JP3170024B2 - Whitening cosmetics - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a whitening cosmetic which is effective for blackening skin by ultraviolet rays or for fading or preventing skin pigmentation such as spots and freckles.

[0002]

2. Description of the Related Art When ultraviolet rays from sunlight are irradiated on the skin, pigments are formed in pigment cells in the skin, causing darkening of the skin and deposition of skin pigments, thereby causing stains and freckles. Is known to occur. Conventionally,
Various whitening cosmetics have been proposed for the purpose of preventing such blackening of the skin and removing stains and freckles. For example, those using a reducing agent such as vitamin C and its derivatives, glutathione, hydrogen peroxide, placenta extract, and a melanin production inhibitor such as kojic acid are known.

[0003] However, vitamin Cs have a disadvantage that they are easily oxidized and cause discoloration and odor of cosmetics containing the same. A reducing agent such as glutathione has an unpleasant odor and also has a problem in transdermal absorption, and hydrogen peroxide is said to have a problem in safety and stability. In addition, an animal tissue extraction system such as a placenta extract is not sufficiently effective,
In addition, there are problems in terms of stability, color, odor and the like. In addition, since a small amount of kojic acid has a problem such as a small effect of preventing skin blackening, it cannot be said that any of these is sufficient as an active ingredient of a whitening cosmetic. As described above, these conventionally known melanin production-inhibiting substances are inadequate in terms of their effects even if they are used alone, and most of those which can be practically used in various aspects such as safety and stability are not used. There is no fact.

[0004] On the other hand, when an unsaturated fatty acid is used in an amount sufficient to produce an effect alone, its safety is concerned.
Accordingly, an object of the present invention is to provide a whitening cosmetic which has an excellent whitening effect, has no side effects and is highly safe, and which solves the above-mentioned conventional problems.

As for isoflavanes, the whitening effect of glabridine is known (JP-A-1-3110).
No. 11, Fragrance Journal 111, 59-66
(1990)) and hispagrabridine A and hispagrabridine B are known to have antibacterial activity (He).
terocycles9 (11), 1533-1538
(1978)), but there was no report on suppression of melanin production. Accordingly, it is an object of the present invention to provide a whitening cosmetic which has an excellent whitening effect, has no side effects and is highly safe, and which solves the above-mentioned conventional problems.

[0006]

The present invention relates to isoflavanes and free fatty acids having 18 to 22 carbon atoms and having two or more unsaturated bonds in the molecular structure, salts thereof, and esters with monohydric or dihydric alcohols. 1 selected from the group consisting of
By blending seeds or two or more components, it was found that the pigmentation of the skin was lightened or a synergistic effect with an excellent preventive effect appeared, and the present invention was completed.

That is, the gist of the present invention is to provide (a) isoflavans, (b) a free fatty acid having 18 to 22 carbon atoms and two or more unsaturated bonds in the molecular structure, a salt thereof, or a monohydric or dihydric alcohol. And a whitening cosmetic comprising one or more components selected from esters of the following.

The isoflavanes used as the component (a) in the present invention may be any of extracts or synthetic products from plants such as licorice, and may be of any type as long as they belong to the isoflavans. Gravlidine A, Hispagrabridine B, Gravlidine, phaseolin isoflavane are preferred.

The amount of the isoflavanes used in the present invention in the whitening cosmetics varies depending on the kind of the cosmetics and the degree of expected whitening effect, but is usually in the range of 0.005% to 1% by weight. . Preferably, it is in the range of 0.01 to 0.5% by weight. If the amount is less than 0.005% by weight, the effect is not sufficient, and if the amount exceeds 1% by weight, the effect corresponding to the amount cannot be expected.
A blending amount of about 1% by weight is sufficient.

The component (b) used in the present invention includes:
For example, linoleic acid, linoleic acid, α-linolenic acid, γ-linolenic acid, dihomo-γ-linolenic acid, arachidonic acid, eicosapentaenoic acid, and the like.Examples of the salts of these free fatty acids include sodium salts, Metal salts such as potassium salts; amino acid salts such as arginine salts and lysine salts; amine salts such as triethanolamine salts and monoethanolamine salts; and the like, and esters of these free fatty acids include methanol, ethanol and isopropyl Esters of monohydric alcohols such as alcohol, ethylene glycol, propylene glycol, 1,
Examples thereof include esters with a dihydric alcohol such as 3-butylene glycol, and one or more of these components are used.

In the present invention, by using these active ingredients in combination with the above-mentioned component (a), isoflavanes, a synergistic whitening effect is exerted on the skin. The amount of the component (b) in the cosmetic is usually 0.1.
1 to 10%. Preferably it is 1.0 to 5.0% by weight. When the amount is less than 0.1% by weight, the effect of lightening pigmentation is not sufficient, and when the amount exceeds 10% by weight, the skin becomes irritating.

The whitening cosmetic of the present invention is characterized by blending the components (a) and (b) as described above, and the whitening cosmetic of the present invention contains these components. In addition, bases and various additives that are usually blended in whitening cosmetics may be blended. For example, an oil, a surfactant, a fragrance, a preservative, and the like are appropriately blended.

The whitening cosmetic of the present invention can be prepared into a lotion, a cosmetic oil, a cream, a milky lotion, a pack, a powder, etc. by a conventional method.

Hereinafter, the present invention will be described in more detail with reference to Examples and Test Examples.

【Example】

Example 1 Preparation of lotion: predetermined amounts of glycerin, citric acid and sodium citrate are dissolved in purified water. Separately, a predetermined amount of linoleic acid, α-linolenic acid, hispagrabridine A, polyoxyethylene hydrogenated castor oil (60E.
O. ), Perfume was dissolved, added to the purified aqueous solution, solubilized, and filtered to obtain a lotion. [Ingredients] [Blending amount (% by weight)] Hispagrabridine A 0.05 Linoleic acid 1.0 α-Linolenic acid 1.0 Glycerin 6.0 Ethanol 9.0 Polyoxyethylene hydrogenated castor oil (60EO) 0.8 Methyl paraoxybenzoate 0.05 Citric acid 0.05 Sodium citrate 0.07 Fragrance 0.1 Water-soluble placenta extract 2.0 Purified water balance

Example 2 Preparation of Cosmetic Oil: The following other components were uniformly dissolved in squalane in predetermined amounts to give the following weight percent to obtain a cosmetic oil. [Ingredient] [Blending amount (% by weight)] Hispagrabridine B 0.05 Ethyl linoleate 1.0 γ-linolenic acid 1.0 Ascorbyl palmitate 0.2 Retinol acetate 0.3 Squalane Remainder

Example 3 Preparation of cream: Of the following components, a predetermined amount of component (A) was mixed in the following amount by weight, and then dissolved by heating.
C. was maintained. Separately, ingredients excluding fragrance (B)
Was mixed in a predetermined amount to give the following weight%, and then heated and melted and maintained at 80 ° C. Ingredient (B) excluding the above fragrance
The mixture of component (A) was added to the mixture with stirring, and the mixture was thoroughly mixed. Thereafter, the mixture was cooled to about 40 ° C. with stirring, and then a fragrance was added. This was further cooled to obtain a cream comprising the following components. [Ingredient] [Blending amount (% by weight)] Component (A) Phaseolin isoflavan 0.1 γ-linolenic acid 2.0 Eicosapentaenoic acid 1.0 Salami beeswax 4.0 Cetanol 2.0 Isopropyl myristate 5 2.0 Lanolin 2.0 Liquid paraffin 9.0 Self-emulsifying glyceryl monostearate 3.0 Polyoxyethylene sorbitan monostearate (20EO) 1.5 Propyl parahydroxybenzoate 0.1 Component (B) Paraoxybenzoic acid Methyl 0.2 Propylene glycol 5.0 Fragrance 0.2 Purified water Remainder

Example 4 Preparation of emulsion: Among the following components, a predetermined amount of component (A) was used.
After mixing to give the following weight%, the mixture was heated and dissolved, and kept at 80 ° C. Separately from this, a predetermined amount of the component (B) excluding the fragrance was mixed so as to be the following weight%, and then heated and dissolved, and kept at 80 ° C. The mixture of the component (A) was added to the mixture of the component (B) excluding the flavor while stirring, and the mixture was thoroughly mixed. Thereafter, the mixture was cooled to about 40 ° C. while stirring, and then the flavor was added. This was further cooled to obtain an emulsion comprising the following components. [Ingredient] [Blending amount (% by weight)] Component (A) 1.0 Linoleic acid 0.05 Gravlidine 2.0 Isopropyl linoleate 5.0 Liquid paraffin 2.0 Vaseline 2.0 Beeswax 1.0 Sesquiolein Sorbitan acid 2.0 Component (B) Epsilon aminocaproic acid 0.2 Polyoxyethylene oleyl ether (20EO) 2.5 Ethyl parahydroxybenzoate 0.2 Propylene glycol 5.0 Carboxyvinyl polymer 0.5 Potassium hydroxide 0.5 Perfume 0.2 Purified water balance

Example 5 Preparation of a pack: α-linolenic acid, hispagrabridine A, docosahexaenoic acid, fragrance and ethanol are uniformly dissolved. This is added to a homogeneous mixture of vinyl acetate-styrene copolymer, polyvinyl alcohol, sorbite, and kaolin. Further, a solution prepared by uniformly dissolving a water-soluble placenta extract and ethyl paraoxybenzoate in purified water was added thereto, and the mixture was uniformly mixed to obtain a pack. [Component] [Blending amount (% by weight)] α-Linolenic acid 3.0 Hispagrabridine A 0.05 Docosahexaenoic acid 0.5 Vinyl acetate / styrene copolymer 10.0 Polyvinyl alcohol 10.0 Sorbitol 5.0 Kaolin 7.0 Ethanol 5.0 Fragrance 2.0 Ethyl paraoxybenzoate 0.2 Purified water Remainder

Test Example 1 The back of an English brown guinea pig was shaved and irradiated with ultraviolet rays (UVB intensity: 0.8 J / cm 2). This operation was repeated for three days, and pigmentation was obtained one week later. Next, a sample obtained by dissolving isoflavanes or other components in ethanol was applied to this site at a coating amount of 10 μl / cm 2.
It was applied cumulatively for a week. As a method of evaluating the lightening of the pigmentation, the pigmentation of the part where the sample was not applied (uncoated) was set to 0, and the degree of the lightening was visually determined according to the following criterion. The results are shown in Table 1. The criteria for determining the effect are as follows. 0: No lightening of pigmentation was observed at all. 1: Lightening of pigmentation is slightly observed. 2: Moderate pigmentation lightening is observed. 3: Light pigmentation of strong pigmentation is observed.

[0020]

[Table 1]

[0021]

[Table 2]

As is evident from Tables 1 and 2, the active ingredients of isoflavanes alone can suppress the pigmentation or reduce the color of the active ingredients. However, when the ingredients such as linoleic acid are used in combination, they are more remarkable. Severe suppression of pigmentation or lightening was observed.

Test Example 2 16 healthy people in their 20s and 40s (8 men, 8 women)
UV of 1.0 mW / cm ² was applied to the four adjacent sites inside the upper arm.
Ultraviolet rays corresponding to 1-1.2 MED (Minimal Erytherma Doses) were irradiated for 3 days to obtain uniform pigmentation. In the meantime, a cream containing no phaseolin isoflavan among the components of Example 3 in each part (abbreviated as cream A), and a cream not containing γ-linolenic acid and eicosapentaenoic acid (cream B) ), A cream consisting of the components of Example 3 (abbreviated as Cream C), and among the components of Example 3, all of phaseolin isoflavan, γ-linolenic acid, and eicosapentaenoic acid. No cream (cream D
) Was applied three times a day for 4 weeks. The application amount was 0.5 mg / cm ² . One month after the start of application, the degree of pigmentation of each of the cream A, B, and C application parts was compared with the degree of pigmentation of the cream D application part, and the results in Table 3 were obtained.

[0024]

[Table 3]

As is evident from Table 3, when only isoflavanes were blended (cream A) and when only unsaturated fatty acids were blended (cream B), no significant lightening effect of pigmentation was observed. . On the other hand, when isoflavans and unsaturated fatty acids are used in combination (cream C)
In this case, remarkable lightening of pigmentation was observed.

[0026]

The cosmetic of the present invention, when applied to the skin, eliminates, darkens or prevents blackening or pigmentation of the skin due to ultraviolet rays, and exhibits an excellent whitening effect.

Claims (2)

(57) [Claims] 1. A (a) isoflavanes, and (b) a free fatty acid having 18 to 22 carbon atoms and an unsaturated bond number of 2 or more in a molecular structure, a salt thereof, and an ester with a monohydric or dihydric alcohol. A whitening cosmetic comprising one or more components selected from the group consisting of: 2. The whitening cosmetic according to claim 1, wherein the isoflavans are hispagrabridine A, hispagrabridine B, glabridine, and phaseolin isoflavane.