KR101444689B1 - Whitening cosmetic composition - Google Patents

Abstract

More particularly, the present invention relates to a cosmetic composition for skin whitening, which comprises 1) an icaline or icarin hydrolyzate; And 2) at least one member selected from the group consisting of salicylic acid, N-acetylglucosamine, and mixtures thereof. The present invention also relates to a skin whitening agent comprising, as an active ingredient, at least one selected from the group consisting of polyphenol derivatives, kojic acid, niacinamide, and 3,4,5-trimethoxyphenyl ester compounds, And more particularly to a cosmetic composition for cosmetics.

Skin whitening, bamboo leaves, melanin, whitening, dullness,

Description

[0001] Whitening cosmetic composition [0002]

More particularly, the present invention relates to a cosmetic composition for skin whitening, which comprises 1) an icaline or icarin hydrolyzate; And 2) at least one member selected from the group consisting of salicylic acid, N-acetylglucosamine, and mixtures thereof. The present invention also relates to a skin whitening agent comprising, as an active ingredient, at least one selected from the group consisting of polyphenol derivatives, kojic acid, niacinamide, and 3,4,5-trimethoxyphenyl ester compounds, And more particularly to a cosmetic composition for cosmetics.

A skin whitening agent or skin lightening agent can be defined as a preventive agent for preventing pigment spot formation by ultraviolet light. In other words, skin whitening regulates the production of melanin to make freckles and stains blurred, generally whitening agent has become recognized as a substance that turns yellowish skin into whitish skin.

For a long time, natural products such as yulmu and cucumber were used for skin whitening. In addition, it has been found that ultraviolet rays promote skin aging in the 1990s, and melanogenesis mechanisms in melanocytes are partly revealed. As a new whitening ingredient, vitamin C derivatives, placenta extract, arbutin, kojic acid and ascorbic acid phosphate ester magnesium A new whitening agent called UV-WHITE was used.

The skin is equipped with physical and chemical UV protection factors and has the function to minimize the skin disorder caused by various photochemical reactions. The stratum corneum attenuates its energy by reflecting and diffusing ultraviolet light. In addition, the melanin pigment, SOD (superoxide dismutase) and other antioxidant components absorb ultraviolet rays penetrating the inside of the skin, and defend the skin by damping its energy or erasing active oxygen secondary to ultraviolet rays . However, when a living body receives a large amount of ultraviolet light exceeding the capability of such a defensive factor, or when its ability is deteriorated with age, various skin disorders occur.

There are various cells in the skin that are responsible for immunity from the living system, such as macrophages and Langerhans cells. By ultraviolet irradiation, these cells are not only reduced in number but also functionally. Among the determinants of skin color, the largest portion is the distribution and the amount of melanin in the skin. Various factors affecting melanin production have been known, such as hyperpigmentation of melanin production caused by ultraviolet rays and subsequent pigmentation, which are very important in the cosmetics field. The basic mechanisms of pharmaceuticals incorporated into whitening cosmetics for pigmentation prevention are 1) inhibition of tyrosinase action, 2) inhibition of tyrosinase production, 3) inhibition of melanin-producing mediators, 4) reduction of existing melanin, Suppression of photooxidation, 5) promotion of melanin excretion, and 6) ultraviolet rays.

When ultraviolet light is irradiated on pigment cells, melanin production is promoted. It is thought that bFGF, vitamin D3, which increases in the skin by ultraviolet rays, and inflammatory chemical mediator, which is increased by ultraviolet ray inflammation, act on the pigment cells as a mediator of melanogenesis promotion.

Epimedium koreanum ) is a plant, also known as Hwangyangkeok, belonging to the family Melanidae and mainly inhabits in the shade of the mountainous region. Epimedium belongs to the genus Melanogaster. Three species of E. brevicornum , E. sagittatum and E. koreanum are recorded before Chinese medicine. Studies on the components of the epimedium plant have been reported mainly as flavonoids, alkaloids and lignans. Especially, the herbal medicine dried on the ground of Epimedium koreanum Nakai is used for the purpose of gangjeong, whole body passive, forgetfulness and neurotic tonic in oriental medicine and private medicine. Active oxygen generated by various physical, chemical and environmental factors such as in vivo enzymes, reductive metabolism, chemicals, pollutants and photochemical reactions can cause non-selective and irreversible destruction of cellular components such as lipids, proteins, It is known to cause various diseases including cancer and senescence. In addition, lipid peroxides and various peroxides such as lipid peroxides produced as a result of lipid peroxidation by these active oxygen also cause oxidative destruction to cells and cause various dysfunctions, thereby causing various diseases.

Accordingly, antioxidants such as free radical scavengers or peroxidation-inhibiting substances are expected to be used as agents for inhibiting or treating various diseases caused by these oxides.

Thus, in the present invention, efforts have been made to find an effective ingredient that inhibits melanocyte formation and inhibits tyrosinase-glycosylation activity in a concentration-dependent manner. As a result, it has been found that when an icarinic or icarin hydrolyzate and salicylic acid, N- acetylglucosamine Or a mixture thereof are used together as an active ingredient, it is possible to obtain an excellent whitening effect owing to their synergistic effect, and thus the present invention has been completed.

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

In order to achieve the above object, the present invention provides a pharmaceutical composition comprising 1) at least one selected from the group consisting of icarin, icaritin, icaricide I and icaricide II; And 2) at least one member selected from the group consisting of salicylic acid, N-acetylglucosamine and mixtures thereof.

In the present invention, in addition to the above-mentioned components as the active ingredient, skin whitening further comprising at least one member selected from the group consisting of polyphenol derivatives, kojic acid, niacinamide, and 3,4,5-trimethoxyphenyl ester compounds The present invention provides a cosmetic composition.

The cosmetic composition for whitening according to the present invention inhibits the formation of melanocytes of the skin and improves the overall skin tone, thereby cleansing the skin, improving the dullness, and imparting an effect of lustering.

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

The icarin used in the present invention is a flavonoid component of the epimedium plant extract. In the present invention, Icarin was extracted from Sanko mushroom leaf using HtGPR (Hetero glycoside position remodeling) technique, which is a new biotransformation technique for regulating sugar binding components of glycoside active material. Icarinin extracted by this technique inhibits melanin formation and is found to inhibit glycosylation of thyrosinase to an excellent extent. Thus, whitening effect is enhanced by salicylic acid and N-acetylglucosamine, which exfoliate . The HtGPR technique is a novel bioconversion technique that locally selectively removes sugar binding components of glycoside active materials.

The icarin hydrolyzate used in the present invention is icarinic, icaricide I and icaricide II represented by the following general formula (1), wherein the icarin hydrolyzate is an acid, a base, an enzyme or a microorganism producing the enzyme It is excellent in antioxidant, anti-aging and whitening effect, and particularly acts as a signal transducer in the cell due to melanin formation and thiorcinase's excellent inhibition, thereby maximizing skin whitening effect:

In this formula,

Icaritine is a compound wherein R1 and R2 are OH,

Icaricid I is a compound wherein R1 is OH, R2 is glucopyranose,

In icariic seed II, R1 is rhamopyranose and R2 is OH.

The process for producing the icarin hydrolyzate used in the present invention is disclosed in Korean Patent Registration No. 10-0803577. In the present invention, by using HtPGR technology, which is a new biotransformation technique, it is possible to inhibit melanocyte formation through a process disclosed in Korean Patent Registration No. 10-0803577 from a trace amount of active ingredient, Icarin, It is possible to produce each of the icarin hydrolysates inhibiting glycosylation (tyrosinase-glycosylation) activity in a concentration-dependent manner.

The whitening cosmetic composition according to the present invention contains the above icaline or icarin hydrolyzate in an amount of 0.05 to 0.2% by weight, preferably 0.1% by weight, based on the total weight of the composition. Icarin reduces melanin synthesis to a statistically significant level compared with arbutin at a concentration 20 times lower than that of arbutin. When the inhibitory effect on melanin synthesis is expressed in terms of concentration in a cell test, 3,4,5-trimethoxyphenyl 5 times as much as the ester compound and 20 times as much as the arbutin.

The cosmetic composition for whitening according to the present invention further contains salicylic acid, N-acetylglucosamine or a mixture thereof together with the above-mentioned icarin or icarin hydrolyzate. The content of salicylic acid, N-acetylglucosamine or a mixture thereof is preferably 0.75 to 1.0 wt% with respect to the total weight of the composition. Salicylic acid has an available content in terms of the system, which is 0.75 wt%. N-acetylglucosamine has been shown to exfoliate because of the use of 1.0 wt.% Of the total weight.

 The salicylic acid used in the present invention has antiphlogistic and analgesic action and is thus used for lowering with sodium salt or calcium salt and for improving solubility, stability and pharmacological properties by binding to various drugs, Warts, corns) are used as a plaster to remove. It has also been used as a food preservative, but it has become toxic and is not currently in use. It is also important as an intermediate to synthesize azo dyes and direct dyes. It forms chelate compounds with metal ions such as copper, titanium and iron and becomes a dark color, so it is also useful as a reagent for chemical analysis of these metals. Preservatives or exfoliation efficacy are known in cosmetics.

The N-acetylglucosamine used in the present invention is a component present in vivo and acts as a precursor component of proteoglycan, and has the effect of enhancing hyaluronic acid and collagen production; Proliferative effects of natural moisturizing ingredients (natural amino acids) and fibroblasts; Increased collagen production and inhibition of MMP-1 (collagenase) activity; And water-soluble, mild exfoliation management effect is excellent.

The cosmetic composition for whitening according to the present invention may further contain at least one selected from the group consisting of polyphenol derivatives, kojic acid, niacinamide, and 3,4,5-trimethoxyphenyl ester compounds as an active ingredient, And may further comprise 0.1 to 3.0% by weight based on the weight.

The polyphenol derivative showed the same effect of inhibiting melanogenesis at the same concentration of 0.1% by weight as in the case of icarin. Koji acid contained only a small amount of 0.3% by weight for the purpose of boosting the efficacy. To increase the efficacy of the ingredients.

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

The kojic acid used in the present invention has been widely used as a whitening ingredient as it has been known to inhibit the synthesis of melanin.

The niacinamide used in the present invention is a component that blocks melanin migration from the skin to the skin surface, and is also referred to as vitamin B3.

The 3,4,5-trimethoxyphenyl ester compounds used in the present invention are 3,4,5-trimethoxyphenylacetic acid, 3,4,5-trimethoxycinnamic acid and 3,4,5-tri As an ester compound of methoxyhydrocinnamic acid, it is represented by the following formula (3) and is known as a whitening component.

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

In the present invention, 3,4,5-trimethoxycinnamic acid is used in the above formula (3).

The cosmetic composition for whitening according to the present invention is not particularly limited in its formulation. For example, softening longevity, convergent lotion, nutritional lotion, nutritional cream, massage cream, essence, eye cream, eye essence, cleansing cream, cleansing foam, cleansing water, pack, powder, body lotion, body cream, body oil, body An essence, a makeup base, or a foundation, and may be formulated into cosmetics for skin whitening or medicines such as ointments and patches.

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

[Examples 1 to 5 and Comparative Example 1]

The cosmetic compositions of Examples 1 to 5 and Comparative Example 1 were prepared according to the composition shown in Table 1 below (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
Cross Polymer / 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 methyl ether 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 Sodium EDTA 0.02 0.02 0.02 0.02 0.02 0.02 Purified water Balance Balance Balance Balance Balance Balance Ikarin 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 - Kojic acid 0.3 - 0.3 - - - Niacinamide - - - 3.0 3.0 - The polyphenol derivative of formula (2) 0.1 0.1 0.1 - - - 3,4,5-trimethoxycinnamic acid - - 3.0 - - - pH acid acid acid neutrality acid

[Experimental Example 1] Evaluation of skin whitening efficacy

A total of 112 Korean women were divided into 6 groups for 4 weeks, and the skin condition of each of the above-mentioned cosmetic compositions prepared in Examples 1 to 5 and Comparative Example 1 was compared and analyzed according to the following evaluation items. Shown in Table 2 and Figs. 1 to 10 (7 point scaling method).

<Evaluation Items>

In the results of the whitening efficacy evaluation question for each item of Figs. 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. That is, Example 2 showed the best whitening effect, and it was confirmed that whitening efficacy synergistic effect was obtained when the icarin and the polyphenol derivative of Chemical Formula 2 were mixed. In addition, the whitening effect of Example 4 which did not contain salicylic acid was lowest, and it was confirmed that whitening efficacy boosting effect was obtained by adding salicylic acid together. It was also confirmed that Examples 1 to 3 and 5 having an acidic pH range of Example 4 having a neutral region are superior in whitening efficacy.

Test substance Evaluation items 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 above, the composition of Example 2 showed higher rankings than the other compositions in almost all of the ten items.

In Fig. 11, Comparative Example 1 containing only icarin and comparative experiment of changes in melanin concentration of arbutin showed that Comparative Example 1 containing icarin was more inhibited by melanin in the skin than albutin have. It was also confirmed that the color of melanin became thin over time.

FIG. 1 is a graph showing skin tone brightness after application of each test substance (1: Examples 1 and 2: Examples 2 and 3: Examples 3 and 4: Examples 4 and 5: Example 5).

FIG. 2 is a graph showing the degree of skin lustering after application of each test substance (Examples 1 and 2: Examples 2 and 3: Examples 3 and 4: Examples 4 and 5: Example 5) .

FIG. 3 is a graph showing the degree of transparency of skin after application of each test substance (1: Examples 1 and 2: Examples 2 and 3: Examples 3 and 4: Examples 4 and 5: Example 5) .

FIG. 4 is a graph showing the evaluation of the degree of stain and dullness after application of each test substance (1: Examples 1 and 2: Examples 2 and 3: Examples 3 and 4: Examples 4 and 5: 5).

FIG. 5 is a graph showing the degree of disappearance of redness of skin after application of each test substance (1: Examples 1 and 2: Examples 2 and 3: Examples 3 and 4: Examples 4 and 5: 5).

FIG. 6 is a graph showing the evaluation of whitening effect after application of each test substance (Examples 1 and 2: Examples 2 and 3: Examples 3 and 4: Examples 4 and 5: Example 5).

FIG. 7 is a graph showing the degree of improvement of skin dullness after application of each test substance (1: Examples 1 and 2: Examples 2 and 3: Examples 3 and 4: Examples 4 and 5: 5).

FIG. 8 is a graph showing the degree of uniformity of skin color after application of each test substance (1: Examples 1 and 2: Examples 2 and 3: Examples 3 and 4: Examples 4 and 5: Example 5) .

FIG. 9 is a graph showing the degree of cleansing of skin after application of each test substance (1: Examples 1 and 2: Examples 2 and 3: Examples 3 and 4: Examples 4 and 5: Example 5) .

FIG. 10 is a graph showing the overall satisfaction after application of each test material (1: Examples 1 and 2: Examples 2 and 3: Examples 3 and 4: Examples 4 and 5: Example 5).

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

Claims (5)

1) at least one selected from the group consisting of icarin, icaritin, icaricide I and icaricide II; And 2) salicylic acid; And 3) a polyphenol derivative represented by the following formula 2 A cosmetic composition for skin whitening comprising: (2)

. The composition according to claim 1, wherein the composition comprises at least one member selected from the group consisting of N-acetylglucosamine, kojic acid, niacinamide, and 3,4,5-trimethoxyphenyl ester compounds represented by the following formula The cosmetic composition for whitening is further characterized by: (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 at least one selected from the group consisting of icarin, icaritin, icaricide I and icaricide 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 the salicylic acid is contained in an amount of 0.75 to 1.0 wt% based on the total weight of the composition, and the polyphenol derivative is contained in an amount of 0.1 to 3.0 wt% based on the total weight of the composition. 3. The composition of claim 2, wherein the N-acetylglucosamine is present in an amount of 0.75 to 1.0% by weight based on the total weight of the composition, and the kojic acid, niacinamide, and 3,4,5-trimethoxy Phenyl ester compound in an amount of 0.1 to 3.0% by weight based on the total weight of the composition.

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