JPH04305509A - External preparation for skin - Google Patents

Abstract

PURPOSE:To provide an external preparation for skin, effective for activating dermatic metabolism and increasing the viscoelastic property of the skin, having excellent skin-protecting and moisture-retaining properties, giving moderate moistness and springiness to the skin and having excellent effect to improve chapped skin. CONSTITUTION:The external preparation for skin having the above effects can be produced by using (A) urea and (B) tranexamic acid, its salt (salt of metal such as Na, Mg, Ca or K, sulfate, etc.), its derivative (vitamin A acid ester, vitamin esters such as vitamin A, C, D or E ester, phenyl ester, N,N- maleoylminotranexamic acid) or their mixture as essential components. The amount of the component A is 0.1-30wt.% (preferably 1-10wt.%) and that of the component B is 0.1-30wt.% (preferably 6-20wt.%) based on the total amount of the external preparation.

Description

[Detailed description of the invention]

0001

[Industrial Application Field] The present invention relates to a novel skin preparation for external use, and more specifically, it has the effect of activating skin metabolism, increasing skin elasticity, and having excellent effects on skin protection and moisture retention. The present invention relates to a skin preparation for external use that provides moisture and has an excellent effect on improving rough skin.

0002

[Prior Art] Urea exists in living organisms, and as a result of changing the polybesotide of proteins, it increases the possibility of antibacterial effects, proteolytic alteration effects, decreases hydration, that is, enhances water retention ability, etc. on the skin. It has chemically important pharmacological effects,
It is used as a treatment for keratosis, and when incorporated into cosmetics, it has the effect of protecting the skin by retaining amino acids suitable for the skin, its moisturizing effect, cell activation effect, and wound healing effect. etc. are expected.

0003

[Problems to be Solved by the Invention] Prior Art However, when urea is added alone to external skin preparations, its expected effects are still not sufficient, and therefore, increasing the amount of urea added to external skin preparations results in It has disadvantages such as having an adverse effect on stability and causing stickiness.

Purpose of the Invention In view of the above circumstances, the present inventors conducted extensive research and found that an external preparation for skin containing urea and tranexamic acid, its salts, or derivatives thereof has a high water retention property. It has been found that the skin increases synergistically, makes the skin smooth, provides appropriate "moisturization" and "firmness," and also has the effect of improving rough skin.Based on these findings, the present invention was completed.

[0005]

[Means for Solving the Problems] That is, the present invention is an external preparation for skin, which is characterized in that it contains urea and tranexamic acid, a salt thereof, a derivative thereof, or a mixture thereof.

The configuration of the present invention will be explained in detail below. As the urea used in the present invention, any commercially available urea may be used.

[0007] The blending amount is generally 0.1 to 30% by weight, preferably 1 to 10% by weight based on the total amount of the skin external preparation. If the amount is less than 0.1% by weight, the effect of the present invention will not be fully exhibited, and if it exceeds 30% by weight, crystal precipitation of urea will likely occur, and no substantial increase in the effect can be expected.

[0008] Tranexamic acid, its salts, or its derivatives used in the present invention are generally used as anti-plasmin agents, and are known as components characterized by high safety in cosmetic applications. (Special request 1977
-36980) The manufacturing method thereof is also known from Japanese Patent No. 240611, Japanese Patent No. 242664, Japanese Patent No. 480411, and Japanese Patent No. 488168.

Tranexamic acid has a melting point of 262-267°C,
It is a white crystal or powder with no odor and a bitter taste. Commonly used salts of tranexamic acid include Na, Mg,
There are metal salts such as Ca and K, sulfates, etc., and derivatives include vitamin A acid esters, vitamin A esters, vitamin E esters, vitamin C esters, vitamin D esters and other vitamin esters, phenyl esters, N,
Examples include N-maleoylminotranexamic acid,
It is not limited to these.

[0010] In the present invention, one or more of the above tranexamic acid, its salts, or its derivatives are arbitrarily selected and used, and the blending amount is as follows:
The amount is 0.1 to 30% by weight, preferably 6 to 20% by weight, based on the total amount of the skin external preparation. If the amount is less than 0.1% by weight, the effect of the present invention will not be fully exhibited, and even if it is added in excess of 30% by weight, no substantial increase in the effect can be expected.

In addition to the above-mentioned essential components, the external skin preparation of the present invention may optionally contain other ingredients commonly used in the pharmaceutical and cosmetic fields, such as edetic acid, di-, tri-, or tetrasodium, and sodium citrate. , sodium metaphosphate, sequestering agents such as sodium metaphosphate, acid inhibitors such as butylated hydroxytoluene (BHT), propyl gallate, dl-α-tocopherol,
Surfactants, ultraviolet absorbers, fragrances, water, alcohols such as ethanol and isopropanol, thickeners, coloring agents, powders, drugs, organic acids such as citric acid and malic acid, and inorganic acids such as phosphoric acid, etc. It can be used within a range that does not impair the effects of the invention.

[0012] The dosage form of the skin external preparation of the present invention is arbitrary;
Any dosage form may be used, such as solution type, solubilized type, emulsion type, powder dispersion type, water-oil two-layer type, water-oil-three-layer type, etc.

[0013] Furthermore, the use of the external skin preparation of the present invention is arbitrary, and it can be used for facial or body skin preparations such as lotions, emulsions, creams, and packs, and for hair such as hair tonics, hair creams, shampoos, and hair rinses. It can be used in external preparations for the skin.

[0014]

[Effects of the Invention] The skin external preparation of the present invention contains tranexamic acid, its salt, and its derivatives in urea, so it activates skin metabolism, increases the skin's viscosity and elasticity, and has skin protection and moisture retention properties. It is an external preparation for the skin that provides moderate moisture and firmness to the skin, and is also excellent in improving rough skin.

[0015]

[Examples] Next, the present invention will be specifically explained with reference to Examples. The present invention is not limited thereby. The blending amount is in weight%.

[0016]

[Practical test] 80 women were divided into four groups each to form a panel. The following Examples 1 to 3 and Comparative Examples 1 to 3 are used as samples.
3 was used.

The first group received the lotions of Example 1 and Comparative Example 1, the second group received the creams of Example 2 and Comparative Example 2, and the third group received the lotions of Example 3 and Comparative Example 3. Tested using water.

Twice a day, in the morning and at night, after washing the face, an appropriate amount of the cosmetic of the example was applied to the left side of the face, and the cosmetic of the comparative example was applied to the right side of the face for two weeks. The evaluation determined the effectiveness of the following four items. The results are shown in Table 1~
It is shown in Table 6.

Example 1 Lotion

Weight% ethanol

8.0 2-pyrrolidone-5
−
2.0
Sodium carboxylate polyoxyethylene (20 mol)
1.8 Oleyl alcohol ether tranexamic acid

0.1 Urea


0.5 Pullulan

0.05 Jojoba oil

0.5
caustic potash

0.015 EDTA-3Na

0.01 fragrance

0.
1 Ion exchange water

Remaining amount Manufacturing method A lotion was manufactured using a conventional method.

Comparative Example 1 Chemical water

Weight% ethanol

8.0 2-pyrrolidone-5
−
2.0
Sodium carboxylate polyoxyethylene (20 mol)
1.8 Oleyl alcohol ether urea

0.5 Pullulan

0.05 Jojoba oil

0.5 caustic potash

0.01
5 EDTA-3Na

0.01 fragrance

0.1 Ion exchange water
Remaining amount
Manufacturing method A lotion was manufactured using a conventional method.

Example 2 Cream

Weight% 1,3-butylene glycol

5.0 Polyethylene glycol 4000

1.0 Glycerin

2.0 Squalane

20.0 Vaseline

5
．． 0 Cetostearyl alcohol

3.0 Polyoxyethylene (20 mol)
1.
5 Oleyl alcohol ether glyceryl monostearate
1.5 Sodium salt of tranexamic acid
0.1
urea

0.5 Sodium lactate

2.0 Xanthan gum (Keltrol brand name)
0.05 Methylparaben

0.1 Ethylparaben
0.
2 EDTA-3Na

0.01 fragrance

0.2 Ion exchange water
Remaining amount
Manufacturing method A cream was manufactured using a conventional method.

Comparative Example 2 Cream

Weight% 1,3-butylene glycol

5.0 Polyethylene glycol 4000
1
．． 0 glycerin

2.0 Squalane

20.0 Cetostearyl alcohol
3.0 Polyoxyethylene (20 mol)
1.5 Oleyl alcohol ether glyceryl monostearate
1.5 Urea

0.5
lactic acid soda

2.0 Xanthan gum (Keltrol brand name) 0.
05 Methylparaben

0.1 Ethylparaben

0.2 EDTA-3Na

0.01 incense
fee

0.2 Ion exchange water

Remaining amount Production method A cream was produced using a conventional method.

Example 3 Emulsion

Weight% glycerin

2.0 Squalane

5.0
Vaseline

1.0 Cetostearyl alcohol

0.3 Polyoxyethylene (20 mol)

1.5 Oleyl alcohol ether glyceryl monooleate

1.5 Potassium salt of tranexamic acid

0.1 Sodium polyacrylate

0.03 Ethylparaben

0.2 Urea

0.5 caustic potash

0.1 EDTA-3Na

0.03 fragrance

0.2
ion exchange water

Remaining amount Production method An emulsion was obtained by a conventional method.

Comparative Example 3 Emulsion

Weight% glycerin

2.0 Squalane

5.0
Vaseline

1.0 Cetostearyl alcohol

0.3 Polyoxyethylene (20 mol)

1.5 Oleyl alcohol ether glyceryl monooleate

1.5 Sodium polyacrylate

0.03 Ethylparaben

0.2 Urea

0.5
caustic potash

0.1 EDTA-3Na

0.03 fragrance

0.2
ion exchange water

Remaining amount Production method An emulsion was obtained by a conventional method.

[0025]

[Table 1]

[0026]

[Table 2]

[0027]

[Table 3]

[0028]

[Table 4]

[0029]

[Table 5]

[0030]

[Table 6]

As is clear from the results in Tables 1 to 6, the cosmetics of the present invention were extremely superior to conventional products in terms of skin moisture, skin firmness, and next morning moisture. Furthermore, it was also excellent in improving skin roughness.

Example 4 Pack

Weight% propylene glycol

2.0 Polyethylene glycol 4000
3.0 Glycerin

15.0 Ethanol

10.0 Vitamin A ester of tranexamic acid
10.0 Polyvinyl alcohol
10.0 Olive oil

3.0 Lactic acid

1.0
urea

5.0 Carboxymethylcellulose
0.07 Methylparaben

0.1 Ethylparaben

0.1 caustic potash

0.
02 EDTA-3Na

0.01 fragrance

0
．． 1 Ion exchange water

Remaining amount Manufacturing method A pack was obtained by a conventional method. The pack of the present invention activates skin metabolism, increases skin elasticity, has excellent skin protection and moisture retention, provides appropriate moisture and skin firmness, and is also excellent in improving skin roughness. .

Example 5 Hair cream

Weight% Beeswax

3.0 Vaseline

15.0 Liquid paraffin

42.0 Polyoxyethylene (5 mol)
3.0
Stearic acid ester polyoxyethylene (6 moles)
2.0
Oleyl alcohol ether polyoxyethylene (6 moles)
1.0
Cetyl alcohol ether Vitamin C ester of tranexamic acid
15.0 Urea


5.0 Purified water

remainder
fragrance

Appropriate amount preservative

Appropriate amount Manufacturing method A hair cream was obtained using a conventional method.

Example 6 Cream

Weight% 1,3-butylene glycol

5.0 Polyethylene glycol 4
000
1.0 Glycerin

2.0
Squalane

20.0 Vaseline

5.0
Cetostearyl alcohol

3.0 Polyoxyethylene (20 mol)

1.5 Oleyl alcohol ether glyceryl monostearate

1.5 Sodium salt of tranexamic acid

0.1 Urea

0.5
Lactic acid sorter

2.0 Xanthan gum (Keltrol brand name)
0.05 Methylparaben

0.1 Ethylparaben

0.2 EDTA-3Na

0.01 fragrance


0.2 Ion exchange water

Remaining amount Production method A cream was produced using a conventional method. The cream of the present invention activates skin metabolism, increases skin viscosity and elasticity, has excellent skin protection and moisture retention, provides appropriate moisture and skin firmness, and is also excellent in improving skin roughness. .

Example 7 Emulsion

Weight% glycerin

2.0 Squalane

5.0 Vaseline

1.0 Cetostearyl alcohol
0.3 Polyoxyethylene (20 mol)
1.5
Oleyl alcohol ether glyceryl monooleate
1.5 Potassium salt of tranexamic acid
15.0 Sodium polyacrylate
0.03 Ethylparaben

0.2 Urea

1.5 Caustic potash


0.1 EDTA-3Na

0.03 fragrance

0.2
ion exchange water

Remaining amount Production method An emulsion was obtained by a conventional method. The emulsion of the present invention activates skin metabolism, increases skin elasticity, and has excellent skin protection and moisture retention.
It provided adequate moisture and firmness to the skin, and was also effective in improving rough skin.

Claims (1)

[Claims] 1. An external skin preparation comprising urea and tranexamic acid, a salt thereof, a derivative thereof, or a mixture thereof.