KR20040087644A - Cosmetic Composition Comprising Pyrus communis L. Extract for Skin Whitening - Google Patents

Abstract

PURPOSE: Provided is a cosmetic composition comprising the Pyrus communis L. extract as an active ingredient for skin whitening. The composition inhibits melanogenesis and has stable formulation, while causing no skin stimulation. CONSTITUTION: The composition for skin whitening comprises, as an active ingredient, 0.01-20.0 wt.% of the Pyrus communis L. extract which is obtained by using, as an extraction solvent, (a) water, (b) C1-4 anhydrous or hydrous lower alcohol, (c) a mixed solvent of the lower alcohol and water, (d) acetone, (e) ethyl acetate, (f) chloroform or (g) 1,3-butyleneglycol. The composition is formulated into suspension, emulsion, paste, gel cream, lotion, powder, oil, powder type foundation, emulsion type foundation, wax type foundation and spray.

Description

Whitening cosmetic composition containing pear extract {Cosmetic Composition Comprising Pyrus communis L. Extract for Skin Whitening}

The present invention relates to a whitening cosmetic composition, and more particularly to a whitening cosmetic composition comprising a pear tree extract as an active ingredient.

Blackening of the skin is caused by the response of skin cells to internal and external factors, a representative factor being UV exposure of the skin. That is, when the skin is exposed to ultraviolet rays, tyrosinase is activated, which acts on tyrosine, a type of amino acid present in the skin tissue, to produce dopa, and then to produce dopaquinone. In the melanocytes, a polymer called melanin is synthesized in the melanosome, which is transferred to keratinocytes, keratinocytes of the skin, which reaches the surface of the skin by keratinization and protects the skin from ultraviolet rays. do.

Therefore, melanin is an indispensable UV protective agent in our human body, and also serves as an effective free radical scavenger that removes various radicals that modify biological components such as proteins, lipids, nucleic acids, etc. When excessively synthesized, or skin physiological function of the skin lesions and aging due to aging, melanin is deposited on the surface of the skin causing blemishes, freckles and various pigmentation.

As the causes and mechanisms of skin blackening are revealed, a method of reducing melanin production by incorporating substances having an inhibitory effect of tyrosinase, an enzyme involved in the skin blackening process, into cosmetics or inhibiting some reactions in melanogenesis. It is commonly used. Representative materials used for this purpose include ascorbic acid, kojic acid, hydroquinone and the like, plant extracts such as lettuce extract, licorice extract.

However, kojic acid has a high tyrosinase activity inhibitory effect, but has a problem in stability, such as lowering the titer due to discoloration and change over time when blended in cosmetics and has a limitation on use due to large skin irritation. Ascorbic acid has a low inhibitory effect on tyrosinase activity and low stability of the molecule itself, and thus is not suitable as a melanin inhibitor. Hydroquinone has a high irritation to the skin and is currently limited in its use in cosmetic formulation due to safety issues. In addition, most plant extracts have a relatively high inhibitory effect on tyrosinase activity only at high concentrations, and at low concentrations, there is a problem such that little inhibitory effect appears. In particular, the biggest problem of the existing melanogenesis inhibitors is that the whitening effect is weak in clinical experiments on human skin.

Accordingly, the present inventors have been used as a herbal medicine or a folk remedy in order to develop a whitening cosmetic that can overcome the problems of weak clinical whitening effect, formulation instability and skin irritation, which are problems of existing melanin production inhibitors. As a result of intensive research on a substance having a whitening effect on natural plants, it has been found that the extract obtained from the pear tree has an excellent melanin production inhibitory effect and can overcome the above-mentioned problems.

Accordingly, it is an object of the present invention to provide a whitening cosmetic composition containing pear extract.

Other objects and advantages of the present invention will become apparent from the following detailed description and claims.

The present invention provides a whitening cosmetic composition comprising pear tree extract as an active ingredient.

Pear ( Pyrus communis L. , Pear) tree extract used as an active ingredient for the whitening effect in the present invention may be any one obtained by extracting from various organs (eg, leaves, flowers, stems, branches, etc.) of the pear tree, but is preferred. It is preferably obtained from the branch of the pear tree, more preferably from the bark (bark) of the pear tree branch. There are no examples of pear extracts used in whitening cosmetics for the purpose of removing blemishes, freckles and various pigmentation.

The above-mentioned pear tree extract can be obtained using various extraction methods known in the art, and preferably, (a) water, (b) anhydrous or hydrous lower alcohol having 1 to 4 carbon atoms (methanol, ethanol, propanol, Butanol, etc.), (c) the mixed solvent of the lower alcohol and water, (d) acetone, (e) ethyl acetate, (f) chloroform or (g) 1,3-butylene glycol. Can be. More preferably, extraction is carried out using an aqueous methanol and ethanol solution, and most preferably, extraction is performed using an ethanol aqueous solution.

On the other hand, it will be apparent to those skilled in the art that the extract of the present invention can be obtained not only the above-mentioned extraction solvent but also other extracting solvent, which has substantially the same effect.

In addition, the extract of the present invention includes not only the extract by the above-described extraction solvent, but also the extract that has undergone a conventional purification process. Obtained by various additional purification methods, such as, for example, separation using ultrafiltration membranes having a constant molecular weight cut-off value, separation by various chromatography (manufactured for separation according to size, charge, hydrophobicity or affinity). The fraction is also included in the pear extract of the present invention.

Pear tree extract of the present invention may be prepared in a powder state by an additional process such as vacuum distillation and freeze drying or spray drying.

Among the methods for obtaining the pear tree extract of the present invention, specific examples of the method using ethanol are as follows: First, pear tree branches are impregnated with water and left for 10-24 hours, and then 70% ethanol aqueous solution is added, Heat at 50-90 ° C for 1-20 hours in the extractor with cooling capacitor. Subsequently, the extraction solvent is concentrated under reduced pressure with a distillation apparatus equipped with a cooling capacitor to obtain a pear tree extract.

Another specific extraction method is as follows: First, pear branches are impregnated with water and left for 10-24 hours, then 70% ethanol aqueous solution is added, followed by extraction at 5-40 ° C. for 1-15 days. Then, the extraction solvent is concentrated under reduced pressure with a distillation apparatus equipped with a cooling capacitor to obtain a pear tree extract.

According to a preferred embodiment of the present invention, the pear extract is included in an amount of 0.01-20.0% by weight, preferably 0.1-10.0% by weight, based on the total weight of the composition.

Ingredients included in the cosmetic composition of the present invention include ingredients commonly used in cosmetic compositions in addition to pear extract as an active ingredient, such as conventional auxiliaries such as antioxidants, stabilizers, solubilizers, vitamins, pigments and flavorings, and Carrier.

The whitening composition of the present invention may be prepared in any formulation conventionally prepared in the art, for example, solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing It may be formulated as cleansing, oil, powder foundation, emulsion foundation, wax foundation, spray, and the like, but is not limited thereto. More specifically, it may be prepared in the form of a flexible lotion, nutrition lotion, nutrition cream, massage cream, essence, eye cream, cleansing cream, cleansing foam, cleansing water, pack, spray or powder.

When the formulation of the present invention is a paste, cream or gel, animal oils, vegetable oils, waxes, paraffins, starches, trachants, cellulose derivatives, polyethylene glycols, silicones, bentonites, silicas, talc or zinc oxide may be used as carrier components. Can be.

When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used, in particular in the case of a spray, additionally chlorofluorohydrocarbon, propane Propellant such as butane or dimethyl ether.

When the formulation of the present invention is a solution or emulsion, a solvent, solubilizer or emulsifier is used as the carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 Fatty acid esters of, 3-butylglycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan.

When the formulation of the present invention is a suspension, liquid carrier diluents such as water, ethanol or propylene glycol, suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystals Soluble cellulose, aluminum metahydroxy, bentonite, agar or tracant and the like can be used.

When the formulation of the present invention is a surfactant-containing cleansing, the carrier component is an aliphatic alcohol sulfate, an aliphatic alcohol ether sulfate, a sulfosuccinic acid monoester, isethionate, an imidazolinium derivative, a methyltaurate, a sarcosinate, a fatty acid amide. Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, lanolin derivatives or ethoxylated glycerol fatty acid esters and the like can be used.

The whitening cosmetic composition of the present invention has a melanin production inhibitory effect, that is, the whitening effect is very excellent by the pear tree extract used as an active ingredient, the formulation is very stable, and has the advantage of hardly causing skin irritation.

Hereinafter, the present invention will be described in more detail with reference to Examples. These examples are only for illustrating the present invention in more detail, it is to those skilled in the art that the scope of the present invention is not limited by these examples in accordance with the gist of the present invention. Will be self-evident.

Preparation Example 1

The pear tree was impregnated with water and left for 10-24 hours, then the peeled bark was collected and dried (1 kg), crushed, and 5 ℓ of 70% ethanol was added to the ground product, followed by an extractor with a cooling capacitor. Extracted by heating at 80 ° C. for 3 h. The extract was filtered through a 350 mesh filter cloth and then filtered through Whatman No. 2 filter paper, and concentrated under reduced pressure at 60 ° C. using a distillation apparatus equipped with a cooling capacitor to obtain an extract having a dry weight of 9.5 g.

Test Example 1 Test of Inhibition of Tyrosinase Activity

First, tyrosine, a substrate, was dissolved in 0.05 M sodium phosphate buffer (pH 6.8) to prepare a 0.1 mg / ml substrate solution. 100 mg of pear tree branch extract of Preparation Example 1 was dissolved in 10 ml of 50% 1,3-butylene glycol, diluted in buffer solution, and the extract sample solution was prepared at 5, 25, 50, 100, 200 and 500 µg / ml. Ready. Subsequently, 0.5 ml of substrate solution was added to a test tube, 0.5 ml of extract sample solution was added thereto, and reacted for 10 minutes in a 37 ° C thermostat. Then, 0.5 ml of 200 U / ml tyrosinase solution (Sigma, USA) extracted from mushrooms was added thereto, followed by stirring. Then, it was reacted for 10 minutes in a 37 ℃ thermostat.

The test tube containing the reaction solution was placed on ice and quenched to stop the reaction. Absorbance was measured at 475 nm with a spectrophotometer to calculate the tyrosinase activity inhibition rate according to Equation 1 below. The results are shown in Table 1. Instead of pear tree branch extract, 0.5 ml of buffer solution was used as a control.

% Inhibition of tyrosinase activity = 100-{100 x (absorbance of each extract / absorbance of control)}

Extract concentration (µg / ml) Tyrosinase activity inhibition rate (%) 5 12.1 25 15.2 50 28.6 100 38.5 200 62.7 500 76.4

As can be seen in Table 1, the concentration of pear tree branch extract that inhibits tyrosinase activity by 50% is 147.52 ㎍ / ㎖, considering that kojic acid is about 5.8 ㎍ / ㎖, upper limb extract is about 0.5 ㎍ / ㎖ The inhibitory effect of pear tree branch extract on tyrosinase activity is not excellent.

Test Example 2: Melanin production inhibitory test

After 5-6 ml of DMEM medium was added to a 25 cm2 T-flask, the cells were inoculated with a cryopreserved mouse-derived B-16 melanoma (ATCC CRL 6323) cell line and incubated at 37 ° C. and 5% CO ₂ for 24 hours. Cells were separated by treatment with 0.05% trypsin containing 0.02% EDTA, followed by incubation in a 25 cm 2 T-flask and incubated for 48 hours. As a result, the cell number obtained was 5.68 × 10 ⁶ per flask. 100 μg / ml pear tree branch extract was diluted in DMEM medium and treated with cultured melanoma cells and cultured at 37 ° C. for 5 days.

After incubation, all of the medium was removed, and the cells were separated by treatment with 1 ml of phosphate saline buffer (PBS) containing 0.02% EDTA and 0.05% trypsin, followed by centrifugation for 5 minutes to collect only cells. The collected cells were treated with 5% trichloroacetate (TCA), stirred, and centrifuged to wash the precipitated melanin with phosphate saline buffer. Subsequently, 1 N NaOH was dissolved and dissolved in the precipitated melanin, the absorbance was measured at 475 nm, and the melanin concentration was determined from the standard concentration curve of the synthetic melanin (Sigma, United States of America).

Hereinafter, the concentrations of the pear tree branch extract untreated group and the pear tree branch extract obtained in the preparation example were adjusted to 10, 50, 100, and 200 µg / ml to determine the melanin content and the inhibition of melanin production by concentration. The results are shown in Tables 2 and 3 below. Meanwhile, the same experiment was conducted using kojic acid as a test substance instead of the pear tree branch extract, and the results are described in Comparative Tables 2 and 3 below.

Experimental concentration (µg / ml) Melanin content (pg / cell) Preparation Example 1 Comparative Production Example 1 No treatment group 4.31 4.31 10 2.59 2.34 50 2.16 2.27 100 1.22 2.09 200 0.81 2.02

Experimental concentration (µg / ml) Melanin production inhibition rate (%) Preparation Example 1 Comparative Production Example 1 No treatment group 4.31 4.31 10 2.59 2.34 50 2.16 2.27 100 1.22 2.09 200 0.81 2.02

As can be seen in Table 2 and Table 3, in the cell culture experiment of melanocytes that produce melanin cells, the melanin production inhibitory ability of the pear tree branch extract is excellent, and showed much superior inhibition than kojic acid.

Taken together, the pear tree branch extract plays a role in reducing melanin production by mainly inhibiting other reactions during melanogenesis, rather than inhibiting tyrosinase activity during the skin blackening reaction mechanism. .

Example 1 and Comparative Example 1

Essence was prepared as a whitening cosmetic composition with the ingredients and contents described in Table 4 below.

ingredient Content (% by weight) Example 1 Comparative Example 1 Pear Tree Branch Extract 3.0 - Kojic acid - 0.8 glycerin 10.0 10.0 Betaine 5.0 5.0 PEG 1500 2.0 2.0 Allantoin 0.1 0.1 DL-panthenol 0.3 0.3 EDTA-2Na 0.02 0.02 Benzophenone-9 0.04 0.04 Hydroxyethyl cellulose 0.1 0.1 Sodium hyaluronate 8.0 8.0 Carboxy Vinyl Polymer 0.2 0.2 Triethanol amine 0.18 0.18 Octyldodecanone 0.3 0.3 Octyldodeceth-16 0.4 0.4 ethanol 6.0 6.0 Incense, preservative, coloring a very small amount a very small amount Purified water to 100 to 100

Test Example 3: Whitening efficacy test by clinical experiment

In order to test the clinical whitening efficacy of the cosmetic composition 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, Applied Example 1 and Comparative Example 1 twice for 12 weeks. Subsequently, the change in skin color was measured by chromatometer (Minolta CR300), and the brightness change (ΔL) of the color was measured. The results are shown in Table 5 below. The degree of whitening efficacy was evaluated by classifying into the following seven grades: -3: very deteriorating; -2 deterioration; -1: slightly worse; 0: no change; 1: slightly improved; 2: improvement; And 3: very improved

Subject Change in brightness of color (ΔL) Objective evaluation of the skilled person Subjective Evaluation of the Subject A group B group A group B group A group B group One 3.5 2.3 2 0 2 0 2 4.2 2.3 One One One One 3 3.2 2.0 0 One 0 One 4 3.2 1.9 One One 3 0 5 4.2 2.0 2 0 0 0 6 3.5 1.8 3 0 One One 7 3.5 1.8 2 0 3 0 8 3.1 2.5 2 One One 0 9 2.8 2.3 2 0 0 0 10 2.9 2.4 3 2 2 One 11 3.8 2.8 One One 0 2 12 3.5 3.6 3 0 One 0 13 3.5 1.5 0 0 0 0 14 3.5 2.5 2 0 2 0 15 4.3 2.3 One One 3 One 16 2.6 2.0 One One One 0 17 3.8 1.8 3 One One One 18 3.5 1.8 2 One 2 One 19 3.9 2.5 One 0 One 0 20 4.2 2.4 2 One 0 One Average 3.54 2.23 1.7 0.6 1.2 0.5

As can be seen in Table 5, the average ΔL value of the A group coated with the cosmetic composition containing the pear tree branch extract of the present invention is 3.54 (p <0.01), B group coated with the cosmetic composition containing kojic acid The average ΔL value of was 2.23 (p <0.05), A group showed 1.7 (p <0.01) and B group 0.6 (p <0.05) in the whitening evaluation by skilled workers. (p <0.05), group B is 0.5 (p> 0.05), and it can be seen that the group A, that is, pear tree branch extract, has superior clinical whitening efficacy than kojic acid.

Test Example 4: Stability Test of Formulation

In order to test the stability of the cosmetic formulation of the present invention, Example 1 and Comparative Example 1 were stored in an opaque glass container for 2 weeks in a constant temperature bath kept at 45 ° C., and also kept at 4 ° C. completely. After storing for 2 weeks in an opaque glass jar in a shaded refrigerator, the degree of discoloration was measured. The experimental results are shown in Table 6. At this time, the degree of product discoloration was evaluated by classifying into the following six grades.

* Product Discoloration Evaluation Criteria *

0: no change 1: very little change 2: little change

3: slightly changed 4: severely changed 5: extremely severe

Temperature Discoloration degree Example 1 Comparative Example 1 45 ℃ 0.5 5.0 4 ℃ 0.0 2.0

As can be seen in Table 5, since the cosmetic composition containing the pear tree branch extract of the present invention is hardly discolored, it can be seen that the stability as a formulation is large, and the stability is higher than that of the conventional cosmetic composition containing kojic acid. It is very large.

Test Example 5: Skin Irritation Test

In order to test the skin irritation degree of the cosmetic of the present invention, Example 1 and Comparative Example 1 were removed after applying for 24 hours by the Patch Test method, and the skin irritation degree appeared at this time was measured and compared. The results are shown in Table 7 below. At this time, skin irritation degree was evaluated by classifying into the following six grades.

* Skin irritation evaluation criteria *

0: no stimulation 1: almost no stimulation 2: little stimulation

3: slight stimulation 4: severe stimulation 5: severe stimulation

Elapsed time Skin irritation degree Example 1 Comparative Example 1 24 hours 0.9 3.3 48 hours 0.0 1.5

As can be seen in Table 7, it can be seen that the cosmetic composition containing the pear tree branch extract of the present invention hardly induces skin irritation, and has a very low skin irritation compared to the conventional cosmetic composition containing kojic acid. Able to know.

Hereinafter, based on the results of the above test examples, by containing a pear tree branch extract to present a cosmetic composition of various formulations that can provide a skin whitening effect. However, the composition of the present invention is not limited to the following formulation examples.

Formulation Example 1: Flexible Lotion (Skin Lotion)

ingredient Content (% by weight) Pear Tree Branch Extract 0.1 1,3-butylene glycol 6.0 glycerin 4.0 Oleyl alcohol 0.1 Polysorbate 20 0.5 ethanol 15.0 Benzophenone-9 0.05 Incense, preservative a very small amount Purified water to 100

Formulation Example 2: Nutrients (Milk Lotion)

ingredient Content (% by weight) Pear Tree Branch Extract 1.0 Propylene glycol 6.0 glycerin 4.0 Triethanol amine 1.2 Tocopheryl Acetate 3.0 Floating paraffin 5.0 Squalane 3.0 Macadamia Nut Oil 2.0 Polysorbate 60 1.5 Solitansesquioleate 1.0 Carboxyvinyl Polymer 1.0 Incense, preservative a very small amount Purified water to 100

Formulation Example 3: Nutrition Cream

ingredient Content (% by weight) Pear Tree Branch Extract 3.0 vaseline 7.0 Floating paraffin 10.0 Beeswax 2.0 Polysorbate 60 2.0 Solitansesquioleate 2.5 Squalane 3.0 Propylene glycol 6.0 glycerin 4.0 Triethanol amine 0.5 Carboxy Vinyl Polymer 0.5 Tocopheryl Acetate 0.1 Incense, preservative a very small amount Purified water to 100

Formulation Example 4: Massage Cream

ingredient Content (% by weight) Pear Tree Branch Extract 0.1 Propylene glycol 6.0 glycerin 4.0 Triethanol amine 0.5 Beeswax 2.0 Tocopheryl Acetate 0.1 Polysorbate 60 3.0 Solitansesquioleate 2.5 Cetearyl Alcohol 2.0 Floating paraffin 30.0 Carboxyvinyl Polymer 0.5 Incense, preservative a very small amount Purified water to 100

Formulation Example 5: Pack

ingredient Content (% by weight) Pear Tree Branch Extract 3.0 Propylene glycol 2.0 glycerin 4.0 Carboxyvinyl Polymer 0.3 ethanol 7.0 PEG-40 Hydrogenated Castor Oil 0.8 Triethanol amine 0.3 Incense, preservative a very small amount Purified water to 100

As described in detail above, the present invention provides a whitening cosmetic composition comprising pear tree extract as an active ingredient. The whitening cosmetic composition of the present invention has a melanin production inhibitory effect, that is, clinical whitening effect is very excellent, as well as the formulation is very stable and hardly cause skin irritation by the pear extract used as an active ingredient.

Claims (7)

Whitening cosmetic composition comprising pear tree extract as an active ingredient. The method of claim 1, wherein the pear extract is (a) water, (b) anhydrous or hydrous lower alcohol having 1 to 4 carbon atoms, (c) a mixed solvent of the lower alcohol and water, (d) acetone, (e) A whitening cosmetic composition, characterized in that ethyl acetate, (f) chloroform, or (g) 1,3-butylene glycol is obtained as an extraction solvent. The whitening cosmetic composition according to claim 1, wherein the pear extract is obtained by using ethanol as an extraction solvent. The whitening cosmetic composition according to claim 1, wherein the content of the pear extract is 0.01-20.0 wt% based on the total weight of the composition. The whitening cosmetic composition according to claim 1, wherein the pear tree extract is obtained from a pear tree branch. The whitening cosmetic composition according to claim 1, wherein the pear extract is obtained from bark of pear branches. The composition of claim 1 wherein the cosmetic composition consists of a solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing, oil, powder foundation, emulsion foundation, wax foundation and spray Whitening cosmetic composition, characterized in that it has a formulation selected from the group.