KR20060116362A - Cosmetic composition for skin-whitening comprising ramulus mori extract and coenzyme q-10 - Google Patents

Abstract

A cosmetic composition for skin-whitening comprising the extract of Ramulus mori and coenzyme Q-10 is provided to improve tyrosinase-inhibiting activity of coenzyme Q-10, and reduce skin irritation of coenzyme Q-10 with the extract of Ramulus mori, so that melanin synthesis is inhibited. The cosmetic composition for skin-whitening comprises the extract of Ramulus mori and coenzyme Q-10 as effective ingredients, wherein the amount of Ramulus mori extract is 0.002-10.0 wt.% and the amount of coenzyme Q-10 is 0.03-5.0 wt.% based on the total weight of composition; the Ramulus mori extract is prepared by extracting Ramulus mori with water, C1-4 anhydrous or hydrous lower alcohol, acetone, ethylacetate, butylacetate or 1,3-butylene glycol; and the composition is formulated as solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing, oil, powder foundation, emulsion foundation, wax foundation or spray.

Description

Cosmetic composition for skin whitening containing upper limb extract and coenzyme VII-10 {Cosmetic Composition for Skin-Whitening Comprising Ramulus Mori extract and Coenzyme VII-10}

The present invention relates to a cosmetic composition, and more particularly, the present invention relates to a cosmetic composition for skin whitening comprising the extract of the upper limbs and coenzyme Q-10 as an active ingredient.

One of the areas of greatest interest to East Asian women in cosmetics is skin whitening. Skin whitening is a concept that adjusts the color 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 excessive production of melanin pigments, which can't be released out of the skin and remain in the skin, cause pigmentation.

In melanocytes of the human body, enzymes such as tyrosinase, tyrosinase related protein (TRP) -1, and TRP-2 are present, and melanin pigments are formed by using tyrosine (L-tyrosine) as a substrate. Acts to produce (Cohen, T., et al. Nucleic Acids Res., 18: 2807-2808 (1990); (Jackson, I. J., 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 in stability in the formulation and their use is limited.

Conventional whitening cosmetics have been developed and applied to improve the stability of the formulation, whitening raw materials to improve the above problems. An example is a lichen extract extracted from the soft branches of mulberry plants.

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

The present inventors have found that coenzyme Q-10 has an excellent effect of inhibiting the activity of tyrosinase, a major rate limiting enzyme in melanin synthesis, but has a high irritation problem in skin application. The present inventors have completed the present invention by confirming that as a result of diligent research efforts to improve this, the whitening effect is increased and the skin irritation by coenzyme Q-10 is improved when coenzyme Q-10 and the upper extremity extract are adjusted to an appropriate ingredient ratio. .

Accordingly, it is an object of the present invention to provide a composition for skin whitening comprising the upper limb extract and coenzyme Q-10 as an active ingredient.

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

The present invention provides a whitening cosmetic composition comprising the upper limb extract and coenzyme Q-10 as an active ingredient.

The upper limb ( Ramulus Mori ) is a dried branch of mulberry plants, the shape of which is long cylindrical, 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 harvest time of upper limbs is between late spring and early summer. After removing the leaves, they are cut to 30-60cm when fresh and dried in the sun. Upper limbs have a bitter taste and have the effect of removing anti-inflammatory, diuretic, tonic, sweating and wind, and has been used as a herbal medicine for a long time.

Coenzyme Q-10, called ubiquinone and ubidecarenone, is known as a natural substance with strong antioxidant effects involved in oxidation and reduction reactions in vivo. Coenzyme Q-10 is widely distributed from bacteria to higher organisms and is present only in mitochondria in higher cells. The isoprenoid side chain that binds to the ubiquinone skeleton depends on the species. In mammals, n = 10 is often used, but in yeast, n = 6 may be used. These are referred to as coenzyme Q-10 and coenzyme Q-6, respectively. Melting point depends on the number of n, but usually 16-45 ℃. It is difficult to dissolve in water and soluble in organic solvents.

The "upper limb extract" used as an active ingredient in the composition of the present invention collectively refers to a material 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 from the upper limb 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 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 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.

According to a preferred embodiment of the present invention, the cosmetic composition of the present invention comprises 0.002-10.0% by weight of the upper limb extract and 0.03-5.0% by weight of coenzyme Q-10.

When the content of the upper limb extract in the cosmetic composition of the present invention is less than 0.002% by weight, there is a problem that can not be expected to inhibit the tyrosinase activity, when it exceeds 10.0% by weight does not increase the apparent effect of the increase in the content of the formulation There is a problem with stability.

When the content of coenzyme Q-10 in the cosmetic composition of the present invention is less than 0.03% by weight, there is a problem in that tyrosinase activity inhibitory effect cannot be expected, and when it exceeds 5.0% by weight, there is no obvious effect increase due to the increase in content There is a problem with the stability.

According to a preferred embodiment of the present invention the amount of upper limb extract is 0.02-10.0% by weight, the amount of coenzyme Q-10 is 0.3-5.0% by weight, more preferably 0.1-10% by weight, the amount of coenzyme Q-10 is 0.5 -4.0 wt%, most preferably the amount of upper limb extract is 5.0 wt% and the amount of coenzyme Q-10 is 2.0 wt%.

The cosmetic composition of the present invention achieves a synergic whitening effect by using the upper limb extract and coenzyme Q-10 together as an active ingredient, respectively, and the skin irritation caused by coenzyme Q-10 extracts the upper limbs. Since it is alleviated by, the problem of skin irritation caused by coenzyme Q-10 can be solved.

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, but are 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.

Through the following examples will be described the present invention in more detail. 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.

Experimental Example 1 Determination of Tyrosinase Activity Inhibition

Tyrosinase from the mushroom detach And Refined Sigma (In the United States of America) Purchase Used. As a substrate L-tyrosine (Sigma) 0.05 M Sodium phosphate Buffer (pH 6.8) Dissolve 0.1 Mg / ml With solution make Used. Test substance 0.05M Sodium Phosphate Buffer (pH 6.8) Proper In concentration Adjusted Dissolved after Used. Coenzyme Q-10 was purchased from Nissin Flour Milling (Japan). L-tyrosine solution 0.5 Ml In a test tube Put Here Sample liquid 0.5 Ml each Putting 37 ℃ In a thermostat 10 minutes It was left. That after bracket In the sample liquid 200 unit / ml Tyrosinase 0.5 Ml Add At 37 ℃ 10 minutes Reacted. this Reaction solution Whether Test tube ice above Let go Quench the reaction Stopped after Spectroscopy With photometer wavelength At 475 nm Absorbance Measured. As a control, 0.5 ml of buffer solution was used instead of the sample solution.

Of each sample liquid Tyrosinase activation Inhibition rate doing In the equation follow Calculate and experiment result doing table 1 and in Table 2 Indicated.

% Inhibition of enzyme activity = 100-{(comparative absorbance / control absorbance) x 100}

Upper extremity extract concentration (µg / ml) Enzyme Inhibition Rate (%) 5 23.5 10 42.8 20 65.1 50 75.8 100 95.4 200 95.7

Coenzyme Q-10 Concentration (µg / mL) Enzyme Inhibition Rate (%) 50 23.6 100 34.7 200 48.6 400 72.0 800 95.3

Coenzyme Q-10 Concentration (µg / mL) Upper limb extract concentration (㎍ / ㎖) Enzyme Inhibition Rate (%) 50 0 23.6 50 2.5 46.7 50 5 73.4 50 10 87.3

As shown in Table 1 and Table 2, the upper limb extract and coenzyme Q-10 showed a relatively high inhibitory effect on tyrosinase activity. On the other hand, as shown in Table 3, when the upper extremity extract and coenzyme Q-10 were used at the same time, the rate of enzyme activity inhibition was significantly increased than when using each.

Preparation Example 1 Preparation of Cream Formulation

In order to identify the proper mixing ratio of the upper extremity extract and coenzyme Q-10 in the whitening cosmetic composition, a cream formulation containing the mixed upper extremity extract and coenzyme Q-10 was prepared.

Cream formulation containing upper extremity extract and coenzyme Q-10 ingredient Content (% by weight) Example Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Comparative Example 6 Comparative Example 7 Comparative Example 8 Comparative Example 9 Comparative Example 10 Comparative Example 11 Comparative Example 12 Comparative Example 13 Comparative Example 14 Upper limb extract 5 - One 3 5 7 9 11 5 5 5 - - One 3 Coenzyme Q-10 2 - - - - - - - One 4 6 One 2 2 2 Glycerin 4.0, petrolatum 3.5, triethanolamine 2.1, liquid paraffin 5.3, squalane 3.0, beeswax 2.6, tocopheryl acetate 5.4, polysorbate 60 3.2, carboxyvinyl polymer 1.0, sorbitassesquioleate 3.1, trace amounts, preservative traces, Purified water level

Experimental Example 2: Stability Test

The stability according to the temperature change of each cosmetic prepared in the preparation example was tested. Each cosmetics are stored in an opaque glass container for 1 week in a thermostatic bath at a constant temperature of 45 ° C. Also, the cosmetics are kept at 4 ° C in a opaque glass container for 1 week and stored for 1 week in a completely shaded refrigerator. Was measured. The results are shown in Table 6 below. At this time, the degree of discoloration of the product was evaluated by classifying to 6 grade of Table 5 below.

Product discoloration evaluation criteria score Evaluation standard 0 No change One Very little change 2 Little change 3 Slightly worse 4 Badly changed 5 Extremely severe

Temperature Discoloration degree of test substance Example Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Comparative Example 6 Comparative Example 7 Comparative Example 8 Comparative Example 9 Comparative Example 10 45 ℃ 0 0 0 0 0 0 0 2 0 0 2 4 ℃ 0 0 0 0 0 0 0 0 0 0 One

As can be seen in Table 6, the stability of the formulation by the other components of the cream in view of the discoloration does not occur in the cream of Comparative Example 1 that does not contain both the upper limb extract and coenzyme Q-10 used in the present invention There was no problem with. In the cream formulations of Examples and Comparative Examples 1-6, 8, and 9 of the present invention, discoloration did not occur, and thus the stability of the formulation was excellent, and 6.0 wt% of Comparative Example 7 and coenzyme Q-10 containing 11.0 wt% of the upper extremity extract were included. Discoloration occurred in the cream of Comparative Example 10, causing a problem in stability.

Experimental Example 3 Measurement of Whitening Effect

Thirty females, 24-41 years old, whose skin color was dark, were measured for the whitening effect of each cosmetic prepared in the preparation. Twelve places of the subject's arms were displayed by 1 cm in width and length, and each of the cosmetics of Preparation Example 1 was applied, and the other one was used as a control. Cosmetics were applied twice a day for two months. After measuring the skin color (L value) after 2 months using Minolta CR 300 as a measuring device to calculate the degree of change of the skin color using the following equation is shown in Table 7 below.

   △ L value = L value before applying cosmetics-L value after 2 months

Whitening clinical trial results division Example Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Comparative Example 6 Comparative Example 8 Comparative Example 9 Comparative Example 11 Comparative Example 12 △ L value 4.76 0.51 0.73 1.98 2.80 2.82 2.85 3.15 4.79 0.62 0.81

As shown in Table 7, the ΔL value increased in proportion to the concentration of the upper limb extract in the cream of Comparative Example 2-6, but there was no change in the ΔL value at the concentration of 5.0 wt% or more. In the creams of Examples, Comparative Examples 8 and 9 containing 5.0% by weight upper limb extract, the ΔL value was increased in proportion to the amount of coenzyme Q-10 added, but the concentration of coenzyme Q-10 was higher than 2.0% by weight (example). The value of ΔL hardly changed. Whitening clinical trials using 1 to 2% by weight of Coenzyme Q-10 alone resulted in a slight whitening effect (Comparative Examples 11 and 12). Coenzyme Q-10 showed tyrosinase inhibitory activity, but the content used in clinical trials alone showed excellent whitening effect, which may be due to the small amount or the fact that its activity was not maintained or expressed in cosmetics. However, the present invention provided an excellent whitening synergy effect when used in combination with the upper limb extract (Example).

Experimental Example 4: Skin Irritation Test

In order to test the skin irritation of each cosmetic prepared in the preparation example, a patch test was carried out using a Haye's Test Chamber on 20 healthy adult men and women. After wiping the test site with 70% ethanol and drying, 15 μg or 15 μl of the prepared test substance was placed in a sealed chamber (Finn chamber, 100x10, EPITEST, Finland) in the forearm of the test subject. 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) 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 8), and the average skin reactivity was calculated by the following equation and the results are shown in Table 9.

 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

Mean skin reactivity (meanscore) = ∑ {(reactivity x number of subjects) / [6 (maximum responsiveness) x 20 (total subjects)]} x 1/2 x 100

Test substance 24 hours 48 hours Average skin reactivity (n = 20) ± + ++ ± + ++ Example  2 - - One - - 0.63 Comparative Example 1 One - - One - - 0.42 Comparative Example 11 4 1- 4 0- 2.08 Comparative Example 12 5 4- 3 1- 3.75 Comparative Example 13 3 2- 2 2- 2.71 Comparative Example 14 2 1- 1 1- 1.46

As shown in Table 9, the skin reactivity of the cream of Comparative Example 1 that does not contain both the upper limb extract and coenzyme Q-10 used in the present invention is very low and does not cause skin irritation by the other ingredients of the cream. And it was found. In the cream of Comparative Example 11-12 containing coenzyme Q-10, the irritation was high in proportion to the concentration of coenzyme Q-10, and in addition to coenzyme Q-10, upper extremity extracts were added to the examples and comparative examples 13-14. In the case of cream, it was found that the irritation was lowered in proportion to the concentration of the upper limb extract.

As described in detail above, the present invention provides a skin whitening cosmetic composition comprising the upper extremity extract and coenzyme Q-10 as an active ingredient. The cosmetic composition of the present invention synergistically increases the whitening effect by using both the upper limb extract and coenzyme Q-10 as an active ingredient, the skin irritation by coenzyme Q-10 is alleviated by the upper limb extract, so there is almost no skin irritation It can be usefully used as a cosmetic composition for.

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 (4)

Cosmetic composition for skin whitening comprising upper extremity extract and coenzyme Q-10 as an active ingredient The cosmetic composition for skin whitening according to claim 1, wherein the upper extremity extract is 0.002-10.0% by weight of the total weight, and coenzyme Q-10 is 0.03-5.0% by weight. The extract 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 method of claim 1 wherein the whitening cosmetic composition is 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 consisting of.