JP2906270B2 - External preparation for skin - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention relates to a storage stability comprising tranexamic acid, a salt thereof, or a derivative thereof, or a mixture thereof and one or more saponins. The present invention relates to an excellent composition, and to a skin external preparation useful in the fields of cosmetics, pharmaceuticals, quasi-drugs, and the like.

[Prior art] The mechanism of the occurrence of spots on the skin is unknown, but in general, melanin pigments are formed due to hormonal abnormalities and irritation from ultraviolet rays from sunlight. It is thought to be an abnormal deposit.

For the treatment of such spots, internal or external preparations containing a substance inhibiting the production of melanin, for example, vitamin C, glutathione, cysteine or hydroquinone are used.

However, vitamin C, glutathione, and cysteine are difficult to formulate due to problems in stability and strong odor. They also have the disadvantage that the onset of the effect is very slow. In addition, although hydroquinone is recognized as having an effect, it has sensitizing properties,
Generally, use is restricted.

The present inventors have been studying a substance having a whitening effect for many years, but tranexamic acid, or a salt thereof, or a derivative thereof is involved in the production of a melanin pigment that causes skin spots and freckles. It has been found that it has an action of suppressing melanocyte activator, and a patent is disclosed for a skin external preparation containing tranexamic acid, or a salt thereof, or a derivative thereof as an active ingredient, utilizing this action. (JP-A-1-93519)
No. 86811) [Problems to be Solved by the Invention] Problems of the Prior Art However, as a result of continued study by the present inventors, the above-mentioned tranexamic acid, or a salt thereof, or a derivative thereof was obtained under severe conditions. It was found that when stored for a long time, discoloration gradually occurred. When blended in a base such as cosmetics or pharmaceuticals, the tendency is strong.

Object of the Invention In view of the above circumstances, the present inventors have repeatedly studied for the purpose of stably incorporating these tranexamic acids, or salts thereof, or derivatives thereof into a system, and as a result, saponin which is one of the plant components Have been found to exhibit excellent effects, and have completed the present invention.

[Means for Solving the Problems] That is, the present invention relates to an external preparation for skin characterized by containing tranexamic acid, or a salt thereof, or a derivative thereof, or a mixture thereof and one or more of saponins. is there.

 Hereinafter, the present invention will be described in detail.

Tranexamic acid, a salt thereof, or a derivative thereof used in the present invention is generally used as an antiplasmin agent, and is known as a component characterized by high safety in cosmetic applications. (Japanese Patent Application No. 42-3698
0, JP-B-47-1479) and its production method is described in Japanese Patent No. 240611.
No. 242,664, 480,411 and 488,168. Tranexamic acid has a melting point of 262-267
° C, white crystals or powder, no odor, bitter taste. Tranexamic acid salts are commonly used salts such as Mg, Ca, K
Derivatives include vitamin A acid esters, vitamin A esters, vitamin E esters, vitamin C esters, vitamin D esters, and other vitamin esters, phenyl esters, and N, N-maleamino. Examples include tranexamic acid, but are not limited thereto.

In the present invention, one or two or more tranexamic acids, or salts thereof, or derivatives thereof are arbitrarily selected and used, and the compounding amount is 0.1 to 30% by weight of the total amount of the external preparation for skin, preferably 6-20% by weight.

On the other hand, saponin used in the present invention is a general term for glycosides widely distributed in the plant kingdom, and is known to produce a colloidal aqueous solution that foams like soap. Has a hemolytic effect at low concentrations, but low oral toxicity. Most saponins are amorphous powders that are soluble in water, methanol, and dilute ethanol, but are poorly soluble in other organic solvents.

In the present invention, besides using saponin, a plant extract containing saponin may be used as it is. Among saponins, particularly luffima saponin is preferred.

In the present invention, one or more kinds of saponins are used.
It is 5% by weight, preferably 0.05-1% by weight.

If the amount is less than 0.01% by weight, the effect of the present invention is not exhibited, and even if the amount exceeds 5% by weight, no further effect can be expected.

The external preparation for skin of the present invention is a general external preparation for skin, for example, a wide range such as an aqueous solution system, a solubilizing system, an emulsifying system, a powder dispersion system, a water-oil two-layer system, a water-oil-powder three-layer system, and the like. It is used for basic cosmetics such as lotions, emulsions, creams, bags, makeup cosmetics such as lipsticks and foundations, cosmetics such as hair cosmetics such as shampoos, rinses, and hair tonics; There are a wide variety of goods, including foreign goods.

The skin external preparation of the present invention, if necessary, as long as the effects of the present invention are not impaired, a humectant, a thickener, an oil, a preservative,
Emulsifiers, antioxidants, sequestering agents, ultraviolet absorbers, powders, drugs, coloring agents, fragrances and the like can be blended.

[Effects of the Invention] The skin external preparation of the present invention is a skin external preparation containing tranexamic acid, or a salt thereof, or a derivative thereof useful as a whitening agent and having good stability without discoloration over time.

[Examples] Next, the present invention will be described in more detail with reference to Examples.

In Table 1, the following formulation (Examples 1-2, Comparative Example 1)
The base was subjected to a stability test with the following lotion.

The degree of discoloration is the result of judging the sample after storage at 50 ° C for one month according to the following criteria.

(Base) Ethanol 13.0 1,3-butylene glycol 10.0 POE (polyoxyethylene, the same applies hereinafter, 15 mol) Oleyl ether 1.0 Ethylparaben 0.1 Perfume 0.05 Purified water residue (degree of discoloration) ◎ No discoloration ○ Some discoloration △ Significantly discolored × Significant discoloration Examples 1-2, Comparative Example 1 As can be seen from Table 1, the cosmetic of the present invention did not discolor and was extremely excellent in safety.

Example 3 Night Cream Weight% A. Cetanol 4.0 Vaseline 7.0 Squalane 21.0 Monoglyceride stearate 2.2 POE (20) Sorbitan monostearate 2.8 Isopropyl myristate 6.0 Ethylparaben 0.3 Perfume 0.2 B. Propylene glycol 10.0 1,3-butylene glycol 5.0 Tranexam Acid Na salt 1.0 Hetimasaponin 1.0 Purified water Residue The components of the oil phase belonging to A and the components of the water phase belonging to B are separately heated and dissolved, and the oil phase is mixed and emulsified in the water phase. Then, the mixture was cooled to room temperature to obtain a cream.

Example 4 Foundation weight% A. Cetanol 3.5 Deodorized lanolin 4.0 Jojoba oil 5.0 Vaseline 2.0 Squalane 6.0 Monoglyceride stearate 2.5 POE (60) Hardened castor oil 1.5 POE (25) Cetyl ether 1.0 Perfume 0.2 B. Glycerin 3.0 Propylene glycol 8.0 Compound powder 12.0 Tranexamic acid 0.5 Hetimasaponin 0.5 Purified water Residue (Preparation method) Heat and dissolve the oil phase component belonging to A. Separately, the components of the aqueous phase belonging to B excluding the blended powder are heated and dissolved, and the blended powder is dispersed therein. The oil phase was mixed and emulsified in the aqueous phase and cooled to room temperature to obtain a foundation cream.

Example 5 Emulsion Weight% Stearic acid 2.5 Cetanol 1.5 Vaseline 5.0 Liquid paraffin 10.0 POE (10) oleate 2.0 Propyl paraben 0.1 Tocopherol acetate 0.05 Perfume 0.2 B. Polyethylene glycol 1500 3.0 Triethanolamine 1.0 K salt of tranexamic acid 0.1 Soybean saponin 0.5 Purification Water residue (Production method) According to Example 3.

Example 6 Water-absorbing ointment Vaseline 40.0 Stearyl alcohol 15.0 Mokurou 15.0 POE (10) oleate 0.25 Stearic acid monoglyceride 0.25 Tranexamic acid 1.0 Hetimasaponin 0.1 Purified water Residue (Preparation method) According to Example 3.

Example 7 Lotion% by weight Ethanol 25.0 Propylene glycol 10.0 POE (15) Oleyl ether 1.0 Tranexamic acid 15.0 Hetimasaponin 0.5 Citric acid 0.05 Sodium citrate 0.1 Ethylparaben 0.1 Perfume 0.05 Purified water Residue (Preparation method) According to Example 1.

Examples 3 to 7 all have good aging stability.
Excellent usability and safety.

Claims (1)

(57) [Claims] 1. An external preparation for skin, comprising tranexamic acid, a salt thereof, or a derivative thereof, or a mixture thereof and one or more saponins.