JPH03279313A - External preparation of skin - Google Patents

Abstract

PURPOSE:To obtain an external preparation of skin having increased stability to discoloration, excellent beautifying effects and high safety, by blending sodium hydrogensulfite with a tranexamic acid. CONSTITUTION:(A) Sodium hydrogensulfite is blended with (B) a tranexamic acid (trans-4-aminomethylcylohexane-1-carboxylic acid) or a salt thereof (e.g. Mg salt, K salt or sulfate) or a derivative thereof (e.g. vitamin ester or phenyl ester) or a mixture thereof. The amount of the component A blended is 0.0001-1 pt.wt., preferably 0.001-1 pt.wt. based on 1 pt.wt. component B and the amount of the component B blended is 0.1-30wt.%, preferably 1-20wt.% based on total amounts of the external preparation.

Description

Detailed Description of the Invention [Industrial Application Field] The present invention improves the stability against coloring of external skin preparations containing tranexamic acid, salts thereof, derivatives thereof, or mixtures thereof, and further improves the whitening effect. The present invention relates to a topical skin preparation that has excellent properties and is highly safe.

[Conventional technology]

The chemical name of tranexamic acid is trans-4-aminomethylcyclohexane-1-carboxylic acid, and it has the effect of suppressing melanocyte activation factors that are involved in the production of melanin pigment, which causes skin blemishes and freckles. Has a whitening effect. Utilizing this effect, patents have been disclosed for external preparations for skin containing tranexamic acid or its derivatives as active ingredients. (JP-A No. 1-93519, JP-A No. 1-186811, etc.) [Problems to be solved by the invention] Problems of the prior art However, tranexamic acid, its salts, and its derivatives cannot be blended into the base material of the preparation. When stored under conditions of exposure to sunlight or at high temperatures, it begins to become colored, and the degree of coloration tends to increase over time and turn brown. It is inevitable that this coloring will reduce the commercial value.Purpose of the InventionThe present inventors have developed various organic acids, e.g. As a result of various studies on citric acid, tartaric acid, sodium hydrogen sulfite, ammonium sulfite, potassium sulfite, sodium sulfite, calcium sulfite, etc., we found that sodium hydrogen sulfite has an excellent coloring prevention effect, and in particular, sodium hydrogen sulfite PH4
It has been found that coloring can be significantly prevented by using it in the weakly acidic to neutral range of 7 to 7, and the present invention has been completed.

[Means to solve the problem]

That is, the present invention is an external skin preparation characterized by blending sodium bisulfite with tranexamic acid, a salt thereof, a derivative thereof, or a mixture thereof.

Hereinafter, the configuration of the present invention will be explained in detail.

Tranexamic acid, its salts, and its derivatives used in the present invention are generally used as antiplasmin agents, and are known as components characterized by high safety in cosmetic applications.

(Patent application 1973-36980) Also, the manufacturing method is patented in the second patent.
No. 40611, Patent No. 242664, Patent No. 4804
No. 11, Japanese Patent No. 488168, etc. Tranexamic acid is a white crystal or powder with a melting point of 262-267° C1, no odor, and a bitter taste. Commonly used salts of tranexamic acid include metal salts such as Mg and Ca5K, sulfates, etc., and derivatives include vitamin A acid ester, vitamin A ester, vitamin E ester,
Examples include, but are not limited to, vitamin esters such as vitamin C ester and vitamin D ester, phenyl esters, N,N-maleoylminotranexamic acid, and the like.

The amount of sodium bisulfite to be blended in the skin external preparation according to the present invention is from o, oooi to 1 part by weight, preferably 0.001 part by weight, per 1 part by weight of tranexamic acid, its salts, or its derivatives, or a mixture thereof. ~0
．． It is 1 part by weight.

Further, the amount of tranexamic acid, salts thereof, derivatives thereof, or mixtures thereof used in the present invention, based on the total amount of the skin external preparation, is usually 0.1 to 30% by weight,
Preferably it is 1 to 20% by weight.

In addition to the above-mentioned essential components, the external skin preparation of the present invention contains various components commonly used in cosmetics, pharmaceuticals, etc., namely, an aqueous component, a powder component, a surfactant, a humectant, a thickener, an ultraviolet absorber, and a color. Agents, fragrances, skin nutrients such as tocopherol acetate, bantothenyl ethyl ether, glycyrrhizinate, etc. can be used within the range that does not impair the effects of the present invention.

The formulation for external use on the skin of the present invention may be in any form, such as a solubilized system such as a lotion, an emulsified system such as a milky lotion or a cream, or an ointment or a dispersion.

〔Effect of the invention〕

The external skin preparation of the present invention is an excellent skin preparation for preventing discoloration of tranexamic acid, its salts, and its derivatives over time, which have whitening effects.

〔Example〕

Next, the present invention will be explained in detail with reference to Examples.

The present invention is not limited thereby.

Coloration prevention effect test In the serum formulation of Example 1 shown below, the amount of sodium bisulfite added was A (0%), B (0°01%), C (
0.03%), and these samples were placed in a constant temperature bath at 60°C.
After leaving it for a month, the 3M color computer (model
5M-4) (Suga Test Instruments Co., Ltd.) to measure ΔE. Note that the reference value used was the value measured on the day of trial production. The results are shown in Table-1.

Example 1 Beauty serum Weight % (A) 95% ethanol 10.0 Polyoxyethylene (20) 1.0 Oleyl ether pantothenyl ethyl ether 0. 1 Methylparaben 0.15 (B) Potassium hydroxide 0. 1(C) Glycerin 5.0 Dipropylene glycol 10.0 Sodium bisulfite
0.03 tranexamic acid
7.0 Carboxyvinyl polymer 0.2 Purified water Production method> Dissolve A and C uniformly, and add A to C to solubilize. B was added in pairs to obtain the serum of the present invention.

Table 1 As can be seen from Table 1, the serum of the present invention was not colored and had excellent stability.

Example 2 Cream (A) Setanol Microcrystalline wax Petrolatum Squalane Cetyl isooctanoate Weight % Jojoba oil 2.0 Polyoxyethylene (20) 2.0 Sorbitan monolaurate Tocopherol acetate 0.05 Bantothenyl ethyl ether 0. 1 fragrance
0.3 ethylparaben
0.3(B) Tranexamic acid salt 5. 0 Sodium bisulfite 0.011.3-Butylene glycol 5. 0 propylene glycol 5. 0 glycyrrhizic acid
0.05 monoammonium salt purified water Dissolve the remaining oil phase A at 70°C. Aqueous phase part B was dissolved at 70°C, A was mixed with B, and after emulsifying with an emulsifier, the emulsion was cooled to 30'C with a heat exchanger to obtain the cream of the present invention.

Example 3 Emulsion (A) Stearic acid peace wax Vaseline Deodorized lanolin Evening primrose oil Isopropyl myristate Polyoxyethylene (60) Hydrogenated castor oil Tocopherol acetate Ethyl paraben Butyl paraben Fragrance (B) Sodium salt of tranexamic acid Sodium bisulfite Glycerin Sodium hyaluronate Carboxyvinyl polymer weight% 10° Potassium hydroxide 0.2 Purified water
The remaining oil phase A is dissolved at 70°C. Aqueous phase part B was dissolved at 70°C, A was mixed with B, and after emulsifying with an emulsifier, the emulsion was cooled to 30°C with a heat exchanger to obtain an emulsion of the present invention.

Example 4 Packed tranexamic acid sodium bisulfite Polyvinyl alcohol (saponification degree 90, polymerization degree 2000) 95% ethyl alcohol Glycerin Olive oil Tocopherol acetate Ethyl paraben Fragrance Purified water Weight % 3.0 0.3 13.0 7, O 1Ol 0 3. 0 0.2 0.2 0.2 Production method> Each component was heated and mixed at 80°C to obtain a pack of the present invention.

Example 5 Two-layer lotion Weight % tranexamic acid 1. 0 Sodium bisulfite o, ooi95% ethanol
10.0 Polyoxyethylene (20)-2-octyldodecyl ether 1. 0 citric acid
0.01 Sodium citrate
0.09 kaolin
0. 2 Bengala
0. 5 Glycyrrhizic acid 0.
05 Monoammonium salt methylparaben 0. 2 fragrance
0. 1 purified water
Remaining manufacturing method> Same as Example 1.

Examples 2 to 5 all showed excellent stability without coloring even after being left in a constant temperature bath at 60°C for one month.
It had an excellent whitening effect.

Claims (3)

[Claims] (1) A skin external preparation characterized by containing sodium bisulfite and tranexamic acid or its salts, or a derivative thereof, or a mixture thereof. (2) The content of sodium bisulfite in the skin external preparation is 0.0001 to 1 part by weight of tranexamic acid or its salts, or its derivatives, or a mixture thereof.
The skin external preparation according to claim 1, which is in parts by weight. (3) The skin external preparation according to claim 1, wherein the content of sodium bisulfite in the skin external preparation is 0.001 to 1 part by weight per 1 part by weight of tranexamic acid, its salts, its derivatives, or mixtures thereof. .