitrate, aluminum lactate and the like can be added. In addition, the addition amount of these optional components can be a usual amount as long as the effects of the present invention are not impaired.

[0018]

EFFECT OF THE INVENTION The oral composition of the present invention is excellent in the effect of inhibiting the adhesion of microorganisms to the tooth surface and the growth of bacteria, can effectively inhibit the formation of plaque, and is effective in preventing oral diseases. Can be used.

[0019]

EXAMPLES Hereinafter, the present invention will be described in detail with reference to experimental examples and examples, but the present invention is not limited to the following examples.

[Experimental Example] As an experiment for inhibiting the formation of plaque on the tooth surface by microorganisms, the components shown in Table 1 were evaluated for the effect of inhibiting the growth of Streptococcus mutans 10449 on a saliva-coated hydroxyapatite plate by the following method. Table 1 shows the results. (1) Hydroxyapatite pieces (manufactured by Asahi Optical Industry Co., Ltd.) were used as tooth models and immersed in filtered human saliva at 37 ° C. for 2 hours. (2) After being immersed in the sample shown in Table 1 for 30 minutes, it was washed with distilled water. (3) The cells were cultured for 12 hours in a liquid medium (Brain Heart Infusion) containing Streptococcus mutans. (4) After washing with distilled water, the cells were stained with fuchsin, and the area of cell attachment was calculated by image analysis. (5) The bacterial growth inhibition rate relative to the control was determined by calculation according to the following formula.

[0021]

(Equation 1)

[0022]

[Table 1]

From the results shown in Table 1, it can be seen that the oral composition comprising the cationic fungicide according to the present invention, a non-anionic compound having a phenolic hydroxyl group and a polyoxyethylene polyoxypropylene block polymerization type surfactant is plaque-forming. To prevent oral diseases (caries prevention and periodontal disease prevention)
It was confirmed that the composition was effective for oral cavity.

[Example 1] Toothpaste Aluminum hydroxide 45% by weight Sorbit 30 Pluronic F-108 3.5 Polyoxyethylene (60) hydrogenated castor oil 0.5 Saccharin sodium 0.1 Propylene glycol 5 Fragrance 1.3 Cetyl chloride Pyridinium 0.05 Triclosan 0.03 Water Balance 100.0% by weight

Example 2 Toothpaste Dibasic calcium phosphate dihydrate 40% by weight Sorbit 30 Pluronic F-127 4 Saccharin sodium 0.1 Propylene glycol 5 Fragrance 1.3 Sodium monofluorophosphate 0.05 Triclosan 0. 05 Benzalkonium chloride 0.05 Water balance 100.0% by weight

Example 3 Toothpaste Silica 20% by weight Sorbit 60 Pluronic F-88 2 Decaglycerin monolaurate 1 Saccharin sodium 0.15 Propylene glycol 5 Fragrance 1.5 Polyvinylpyrrolidone 0.5 Sodium fluoride 0.1 Poly Oxyethylene glycol # 4000 0.5 Benzethonium chloride 0.1 Triclosan 0.1 Water Residue 100.0% by weight

Example 4 Mouthwash Denatured ethanol 1.6% by weight Pluronic F-108 0.5 Citric acid 0.01 Trisodium citrate 0.3 Sodium saccharin 0.1 Cetylpyridinium chloride 0.03 Triclosan 03 Fragrance 0.5 Xylit 2 Glycerin 7 Water Balance 100.0% by weight

Example 5 Mouthwash Ethanol 10% by weight Sodium saccharin 0.05 Chlorohexidine gluconate 0.01 Dye 0.01 Sodium benzoate 0.05 Antioxidant 0.01 Fragrance 0.3 Xylit 5 Pluronic F- 127 0.5 Polyoxyethylene (60) hydrogenated castor oil 0.5 Sodium monofluorophosphate 0.05 Benzalkonium chloride 0.02 Triclosan 0.03 Water Balance 100.0% by weight

Example 6 Mouthwash 90% Ethanol 20% by weight Pluronic F-108 0.5 Fragrance 1.5 Sodium monofluorophosphate 0.05 Benzalkonium chloride 0.02 Triclosan 0.02 Water Balance 100 0.0% by weight

Claims (1)

[Claims] An oral composition comprising a cationic germicide, a non-anionic compound having a phenolic hydroxyl group, and a polyoxyethylene polyoxypropylene block polymerization type surfactant having a cloud point of 80 ° C. or higher.