KR20030020811A - Whitening cosmetics containing natural extracts - Google Patents

Abstract

PURPOSE: Provided is a whitening cosmetics which contains natural extracts and is excellent in improvement of discoloration on the face, freckles, skin pigmentation disorders, etc. CONSTITUTION: The cosmetic composition is characterized by comprising at least one kind of extract selected from Daphne genkwa Sieb. Et Zucc. and peach seeds, wherein the Daphne genkwa Sieb. Et Zucc. and the peach seeds are sequentially extracted by using a first extraction solvent, such as ethanol, methanol, propanol, butanol, amylalcohol, isopropanol, acetone, ethylmethylketone, et.c, then by using a second extraction solvent , such as ethylacetate, dimethylether, benzene, dichloromethane, chloroform, etc.

Description

Whitening cosmetics containing natural extracts

The present invention relates to a whitening cosmetics containing natural extracts that have an effect of improving the appearance of blemishes, freckles, blemishes, and the like, and more specifically, extracts from a polar solvent and a low polar solvent, which are excellent in melanin production inhibitory effect, in a sequential manner. It relates to a cosmetic composition for skin whitening containing as an active ingredient.

The skin is exposed to various harmful substances such as air and ultraviolet rays caused by air pollution, which can cause various skin problems. Among them, blemishes, freckles and blemishes are one of the biggest skin problems, and much effort has been made to improve them.

Human skin color is determined by red blood cells, carotene, and melanin in the blood, but differences in race color, hyperpigmentation such as blemishes and freckles are caused by melanin. Melanin in the outer skin layer, which is the outer skin of the skin, acts as a sunscreen to protect skin organs below the dermis and also to protect free radicals generated in the skin and to protect proteins and genes in the skin. . The production of melanin in vivo is made by non-enzymatic oxidation reaction after the action of tyrosine (tyrosine) tyrosinase, which is a kind of amino acid, is converted into dopa and dopaquinone. The production of free radicals increases, melanin production increases when there is an inflammatory reaction or ultraviolet rays. In particular, ultraviolet rays may increase the production of melanin, causing melanin, which is partially increased, to develop blemishes, resulting in undesired results, or even worse, inducing skin cancer. In order to overcome the problems caused by the excessive production of melanin, various cosmetics and drugs are being actively developed. In other words, to inhibit the melanin formation process, hydroquinone, ascorbic acid, kojic acid, glutathione, cysteine, etc. Thiol compounds have been used for the purpose of skin whitening, blemishes, and freckles, but hydroquinone-containing whitening agents have some effect, but they cause pigment denaturation, impair cellular function, or cause death. As a result of side effects, the skin irritation is severe and its use is limited to medicines (see J. Soc. Cosmet. Chem. 42,362 (1991)). In addition, although arbutin, a sugar derivative of hydroquinone, has been commercialized, its effect is weak. Ascorbic acid has a problem in oxidative stability, and thiol-based compounds such as glutathione and cysteine have peculiar odor and transdermal absorption. There is no whitening agent having a satisfactory whitening effect. In addition, natural extracts, widely known in the folklore, have a small amount of active ingredients and vary in content depending on the place of production or harvest time, making it difficult to have homogeneity in quality. In addition, since various compounds are extracted together, they have disadvantages in skin side effects and colors. In order to overcome this point, purification is required, but the cost is high, and there is a problem in that it is not applied to actual mass production. For example, licorice extract and lettuce extract known for their whitening efficacy are extremely different depending on the region, and it is difficult to maintain product homogeneity. (Fragrance. J., 6, 59 (1990))

Therefore, the present inventors overcome the problems of conventional whitening materials for various natural natural products that have been used as herbal medicines by using human tyrosinase that can screen a substance that inhibits melanin synthesis induction itself. In order to develop a new whitening agent with superior efficacy, studies have shown that Doin extract and Wonhwa extract have melanin production inhibitory effect, and purification method using polarity difference of solvent to maximize its safety and efficacy Simultaneously with the development, it was found that there is a synergistic effect when combining them in an appropriate ratio.

Accordingly, the present invention provides a cosmetic composition for skin whitening, containing as an active ingredient, which is extracted sequentially from the polar solvent to the low polar solvent, excellent in melanin production inhibitory effect.

The original painting is Daphne genkwa Sieb. Of the family Thymeleaceae. The bud of Et Zucc. (Original, Red Bean) is Latin name Flos Genkwae. Wonhwa has been used as a herbal medicine to treat diuretic and phlegm and to treat asthma, seawater, species, and food poisoning (Chinese metabolism dictionary). Wonhwa has also been used as an anti-virus, anti-HIV patent (JP10287617) and anti-cancer ingredients. Effects (Zhongcaoyao, 1994, 19 (9)) on the effect, blood circulation promoting effect, but not related to the present invention. Existing original ingredient studies have reported substances such as Syringin, Daphnoretin, Daphnorin, Furfural, Luteolin, Yuankanin, Yuanhuanin.

Doin is a blood clot (혈), blood, anti-inflammatory, analgesic, menstrual irregularity, constipation is effective in improving blood circulation. Generally, the fruits of radish trees belonging to the Rosaceae are collected after maturation to remove the pulp and core grains, and only the seedlings are dried and dried to make powder.The ingredients are 40 ~ 50% fatty oil, 3.49% cyanide glycoside, 3.49% prunasin, emusin , And anticoagulant active substances, and has anticoagulant action and weak hemolysis action to release blood stiffness, thus releasing the blood and softening the dry ones, resulting in bruises and swelling pains.瘀血 腫痛) to loosen (Chinese medicine dictionary, p1788) has the effect of turning the blood well. In addition, bleeding, expectoration and lubricating action is pharmacological action.

The present invention primarily extracts wild or cultivated cabbage and Wonhwa in anhydrous or lower alcohols, acetone, and then secondary extraction with low polar solvents such as ethyl acetate, diethyl ether, benzene and chloroform to increase the content of active ingredients. To remove the impurities and improve the stability and at the same time maximize the efficacy of the cosmetics, that is to say, softening water (skin), nutrient cosmetics (lotion), nourishing cream, massage cream, essence, pack.

The present invention will be described in more detail as follows. Commercially available phosphorus and Wonhwa, which are commercially available as a herbal medicine, are finely pulverized and mixed with water or a polar solvent such as acetone or lower alcohols such as ethanol, methanol, propanol and butanol, respectively, as an extraction solvent based on the dry weight of the ground product. The volume was added, the volume was extracted by immersion, filtered, and the filtrate was concentrated under reduced pressure. After dispersion by adding water to the concentrate, an equal amount of low polar organic solvent, ie, ethyl acetate, diethyl ether, benzene, chloroform, etc., is added to the dispersion and shaken. The organic layer is separated and concentrated under reduced pressure to obtain an extract having excellent inhibitory activity on tyrosinase activity. As the extraction method, a cooling capacitor is installed to extract the active ingredient by heating at 50-95 ° C. for 4-20 hours while preventing the active ingredient from evaporating, or extracting the active ingredient by depositing at 5-37 ° C. for 1-15 days. After filtering with a filter cloth, the residue is extracted one more time in the same manner. The primary extract is dispersed in water and then extracted twice with a low polar solvent. The combined organic layers were combined, dried over anhydrous sodium sulfate, concentrated under reduced pressure, and lyophilized or spray dried to obtain a dry extract.

Dried cabbage and Wonhwa extracts exhibit very potent melanin synthesis inhibitory effects when extracted with human tyrosinase compared to conventional polar solvents.

The phosphorus and wonhwa extract obtained as described above is made of a cosmetic such as skin ointment or lotion, and when applied to human skin, the skin whitening effect is very excellent. In addition, it does not cause any side effects, it can be seen that the extracts of causality and wonhwa are safe and very effective, blemishes and freckles improve and skin whitening agent.

In the combination of the phosphorus and the won of the present invention, the combination ratio of the phosphorus and the won is preferably 2: 3 to 3: 2. The content of the phosphorus and the original extract contained in the preparation of the skin ointment or cosmetics is preferably 0.0001-10.0 weight, preferably 0.0005-5.0 weight in dry weight. A clear effect could not be expected at concentrations below 0.0001 weight, and no increase in effect was seen at concentrations above 5 wt.

Next, the present invention will be described in detail with reference to Examples. However, the present invention is not limited by the examples.

Example 1

100 g of a commercially available ceramic powder was put in 2 L of 80% methanol solution, immersed at room temperature for 24 hours, extracted, filtered and the residue was extracted once more in the same manner. Each extract is combined and filtered using Whatman No. 2 filter paper at room temperature to remove insoluble matters, and then concentrated under reduced pressure in a distillation apparatus equipped with a cooling condenser. The mixture was dispersed in 10 ml of water, extracted again with 200 ml of ethyl acetate, and the organic layer was concentrated and lyophilized to obtain a dry weight of 5 g.

Example 2

100 g of a commercially available commercialized powder is put in 5 L of 80 ° C. methanol solution, which is immersed at room temperature for 24 hours, extracted, and filtered. The residue was extracted once more in the same way. Each extract is combined and filtered using Whatman No. 2 filter paper at room temperature to remove insoluble matters, and then concentrated under reduced pressure in a distillation apparatus equipped with a cooling condenser. The mixture was dispersed in 200 ml of water, extracted again with 300 ml of ethyl acetate, and the organic layer was concentrated and lyophilized to obtain a dry weight of 6.5 g.

Example 3

100 g of a commercially available ceramic powder was put in 2 L of 80% methanol solution, extracted by heating under reflux for 2-3 hours, filtered and the residue was extracted once more in the same manner. Each extract is combined and filtered using Whatman No. 2 filter paper at room temperature to remove insoluble matters, and then concentrated under reduced pressure in a distillation apparatus equipped with a cooling condenser. This was extracted with dichloromethane again, concentrated and lyophilized to obtain a dry weight of 7g.

Example 4

100 g of a commercially available commercialized powder was put in 5 L of 80% methanol solution, extracted by heating under reflux for 2-3 hours, filtered and the residue was extracted once more in the same manner. Each extract is combined and filtered using Whatman No. 2 filter paper at room temperature to remove insoluble matters, and then concentrated under reduced pressure in a distillation apparatus equipped with a cooling condenser. This was extracted again with dichloromethane, concentrated and lyophilized to obtain a dry weight of 8g.

Example 5

The extracts of Examples 1 and 2 are mixed at a weight ratio of 1: 1.

Comparative Example 1

Purchasing commercially available ceramics, 100 g of the ground pulverized product is put into 80% and 5 L of methanol solution, which is immersed at room temperature for 24 hours, extracted, and filtered. The residue was further extracted once in the same manner. Each extract is combined and filtered using Whatman No. 2 filter paper at room temperature to remove insoluble matters, and then concentrated under reduced pressure in a distillation apparatus equipped with a cooling condenser. It was dispersed in 200 ml of water and extracted again with 300 ml of butanol, and then the organic layer was concentrated and lyophilized to obtain a dry weight of 4.5 g.

Comparative Example 2

100 g of a commercially available commercialized powder is put in 5 L of 80% methanol solution, which is immersed at room temperature for 24 hours, extracted, and filtered. The residue was extracted once more in the same way. Each extract is combined and filtered using Whatman No. 2 filter paper at room temperature to remove insoluble matters, and then concentrated under reduced pressure in a distillation apparatus equipped with a cooling condenser. The mixture was dispersed in 200 ml of water and extracted again with 300 ml of butanol, and then the organic layer was concentrated and lyophilized to obtain a dry weight of 5.5 g.

Test Example 1; Inhibitory Effect on Human Skin Pigment Cell Tyrosinase Activity

[Test Methods]

Enzyme tyrosinase used human tyrosinase. The activity of the enzyme was measured at 475 nm to produce DOPA chrome, the browning product of L-DOPA. Add 760ul of 50mM Tris-HCI buffer solution (pH 7.5) to the test tube to maintain 37 ° C, add 20mM L-DOPA 190ul, enzyme solution 50ul, whitening activity measurement sample and mix well and measure the absorbance change at 475nm. At this time, measure the sample without the target sample. When the enzyme activity of the control was seen as 100, each enzyme inhibition activity was expressed in% compared to the control. The relative activity of arbutin widely used in whitening cosmetics was compared to observe the relative strength of tyrosinase inhibitory activity of the cabbage or Wonhwa extract.

Tyrosinase Inhibition Activity (%) by Target Samples = (absorbance / Control Absorbance at Specimen Addition) × 100

Table 1 Inhibition of Tyrosinase Activity of Won-In and Phosphorus Extracts

Test Example 2: Whitening effect test on human skin

[Experimental Method] A opaque tape with 6 holes of 1.5cm diameter was attached to the upper forearm of 20 healthy men and irradiated with UVB (1.5-2 times the minimum erythema of each subject). After inducing skin blackening and applying test materials two months later, the contrast of the skin was measured using a colorimeter. Each test material was dissolved in a vehicle of propylene glycol / ethanol (8/2) to a concentration of 1% and corrected twice daily (morning and evening).

The contrast of the skin is expressed as the 'L' value and ranges from 0 (black) to 100 (pure white) (Koreans generally have values between 50 and 70).

When the test substance is applied, the L value gradually increases when it is effective, and the comparison between the test substances is expressed as ΔL (final L value-the value immediately before applying the test substance).

[Test result]

<Table 2>

Test Example 3: Whitening Clinical Effect

[Test Method] Samples containing the present invention (Examples 1-5, Comparative Examples 1-2) and existing for 100 subjects (20 people per sample) who suffer from pigmentation such as blemishes on the face A control sample (arbutin) containing a known whitening agent was dissolved in a vehicle of propylene glycol / ethanol (8/2) to a concentration of 1% and applied to the spots of the face twice daily for 3 months, once every morning and evening. .

EVALUATION METHOD The improvement of pigmentation after use was judged according to the following criteria. The results are shown in Table 3.

<Table 3>

Excellent effect: Pigmentation is hardly noticeable.

With effect: Pigmentation is very soft.

Slightly effective: Pigmentation is softened.

No effect: no change.

Test Example 4 Skin Safety Test

Skin safety was compared with respect to the extract prepared in Example 1-5. As for the safety of the skin, a conventional patch test was conducted. Thirty people were divided into three groups and used for 10 days of facial treatment, and then the average value was calculated according to the intensity of stimulation. The results are shown in Table 4 below.

(Score)

4: very irritating and unsuitable for use

3: It is better not to use because of severe irritation

2: slight irritation and need attention when using

1: almost no irritation

0: No irritation at all, suitable for sensitive skin

Table 4

From the results of Table 4, there is no significant difference between the samples and there is little irritation, so the extract of the present invention is evaluated to be suitable for use as a cosmetic raw material.

Based on the results of the test examples described above, by extracting the phosphorus and wonhwa sequentially from a polar solvent to a low polar solvent as an active ingredient, it has a melanin production inhibitory effect without skin irritation, such as skin burning with spots, freckles and sunlight Basic cosmetic compositions of various formulations that can provide skin whitening effects, such as preventing skin pigmentation, are presented. However, the composition of the present invention is not limited to the following prescription example.

[Prescription Example 1]

A prescription example of supple cosmetics (skin) is as follows.

Compounding weight%

Example 1 0.1

Example 2 0.1

Glycerin 2.0

Butylene Glycol 1.0

Propylene Glycol 2.0

Sodium Hyaluronate 0.1

Ethanol 10.0

Triethanolamine 0.1

Preservative traces

A small amount of pigment

A small amount of spices

Purified Water Balance

[Prescription 2]

A prescription example of nutrient lotion (lotion) is as follows.

Compounding weight%

Example 1 0.5

Example 2 0.5

Beeswax 4.0

Polysorbate 60 1.5

Solbitan Sesquioleate 0.5

Liquid Paraffin 5.0

Squalane 5.0

Capricric / Capric Triglycerides 5.0

Glycerin 5.0

Butylene Glycol 3.0

Propylene Glycol 3.0

Carboxy Vinyl Polymer 0.1

Triethanolamine 0.2

Preservative traces

A small amount of pigment

A small amount of spices

Purified Water Balance

[Prescription 3]

A prescription example of nutrition cream is as follows.

Compounding weight%

Example 1 1.0

Example 3 1.0

Cetostearyl Alcohol 3.0

Stearic Acid 1.5

Glycerin Monostearate 3.0

Silicone Oil 0.5

Lanolin Oil 5.0

Squalane 15.0

Polyoxyethylene sorbitan monostearate 2.0

Sorbitan Monostearate 0.5

Glycerin 5.0

Triethanolamine 0.2

Preservative traces

A small amount of pigment

A small amount of spices

Purified Water Balance

As described above, according to the present invention, by containing the extract extracted from the polar solvent with the excellent melanin production inhibitory effect from the polar solvent to the low polar solvent as an active ingredient, it has a melanin production inhibitory effect, such as skin burning in the spots, freckles and sunlight The skin whitening effect, such as to prevent skin pigmentation, can be improved.

As mentioned above, although the invention made by this inventor was demonstrated according to the said Example, this invention is not limited only to the said Example.

Claims (3)

Cosmetic composition containing at least one of Wonhwa or Doin extract. The method of claim 1, wherein the extraction method is a method of extracting the original or phosphorus first with a polar solvent, concentrated and then secondly extracted with a low polar solvent, the primary extraction solvent is ethanol, methanol, propanol, butanol, amyl alcohol, isopropanol, A whitening cosmetic, characterized in that the second extraction solvent is ethyl acetate, dimethyl ether, benzene or dichloromethane, chloroform, alone or mixed solvents such as acetone, ethyl methyl ketone and the like. The method according to claim 1, wherein the original extract or the phosphorus extract and / or the mixed extract thereof are contained in an amount of 0.00001-5% (w / v), preferably 0.001-2% (w / v) as dry weight thereof. Whitening cosmetics characterized by.