KR100678865B1 - Cosmetic composition for skin whitening comprising ramulus mori extract and carnitine as active ingredient - Google Patents

Abstract

Provided is a cosmetic composition capable of offering higher skin-whitening effect, increasing the cell regeneration by using the carnitine, and securing the formulation stability by comprising the extract of Ramulus mori, without skin irritation, which is caused by conventional keratin peeling agent. The cosmetic composition for skin-whitening comprises an extract of Ramulus mori and carnitine as effective ingredients. Regarding the total weight of the composition, 0.002-10.0 wt.% of the extract of Ramulus mori and 0.01-10.0 wt.% of the carnitine are contained. The extract is obtained by using a solvent selected from the group consisting of water, C1-4 alcohol, acetone, ethylacetate, butyl acetate, chloroform and 1,3-butyleneglycol. The cosmetic composition is in the formulation selected from the group consisting of solution, suspension, emulsion, paste, gel, cream, lotion, surfactant-containing cleansing, oil, powder foundation, emulsion foundation, and spray.

Description

Cosmetic composition for skin whitening containing upper extremity extract and carnitine as active ingredient {Cosmetic Composition for Skin Whitening Comprising Ramulus mori Extract and Carnitine as Active Ingredient}

The present invention relates to a cosmetic composition for skin whitening, and more particularly, the present invention relates to a cosmetic composition for skin whitening containing the upper limb extract and carnitine as an active ingredient.

One of the areas of greatest interest to East Asian women in the field of cosmetics is skin whitening. Skin whitening is a concept that prepares the change of skin color due to excessive production of melanin pigment in the skin by external stimulation.

In general, the blackening of the human skin is caused by melanin pigment produced by the skin. In normal condition, excessive production of melanin does not occur, but the skin is exposed to external stimuli such as ultraviolet rays, environmental pollution, stress, or hormonal or inflammatory response parameters. Responding to internal factors such as overproduction produces melanin pigment, which can't get out of the skin and remains in the skin, causing pigmentation.

In melanocytes of the human body, enzymes such as tyrosinase, tyrosinase related protein (TRP) -1, and TRP-2 are present and melanin pigments based on tyrosine (L-tyrosine) present in vivo (Cohen, T., et al . Nucleic Acids Res ., 18: 2807-2808 (1990); Jackson, IJ, et al ., EMBO J. , 11: 327-535 (1992)). This enzymatic reaction occurs in melanocytes, the organelles of pigmented cells, and the newly produced melanin containing melanin is distributed to adjacent keratinocytes through the dendrite of pigmented cells. Causes skin color to appear

Tyrosinase is an enzyme inserted into the membrane located in the melanosome. It has copper ions at the active site and is a major rate limiting enzyme in a series of melanin synthesis. Therefore, inhibitors that inhibit tyrosinase activity have been actively developed as whitening agents. Examples of such tyrosinase activity inhibitors include kojic acid, arbutin, hydroquinone, vitamin C and derivatives thereof, and licorice extract. have. However, they have problems with skin irritation and stability in the formulation and their use is limited.

Conventional whitening cosmetics have been developed by applying a whitening raw material to improve the above problems, for example, the extract of the upper limbs ( Ramulus mori ) extracted from the soft branches of the mulberry plant.

Republic of Korea Patent No. 253842 discloses a whitening cosmetics containing melbourne extracted from the upper limbs of the soft branch of the mulberry plant, Republic of Korea Patent No. 230130 discloses a whitening cosmetics containing the extract of the upper limbs, registered in Korea Patent No. 260510 discloses a whitening cosmetic containing a dispensing extract of the upper limb extract.

In healthy skin, the cells in the outermost layer of the stratum corneum are constantly detached and replaced with newly created cells in the basal layer of the epidermis. The time required for the migration of newly created cells from the basal layer to the outermost layer of the stratum corneum is called the epidermal renewal time. As skin homeostasis changes, dead cells accumulate in the outermost layer, slowing the rate of renewal and lengthening the time of renewal. As you age, the time needed to renew your skin increases. For young or middle-aged adults, the renewal time is approximately 20 days, whereas for adults 50 and older, the rate of renewal is slower than 30 days (Aging and the skin, Raven Press, New York, 1989, 193-204).

In general, by removing dead skin cells and increasing the rate of skin renewal, the result can be a brighter and younger skin. In particular, regulating the rate of skin renewal may be used to increase the whitening effect. For this purpose, hydroxy acids having a peeling effect such as glycolic acid and lactic acid are used. However, hydroxy acid has a disadvantage of high effect and low irritation at low pH (3.5 to 4.5).

Throughout this specification, many papers and patent documents are referred to and their citations are indicated. The disclosures of cited papers and patent documents are incorporated herein by reference in their entirety, so that the level of the technical field to which the present invention belongs and the contents of the present invention are more clearly explained.

The present inventors have diligently researched to develop a cosmetic composition having excellent skin whitening effect with low skin irritation and excellent formulation stability, and the whitening effect is synergistically exhibited when the upper limb extract and carnitine are included as an active ingredient. By using carnitine to increase the rate of cell renewal, the skin irritation caused by conventional keratin exfoliants was solved and the stability of the formulation caused by the addition of carnitine was lowered by buffering action of the upper limb extract. Thus, the present invention has been completed.

The present invention provides a cosmetic composition for skin whitening containing the upper limb extract and carnitine as an active ingredient.

Upper limb ( Ramulus mori ) is a dried branch of mulberry plants. The shape is long columnar, rarely branched, not uniform in size, and 0.5-1.5 cm in diameter. The surface is grayish yellow or yellowish brown, with many yellowish brown spotted pores and fine crusts. There are grayish white semicircular leaf traces and yellowish brown solution. The thickness of the section is 0.2-0.5 cm, the outer part is relatively thin, the wood part is yellowish white, the diagonal is radial, and the male part is white or yellowish white. The upper limbs are collected between late spring and early summer, and after removing the leaves, they are cut to 30-60 cm when fresh and sun-dried. Upper limbs are slightly bitter and have the effect of eliminating anti-inflammatory, diuretic, tonic, sweating and wind, and have been used as herbal medicine for a long time.

The "upper limb extract" used as an active ingredient in the composition of the present invention refers to a substance extracted from the upper limbs which are the young branches of mulberry. The upper limb extract may be a variety of extraction solvents, for example, water, anhydrous or hydrous lower alcohol having 1 to 4 carbon atoms (methanol, ethanol, propanol, butanol, etc.), a mixed solvent of the lower alcohol with water, acetone, ethyl acetate, Chloroform, 1,3-butylene glycol and butyl acetate can be obtained as an extraction solvent. More preferably, the upper limb extract of the present invention is obtained using a hydrous lower alcohol, most preferably ethanol.

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-described extraction solvent but also the extract of the upper limbs having substantially the same effect using other extraction solvents.

In addition, the extract of the present invention includes not only the extract by the aforementioned extraction solvent, but also an 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 active fraction is also included in the upper limb extract of the present invention. In addition, the range of “upper limb extract” includes “melbourne” and other processed products of upper limbs extracted and processed from upper limbs.

 The upper limb extract of the present invention may be prepared in powder form by additional processes such as distillation under reduced pressure and freeze drying or spray drying.

“L-carnitine”, which is used as an active ingredient in the composition of the present invention, is an naturally occurring amino acid-like substance that is produced endogenously in the body and is also consumed from red meat such as beef or lamb. Carnitine is a white crystalline, hygroscopic solid.

Carnitine is generally known to play an important role in fat metabolism and is used as a composition for regulating cellulite in cosmetics (Korean Patent Publication No. 2005-67837). Recent studies have reported that carnitine has the effect of activating cellular metabolism. In particular, carnitine has been found to promote cell proliferation by increasing the metabolic activity of mammalian cells (Cosmetics and Toiletries Manufacture Worldwide, 120-126).

The cosmetic composition of the present invention may include other whitening active ingredients in addition to the upper limb extract and carnitine as the active ingredient. However, the cosmetic composition of the present invention shows a very good whitening effect even with an active ingredient consisting only of the upper limb extract and carnitine.

According to a preferred embodiment of the present invention, the content of the upper limb extract and carnitine is 0.002-10.0% by weight and 0.01-10.0% by weight relative to the total weight of the cosmetic composition, more preferably 0.1-5.0% by weight and 0.1-5.0, respectively Weight percent.

At this time, when the content of the upper limb extract is less than 0.002% by weight, the content of carnitine is less than 0.01% by weight, the effect is less likely to appear, when the content of the above components is more than 10.0% by weight, it is highly likely to cause irritation to the skin, stabilization of the formulation Can have a big impact.

The components included in the cosmetic composition of the present invention include, as an active ingredient, ingredients commonly used in cosmetic compositions in addition to the active ingredients, and include, for example, conventional auxiliaries such as antioxidants, stabilizers, solubilizers, vitamins, pigments, and perfumes, And carriers.

Cosmetic compositions of the present invention may be prepared in any formulation conventionally prepared in the art and include, for example, solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing cleansing , Oils, powder foundations, emulsion foundations, wax foundations and sprays, and the like can be formulated, 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 oil, vegetable oil, wax, paraffin, starch, trakant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide, etc. 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, polyethyleneglycol 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 aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, 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 cosmetic composition of the present invention is a combination of the upper limb extract and carnitine as an active ingredient, the tyrosinase inhibitory effect of the upper limb extract and the exfoliation effect of carnitine appear in combination, which is more synergistic than the use of each of the above ingredients alone (synergic) Whitening effect can be achieved. In addition, the use of carnitine as a keratin exfoliant improves the problem that the skin irritation occurs due to the use of hydroxy acid, and the instability of the formulation caused by the addition of carnitine can be solved by the addition of the upper limb extract. This fact is specified in the following examples.

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, and it will be apparent to those skilled in the art that the scope of the present invention is not limited by these examples according to the gist of the present invention. .

Preparation Example 1 Preparation of Upper Limb Extract

The upper extremity extract contained in the cosmetic composition of the present invention was prepared as follows: First, the upper extremity powder was washed with purified water and dried and then broken into small pieces into 10 times 70% ethanol, and extracted at 15-35 ° C. for 5 days. After filtration with a 300 mesh filter cloth, the mixture was left to mature for 7-10 days at 5-10 ° C. and filtered with Whatman filter paper. This extract was then dried at 65 ° C. on a rotary reduced pressure evaporator to yield an upper extremity extract powder. The upper limb extract powder was dissolved in a solution in which water and 1,3-butylene glycol were mixed in the same amount to obtain the upper limb extract of the present invention.

Preparation Example 2 Preparation of Cosmetics in Cream Formulation

Cream formulations were prepared using various ingredients in the composition ratios shown in Table 1 below for the whitening effect, stimulation test, and stability test of the composition containing the upper limb extract and carnitine. Upper extremity extract used in the preparation of the composition is the extract prepared in Preparation Example 1, carnitine is a Natrulon product of LONZA (Switzerland).

division Content (% by weight) ingredient Example Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Upper limb extract 3.0 - 3.0 - - - Carnitine 1.0 - - 1.0 - - Lactic acid - - - - 1.0 - Glycolic acid - - - - - 1.0 Butylene glycol 2.0 2.0 2.0 2.0 2.0 2.0 Propylene glycol 6.0 6.0 6.0 6.0 6.0 6.0 Carboxy Vinyl Polymer 0.5 0.5 0.5 0.5 0.5 0.5 Beeswax 2.0 2.0 2.0 2.0 2.0 2.0 vaseline 7.0 7.0 7.0 7.0 7.0 7.0 Polysorbate 60 2.0 2.0 2.0 2.0 2.0 2.0 Sorbitan sesquioleate 2.5 2.5 2.5 2.5 2.5 2.5 Squalane 3.0 3.0 3.0 3.0 3.0 3.0 Liquid paraffin 10.0 10.0 10.0 10.0 10.0 10.0 Triethanolamine 0.5 0.5 0.5 0.5 0.5 0.5 Tocopheryl Acetate 0.1 0.1 0.1 0.1 0.1 0.1 Spices, preservatives a very small amount a very small amount a very small amount a very small amount a very small amount a very small amount Purified water Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Sum 100 100 100 100 100 100

Experimental Example 1: Measurement of the whitening effect

For 20 women aged 34-45 years, the whitening effect of each cosmetic product prepared in Preparation Example 2 was measured. Seven areas of the subject's arm were displayed by 1 cm by 1 × width, and UV-A was irradiated with a light amount of 15 J / cm 2 to cause blackening, and each of the cosmetics of Preparation Example 2 was applied twice a day for 1 month. Skin color (L value) was measured after 1 month using Minolta CR 300, a skin color measuring instrument, and the degree of change in skin color was calculated using the following equation, and the results are shown in Table 2 below.

ΔL value = L value before cosmetic application-L value after 1 month

Whitening clinical trial results division Example Comparative Example 1 Comparative Example 2 Comparative Example 3 ΔL value 4.89 0.46 1.64 1.87

According to the results of Table 2, the formulation of the Example containing both the upper extremity extract and carnitine is about three times compared to the cream containing only the upper extremity extract (Comparative Example 2), about compared to the cream containing only carnitine (Comparative Example 3) It showed 2.6 times higher whitening effect. Therefore, it could be seen that synergistically significantly increasing the whitening effect when the upper limb extract and carnitine were simultaneously contained as in the composition of the present invention.

Experimental Example 2 skin irritation test

In order to test the skin irritation of each of the cosmetic preparations prepared in Preparation Example 2, a patch test was conducted using a Haye's Test Chamber on 20 healthy men and women. Wipe the test site with 70% ethanol and dry, and then use a chamber (Finn chamber, 100x10, EPITEST, Finland) in which 15 μg or 15 μl of the prepared test substance (cosmetics of Preparation Example 2) was added dropwise. ) It was sealed in the inner part. The patch was applied for 24 hours, the patch was removed, and the test site was marked with a marker pen. 1 hour and 24 hours after each removal (1 hour after removal, 24 hours = 24 hours, 48 hours including patch attachment) using a magnifying glass (8MC-150, DAZOR, United States of America) to observe the test site for erythema and edema Was observed. Skin response was determined according to the regulations of the International Contact Dermatitis Research Group (ICDRG) (Table 3), the average skin reactivity was calculated by the following equation and the results are shown in Table 4.

 Evaluation criteria and score of skin reaction sign score Evaluation standard - 0 No response, normal skin ± 0.5 Faint or light erythema + 1.0 Boundary but weak erythema, edema and papules + 2.0 Pronounced erythema, papules and vesicles +++ 3.0 Severe erythema and vesicle formation ++++ 6.0 Cannon formation

Test substance 24 hours 48 hours Average skin reactivity (n = 20) ± + + + ± + + + Example 1 1- --- 0.63 Comparative Example 1 One - - --- 0.21 Comparative Example 3 1 1- --- 0.63 Comparative Example 4 5 3- 3 2- 3.75 Comparative Example 5 4 4- 3 1- 3.54

As shown in Table 4, the skin reaction was very low in the formulation containing carnitine (Comparative Example 3) in contrast to the results of high skin irritation in the formulation containing lactic acid or glycolic acid (Comparative Examples 4 and 5) In the cream formulation containing both the upper limb extract and carnitine used in the present invention, there was also almost no skin irritation, and the upper limb extract and carnitine were found to be components that hardly cause skin irritation.

Experimental Example 3: Stability Test of the Formulation

Each cosmetic prepared in Preparation Example 2 was tested for the stability of the formulation according to the temperature change. The following evaluation criteria for long-term storage stability by putting each cosmetic in an opaque glass container in units of 1 week, 1 month, and 6 months in a thermostat and a room temperature of 4 ° C, 45 ° C, 50 ° C, and Cycle (4 ° C-45 ° C) It is evaluated as shown in Table 5 below.

<Storage Stability Evaluation Criteria>

Good: ○, Unstable: ×, Separation: △

Preservation condition Example Comparative Example 1  Comparative Example 3 4 ℃ 1 week 0 0 0 1 month 0 0 0 6 months 0 0 0 45 ℃ 1 week 0 0 0 1 month 0 0 0 6 months 0 0 X 50 ℃ 1 week 0 0 0 1 month 0 0 0 6 months 0 0 X Cycle 1 week 0 0 0 1 month 0 0 X 6 months 0 0 X Room temperature 1 week 0 0 0 1 month 0 0 0 6 months 0 0 0

As shown in Table 5, the formulation containing only carnitine (Comparative Example 3) was very low in long-term storage stability, but in the formulation (Example) containing both carnitine and the upper limb extract of the present invention, the stability was excellent, the upper limb extract Has been shown to improve the stability of carnitine containing formulations.

Hereinafter, on the basis of the results of the above experimental examples, a cosmetic composition containing the upper limb extract and carnitine as an active ingredient is presented. However, the composition of the present invention is not limited to the following formulation examples.

Formulation Example 1: Softener (Skin Lotion)

ingredient Content (% by weight) Upper limb extract 3.0 Carnitine 1.0 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 Remaining amount

Formulation Example 2: Nutrients (Milk Lotion)

ingredient Content (% by weight) Upper limb extract 3.0 Carnitine 1.0 Propylene glycol 6.0 glycerin 4.0 Triethanolamine 1.2 Tocopheryl Acetate 3.0 Floating paraffin 5.0 Squalane 3.0 Macadamia Nut Oil 2.0 Polysorbate 60 1.5 Sorbitan sesquioleate 1.0 Carboxyvinyl Polymer 1.0 Incense, preservative a very small amount Purified water Remaining amount

Formulation Example 3: Nutrition Cream

ingredient Content (% by weight) Upper limb extract 3.0 Carnitine 1.0 vaseline 7.0 Liquid paraffin 10.0 Beeswax 2.0 Polysorbate 60 2.0 Sorbitan sesquioleate 2.5 Squalane 3.0 Propylene glycol 6.0 glycerin 4.0 Triethanolamine 0.5 Carboxy Vinyl Polymer 0.5 Tocopheryl Acetate 0.1 Incense, preservative a very small amount Purified water Remaining amount

Formulation Example 4: Massage Cream

ingredient Content (% by weight) Upper limb extract 3.0 Carnitine 1.0 Propylene glycol 6.0 glycerin 4.0 Triethanolamine 0.5 Beeswax 2.0 Tocopheryl Acetate 0.1 Polysorbate 60 3.0 Sorbitan sesquioleate 2.5 Cetearyl Alcohol 2.0 Liquid paraffin 30.0 Carboxy Vinyl Polymer 0.5 Incense, preservative a very small amount Purified water Remaining amount

Formulation Example 5: Pack

ingredient Content (% by weight) Upper limb extract 3.0 Carnitine 1.0 Propylene glycol 2.0 glycerin 4.0 Carboxy Vinyl Polymer 0.3 ethanol 7.0 Fiji-40 Hydrogenated Castor Oil 0.8 Triethanolamine 0.3 Incense, preservative a very small amount Purified water Remaining amount

As described in detail above, the present invention provides a cosmetic composition for skin whitening containing the upper limb extract and carnitine as an active ingredient. Cosmetic composition of the present invention by using the upper limb extract and carnitine as an active ingredient, the tyrosinase inhibitory effect of the upper limb extract and the keratin exfoliation effect of the carnitine appear in combination, which is more synergistic than the use of each of the active ingredients alone (synergic) A) whitening effect can be achieved, and it can be usefully used as a cosmetic composition for skin whitening with little skin irritation and excellent stability.

Having described the specific part of the present invention in detail, it is apparent to those skilled in the art that such a specific technology is only a preferred embodiment, and the scope of the present invention is not limited thereto. Therefore, the substantial scope of the present invention will be defined by the appended claims and equivalents thereof.

Claims (5)

Cosmetic composition for skin whitening containing the upper limb extract and carnitine as an active ingredient. The cosmetic composition for skin whitening according to claim 1, wherein the content of the upper limb extract is 0.002-10.0 wt% of the total weight of the cosmetic composition. The cosmetic composition for skin whitening according to claim 1, wherein the content of carnitine is 0.01-10.0 wt% of the total weight of the cosmetic composition. The method of claim 1, wherein the upper limb extract is extracted using a solvent selected from the group consisting of water, anhydrous or hydrous lower alcohol having 1 to 4 carbon atoms, acetone, ethyl acetate, butyl acetate and 1,3-butylene glycol Cosmetic composition for skin whitening, characterized in that. 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 Cosmetic composition for skin whitening, characterized in that it has a formulation selected from the group.