KR20090091511A - Whitening cosmetic composition - Google Patents

Abstract

A cosmetic composition for skin whitening is provided to suppress melanogenesis, improve skin tone and have whitening effect. A cosmetic composition for skin whitening comprises: 0.05~0.2 weight% of ingredient comprising an icarlin, icaritin, icariside I and icariside II; and 0.75~1.0 weight% of one or more kinds of salicylic acid, N-acetylglucosamine and their mixture. The composition further comprises polyphenol derivative, kojic acid or 0.1~3.0 weight% of 3,4,5-trimethoxy phenyl based ester compound.

Description

Whitening cosmetic composition

The present invention relates to a cosmetic composition for skin whitening, more specifically, as an active ingredient 1) Icarin or Icarin hydrolyzate; And 2) salicylic acid, N-acetylglucosamine, and mixtures thereof. The present invention relates to a cosmetic composition for skin whitening containing. In another aspect, the present invention is a skin whitening further comprising at least one selected from the group consisting of polyphenol derivatives, koji acid, niacinamide, and 3,4,5-trimethoxy phenyl-based ester compounds in addition to the above components as an active ingredient It relates to a cosmetic composition for.

Skin whitening agent or skin lightening agent may be defined as a preventive agent for preventing pigment spot formation by ultraviolet rays. In other words, the skin whitening agent controls melanin production to blur freckles and blemishes. In general, the whitening agent is recognized as a substance that turns yellowish skin with blemishes into white skin.

Long time ago, natural products such as yulmu and cucumber have been used for skin whitening purposes. In the 1990s, it was also revealed that ultraviolet light promotes skin aging, and the mechanism of melanin production in melanocytes is revealed. As a new source of whitening, vitamin C derivatives, placenta extract, arbutin, kojic acid and ascorbic acid magnesium phosphate With the development of the lamp, a new whitening agent called UV-white was used.

The skin is equipped with physical and chemical UV protective factors and has a function to minimize skin disorders caused by various photochemical reactions. The stratum corneum attenuates its energy by reflecting and diffusing ultraviolet light. In addition, melanin, superoxide dismutase (SOD), and other antioxidants protect against skin disorders by absorbing ultraviolet light that penetrates inside the skin, and attenuates its energy or eliminates free radicals secondary to UV radiation. . However, various skin disorders occur when a living body receives a large amount of ultraviolet rays exceeding the ability of these defense factors or its capacity decreases with age.

There are many cells in the skin that are immune to the living body, including macrophages and Langerhans cells. Irradiation of ultraviolet light causes these cells not only to decrease numerically but also to functionally impair. The largest part of skin color determinants is the distribution and amount of melanin in the skin. Many factors affect melanin production, and the increase of melanin production caused by ultraviolet rays and the subsequent pigmentation are very important in the cosmetic field. The basic mechanisms of drugs formulated in whitening cosmetics for the purpose of preventing pigmentation include 1) inhibiting tyrosinase action, 2) inhibiting tyrosinase production, 3) inhibiting melanogenesis mediators, and 4) reducing existing melanin and Photooxidation inhibition, 5) promotion of melanin excretion, and 6) UV cut.

Ultraviolet radiation to pigment cells promotes melanin production. As one of these mechanisms, it is thought that bFGF, vitamin D3, and inflammatory chemical mediators increased by inflammation caused by ultraviolet rays act on pigment cells as mediators for promoting melanogenesis.

Trilobite leaf koreanum ) is a plant called Yin Yang Kwak and belongs to the barberry family and lives mainly in the shade of trees in the mountains. Epimedium plants belong to the barberry family, and three Chinese medicinal plants record E. brevicornum , E. sagittatum, and E. koreanum . Flavonoids, alkaloids, and lignans have been reported as main ingredients in epimedium plants. In particular, the herbal medicine dried on the ground portion of Epimedium koreanum Nakai is used for the purpose of gangjeong, systemic involuntary, forgetfulness and nervous tonic in oriental medicine and folk medicine as yin and yang. Free radicals produced by various physical, chemical and environmental factors such as enzymes, reducing metabolism, chemicals, pollutants and photochemical reactions in the body are non-selective and irreversible destruction of cell components such as lipids, proteins, sugars and DNA. It is known to cause various diseases including cell aging or cancer by acting. In addition, various peroxides in the body, including lipid peroxides produced as a result of lipid peroxidation by these free radicals, can cause oxidative destruction of cells and cause various functional disorders.

Accordingly, antioxidants such as free radical scavengers or peroxide production inhibitors are expected as agents for inhibiting or treating aging and various diseases caused by these oxides.

In the present invention, as a result of trying to find an active ingredient that inhibits melanin cell formation and inhibits tyrosinase-glycosylation activity in a concentration-dependent manner, Icarin or Icarin hydrolysates and salicylic acid, N-acetylglucosamine Or when using a mixture of these as an active ingredient to discover the excellent whitening effect due to their synergistic effect was completed the present invention.

Therefore, an object of the present invention is to provide a cosmetic composition for skin whitening excellent skin whitening efficacy.

In order to achieve the above object, in the present invention, 1) at least one selected from the group consisting of Icarin, Ikaritin, Ikariside I and Ikariside II; And 2) salicylic acid, N-acetylglucosamine, and mixtures thereof. Provides a cosmetic composition for skin whitening.

In the present invention, the skin whitening further comprises at least one selected from the group consisting of polyphenol derivatives, kojic acid, niacinamide, and 3,4,5-trimethoxy phenyl ester compounds in addition to the above components as an active ingredient. It provides a cosmetic composition for.

The cosmetic composition for whitening according to the present invention inhibits the formation of skin melanin cells and improves the overall skin tone, thereby giving the effect that the skin is clean, dull and improved.

Hereinafter, the present invention will be described in more detail.

Icarin used in the present invention is a flavonoid component of the plant extract of the genus Epimedia. In the present invention, Icarin was extracted from trilobite vinegar using HtGPR (Hetero glycoside position remodeling) technology, which is a novel bioconversion technique for the position-selective control of glycosides. Icarin extracted by this technique was found to inhibit melanin formation and inhibit glycosylation of tyrosinase, and enhanced the whitening effect with salicylic acid and N-acetylglucosamine . HtGPR technology is a novel bioconversion technology that removes by selectively controlling the glycobinding component of glycoside active material.

Icarin hydrolyzate used in the present invention is Icarine, Icaride I and Icaride II represented by the following formula (1), Icarin hydrolyzate is an acid, base, enzyme or microorganism that produces the enzyme It is hydrolyzed by using, and it has excellent antioxidant, anti-aging and whitening effect, and in particular, by melanin formation and excellent inhibition of tyrosinase, it acts as a signaling agent in cells to maximize the skin whitening effect:

Where

Ikaritin is R1 and R2 is OH,

Icarsid I is R1 is OH, R2 is glucopyranose,

Icarsid II is R1 is rhamnopyranose and R2 is OH.

The manufacturing process of the Icarin hydrolyzate used in the present invention is disclosed in Korean Patent Publication No. 10-0803577. In the present invention, using a new biotransformation technique, HtPGR technology to inhibit melanocyte formation from the process described in Korean Patent Publication No. 10-0803577 from Icarin, an extremely small amount of active ingredient extracted from Trichophyte herb, and tyrosinase- Icarin hydrolysates that concentration-dependently inhibit Tyrosinase-glycosylation activity can be prepared respectively.

The cosmetic composition for whitening according to the present invention contains the Icarin or the Icarin hydrolyzate as 0.05 to 0.2% by weight based on the total weight of the composition, preferably 0.1% by weight. Icarin reduces melanin synthesis to a statistically significant level compared to arbutin at a concentration 20 times lower than that of arbutin, and the expression of the melanin inhibitory effect in the cell test in terms of concentration is 3,4,5-trimethoxy phenyl. It was shown to be 5 times more effective than the ester compound and 20 times more effective than arbutin.

In addition, the cosmetic composition for whitening according to the present invention further contains salicylic acid, N-acetylglucosamine or a mixture thereof with the ikarin or ikarin hydrolysate. The content of the salicylic acid, N-acetylglucosamine or a mixture thereof is preferably 0.75 to 1.0% by weight based on the total weight of the composition. Salicylic acid has a usable content in terms of drafting, which is 0.75% by weight. N-acetylglucosamine has been shown to be exfoliated due to the use of about 1.0% by weight of the total weight.

 Since salicylic acid used in the present invention has the action of antipyretic and analgesic, it is used to improve the solubility, stability and pharmacological properties by incorporating sodium salt or calcium salt and binding to various drugs. Used as a plaster to remove warts and corns. In addition, it was used as a food preservative, but toxicity is a problem, and it is not used at present. In addition, it is also important as an intermediate for synthesizing mordant azo dyes or direct dyes. Metal ions such as copper, titanium, and iron are made to chelate compounds and become dark, which is also useful as a reagent for chemical analysis of these metals. In cosmetics, preservatives or exfoliants are known.

N-acetylglucosamine used in the present invention is a component present in the living body and acts as a proteoglycan proteoglycan (Proteoglycan), hyaluronic acid and collagen production enhancing effect; Proliferative effect of natural moisturizing ingredients (natural amino acids) and fibroblasts; Increased collagen production and inhibitory effect of MMP-1 (Collagenase) activity; And water-soluble, mild exfoliation effect is excellent.

In addition, the cosmetic composition for whitening according to the present invention is an active ingredient comprising at least one selected from the group consisting of polyphenol derivatives, kojic acid, niacinamide, and 3,4,5-trimethoxy phenyl ester compounds. It may further include 0.1 to 3.0% by weight relative to the weight.

Polyphenol derivatives showed the effect of inhibiting melanin production in the content of 0.1% by weight like Icarin, and kojic acid contained only 0.3% by weight for the purpose of boosting efficacy, and the remaining components were all used by 3.0% by weight. It was intended to increase the efficacy of the ingredients.

 The polyphenol derivative used in the present invention is represented by the following formula (2):

Kojic acid used in the present invention is widely used as a whitening component while the effect of inhibiting melanin synthesis is known.

Niacinamide used in the present invention is a component that blocks the movement of melanin from the skin to the skin surface, also called vitamin B3.

The 3,4,5-trimethoxy phenyl ester compound used in the present invention is 3,4,5-trimethoxy phenylacetic acid, 3,4,5-trimethoxycinnamic acid and 3,4,5-tri As an ester compound of methoxy hydrocin Namsan, it is represented by the following formula (3), it is known as a whitening component.

Wherein R ₁ is -CH = CH- and R ₂ is thymyl or carvacryl.

Meanwhile, in the present invention, 3,4,5-trimethoxycinnamic acid in Chemical Formula 3 was used.

The cosmetic composition for whitening by this invention is not specifically limited in the formulation. For example, supple cosmetics, astringent cosmetics, nourishing cosmetics, nourishing cream, massage cream, essence, eye cream, eye essence, cleansing cream, cleansing foam, cleansing water, pack, powder, body lotion, body cream, body oil, body It may be formulated as an essence, makeup base or foundation, or may be formulated as a cosmetic such as skin whitening cosmetics or ointments and patches.

Hereinafter, preferred examples and comparative examples of the present invention will be described in more detail. However, the following embodiments are merely preferred embodiments of the present invention, and the present invention is not limited to such embodiments.

[Examples 1-5 and Comparative Example 1]

According to the composition shown in Table 1 below, the cosmetic compositions of Examples 1 to 5 and Comparative Example 1 were prepared (unit: wt%).

ingredient Example 1 Example 2 Example 3 Example 4 Example 5 Comparative Example 1 Decamethylcyclopentasiloxane 4.5 4.5 4.5 4.5 4.5 4.5 Dimethicone / dimethicone PEG-10,15 crosspolymer / cyclopentasiloxane 1.0 1.0 1.0 1.0 1.0 1.0 Polymethylsilsesquioxane 2.0 2.0 2.0 2.0 2.0 2.0 Butylene glycol 4.0 4.0 4.0 4.0 4.0 4.0 glycerin 2.0 2.0 2.0 2.0 2.0 2.0 Betaine 3.0 3.0 3.0 3.0 3.0 3.0 β-glucan 4.0 4.0 4.0 4.0 4.0 4.0 Hydrogenated Lecithin / C12-16 Alcohol / Palmitic Acid 1.0 1.0 1.0 1.0 1.0 1.0 Ammonium Acryloyldimethyltaurate VP Copolymer 0.4 0.4 0.4 0.4 0.4 0.4 PEG-60 hydrogenated castor oil 0.5 0.5 0.5 0.5 0.5 0.5 Bis-PEG-18 Methylether Dimethylsilane 0.25 0.25 0.25 0.25 0.25 0.25 Polyacrylate-13 / Polyisobutene / Polysorbate 20 1.10 1.10 1.10 1.10 1.10 1.10 Disodium EDTA 0.02 0.02 0.02 0.02 0.02 0.02 Purified water Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Icarin 0.1 0.1 0.1 0.1 0.1 0.1 Salicylic acid 0.75 0.75 0.75 - 0.75 - N-acetylglucosamine 1.0 1.0 1.0 1.0 1.0 - Kojisan 0.3 - 0.3 - - - Niacinamide - - - 3.0 3.0 - Polyphenol Derivatives of Formula 2 0.1 0.1 0.1 - - - 3,4,5-trimethoxycinnamic acid - - 3.0 - - - pH acid acid acid neutrality acid

Test Example 1 Evaluation of Skin Whitening Efficacy

The 112 Korean women were divided into six groups for four weeks, and the cosmetic compositions prepared in Examples 1 to 5 and Comparative Example 1 were used daily, and the skin conditions were compared and analyzed by the following evaluation items. It is shown in Table 2 and FIGS. 1-10 (7-point scale method).

<Evaluation Item>

In the results of the whitening efficacy evaluation questionnaire of each item of Figures 1 to 10, the overall ranking was in the order of Example 2, Example 3, Example 1, Example 5, Example 4 and Comparative Example 1. In other words, Example 2 was found to have the best whitening efficacy, it was confirmed that the synergistic effect of whitening efficacy when mixing the polyphenol derivatives of Icarin and formula (2). In addition, it was confirmed that there was a boosting effect of the whitening effect by adding salicylic acid together through the lowest whitening effect of Example 4, which did not include salicylic acid. In addition, it was confirmed that Examples 1 to 3 and 5 having a pH of an acidic region have better whitening efficacy than those of Example 4 having a neutral region.

Test substance Evaluation item Average One 2 3 4 5 6 7 8 9 10 Example 1 4 4 4 4 One 3 4 3 2 3 3.2 Example  2 One One 2 2 4 One One One One One 1.5 Example 3 3 2 One 5 3 2 2 2 3 2 2.5 Example 4 5 5 5 One 5 5 5 5 5 5 4.6 Example 5 2 3 3 3 2 4 3 4 4 4 3.2 Comparative Example 1 2 2 3 2 4 2 3 2 3 2 2.5

In the results of Table 2, the composition of Example 2 showed a higher rank than the other compositions in almost all of the 10 items.

FIG. 11 shows that Comparative Example 1 containing only Icarin and a change in melanin concentration of arbutin showed that Comparative Example 1 containing Icarin was more suppressed according to the concentration of melanin in the skin than arbutin. have. It was also confirmed that the color of melanin faded over time.

1 is a graph evaluating skin tone brightness after application of each test substance (1: Example 1, 2: Example 2, 3: Example 3, 4: Example 4, 5: Example 5).

2 is a graph evaluating the degree of brightening of the skin after application of each test substance (1: Example 1, 2: Example 2, 3: Example 3, 4: Example 4, 5: Example 5) .

3 is a graph evaluating the degree of skin clarity after application of each test substance (1: Example 1, 2: Example 2, 3: Example 3, 4: Example 4, 5: Example 5) .

4 is a graph evaluating the degree of disappearance of blemishes and blemishes after application of each test substance (1: Example 1, 2: Example 2, 3: Example 3, 4: Example 4, 5: Example 5).

5 is a graph evaluating the degree of disappearance of the red group of the skin after the application of each test substance (1: Example 1, 2: Example 2, 3: Example 3, 4: Example 4, 5: Example 5).

6 is a graph evaluating the whitening effect after application of each test substance (1: Example 1, 2: Example 2, 3: Example 3, 4: Example 4, 5: Example 5).

7 is a graph evaluating the degree of improvement in the dullness of the skin after application of each test substance (1: Example 1, 2: Example 2, 3: Example 3, 4: Example 4, 5: Example 5).

8 is a graph evaluating the degree of uniform skin color after application of each test substance (1: Example 1, 2: Example 2, 3: Example 3, 4: Example 4, 5: Example 5) .

9 is a graph evaluating the degree of skin cleanness after application of each test substance (1: Example 1, 2: Example 2, 3: Example 3, 4: Example 4, 5: Example 5) .

10 is a graph evaluating the overall satisfaction after the application of each test substance (1: Example 1, 2: Example 2, 3: Example 3, 4: Example 4, 5: Example 5).

11 is a graph showing a change in melanin concentration in the skin of Comparative Example 1 and arbutin.

Claims (5)

1) at least one member selected from the group consisting of icarin, icaritin, icarsid I and Icaridide II; And 2) at least one selected from the group consisting of salicylic acid, N-acetylglucosamine and mixtures thereof; cosmetic composition for skin whitening containing as an active ingredient. According to claim 1, wherein the composition is a polyphenol derivative represented by the following formula (2), koji acid, niacinamide, and 3,4,5-trimethoxy phenyl ester compound represented by the following formula (3) Whitening cosmetic composition, characterized in that it further comprises one or more selected: [Formula 2]

[Formula 3]

Wherein R ₁ is -CH = CH- and R ₂ is thymyl or carvacryl. The cosmetic composition for skin whitening according to claim 1, wherein the at least one selected from the group consisting of Icarin, Icarritin, Icarsid I and Icaridide II is contained in an amount of 0.05 to 0.2% by weight based on the total weight of the composition. . The cosmetic composition for skin whitening according to claim 1, wherein at least one selected from the group consisting of salicylic acid, N-acetylglucosamine and mixtures thereof is contained in an amount of 0.75 to 1.0 wt% based on the total weight of the composition. According to claim 2, wherein the polyphenol derivative, koji acid, niacinamide, and at least one selected from the group consisting of 3,4,5-trimethoxy phenyl ester compound represented by the formula (3) is the total weight of the composition Cosmetic composition for skin whitening, characterized in that contained in 0.1 to 3.0% by weight.

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