JP2002029920A - Bleaching cosmetic - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a more excellent bleaching cosmetic for controlling melanin production in the upstream and downstream of melanin production. SOLUTION: This cosmetic, especially preferably a bleaching cosmetic comprises (1) an essence of Sophora flvescens Aitin of the family Leguminosae and (2) a melanin production inhibitor.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a cosmetic suitable for whitening.

[0002]

2. Description of the Related Art White skin is desired not only by men, but also by humans as a whole, including women. For this reason, various whitening cosmetics are exhibited at pharmacies these days, and many of them are displayed. Are purchased by consumers. As whitening active ingredients used in such cosmetics, ascorbic acid such as ascorbic acid, ascorbate, magnesium ascorbic acid phosphate, ascorbic acid glycoside and related substances, cysteine, glutathione, glutathione Glutathione and its derivatives such as N-acylated glutathione and glutathione esters, hydroquinone and its derivatives such as hydroquinone and hydroquinone glycosides, and kojic acid and kojic acid salts, ferulic acid and ferulic acid And phenolic substances such as isoferulic acid, isoferulic acid salts, caffeic acid, caffeic acid salts, resorcinols, ergoic acid and salts thereof, and derivatives thereof. or,
In addition to this, a biological component such as a placenta extract is also included in the melanin production inhibitor. The mechanism of the effect of these active ingredients for whitening is to inhibit the activity of tyrosinase or suppress the oxidation of tyrosine by reduction in the process of tyrosin being oxidized by tyrosinase to produce melanin, resulting in melanin production. Is to suppress. However, it seems that a bypass exists in such a route, and such downstream suppression has a limited effect, and further improvement of the effect has been desired.

[0003] On the other hand, legume Clara is the base plant of Chinese herbal medicine Kusan, and its hot water extract is already known to have a medicinal effect such as an anti-hyperlipidemic effect. However, it has an inhibitory effect on α-MSH (α-melanotropin), which controls the upstream part of melanin production, and therefore may inhibit melanin production by a mechanism different from the inhibition of tyrosinase oxidation. However, it has not been known at all that the cosmetics contain a combination of this and the above-mentioned whitening agent having a mechanism for suppressing tyrosine oxidation, and that such cosmetics have an extremely excellent whitening effect.

[0004]

DISCLOSURE OF THE INVENTION The present invention has been made under such circumstances, and suppresses the production of melanin upstream and downstream of melanin production, thereby providing a more excellent whitening cosmetic. Is provided.

[0005]

In view of such a situation, the present inventors have studied intensively in order to suppress the melanin production upstream and downstream of the melanin production and to find a more excellent whitening cosmetic. As a result of repeated efforts, α-
The present inventors have found that such cosmetics can be obtained by combining a MSH inhibitor and a melanin production inhibitor in cosmetics, and have completed the invention. That is,
The present invention relates to the following technology. (1) A cosmetic comprising 1) an α-MSH inhibitor and 2) a melanin production inhibitor. (2) The melanin production inhibitor is selected from ascorbic acid and its related substances, glutathione and its derivatives, hydroquinone and its derivatives, and phenolic substances and its derivatives, (1)
The cosmetic according to any one of the above. (3) The cosmetic according to (1) or (2), wherein the α-MSH inhibitor is an extract of leguminous Clara (bitter soybean; kujin). (4) The cosmetic according to any one of (1) to (3), wherein the extract of leguminous Clara is a polar solvent extract of root and / or a solvent-removed product thereof. (5) It is a whitening cosmetic, (1)
-(4) The cosmetic according to any one of the above. (6) the whitening effect is prevention or improvement of pigmentation due to transfer of melanin granules to the dermis,
The cosmetic according to (5). (7) A cosmetic, comprising: 1) an extract of leguminous Clara and 2) a melanin production inhibitor. (8) The cosmetic according to (7), wherein the extract of leguminous Clara is a polar solvent extract of root and / or a solvent-removed product thereof. (9) The cosmetic according to (7) or (8), which is used for whitening. Hereinafter, the present invention will be described in more detail focusing on embodiments.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION (1) (1) α-MSH inhibitor which is an essential component of the external preparation for skin of the present invention The external preparation for skin of the present invention contains an α-MSH inhibitor as an essential component. Features. Α-MS referred to in the present invention
The H inhibitor refers to a group of substances that inhibit the production of α-melanotropin that is deeply involved in melanin production, and such an action on α-MSH reduces cultured cells (melanoma B-16 cells). Using, cyclic AMP
Screening can be carried out by examining the production amount of as an index. That is, the cells were cultured in a 96-well plate at 10% FBS in MEM (Eagle's minimal medium) at 5% CO 2 and 95% at 37 ° C. in a 96-well plate.
Culture overnight at 160 μl / well of medium and add α
Add MSH (1 × 10 −7 M) and various concentrations of test substance and measure as spectrophotometer at 450 nm using Amersham Biolake Cellular Communication Assay cAMP enzyme immunoassay system (code RPN225) By doing
-MSH inhibitory action can be screened.
As substances having such α-MSH inhibitory activity, the present inventors have proposed Arnica (Arnica Montana L), Hamamelis (Hamamelis virginiana) and Leguminosae Clara (Bitter;
Kujin) and other extracts of plants based on crude drugs. Of these, Clara is particularly preferred. Here, the extract referred to in the present invention is a plant itself, a processed product obtained by drying, shredding, pulverizing, etc., a plant, an extract obtained by adding a solvent to the plant or its processed product, and extracting, A solvent-removed product from which the solvent has been removed, an extract or a generic term such as a purified product obtained by subjecting the solvent-removed product to column chromatography or liquid-liquid extraction. Among these, an extract is particularly preferred, and among them, an extract such as water or alcohol is preferred. A polar solvent extract extracted with a polar solvent is particularly preferred. Extraction may be performed according to a usual method.For example, a plant or a processed product thereof is added with a solvent in an amount of 1 to 10 times, and immersed for several days at room temperature and several hours at a temperature near the boiling point. Well, then, if necessary, remove insolubles by filtration or the like,
The solvent may be removed by concentration under reduced pressure or freeze drying. The α-MSH inhibitor of the present invention thus obtained comprises:
Inhibiting α-MSH, which is a command system of melanin production, inhibiting melanin production upstream and inhibiting tyrosin from oxidizing tyrosine to produce melanin, when used with a melanin production inhibitor described below, Inhibits the production of melanin at the reaction point, thus exhibiting an excellent whitening effect. Α-MS in the skin external preparation of the present invention
The preferred content of the H inhibitor is 0.01 to 10% by weight, and more preferably 0.05 to 5% by weight. If the amount is too small, the synergistic effect with the later-described melanin production inhibitor may not be exhibited, and if the amount is too large, the synergistic effect may reach a plateau and the flexibility of prescription may be impaired.
Further, the α-MSH inhibitor of the present invention has another medicinal effect. Even if it is contained for the purpose of such a medicinal effect, the effect of the present invention can be attained if it is combined with a melanin production inhibitor described below in composition. Therefore, such a case also belongs to the technical scope of the present invention.

(2) Melanin production inhibitor which is an essential component of the cosmetic of the present invention The cosmetic of the present invention contains the above-mentioned α-MSH inhibitor and also contains a melanin production inhibitor as an essential component. The melanin production inhibitor that can be used in the present invention can be used without any particular limitation as long as it is conventionally known to have an effect of inhibiting melanin production, for example, ascorbic acid, ascorbate, ascorbate Ascorbic acid and its related substances such as magnesium acid phosphate and ascorbic acid glycoside, cysteine, glutathione, salts of glutathione, glutathione and derivatives thereof such as N-acylated glutathione and glutathione esters, salts of hydroquinone and hydroquinone, hydroquinone Hydroquinone and its derivatives such as glycosides and kojic acid, salts of kojic acid, ferulic acid, salts of ferulic acid,
Preferable examples include isoferulic acid, salts of isoferulic acid, caffeic acid, salts of caffeic acid, phenolic substances such as resorcinols, and derivatives thereof. Of these, particularly preferred are ascorbic acid, ascorbic acid glucoside, magnesium ascorbate phosphate, kojic acid, isoferulic acid, and hydroquinone glucoside (arbutin). These can be used alone or in combination of two or more. The preferable content of these in the cosmetic of the present invention is 0.01 to 10% by weight, more preferably 0.05 to 5% by weight, based on the total amount of the cosmetic. If this is too small, it may not work,
This is because if the amount is too large, the effect reaches a plateau and the degree of freedom of prescription may be impaired.

(3) Cosmetic of the present invention The cosmetic of the present invention is characterized by containing the above essential components. By adopting such a configuration, it has the characteristic of suppressing melanin production both upstream and downstream of melanin production. Accordingly, the cosmetic of the present invention is preferably used for whitening, and is preferably used for preventing or improving pigment abnormality. As a preferable form of the cosmetic of the present invention, it is further mentioned that the cosmetic does not contain a hydrophilic nonionic surfactant. This is because the cosmetic of the present invention has an emulsifying or solubilizing effect by itself by adopting the above constitution, and by not containing such a hydrophilic nonionic surfactant, This is because it is possible to prevent troubles caused by such components.
In addition, the cosmetic of the present invention also has a whitening effect, and is suitable for people who expect such an effect on sensitive skin.

[0009] In addition to the above essential components, the composition for external use on the skin of the present invention can contain optional components usually used in such compositions. Examples of such optional components include hydrocarbons such as squalane, petrolatum and microcrystalline wax, jojoba oil, carnauba wax, esters such as octyldodecyl oleate, triglycerides such as olive oil, tallow, coconut oil, and stearic acid. Oleic acid, fatty acids such as ritinoleic acid, higher alcohols such as oleyl alcohol, stearyl alcohol, octyldodecanol, polyhydric alcohols such as polyethylene glycol, glycerin and 1,3-butanediol, thickening / gelling agents, oxidation Examples include an inhibitor, an ultraviolet absorber, a coloring agent, a preservative, and a powder. Of these, particularly preferred optional components include glycerin as a humectant and carboxyvinyl polymer and / or a salt thereof as a thickener. The preferred content of glycerin is 1 to 10% by weight, more preferably 2 to 5% by weight. This is because in this amount range, the trouble occurrence suppressing effect can be remarkably obtained. As the carboxyvinyl polymer salt, alkali metal salts and organic amine salts can be preferably exemplified, and potassium salts and sodium salts are particularly preferable in terms of contribution to stability. The total amount of the carboxyvinyl polymer and its salt is 0.1 to 1
It is preferred that the content be contained by weight% from the balance between stability and safety. The composition of the present invention can be produced by treating these optional components and essential components according to a conventional method.

[0010]

EXAMPLES Hereinafter, the present invention will be described in more detail with reference to examples, but the present invention is not limited to these examples.

Example 1 An emulsion (cosmetic), which is a composition for external use on the skin, of the present invention was prepared according to the following formulation. That is, the components (a), (b) and (c) are heated to 80 ° C., and (b) is gradually added to (a) while stirring, and further (c) is gradually stirred and neutralized, and then the emulsified particles are homogenized by a homomixer. An emulsion was obtained. Ascorbic acid-2-
Comparative Example 1 in which glucoside was changed to Clara extract and Comparative Example 2 in which Clara extract was replaced with ascorbic acid-2-glucoside were also prepared. The effects of these samples were compared in a test using the inner part of a human upper arm. That is, four 2 cm × 2 cm sites were formed on the inner part of the upper arm, and each site was irradiated with ultraviolet rays having a minimum erythema amount of 1.2 times, and pigmentation was confirmed 48 hours after irradiation. One is the emulsion of Example 1, one is the emulsion of Comparative Example 1, one is the emulsion of Comparative Example 2, the other is untreated, and 0.01 ml is applied once a day, Processed for days. Two weeks after the last administration, the color difference from the surrounding unirradiated site was determined. Table 1 shows the results. From this table, it can be seen that the skin external preparation of the present invention has an excellent whitening effect, and this effect is caused by the combination of the two essential components of the present invention. I Squalane 10 parts by weight Sorbitan sesquistearate 2 parts by weight Ascorbic acid-2-glucoside 1 part by weight butyl paraben 0.1 part by weight b 1,3-butanediol 5 parts by weight Xanthan gum 0.1 part by weight Carboxyvinyl polymer 0.2 Parts by weight Methyl paraben 0.1 parts by weight Solvent removed from ethanol extract of Clara 1 part by weight Water 50 parts by weight C Potassium hydroxide 0.1 part by weight Water 30.4 parts by weight

[0012]

[Table 1]

Example 2 An emulsion (cosmetic), which is a composition for external use on the skin, of the present invention was prepared according to the following formulation. That is, the components (a), (b) and (c) are heated to 80 ° C., and (b) is gradually added to (a) while stirring, and further (c) is gradually stirred and neutralized, and then the emulsified particles are homogenized by a homomixer. An emulsion was obtained. Ascorbic acid phosphoric acid 2
Comparative Example 3 in which magnesium was replaced with an arnica extract and Comparative Example 4 in which the arnica extract was replaced with dimagnesium ascorbate were also prepared. The effects of these samples were compared in a test using the inner part of a human upper arm. That is, four 2 cm × 2 cm sites were formed on the inner part of the upper arm, and each site was irradiated with ultraviolet rays having a minimum erythema amount of 1.2 times, and pigmentation was confirmed 48 hours after irradiation. One is Example 2
, One was the emulsion of Comparative Example 3, one was the emulsion of Comparative Example 4, and the remaining one was untreated, and 0.01 ml was applied once a day and treated for 10 days. Two weeks after the last administration, the color difference from the surrounding unirradiated site was determined. Table 2 shows the results. From this table, it can be seen that the skin external preparation of the present invention has an excellent whitening effect, and this effect is caused by the combination of the two essential components of the present invention. I Squalane 10 parts by weight Sorbitan sesquistearate 2 parts by weight 2-magnesium ascorbate phosphate 1 part by weight butyl paraben 0.1 part by weight b 1,3-butanediol 5 parts by weight Xanthan gum 0.1 parts by weight Carboxyvinyl polymer 0. 2 parts by weight Methyl paraben 0.1 parts by weight Solvent removal from water extract of arnica 1 part by weight Water 50 parts by weight C Potassium hydroxide 0.1 part by weight Water 30.4 parts by weight

[0014]

[Table 2]

<Examples 3 to 5> Emulsions were prepared according to the following recipes. That is, a, b, and c are each 70
The mixture was heated to C, neutralized by adding ロ to イ, and gradually added while stirring to emulsify and stirred and cooled to obtain an emulsion of the present invention. Table 3 shows the results of examination of these samples in the same manner as in Examples 1 and 2. This indicates that, in the external preparation for skin of the present invention, Clara extract is particularly preferable as the α-MSH inhibitor. A 1,2-pentanediol 5 parts by weight 1,3-butanediol 5 parts by weight glycerin 3 parts by weight Acrylic acid / alkyl methacrylate copolymer 0.6 parts by weight Phenoxyethanol 0.2 parts by weight Water 30 parts by weight α-MSH inhibitor * 0.1 part by weight Arbutin 0.2 part by weight b 10% aqueous potassium hydroxide solution 3 parts by weight Water 37 parts by weight Husqualane 5 parts by weight Jojoba oil 5 parts by weight Dimethicone 6 parts by weight * Details are shown in Table 3.

B

[Table 3]

Example 6 An emulsion was prepared according to the following recipe. That is, each of (a), (b) and (c) was heated to 70 ° C., (b) was neutralized by adding (b) to the mixture, and (c) was added gradually while stirring to emulsify and stirred and cooled to obtain an emulsion of the present invention.
It had an excellent whitening effect. A 1,2-pentanediol 5 parts by weight 1,3-butanediol 5 parts by weight glycerin 3 parts by weight Acrylic acid / alkyl methacrylate copolymer 0.6 parts by weight Phenoxyethanol 0.2 parts by weight Water 30 parts by weight Kuzin's 1,3 -Butanediol extract 0.1 parts by weight b 10% aqueous potassium hydroxide solution 3 parts by weight Water 37 parts by weight Husqualane 5 parts by weight Jojoba oil 5 parts by weight Dimethicone 6 parts by weight Ferulic acid ethyl ester 0.2 parts by weight

Example 7 An emulsion was prepared according to the following recipe. That is, each of (a), (b) and (c) was heated to 70 ° C., (b) was neutralized by adding (b) to the mixture, and (c) was added gradually while stirring to emulsify and stirred and cooled to obtain an emulsion of the present invention.
It had an excellent whitening effect. A 1,2-pentanediol 5 parts by weight 1,3-butanediol 5 parts by weight glycerin 3 parts by weight Acrylic acid / alkyl methacrylate copolymer 0.6 parts by weight Phenoxyethanol 0.2 parts by weight Water 30 parts by weight Kuzin's 1,3 -Butanediol extract 0.1 parts by weight b 10% aqueous potassium hydroxide solution 3 parts by weight Water 37 parts by weight Husqualane 5 parts by weight Jojoba oil 5 parts by weight Dimethicone 6 parts by weight Kojic acid ethyl ester 0.2 parts by weight

[0019]

According to the present invention, upstream of melanin production,
On the downstream side, the melanin production can be suppressed, and a more excellent whitening cosmetic can be provided.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61P 43/00 111 A61P 43/00 111 // A61K 31/05 A61K 31/05 31/375 31/375 35 / 78 35/78 J 38/00 45/06 45/06 37/02 (72) Inventor Natsue Watanabe 27-1, Takashimadai, Kanagawa-ku, Yokohama-shi, Kanagawa-ken, Japan Polar Research Institute Yokohama Research Laboratory (72) Inventor Sugiyama Takudo 27-1 Takashimadai, Kanagawa-ku, Kanagawa-ku, Kanagawa Prefecture Inside the Yokohama Laboratory, Polar Chemical Industry Co., Ltd. (72) Inventor Yasuhiro Fukuda 27-1, Takashimadai, Kanagawa-ku, Yokohama-shi, Kanagawa Prefecture F-term in Yokohama Research Laboratory, Yokohama Reference) 4C083 AA111 AA112 AA122 AB032 AC022 AC122 AC172 AC232 AC442 AC471 AC482 AC842 AC902 AD092 AD202 AD252 AD352 AD411 AD641 AD642 CC01 CC05 DD27 DD31 EE16 4C084 AA02 B A01 BA15 BA23 DC31 MA63 NA05 ZA891 ZC202 4C086 AA01 BA18 GA17 MA02 MA04 MA63 NA05 ZA89 ZC20 ZC75 4C088 AB59 AC11 BA08 BA37 CA09 CA11 MA63 NA05 ZA89 ZC20 ZC75 4C206 AA01 CA17 CA19 KA01 MA02 MA04 Z83

Claims (9)

[Claims] 1. A cosmetic comprising 1) an α-MSH inhibitor and 2) a melanin production inhibitor. 2. The melanin production inhibitor is selected from ascorbic acid and its related substances, glutathione and its derivatives, hydroquinone and its derivatives, and phenolic substances and its derivatives. The cosmetic according to any one of the above. 3. The cosmetic according to claim 1, wherein the α-MSH inhibitor is an extract of a leguminous Clara (Russia; Kujin). 4. The extract of leguminous Clara is a polar solvent extract of root and / or a solvent-removed product thereof.
3. The cosmetic according to any one of 3. 5. The cosmetic according to claim 1, which is a whitening cosmetic. 6. The cosmetic according to claim 5, wherein the whitening effect is prevention or improvement of pigmentation due to transfer of melanin granules to the dermis. 7. A cosmetic, comprising: 1) an extract of leguminous Clara and 2) a melanin production inhibitor. 8. The cosmetic according to claim 7, wherein the extract of leguminous Clara is a polar solvent extract of root and / or a solvent-removed product thereof. 9. The cosmetic according to claim 7, wherein the cosmetic is for whitening.