JP3136421B2 - Cetylpyridinium stabilizer - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

This invention relates to cetylpyridinium stabilizers.

[0002]

2. Description of the Related Art Cetylpyridinium is a substance known as an antibacterial agent. It is also known that stability can be obtained by keeping the substance weakly alkaline in order to stabilize the substance.

[0003]

Generally, cetylpyridinium chloride needs to be weakly alkaline for its stability. However, in the presence of a fragrance, coloring occurs. The objective was to obtain a stabilizer that can be used in a weakly acidic region that can simultaneously satisfy color suppression and stabilization, and was completed as a result of earnest research. .

[0004]

SUMMARY OF THE INVENTION The present invention relates to vanillin ,
Selected from ruvanillin, isovanillin and orthovanillin
At least one type (hereinafter referred to as vanillin)
C) as an active ingredient, and a cetylpyridinium stabilizer usable in a weakly acidic region.

[0005]

[0006] The amount of vanillin is not limited as long as it is incorporated in an effective amount.
Usually, 0.3 to 5 parts by weight of vanillin can be added to 1 part by weight of cetylpyridinium. In the present invention, cetylpyridinium refers to a salt or a derivative thereof. The stabilizer of the present invention can be used in oral compositions, various cosmetics, pharmaceuticals, and the like, but is not limited thereto.

In obtaining an oral composition using the stabilizer of the present invention, appropriate components are used depending on the type of the oral composition. For example, in toothpastes such as toothpaste, powder toothpaste, water toothpaste, mouthwash, etc., abrasives, binders, thickeners, foaming agents, flavors, sweeteners, preservatives, medicinal ingredients, etc. can be added. The components of geraniol denatured alcohol, octaacetyl sucrose denatured alcohol,
Phenyl ethyl alcohol denatured alcohol, brucine denatured alcohol, linalool denatured alcohol, diethyl phthalate denatured alcohol, linalool acetate denatured alcohol, benzyl acetate denatured alcohol, 10
% Denitenium benzoate alcohol solution denatured alcohol, sodium N-acyl-L-glutamate, ascorbic acid, allantoinchlorohydroxyaluminum, sodium alginate, aloe extract, benzoic acid,
Sodium benzoate, titanium mica, ethanol, ethylenediaminetetrapolyoxyethylene polyoxypropylene, disodium edetate, tetrasodium edetate dihydrate, zinc chloride, sodium chloride, alkyldianoethylglycine hydrochloride, chlorhexidine hydrochloride, pyridoxine hydrochloride, Eugenol, Orgon extract, γ-oryzanol, kaolin, brown algae extract, carrageenan, carboxyvinyl polymer, sodium carboxymethylcellulose, hydrous amorphous silicon oxide, licorice extract, dried aluminum hydroxide gel, agar, diluted hydrochloric acid, xanthan gum, guaiazulene, citric acid, citric acid Sodium acid,
Glycerin, glycyrrhizic acid and salts thereof, chlorhexidine gluconate, gunjou, aluminum magnesium silicate, sodium silicate, soft calcium carbonate, cinnamon alcohol, cinnamaldehyde, crystalline cellulose, N-softened bovine fatty acid acyl-sodium L-glutamate, Synthetic sodium magnesium silicate, wheat germ oil, saccharin, saccharin sodium, methyl salicylate, aluminum oxide, titanium oxide, sicon extract, heavy calcium carbonate, tartaric acid, distilled peppermint water, sucrose fatty acid ester, glycerin monostearate, Aluminum hydroxide, sodium hydroxide, sodium N-stearoyl-L-glutamate, stevia extract, spearmint oil, purified water, sage extract, sodium cetyl sulfate, soap Earth, gelatin, sodium cellulose glycolate, sorbitol, potassium sorbate,
Talc, sodium bicarbonate, thymol, sodium dehydroacetate, sodium copper chlorophyllin, sodium lactate, lactose, glycerin, sucrose, peppermint oil, calcium hydrogen phosphate for dentifrice, isobutyl parahydroxybenzoate, isopropyl paraoxybenzoate, ethyl paraoxybenzoate, Butyl paraoxybenzoate, propyl paraoxybenzoate, methyl paraoxybenzoate, hydroxyethyl cellulose, calcium pyrophosphate, 1,3-butylene glycol, glucose, propanol, propylene glycol, bentonite, sodium polyacrylate,
Polyethylene glycol 300, polyethylene glycol 400, polyethylene glycol 1500, polyethylene glycol 6000, polyoxyethylene hydrogenated castor oil, polyoxyethylene stearyl ether, polyoxyethylene cetyl ether, polyoxyethylene (2
00) polyoxypropylene glycol (70), polyvinylpyrrolidone, sodium polyphosphate, d-borneol, microcrystalline wax, maltitol, beeswax, myristic acid diethanolamide, anhydrous ethanol, anhydrous citric acid, anhydrous silicic acid, anhydrous aluminum silicate , Anhydrous sodium pyrophosphate, methylcellulose, 1-menthol, dl-menthol, sorbitan monooleate, polyoxyethylene sorbitan monooleate (addition of 20 mol), polyoxyethylene sorbitan monopalmitate (addition of 20 mol), monolauric acid Sorbitan, polyoxyethylene sorbitan monolaurate (20 mole addition), coconut oil fatty acid diethanolamide, eucalyptus oil, lauryl sulfate diethanolamide,
Examples thereof include liquid paraffin, sodium monohydrogen phosphate, sodium dihydrogen phosphate, trisodium phosphate, calcium hydrogen phosphate, magnesium phosphate, and fragrance. Pharmaceutical ingredients include dextranase, lytic enzyme (lysozyme chloride, etc.), mutanase, sorbic acid, alexidine, hinokitiol, cetylpyridinium chloride, alkylglycine, alkyldiaminoethylglycine salt, allantoin, β-aminocaproic acid, tranexamic acid, azulene, vitamin E, sodium monofluorophosphate,
An active ingredient such as sodium fluoride, cuprous fluoride, a water-soluble primary or secondary phosphate, or a quaternary ammonium compound can also be blended. And as a crude drug extract,
Cherry, spinach, ryukyu, pea, cashew, kuromoji, nantenjitsu, sanzan, buttonhi, koju, onji, kyounin, tonin, perilla, ginseng, ginseng, rhododendron, rhubarb, akamegashiwa,
Extracts such as gennoshoko, fennel, fennel, and dwarf can also be used. Further, components such as coating agents, mouthwashes, mouth fresheners, drinks and the like are appropriately compounded according to the properties of the products.

[0008]

According to the present invention, as described above, vanillin can exert an extremely excellent effect on the stability of cetylpyridinium. This seems to be due to the fact that the phenol site of vanillin acts on stabilization of cetylpyridinium.

[0009]

EXAMPLES The stabilizers and oral compositions of the present invention are described in detail below based on Examples and Test Examples, but the present invention is not limited to these Examples.

Examples 1 to 10 The components were mixed at the mixing ratios shown in Table 1 below, and the pH was adjusted to be weakly acidic. The oral composition of the present invention was obtained by a conventional method.

[0011]

[Table 1]

Stability test method Ethyl vanillin of varying concentrations was added to a preparation containing a fruit flavor and a preparation not containing a fruit flavor (Base). Each of these was placed in a glass vial (10 cc) and sealed with a butyl rubber stopper.
After the heat treatment for an hour, the stability of cetylpyridinium chloride was confirmed by HPLC (liquid high performance chromatography), and the results are shown in Table 2.

[0013]

[Table 2]

Note: The composition of the above conc is a 1% aqueous solution of ethanol containing 0.01% w / v of cetylpyridinium chloride and adjusted to pH 6.5.

Consideration From the above results, it is clear that if ethyl vanillin is 3 mg / 100 ml or more, cetylpyridinium chloride can be stabilized even if the preparation has a pH of 6.5. 1%
Thus, it was confirmed that cetylpyridinium chloride exerted an antiseptic effect even at a low concentration, and an extremely excellent preparation was obtained.

[0016]

As described above, the present invention stabilizes cetylpyridinium in a weakly acidic region by containing vanillin as an active ingredient, and stabilizes cetylpyridinium. Preservative efficacy can be maintained, so that only one alcohol in the formulation
%, A very excellent preparation can be obtained even at a low concentration of 0.1%.

Continuation of the front page (56) References JP-A-4-75427 (JP, A) JP-A-59-5109 (JP, A) JP-A-60-142912 (JP, A) JP-A-60-255717 (JP) JP-A-3-127718 (JP, A) JP-A-1-305022 (JP, A) JP-A-4-124123 (JP, A) (58) Fields investigated (Int. Cl. ⁷ , DB Name) C07D 213/00-213/20 A61K 7/00-7/22

Claims (2)

(57) [Claims] 1. Vanillin , ethyl vanillin, isovanillin
A cetylpyridinium stabilizer which can be used in a weakly acidic region, comprising as an active ingredient at least one selected from the group consisting of butane and orthovanillin . 2. Cetylpyridinium is converted to vanillin and ethyl.
Selected from vanillin, isovanillin and orthovanillin
A composition for oral cavity characterized by being blended with at least one of the following.