JPH0920611A - Skin preparation for external use - Google Patents

Abstract

PURPOSE: To obtain a skin preparation for external use excellent in the prevention and the improvement of rough skin and further having beautifying effect by concomitantly using specific two different materials excellent in safety. CONSTITUTION: One or more than one kind selected from tranexamic acid, its salts and its derivatives is compounded with nordihydroguaiaretic acid of the formula. Tranexamic acid, its salt or its derivative and nordihydroguaiaretic acid of the formula are preferably compounded in 0.1-5.0wt.% and 0.1-5.0wt.%, respectively. This skin preparation for external use is extremely effective against proliferative pachymenia, dry skin associated with erythema and a desquamative change of skin condition, and further effectively prevents and improves pigmentation. An example of the salt of tranexamic aid is its salt of a metal such as Mg, Ca or K or its sulfate, etc. The example of the derivative is a vitamin ester such as a vitamin A ester.

Description

Detailed Description of the Invention

[0001]

FIELD OF THE INVENTION The present invention relates to a skin external preparation. More specifically, the present invention relates to a highly safe external preparation for skin which prevents and improves rough skin and has an excellent whitening effect on the skin.

[0002]

2. Description of the Related Art Various external medicines have been incorporated into external preparations for skin. Among them, the skin roughening prevention and skin roughening improving effects are also one of the medicinal effects required of external skin preparations, and the external skin preparations such as cosmetics for this purpose have been demanded. Under these circumstances, various raw materials extracted from natural products, such as proteins, polysaccharides, extracted extracts, and natural polymers, have conventionally been blended in the skin external preparation because of their characteristic use effects.

A whitening effect is also one of the medicinal effects required for external preparations for skin. Although there are some unclear points regarding the mechanism of skin stains and the like, in general, melanin pigment is formed due to hormonal abnormalities and irritation of ultraviolet rays from sunlight, and this causes abnormal deposition in the skin. It is thought to do. Such a method for treating spots and bruises includes a substance that suppresses the production of melanin, for example, a method of administering a large amount of vitamin C, a method of injecting glutathione, etc., or an ointment, cream, lotion of L-alcorbic acid, cysteine, etc. In such a form, a method of applying it locally is adopted.

[0004]

However, the effect is not sufficient, and there has been a long-awaited development of a skin external preparation having more excellent effect.

In view of the above circumstances, the inventors of the present invention have earnestly studied in order to obtain a substance that is excellent in the effect of preventing rough skin and improving rough skin, and also having a whitening effect, among substances having excellent safety. As a result of overlapping, by blending one or more selected from tranexamic acid, or a salt thereof, or a derivative thereof, and nordihydroguaiaretic acid, proliferative epidermal thickening, dryness with erythema, and desquamation It was found that a skin external preparation that is extremely effective against changes in the above-mentioned and that can also effectively prevent and improve pigmentation is obtained, and completed the present invention.

An object of the present invention is to provide an external preparation for skin which is excellent in the effects of preventing rough skin and improving rough skin, and also has a whitening effect.

[0007]

That is, the present invention is characterized by containing nordihydroguaiaretic acid and one or more selected from tranexamic acid, salts thereof, or derivatives thereof. An external preparation for skin is provided.

The present invention also contains 0.1 to 5.0% by weight of one or more selected from the above tranexamic acid, salts thereof, or derivatives thereof, and the above nordihydroguaiaretic acid. 0.01 to 5.0
The external preparation for skin according to the above is characterized in that it is contained in a weight percentage.

The structure of the present invention will be described in detail below. Tranexamic acid used in the present invention, or a salt thereof,
Alternatively, a derivative thereof is generally used as an antiplasmin agent and is known as a component characterized by high safety in cosmetic use (JP-A-42-369).
No. 80).

The manufacturing method is disclosed in Japanese Patent No. 230611.
Japanese Patent, Japanese Patent No. 242664, Japanese Patent No. 48041
It is known from Japanese Patent No. 1 and Japanese Patent No. 488168.

Tranexamic acid has a melting point of 386-390.
C, white crystals or powder, odorless, taste bitter. The salt of tranexamic acid is Mg, which is a commonly used salt.
There are metal salts such as Ca and K, sulfates, and the like, and as the derivatives, vitamin esters such as vitamin A ester, vitamin E ester, vitamin C ester, and vitamin D ester, and N, N-maleoylminotranexamic acid. However, the present invention is not limited thereto.

In the present invention, the above tranexamic acid,
Alternatively, one kind or two or more kinds are arbitrarily selected and used from the salts or the derivatives thereof, and the compounding amount thereof is preferably 0.01 to 10.0% by weight in the total amount of the external preparation for skin, and 0.1% by weight is preferable. It is more preferably ˜5.0% by weight. 0.0
If the amount is less than 1% by weight, the effect of preventing and improving skin roughness and the whitening effect of the present invention cannot be sufficiently obtained, and if the amount exceeds 10.0% by weight, no further effect can be obtained.

The nordihydroguaiaretic acid used in the present invention is a substance represented by the following formula.

Embedded image

The above-mentioned nordihydroguaiaretic acid is
Generally, it is a substance known as an antioxidant or a lipoxygenase inhibitor. So far, it is a substance that has been applied to cosmetics, hair restorers, dentifrices, pharmaceuticals, etc. as an antioxidant of unsaturated fatty acids and a stabilizer of drugs, and for the purpose of antioxidant and drug stabilization ( Japanese Patent Laid-Open No. 4-217
626, JP 3-20205 A, JP 6
No. 1-238718, JP-A-61-238715).

In the present invention, the amount of nordihydroguaiaretic acid added to the external skin preparation is 0.01 based on the total amount of the composition.
~ 10.0% by weight is preferred, 0.01-5.0% by weight
Is more preferred. If it is less than 0.01% by weight, the effect of the present invention is not sufficient, and if it exceeds 10.0% by weight, it is not preferable in terms of formulation and it is uneconomical.

In the present invention, the above tranexamic acid,
Alternatively, the combined use of nordihydroguaiaretic acid with one or two or more selected from salts or derivatives thereof can further improve the prevention of rough skin, the improving effect and the whitening effect.

In addition to the above-mentioned essential components, the external preparation for skin of the present invention is, if necessary, within the range that does not impair the effects of the present invention, and is generally used in cosmetics, quasi drugs, pharmaceuticals, etc. Ingredients, aqueous ingredients, moisturizers, thickeners, ultraviolet absorbers, preservatives, antioxidants, fragrances, colorants, drugs, crude drugs and the like can be added.

The dosage form of the external preparation for skin of the present invention is arbitrary. For example, a solubilizing system such as lotion, an emulsifying system such as emulsion or cream, or an ointment, powder dispersion system, water-oil two-layer system. ,
Any formulation such as water-oil-powder three-layer system may be used.

[0019]

EXAMPLES Next, the present invention will be described in detail with reference to examples, but it goes without saying that the technical scope of the present invention is not limited to these examples. The blending amount in the examples is% by weight. Prior to the examples, test methods and evaluation methods used in the present invention will be described.

The effect of external skin application of the skin external preparation according to the present invention was evaluated from the improvement rate for rough skin, razor loss and pigmentation.

[Skin Roughness Improvement Effect Test] 60 lots of subjects suffering from skin roughening or hot flashes after sunburn were carried out on each of 60 subjects, and lotions having the compositions of Example 1 and Comparative Examples 1 to 3 shown in “Table 1” were applied to the face. After 2 weeks, the skin condition was visually evaluated. In addition, Example 1 and Comparative Example 1 shown in "Table 1" immediately after shaving were performed on 60 male subjects who lost razors.
A lotion having a composition of ˜3 was applied and the effect on razor loss was evaluated. Each criterion was as follows.

"Amelioration effect on rough skin" Remarkable effect: symptom disappeared Effective: symptom weakened somewhat effective: symptom slightly weakened Ineffective: symptom unchanged

"Effect of improving razor loss" Remarkable effect: razor loss of loss Effective: razor loss of weakness Some effect: razor loss of weakness Invalid: razor loss of no change

(Judgment) ⊚: The rate at which the test subject is markedly effective, effective and slightly effective (effective rate) is 80% or more. ◯: The ratio at which the test subject is markedly effective, effective and slightly effective (effective rate) is 50% or more. 〜Less than 80% △: The rate at which the subject is markedly effective, effective and slightly effective (effective rate) is 30% or more and less than 50% ×: the rate at which the subject is markedly effective, effective and slightly effective (effective rate) is 30 %Less than

[0025]

[Table 1]

[0026]

[Table 2]

As is clear from Table 2, the lotions of Example 1 of the present invention containing tranexamic acid and nordihydroguaiaretic acid are blank lotions of Comparative Example 1, Comparative Example 2 and Comparative Example 3. As a result, it showed an excellent improving effect against rough skin and razor loss.

[Effect of Roughness of Skin] Example 1 and Comparative Examples 1 to 1
A lotion of 3 was used to perform a skin roughening improvement effect test on a human body panel. That is, the skin surface morphology of a healthy female person (face) was taken using a replica method using myrisin resin, and the skin was taken and observed under a microscope (17 times). What was judged to be rough skin evaluation 1 or 2 based on the criteria shown in "Table 3" based on the condition of the skin print and the peeling condition of the stratum corneum (rough skin panel) 20
The lotions of Example 1 and Comparative Examples 1 to 3 were applied to the left and right half of the face once a day for 2 weeks. Two weeks later, the skin condition was observed again according to the above-mentioned replica method, and evaluated according to the criteria of "Table 3". The results are shown in "Table 4".

[0029]

[Table 3]

[0030]

[Table 4]

As can be seen from "Table 4", the lotion of Example 1 of the present invention was found to have a remarkable effect of improving rough skin as compared with the lotions of Comparative Examples 1 to 3.

[Pigmentation Effect and Side Effects] 8-MOP-treated phototoxic pigmentation Weiser Maple GP was used to apply 50 μl of the test sample to the shaved back once a day in the range of about 4 cm ² for 8 weeks, The four-point evaluation method (+
The evaluation score of (-) is represented by the decolorizing effect, and the evaluation score of-is represented by side effect). The sample used was an ascorbine 1% acid solution and a mixed solution of 1% tranexamic acid and 1% nordihydroguaiaretic acid (invention product). Table 6 shows the results.

[0033]

[Table 5]

[0034]

[Table 6]

As is clear from "Table 6", long-term continuous use of ascorbic acid causes pigmentation as a side effect, whereas a mixed solution of tranexamic acid and nordihydroguaiaretic acid has an excellent decolorizing effect and a long-term effect. There were no side effects from repeated use.

[Actual Use Test] As a panel of 100 subjects with facial pigmentation, 25 subjects each were allowed to use Example 1 and Comparative Examples 1 to 3 on the face 2-3 times a day. After 3 consecutive months of use, the doctor judged the lightening effect with the naked eye. As is clear from the results shown in "Table 7", the anti-pigmenting agent of Example 1 containing tranexamic acid and nordihydroguaiaretic acid was mixed in various types such as sporadic egg spots, melasma, and senile pigment spots. It was suggested that it has a remarkable effect on the pigmentation disease.

[0037]

[Table 7]

When each of the external preparations for skin was prepared by the conventional method with the compositions of Examples 2 to 6 below, good effects of preventing and improving rough skin and whitening effects were obtained.

Example 2 Skin Lotion Wt% tranexamic acid 5.0 nordihydroguaiaretic acid 0.01 glycerin 1.0 ethanol 7.0 polyoxyethylene (20 mol) oleyl alcohol ether 0.5 methylparaben 0.05 citric acid 0.01 sodium citrate 0.1 perfume 0.01 purified water balance

Example 3 Cream wt% cetostearyl alcohol 3.5 Squalane 30.0 Beeswax 3.0 Reduced lanolin 5.0 Ethylparaben 0.3 Polyoxyethylene (20 mol) oleyl alcohol ether 2.0 Stearic acid monoglyceride 2.0 Tranexamic acid 3.0 Nordihydroguaiaretic acid 3.0 Glycerin 15.0 Fragrance 0.03 Purified water balance

Example 4 Pack weight% Tranexamic acid 10.0 Nordihydroguaiaretic acid 5.0 Polyvinyl alcohol 10.9 Propylene glycol 7.0 Ethanol 10.0 Methylparaben 0.05 Perfume 0.05 Purified water balance

Example 5 Lipstick wt% Microcrystalline wax 1.0 Beeswax 2.0 Lanolin 2.0 Liquid paraffin 20.0 Squalane 10.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 mol) sorbitan monooleate 4.0 Tranexamic acid 0.5 Nordihydroguaiaretic acid 0.01 Preservative / antioxidant Appropriate amount Perfume Appropriate amount Purified water Balance

Example 6 Lotion lotion 95% Ethanol 25.0 Polyoxyethylene (40 mol) hydrogenated castor oil 4.0 Preservative / antioxidant Appropriate amount Perfume Appropriate amount Dipropylene glycol 12.0 Glycerin 5.0 Arabitol 7.0 Tranexamic acid 0.1 Nordihydroguaiaretic acid 10.0 Deionized water balance

Example 7 Lipstick wt% Microcrystalline wax 1.0 Beeswax 2.0 Lanolin 2.0 Liquid paraffin 20.0 Squalane 10.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 mol) sorbitan monooleate 4.0 Tranexamic acid 0.01 Nordihydroguaiaretic acid 0.01 Preservative / antioxidant Appropriate amount Perfume Appropriate amount Purified water Balance

[0045]

EFFECTS OF THE INVENTION The external preparation for skin of the present invention is excellent in the effects of preventing and improving rough skin, and also in the effect of whitening the skin, and is highly safe.

Continuation of the front page (51) Int.Cl. ⁶ Identification code Office reference number FI Technical display area C07C 39/16 C07C 39/16 229/46 9450-4H 229/46

Claims (2)

[Claims] 1. One or more selected from tranexamic acid, salts thereof, or derivatives thereof,
A skin external preparation containing nordihydroguaiaretic acid. 2. 0.1 to 5.0% by weight of one or more selected from the above tranexamic acid, salts thereof, or derivatives thereof, and 0.01 to 5.0 of the nordihydroguaiaretic acid. The external preparation for skin according to claim 1, which contains 5.0% by weight.