KR20090105224A - The skin bleaching cosmetic composition - Google Patents

Abstract

PURPOSE: A cosmetic composition for skin whitening is provided to ensure the effect of suppressing melanogenesis and tyrosinase activity and ensure antioxidative activity. CONSTITUTION: A skin whitening cosmetic composition contains 0.005-50 weight% of Pleuropterus multiflorus extract based on the total weight. The extract is obtained using polar solvent selected from water, low alcohol of 1-4 carbon atoms or their solvent. The composition expresses skin whitening effect by suppressions of melanogenesis and tyrosinase activation.

Description

The skin bleaching cosmetic composition

The present invention relates to a cosmetic composition for skin whitening, more specifically sewage ( Pleuropterus) Multiflorus ) extract containing 0.005 to 50% by weight, based on the total weight of the composition, inhibits melanin production, inhibits tyrosinase activity, and excellent antioxidant activity due to sewage extracts. will be.

Skin is a very important tissue that has direct contact with the external environment, protects the human body and has biochemical and physical functions. This tissue is largely divided into three parts: the epidermis, the dermis, and the hypodermis. Melanin is a pigment in the epidermal layer of the skin, made from melanocytes in the basal layer of the epidermis and migrates to epidermal cells called keratinocytes. There are no enzymes in the body that break down melanin, but they are removed by falling off the skin as keratinocytes fall off the epidermis.

In the melanin synthesis process, tyrosine is first converted into dopaquinone via dopa (DOPA) by an enzyme called tyrosinase in a melanocyte vesicle in melanocytes, and an automatic oxidation reaction and enzyme from dopaquinone The reaction gives melanin, a blackish brown copolymer, through dopachrome. The melanin thus produced is transferred to keratinocytes through the melanosomes, where it is lost to the surface of the skin along with the keratinization process for about 28 days.

Melanin absorbs the light energy of sunlight UV to protect skin organs under the dermis from UV damage, and it protects the skin from external harmful factors such as trapping harmful oxygen and free radicals generated in skin skin. Play a role. In addition, the skin color of a person is determined by the amount of melanin in the skin cells. People with high melanin pigments have brown or black skin, while those with low melanin pigments have white skin.

However, abnormally low production of melanin causes skin lesions such as vitiligo and, conversely, damage to the skin if the melanin is not completely synthesized due to excessive synthesis or keratinization due to daylight, hormonal changes, inflammation, or drugs. In addition to the skin pigments are deposited to form blemishes, freckles, and even from these lesions may cause skin cancer. Therefore, in order to prevent such a pigmentation phenomenon, it is necessary to inhibit a part of melanogenesis process to reduce melanin production.

Today, Asian women prefer white and clean skin like white jade and make it an important standard of beauty. Therefore, the development of whitening agent for treatment of abnormal skin pigmentation and satisfying beauty needs is being actively developed.

At present, in the development of a whitening agent for skin beauty, a method of reducing the generated melanin pigment by decolorization and a method of inhibiting the activity of tyrosinase, an enzyme that forms melanin pigment, are known. However, the whitening agent using tocopherol, vitamins, etc. which are used for reducing melanin pigment | dye is known that the decolorization effect of melanin pigment is insignificant. Accordingly, attention has been paid to inhibitors that inhibit the production of melanin pigment by inhibiting the activity of tyrosinase.

In the conventional cosmetic field, as a whitening component, for example, substances that inhibit tyrosinase enzyme activity such as kojic acid, arbutin, hydroquinone, vitamin-C (L-Ascorbic acid) and Their derivatives and various plant extracts have been used.

However, the stability in the prescription system is poor, the color is degraded, or the use thereof is limited due to the occurrence of off-flavor, efficacy at the biological level, unclear effect and safety problems. Kojic acid inhibits enzymatic activity by adsorbing copper ions present in the active site of tyrosinase, but has been discontinued as a raw material for cosmetics because of its instability, skin side effects and recent animal experiments. Vitamin-C and its derivatives are difficult to use as raw materials for cosmetics due to their oxidative instability. Hydroquinone has excellent whitening effect on the skin but causes allergy, toxicity to melanocytes, and permanent depigmentation to the skin. It is highly irritating to skin, and is recently prescribed as a carcinogenic substance, so its use is banned and only a limited concentration is allowed in each country. In addition, arbutin is a derivative in which glucopyranoside is combined with hydroquinone, and has little side effects when using hydroquinone and inhibits the synthesis of melanin pigment without toxicity to the human body, thereby increasing melanin pigmentation. Applicability has been suggested as a therapeutic agent for skin diseases, but it has a disadvantage of being partially degraded by skin enzymes.

In addition to these whitening substances, research has been conducted to find whitening active ingredients in natural products, especially plants. Among them, white skin (Japanese Patent Application Laid-Open No. 55-44375, Small 64-26507, Small 64-83009, Pyeong 1-25687 No. 5-139950, Korean Patent Publication Nos. 92-002109, 97-021273, Licorice (Japanese Patent Laid-Open No. 60-214721, No. 60-214728, No. 63-23809, No. 64- 63506, Hei 1-149706, and Korean Patent Nos. 92-002109, 97-025601), Peony (Japanese Patent Laid-Open No. 61-246109 and Korean Laid-Open Patent No. 92-002111), Cinnamon Patent Nos. 63-30403, Hep. 5-139954), Gosam (Japanese Patent Laid-Open No. 64-26507 and Korean Patent Laid-Open No. 92-002110), Brown root (Japanese Laid-Open Patent Nos. 60-214727, Small 64-16709 ), Angelica (Japanese Patent Laid-Open No. 56-92211, Hei 4-26610), Mokdanpi (Japanese Laid-Open Patent No. 60-214721, No. 61-50915, No. 61-246109), Banha (Japanese Laid-Open Patent Publication) Pyeong 2-207028, Korea Publication No. 96-033442), aloe (Japanese Patent Laid-Open No. 52-44375, Hei 2-207030, Hei 5-139950) and many plant extracts and herbal extracts act on tyrosinase to produce melanin Although it has been found to suppress the, they also have a lot of problems in the use of more than the effective concentration in cosmetics or pharmaceuticals in terms of safety, discoloration, etc., and still does not show an excellent effect.

Accordingly, an object of the present invention is to provide a cosmetic composition for skin whitening that inhibits melanin production, inhibits tyrosinase activity, has excellent antioxidant activity, and in particular, shows little cytotoxicity.

In order to achieve the above objects as well as other objects that are easily expressed, sewage ( Pleuropterus) in the present invention. multiflorus ) extract containing 0.005 to 50% by weight based on the total weight of the composition to obtain a cosmetic composition for inhibiting melanin production, inhibiting tyrosinase activity, having excellent antioxidant activity and showing little cytotoxicity due to sewage extract. Could.

That is, the present inventors, while studying the physiological activity of sewage, a plant that is native to China but is currently cultivated in Korea, the sewage extract contains a large amount of resveratrol with excellent antioxidant effect. The present invention was completed by confirming that it can reduce melanin production, inhibit tyrosinase activity, have an antioxidant effect, and be useful as a composition for skin whitening.

Skin whitening composition according to the present invention has the effect of inhibiting melanin production, tyrosinase activity, excellent antioxidant activity and little cytotoxicity due to sewage extract.

Skin whitening composition according to the present invention is characterized by containing 0.005 ~ 50% by weight of sewage extract based on the total weight of the composition.

Sewage ( Pleuropterus multiflorus ) used in the present invention It is known to come from China and has been cultivated for a long time. The height is 3 ~ 4m and the roots are extended to the side, often forming tubers. Heart-shaped leaves are about 3-6cm long and 2.5 ~ 4.5cm wide, with petioles and chin leaves, but without jagged edges. Flowers bloom in August-September in conical inflorescences. There are no petals and 5 calyxes. Fruits are ovate, glossy, 2.5mm long.

The reddish brown tuber is called Shouo in one shot. Shouo is famous as a herb that strengthens kidney function, enhances energy, darkens hair and makes people live longer without disease. The function of the liver to get rid of tiredness, multiply the skin, strengthen the bones and muscles, and strengthen the heart is also effective in nervous breakdowns and insomnia. Its excellent hematopoietic effect makes it an excellent treatment for anemia and is widely used in women's menstrual disorders, uterus and chronic constipation. Sewage is also a good medicine to boost the energy of the elderly. Improves kidney function so that hair does not whiten, hair does not fall out, and eating longer prevents aging. Chinese people consider HaoSuo to be the three greatest medicines with ginseng and wolfberry.

Resveratrol, a substance found in sewage, is a substance belonging to the polyphenol family, which is an antioxidant found in plants, and is known to be contained in grapes, mulberries, and peanuts, and is particularly contained in red wine. Resveratrol has been known to have anti-cancer and anti-oxidant effects, and has also been shown to be effective in reducing coronary artery damage and preventing blood clotting, a dangerous phenomenon that causes heart attacks and strokes.

Sewage extract in the present invention can be prepared as follows.

The sewage is washed thoroughly with water and dried in the shade. Dry sewage is placed in an extraction container and extracted for a predetermined time at an appropriate temperature in an appropriate amount of extraction solvent. The extract may be filtered and concentrated using a vacuum rotary evaporator or the like.

As the extraction solvent, a polar solvent selected from water (purified water), a lower alcohol having 1 to 4 carbon atoms, or a mixed solvent thereof may be used. Preferably, ethanol is effective, and the amount of the extraction solvent is 2 to 10 of the dry weight of the herbal medicine. Double it.

The extraction method may be an extraction method such as water bath extraction, reflux cooling extraction, ultrasonic extraction, etc., preferably extracting 1 to 5 times as an extraction method of water bath extraction.

Maintaining the extraction temperature is 30 ~ 70 ℃, more preferably 40 ~ 60 ℃, most preferably about 50 ℃ effective for the prevention of decay, discoloration and odor, extraction time is 5 to 20 hours, preferably It is effective to do for 10 hours.

After obtaining the sewage extract, the solids may be removed using a filter paper, the suspension may be centrifuged, and the supernatant may be filtered under reduced pressure.

The filtered extract may be concentrated under reduced pressure at 20 ~ 100 ℃, preferably 50 ~ 70 ℃ with a vacuum rotary concentrator.

Sewage extract according to the present invention reduces melanin production by melanocytes, has a whitening effect of inhibiting tyrosinase activity, has an antioxidant effect of eliminating free radicals, and inhibits excessive melanin production due to less cytotoxicity. It can be effectively used as a whitening composition.

In the present invention, the sewage extract is preferably contained in an amount of 0.005 to 50% by weight based on the total weight of the composition, when the content is less than 0.005% by weight, the additive effect is weak, and when the content exceeds 30% by weight There is a problem of poor stability.

The composition of the present invention may contain one or more active ingredients exhibiting the same or similar functions in addition to the sewage extract.

Cosmetics prepared with a cosmetic composition containing the sewage extract of the present invention as an active ingredient can be prepared in the form of a general emulsion formulation and solubilized formulation. Cosmetics of the emulsified formulations include nutrient cosmetics, creams, essences, etc., and cosmetics of the solubilized formulations are flexible cosmetics. In addition to the cosmetic containing the sewage extract of the present invention, by containing a dermatologically acceptable medium or base can be prepared in the form of adjuvants that can be applied topically or systemically applied commonly used in the field of dermatology.

Formulations of suitable cosmetics include, for example, emulsions, suspensions, microemulsions, microcapsules, microgranules or ionics (liposomes), nonionics, obtained by dispersing an oil phase in a solution, gel, solid or pasty anhydrous product, aqueous phase. Can be provided in the form of a vesicle dispersant, cream, skin, lotion, powder, ointment, spray or conceal stick. It may also be prepared in the form of a foam or in the form of an aerosol composition further containing a compressed propellant.

In addition, the cosmetic composition of the present invention, in addition to sewage extract, fatty substances, organic solvents, solubilizers, thickening and gelling agents, emollients, antioxidants, suspending agents, stabilizers, foaming agents, fragrances, surfactants, water Commonly used in ionic or nonionic emulsifiers, fillers, metal ion sequestrants and chelating agents, preservatives, vitamins, blockers, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles or cosmetics It may contain adjuvants conventionally used in the cosmetic or dermatology field, such as any other ingredient. In addition, the above components may be introduced in an amount generally used in the dermatology field.

Examples of products to which the cosmetic composition of the present invention may be added include, for example, cosmetics such as astringent cosmetics, soft cosmetics, nourishing cosmetics, various creams, essences, packs, foundations, and the like, cleansing agents, soaps, treatments, and essences. Etc.

Specific formulations of the cosmetic composition of the present invention include skin lotion, skin softener, skin toner, astringent, lotion, milk lotion, moisturizing lotion, nutrition lotion, massage cream, nutrition cream, moisture cream, hand cream, essence, nutrition essence, pack, Formulations such as soaps, shampoos, cleansing foams, cleansing lotions, cleansing creams, body lotions, body cleansers, emulsions, press powders, loose powders, eye shadows and the like.

The following Examples and Experimental Examples illustrate the present invention in more detail, but do not limit the scope of the invention.

Production Example  1: for skin whitening Shouao  Preparation of Extract

50 g of the collected sewage was immersed in 200 ml of 100% ethanol and warmed in a 50 ° C. water bath for 10 hours. The extract was cooled to room temperature and filtered through a filter paper to obtain a filtrate. Ethanol was evaporated from the filtrate using nitrogen, concentrated, and then dissolved in 10% ethanol to produce a sewage extract.

Test Example  One : Intracellular  Melanin inhibitory effect

B16F1 melanoma cells, which are generally used for screening whitening substances as cell lines producing melanin, were provided and cultured by the Korea Cell Line Bank.

The medium for culturing the cells was sterile by adding DMEM, 10% FBS, 1% penicillin / streptomycin, the cell culture was incubated in an incubator of 37 ℃, 5% CO ₂ . Melanoma cells were cultured and passaged when the 100 mm Petri dishes were about 90% full.

In order to measure the whitening effect of sewage extract, the amount of melanin produced by treating B16F1 melanoma cells was measured. Cells were seeded on the 6 well plate and treated with 200 g / ml of the sewage extract prepared in Preparation Example 1, and then cultured for 2 days to recover the cells, and the recovered cells were treated with 1N NaOH containing 10% DMSO. After the reaction was carried out at 90 ° C. for 1 hour to be sufficiently dissolved in melanin, absorbance was measured at a wavelength of 405 nm using an ELISA reader.

Experimental results were calculated using the following equation, the inhibition is shown in Table 1.

Melanin Formation (%) = Treatment Absorbance / Untreated Absorbance × 100

Sample Name Untreated Arbutin Shouao  extract Melanin Production (%) 100 72.6 52.1

As can be seen from Table 1, arbutin, which is known as a general whitening substance, has a melanin content of 72.6% at a concentration of 200 µg / ml, compared to untreated, whereas sewage extract is 52.1%, about 1.75 times higher than arbutin. It was confirmed that it has a higher melanin production inhibitory effect.

Test Example  2: measurement of tyrosinase activity inhibition

It was determined whether sewage extracts affected tyrosinase enzyme activity, which plays an important role in producing melanin.

210 μl of 0.1 M phosphate buffer (pH 6.8) is added to the 96-well plate, and 30 μl of sewage extract or distilled water with a final concentration of 200 μg / ml is added followed by 20 μl of mushroom-derived tyrosinase. . 40 μl of 5 mM L-DOPA was added as a substrate, and then reacted at 37 ° C. for 10 minutes, and then absorbance was measured at a wavelength of 475 nm using an ELISA reader.

Tyrosinase activity was calculated using the following formula, and the melanin inhibitory effect of koji acid and the extract, which was widely used as a whitening agent, is shown in Table 2.

Tyrosinase Activity (%) = Treated Absorbance / Untreated Treated Absorbance × 100

Sample Name Untreated Kojisan Shouao  extract Tyrosinase Activity (%) 100 2.5 42.4

As can be seen from Table 2, only 2.5% of the total activity was obtained when koji acid was treated, while the sewage extract was about 42.4%. Although the inhibitory effect was less than that of kojic acid, sewage extract was also inhibited by more than 57.6% of tyrosinase enzyme activity compared to untreated.

Test Example  3: toxicity test

In order to use the sewage extract as a whitening cosmetic, an experiment was conducted to determine whether or not cytotoxicity. Cells were inoculated into 96 well plates, treated with 200 ㎍ / ml sewage extract, and after 2 days, the medium was removed and the reaction was carried out at 30 ° C. for 4 hours by the addition of 100 μl of MTT solution. After dissolving the cells, the absorbance was measured at a wavelength of 540 nm using an ELISA reader.

Cell viability was calculated using the following formula, and the results are shown in Table 3.

Cell viability (%) = (1-treated absorbance / untreated absorbance) × 100

Sample Name Untreated Arbutin Shouao  extract Cell survival rate (%) 100 98.3 98.8

As can be seen from Table 3, when compared with the cells that were not treated with sewage extract, it can be seen that despite the high concentration of 200 μg / ml, the viable cell rate was 98.8%, which shows little cytotoxicity.

Test Example  4: antioxidant activity experiment

In order to check the antioxidant activity of the sewage extract, it was generally measured using a DPPH solution, which is a method of measuring antioxidant activity.

200 μg / ml of sewage extract and DPPH solution, an antioxidant measurement solution, were mixed and reacted for 30 minutes at 37 ° C., and then absorbance was measured at a wavelength of 517 nm using an ELISA reader.

Experiments with vitamin C, known as antioxidants, compared the relative levels of activity of extracts.

% Antioxidant activity = (1-treated absorbance / untreated absorbance) × 100

Sample Name Vitamin c Shouao  extract Antioxidant activity (%) 66.2% 86.5%

As can be seen from Table 4, it was found that the antioxidant activity of the sewage extract was 86.5%, so it has a strong antioxidant power, and the peculiar point is that the sewage extract shows better antioxidant activity than vitamin C.

Production Example  2 : Example  And Comparative example

A cosmetic composition containing the sewage extract of Preparation Example 1 was prepared, and a cosmetic composition lacking the sewage extract was prepared in the composition ratio of Table 5 below to compare with this.

division Content (% by weight) ingredient Example Comparative example Sewao Extract 4.0 - Cetearyl Octanoate 5.0 5.0 Isopropyl Palmitate 5.0 5.0 Polyacrylamide / C13-14 Isoparaffin / Laureth-7 2.0 2.0 Polysorbate 60 1.7 1.7 Solbitan Sesquioleate 1.3 1.3 Spices, preservatives dose dose Purified water Remaining amount Remaining amount Sum 100 100

Test Example  5

In order to test the clinical whitening efficacy of the cosmetics of the present invention, 40 healthy adult men and women with blemishes, freckles, and pigmentation were randomly divided into two groups (A and B) of 20 people, In Example B, a comparative example was applied twice a day for 12 weeks for group B, and then the change in skin color was measured using chromatameter (Minolta CR300) to measure the change in brightness (ΔL) of color. The whitening effect was measured by objective visual observation by an expert and subjective visual observation by a subject. The results are shown in Table 6 below. At this time, the degree of whitening efficacy was classified into the following seven ratings.

Evaluation criteria for whitening efficacy

-3: worse, -2: worse, -1: slightly worse

 0: no change 1: slight improvement 2: improvement

 3: highly improved

Subject Change in brightness of skin color (△ L) Objective evaluation of the skilled person Subjective Evaluation of Subject A group B group A group B group A group B group One 4.7 2.3 One 0 One One 2 5.0 2.9 2 0 2 0 3 4.6 3.2 3 One 3 One 4 4.4 2.3 One 0 One One 5 4.9 2.1 2 0 One 0 6 4.6 3.4 3 One 2 One 7 4.7 0.7 One 0 2 One 8 4.2 0.7 3 One One 2 9 4.8 2.5 One One 2 One 10 4.2 2.6 2 0 0 0 11 3.9 3.5 One 0 0 -One 12 3.7 3.8 3 0 One 0 13 4.5 2.4 2 0 2 One 14 4.4 1.5 0 0 One 0 15 4.3 2.2 3 One 3 One 16 4.7 2.9 2 One 0 0 17 5.6 2.4 One 0 One 0 18 5.0 3.0 One 0 0 One 19 5.2 2.9 0 0 0 0 20 5.1 2.7 3 2 One 0 Average 4.6 2.5 1.8 0.4 1.2 0.5

As can be seen from Table 6, the change in skin brightness was 1.84 times more effective in applying the Example than in the Comparative Example, and the objective evaluation of the expert and the subjective evaluation of the subject were also applied when the Example was applied to the comparison. Compared with each other, it was confirmed that the 4.5- and 2.4-times improvement was respectively high, and the cosmetics containing sewage extract exhibited excellent effects as enhancing the skin whitening effect.

Formulation example  1: flexible lotion

To a flexible lotion was prepared in a conventional manner as in the composition of Table 7.

Raw material Content (% by weight) Sewao Extract 10.00 1,3-butylene glycol 1.00 Disodium ID 0.05 Allantoin 0.10 Dipotassium glycylizate 0.05 Citrix Acid 0.01 Sodium citrate 0.02 Glyceres-26 1.00 Arbutin 2.00 Hydrogenated Castor Oil 1.00 ethanol 30.00 Preservative a very small amount coloring agent a very small amount Flavor a very small amount Purified water Remaining amount

Formulation example  2: nutrition cream

Nutritional cream was prepared in a conventional manner as in the composition of Table 8.

Raw material Content (% by weight) Sewao Extract 10.0 1,3-butylene glycol 7.0 glycerin 1.0 D-panthenol 0.1 Plant extracts 3.2 Magnesium Aluminum Silicate 0.3 PEG-40 Stearate 1.2 Stearic acid 2.0 Polysorbate 60 1.5 Lipophilic glyceryl stearate 2.0 Sorbitan sesquioleate 1.5 Cetearyl Alcohol 3.0 Mineral oil 4.0 Squalane 3.8 Carlylic / Capric Triglycerides 2.8 vegetable oil 1.8 Dimethicone 0.4 Dipotassium glycylizate a very small amount Allantoin a very small amount Sodium hyaluronate a very small amount Tocopheryl Acetate Quantity Triethanolamine Quantity Preservative Quantity Flavor Quantity Purified water Remaining amount

Claims (5)

Sewage ( Pleuropterus) multiflorus ) The cosmetic composition for skin whitening, characterized in that it contains 0.005 to 50% by weight relative to the total weight of the composition. The cosmetic composition for skin whitening according to claim 1, wherein the extract is hydrothermally extracted by adding a polar solvent selected from water, a lower alcohol having 1 to 4 carbon atoms, or a mixed solvent thereof. The cosmetic composition for skin whitening according to claim 1, wherein the composition is that the skin whitening effect is expressed by inhibiting melanin production. The cosmetic composition for skin whitening according to claim 1, wherein the composition is to express a skin whitening effect by inhibiting tyrosinase activity. The composition of claim 1, wherein the composition is a skin lotion, a skin softener, a skin toner, an astringent, a lotion, a milk lotion, a moisturizer lotion, a nourishing lotion, a massage cream, a nourishing cream, a moisturizing cream, a hand cream, an essence Skin characterized by taking one of the following formulas: nutrition essence, pack, soap, shampoo, cleansing foam, cleansing lotion, cleansing cream, body lotion, body cleanser, latex, press powder, loose powder and eye shadow Whitening cosmetic composition.