JPH0470284B2 - - Google Patents

Description

[Detailed description of the invention]

[Industrial Field of Application] The present invention relates to a melanin production-inhibiting topical drug containing galactosamine or mannosamine as an active ingredient and effective in treating and preventing pigmentation such as melasma. [Prior Art] Cosmetics containing peroxides such as hydrogen peroxide and zinc peroxide have been used since ancient times to remove spots such as spots and freckles that appear on the skin.
However, since these peroxides are extremely unstable substances, they have problems in storage stability and incorporation into cosmetic bases, and furthermore, they do not have sufficient skin-whitening effects. In addition, vitamin C, cysteine,
Cosmetics containing colloidal sulfur and the like have come to be used for the purpose of fairing the complexion, but their effects have not yet been fully satisfactory. Furthermore, fair skin cosmetics using kojic acid (Special Publications 1986)
-18569 Publication), ointments for suppressing melanin production using kojic acid (Japanese Patent Publication No. 10447, 1983), skin-fairing cosmetics containing kojic acid derivatives (Japanese Patent Publication No. 18569),
No. 60801, Special Publication No. 61-60802, Japanese Patent Publication No. 79616 (1982)
Publications, etc.) have been disclosed. In addition, fair skin cosmetics containing quercetin and flavonol compounds (JP-A-55-92305, JP-A-55-111410, JP-A-55-111411, JP-A-55-143908, etc.) have been disclosed. has been done. Furthermore, skin whitening cosmetics containing placenta extract (Japanese Patent Publication No. 48-30370), melanin production inhibiting external preparations containing vitamin E and kojic acid (Japanese Patent Application Laid-open No. 62-178506), vitamin E in water It has also been disclosed that the compound can be dissolved in whitening cosmetics and used in whitening cosmetics (Japanese Patent Application Laid-Open No. 75421/1983). On the other hand, cosmetics containing amino sugars and N-acetylamino sugars have a smooth feeling on the skin, a moisturizing feeling, a softening effect, and a skin revitalizing effect (Japanese Patent Laid-Open No. 59
-13708), skin-lightening cosmetics containing glucosamine and acylated glycosamine derivatives (JP-A-13708),
36306), and a cosmetic containing N-alkylamino sugar sugar alcohol that provides a smooth feeling on the skin, a moisturizing feeling, a softening effect, and a skin revitalizing effect (Japanese Patent Application Laid-open No. 59-212419). ing. [Problems to be Solved by the Invention] In the conventional technology, among the ingredients used in skin-lightening cosmetics, peroxide has the effect of directly reducing and bleaching pigments such as melanin produced on the skin, and has not been used in excessive amounts. When used, there was a risk that the natural color of the skin would be bleached and the skin would turn white. In addition, kojic acid, flavonol, vitamin E, etc. directly inhibit the production of melanin in cells, and are useful drugs that produce a skin-whitening effect, but their formulation methods have been problematic. [Means for Solving the Problems] The present inventor has researched the melanin production inhibiting effect of galactosamine and mannosamine, which are known as substances that give the skin a smooth feel, a moisturizing feeling, and a softening effect. About Access When we investigated B16 cells derived from mouse melanoma, we found that galactosamine and mannosamine significantly suppressed melanin production in B16 cells. The invention has been completed. The present invention provides galactosamine or its salts and/or
Alternatively, it is an external melanin production suppressing drug containing mannosamine or its salts as an active ingredient. The salts of mannosamine and galactosamine, which are the active ingredients of the present invention, include hydrochloride, sulfate, nitrate, phosphate, etc., and hydrochloride is preferred. The topical drug of the present invention can be applied to the affected area in the form of an emulsion, lotion, liniment, ointment, or the like to treat or prevent pigmentation caused by melasma. The topical drug of the present invention contains the active ingredients galactosamine and mannosamine alone or as a mixture in an emulsion,
Using bases and auxiliary agents commonly used in the preparation of lotions, liniments, ointments, etc.
It can be obtained by conventional formulation methods. The content of the active ingredient of the present invention is 0.001 to 20% (weight), preferably 0.01 to 10%, based on the total amount of the external preparation.
(weight). Test examples showing the inhibition of melanin production by the melanin production-inhibiting topical drug of the present invention will be given below. Test Example 1 0.50 mg/ml and 0.25 mg/ml concentrations of D-mannosamine, D-galactosamine, D-mannosamine hydrochloride, and D-galactosamine hydrochloride were added to a mouse melanoma-derived B16 cell (hereinafter abbreviated as B16 cell) solution. were added to the culture medium, the cells were cultured at 37°C for 5 days, and the number of cells was measured. Thereafter, the degree of blackness (degree of melanin production) of each cell pellet was observed with the naked eye. As controls, N-acetyl-D-glucosamine, glucosamine (a known melanin production inhibitor) and N-acetyl-D-mannosamine, N-
Acetyl-D-galactosamine (a similar compound to the active ingredient of the invention) was added at a similar concentration and the same test was performed. In addition, as a control, a similar test was conducted on a sample to which no active ingredient was added. The test results were as shown in Table 1 below.

〔Example〕

Example 1 (Emulsion) Weight part A Polyoxyethylene glycol monostearate (40E.O.) 2.00 Self-emulsifying glyceryl monostearate 5.00 Stearic acid 5.00 Behenyl alcohol 1.00 Liquid paraffin 1.00 Glyceryl trioctanoate 10.00 Preservative Appropriate amount Flavor Trace amount B 1 , 3-butylene glycol 5.00 Galactosamine 0.50 Purified water Residual The components belonging to A are dissolved by heating (oil phase). Separately,
Components belonging to B are dissolved by heating (aqueous phase). The aqueous phase was added to the oil phase, emulsified with stirring, and then cooled to obtain an emulsion. Example 2 (Lotion agent) Part by weight polyoxyethylene hydrogenated castor oil (60E.O.) 1.00 Ethanol 15.00 Citric acid 0.10 Sodium citrate 0.30 1,3-butylene glycol 4.00 Mannosamine hydrochloride 0.05 Preservative Appropriate amount Flavoring Trace amount Purified water Residual Each component was uniformly stirred and mixed and dissolved to obtain a lotion agent. Example 3 (Ointment) Weight part A Polyoxyethylene sorbitan monostearate (60E.O.) 1.00 Polyoxyethylene sorbitan tetraoleate (60E.O.) 1.00 Rensorbitan (60E.O.) 1.50 Self-emulsifying mono Glycerin stearate 1.50 White beeswax 2.00 Paraffin 2.00 Stearic acid 3.00 Behenyl alcohol 3.00 Liquid paraffin 5.00 Preservatives Appropriate amount Fragrance Trace amount B 1,3-butylene glycol 5.00 Citric acid 0.30 Mannosamine 1.00 Purified water Remaining Dissolve the ingredients belonging to A by heating ( oil phase ). Separately,
Components belonging to B are dissolved by heating (aqueous phase). The aqueous phase was added to the oil phase, stirred and emulsified, and then cooled to obtain an ointment. [Effects of the Invention] As described above, the present invention is a useful invention that provides an extremely excellent melanin production-inhibiting topical drug that has almost no cytotoxicity and significantly inhibits melanin production.

Claims (1)

[Claims] 1. An external melanin production suppressing drug characterized by containing galactosamine or its salts and/or mannosamine or its salts as an active ingredient.