KR20030071893A - Water soluble whitening composition and cosmetic composition for whitening skin comprising the same - Google Patents

Abstract

PURPOSE: A skin whitening cosmetic composition containing an aqueous whitening composition in a mixing ratio for providing an optimum synergistic whitening effect at a small amount is provided which causes no skin irritation while overcoming the problem of a change in quality over a predetermined time period. CONSTITUTION: A skin whitening cosmetic composition comprises an aqueous whitening composition and an adjuvant in a weight ratio of 0.1 to 10.0:1. The aqueous whitening composition contains: a citrus unshiu peel extract; aminoethylphosphinic acid; one or more of waltheria indica leaf extracts and Guava phenone; and hydrolyzed yeast in a weight ratio of 5:0.5 to 4:0.1 to 3:1 to 8. The adjuvant is one or more selected from the group consisting of arbutin, kojic acid and ellagic acid. The whitening cosmetic has excellent storage stability and whitening activity.

Description

Water-soluble whitening composition and cosmetic composition for skin whitening containing the same {WATER SOLUBLE WHITENING COMPOSITION AND COSMETIC COMPOSITION FOR WHITENING SKIN COMPRISING THE SAME}

The present invention not only provides an excellent synergistic whitening effect even in a small amount, but also overcomes problems such as changes over time that may be present during the manufacturing process or storage of the product, and exhibits an effect such as no irritation to the skin. And it relates to a cosmetic composition for skin whitening containing the same. More specifically, the water-soluble whitening composition of the present invention is a citrus ounce oil peel extract; Aminoethylphosphonic acid; At least one of Walderian Indica leaf extract and guavaphenone; And a hydrolyzed yeast aqueous solution. In addition, the cosmetic composition for skin whitening of the present invention contains the water-soluble whitening composition, and if necessary, further contains one or more selected from the group consisting of arbutin, kojic acid, eric acid, and rucinol, which are existing whitening ingredients, as auxiliary ingredients. It is characterized by being manufactured.

Skin is a very important tissue that protects the human body while having direct contact with the external environment and has biochemical and physical functions. This tissue is largely divided into three parts: epidermis, dermis and subcutaneous tissue. Human skin color depends mainly on the number, size, type and distribution of melanocytes containing melanin in skin cells. Melanosomes are produced by melanocytes and melanin, a black pigment produced in the epidermis, is produced in cells called melanocytes. Melanin absorbs ultraviolet light energy from sunlight, preventing deeper cells from being damaged by ultraviolet light. When abnormally low melanin is produced, skin lesions such as vitiligo are induced, and on the contrary, excessive synthesis of melanin by ultraviolet light not only damages the skin, but also forms spots, freckles, and further causes skin cancer.

The most important role in melanin formation is known as tyrosinase enzyme, which produces dopaquinone, which acts on an amino acid called tyrosine in tissues. The pigment melanin is produced. Therefore, the composition for whitening may be made in several ways as follows depending on which process of the step to inhibit melanin production.

First, it contains a component that can block ultraviolet rays, which is the main cause of melanin production, and the composition according to this method contains a light scattering agent or a light blocking agent to reduce DNA damage or inflammation caused by ultraviolet rays, such as glucosamine and tyrosinia. By inhibiting the synthesis of core carbohydrates necessary for me to be active, melanin production can be suppressed (acting on the whitening A stage). The second is to use substances that interfere with the function of tyrosinase involved in melanogenesis, such as enzymatic acid (kojic acid), rucinol, eric acid or arbutin (acting on the whitening B stage). Third, there is a method of stabilizing dopachrome to stop the progression to black melanin (Eu-Melanin) (acts on the whitening C stage). Fourth, while tyrosine undergoes complex oxidation and condensation reactions through dopa and dopachrome, it uses a substance such as vitamin C that has a strong antioxidant effect and can produce a whitening effect (acting on the whitening step D). Fifth, there is a method that can remove and reduce the melanin produced in the stratum corneum by using enzymes or AHA (Alpha Hydroxy Acid) (acts on the whitening step E).

However, conventional ascorbic acid (Japanese Patent Application Laid-Open No. 4-9320), hydroquinone (Japanese Patent Application Laid-Open No. 6-192062), kojic acid (Japanese Patent Application Laid-Open No. 56-7710), arbutin (Japanese Patent Application Laid-Open No. 4-9315), and some extracts, etc. Although it is used as a whitening cosmetic because it has a cinnase inhibitory activity, they are degraded due to poor stability in the prescription system, and there are problems such as the occurrence of odor, efficacy at the biological level, unclearness and safety of the use, etc. This situation is limited. Therefore, to use such existing whitening agents in cosmetics, such as stabilizing agents or stabilizing capsules and water-in-oil emulsions, such as formulations or formulations to achieve phase stabilization and skin safety, but the side effects of the added stabilizer This may also occur and it was difficult to stabilize the amount sufficient to give a whitening effect. In addition, the inhibitory effect of tyrosinase was demonstrated, but there were many substances that showed low effect in melanogenesis and human clinical experiments of melanoma B16, which is similar to the actual biological level.

Therefore, while overcoming the problems of the conventional whitening agent, while using a small amount than the existing whitening agent has an excellent whitening effect and it is necessary to develop a whitening agent without side effects such as irritation to the skin.

Accordingly, the present inventors conducted intensive research to solve the conventional problems, and in the process, when selecting the appropriate ingredients among the 10 kinds of whitening agents that were recognized as excellent whitening efficacy effect, whitening than each whitening material while overcoming the problems of the existing whitening agent It has been found that water soluble whitening compositions can be provided with significantly improved effects. In addition, when the water-soluble whitening composition thus developed and arbutin, kojic acid, ericic acid or rucinol used in the previous stage of whitening B are used in combination, the effect is not only significantly improved than when using a whitening agent such as arbutin alone. It has been found that the effect is increased over the above water-soluble whitening composition containing no whitening agent.

1 is a comparison of dopa-oxydase activity to see the effect of inhibiting tyrosinase activity of the water-soluble whitening composition according to the present invention.

2 is a skin tissue diagram when purified water is used as a control.

3 is a skin tissue diagram when using the example composition according to the present invention.

<Explanation of simple sign>

B: Stratum Basale

SC: Stratum Corneum

MC: Melanin Pigment Granules

The present invention relates to a water-soluble whitening composition having excellent skin whitening effect and a cosmetic composition for skin whitening containing the same. More specifically, the water-soluble whitening composition of the present invention except for group B, which is known to be excellent in tyrosinase inhibitory effect, except for soldier A group, more specifically, citrus milk oil peel extract; Group C, more specifically aminoethylphosphonic acid; At least one of group D, more specifically, Walderian indica leaf extract or guavaphenone; Group E, more specifically, characterized in that the mixture is made by mixing a hydrolyzed yeast aqueous solution, the water-soluble whitening composition provides a synergistic whitening effect significantly superior to the respective whitening components. In addition, when the water-soluble whitening composition of the present invention is used in combination with one or more of the conventional whitening agent group B, that is, a whitening agent consisting of arbutin, kojic acid, eric acid and rucinol, the whitening effect is further increased.

Here, group A refers to a group capable of inhibiting melanin production by acting on the whitening A stage, that is, reducing DNA damage or inflammation caused by ultraviolet rays and inhibiting tyrosinase production. By action, that is, a group capable of inhibiting melanin production by interfering with the function of tyrosinase involved in the production of melanin, C group means by acting on the whitening C stage, that is, stabilizing the generated dopachrome black Melanin means a group that can prevent the production of u-melanin, D group means a group having a strong antioxidant ability to act on the whitening D stage, that is, inhibit the oxidation of tyrosine by ultraviolet light, , E group refers to the group that acts on the whitening E stage, that is, the melanin produced and removed from the stratum corneum.

In order to exhibit a more preferable whitening effect of the water-soluble whitening composition of the present invention, the citrus seed oil peel extract (group A); Aminoethylphosphonic acid (group C); At least one of Walderian Indica leaf extract or guavaphenone (group D); It is preferable that hydrolysis yeast aqueous solution (group E) is mixed by the weight ratio of 5: 0.5-4: 0.1-3: 1-8. More preferably, A: C: D: E is in a ratio of 5: 1: 0.3: 2.

The reason why the ratio of group A in the mixing ratio is high is that the effect of tyrosinase is most significant in the whitening step, and therefore, a method of minimizing the formation of tyrosinase should be considered first. In addition, the E phase whitening agent, which removes and reduces completely melanin from the stratum corneum, should take up the next weight to obtain excellent results in the final clinical results. In the case of the C and D stage whitening agents, the melanin oxidation process is delayed or alleviated. Therefore, they complement the synergistic effects of the A, B and E stages.

Therefore, in the case of the citrus seed oil peel extract of step A, when the content is small, as in the known general extract, it is difficult to give the natural effect of whitening, and if it is too large, the stability of the natural product may be lowered in the product, so that it is included in the above content. In the case of the hydrolysis yeast aqueous solution of the step E, it is preferable that the above ratio because the excessive application in the product in terms of phase stability may be difficult.

Among the constituents of the water-soluble whitening composition of the present invention, the citrus seed oil peel extract is generally extracted with purified water, the Walderian indica leaf extract is extracted with mannitol, and the hydrolyzed yeast aqueous solution contains 4% or more of hydrolyzed yeast. Aqueous solution. The components of the present invention (citrus unwashed oil peel extract, aminoethylphosphonic acid, Walderian indica leaf extract, guavaphenone, hydrolyzed yeast aqueous solution) and the like can be purchased and used in the form of commercially available products. For example, the citrus unwashed oil peel extract is Whitegenic 1 (manufactured by Sederma, France), and aminoethylphosphic acid is Whitegenic 2 (manufactured by Exymol, Monaco). Walzenian indica leaf extract is Whitegenic 3 (manufactured by Sero, France), and guava phenone is Guava Phenone (Bizen Chemical Co., Ltd.) As a hydrolyzed yeast aqueous solution, Whitegenic 4 (manufactured by Sapporo, Japan) may be used as an aqueous solution of Japan, and the above-listed products were purchased and used. In addition, the existing whitening agent components arbutin, kojic acid, eric acid or rucinol and the like can be purchased and used in the market.

In addition, the present invention is a skin whitening cosmetic composition containing one or more selected from the group consisting of arbutin, kojic acid, erric acid, and rucinol, which are the existing whitening agent components, as necessary, in the water-soluble whitening composition of the present invention as described above. It is characterized by providing a composition.

As described above, the water-soluble whitening composition according to the present invention not only provides a superior synergistic whitening effect in a small amount, alone or in combination with an adjuvant component, but also may change over time during the manufacturing process or during storage of the product. Overcoming the problems of the stability was improved, and showed a safe effect such as no irritation to the skin. In addition, even in a test result of directly applying the skin whitening cosmetic composition prepared by mixing the water-soluble whitening composition to a certain concentration directly on the human skin, it showed a clear whitening effect.

Specifically, the water-soluble whitening composition according to the present invention is preferably contained in the cosmetic composition 0.1 to 50% by weight in terms of whitening effect, stability and safety, and when used in combination with the group B whitening agent and the water-soluble whitening composition It is preferable to use the adjuvant of group B in the weight ratio of 0.1-10.0: 1.

Experiments were performed to determine the whitening physiological activity, which is a synergistic effect with certain concentrations and known whitening agents, of water-soluble mixed whitening compositions as follows:

First, water-soluble whitening compounds were divided into pathways capable of inhibiting melanin production, and the inhibitory effect of the melanoma cell culture similar to the biological level was measured to obtain a compounding ratio that can be effective in actual clinical conditions, thereby preparing a water-soluble whitening composition. And it was tested how much whitening effect is enhanced when the composition is used in combination with the known whitening agents.

In addition, the inhibitory activity of tyrosinase enzyme, which plays the most important role in melanin formation process, was confirmed, and the effect was confirmed through the change of melanin production rate and melanin synthesis rate in melanocytes of human epidermal tissue. And skin irritation experiments were conducted to know the skin safety according to the parallel use of these water-soluble whitening composition and the existing whitening agents. This experiment was a patch test on a normal adult skin. Phase stability was confirmed by measuring the color change and whitening effect over time at 40 ℃, daylight. In addition, the water-soluble whitening composition, the existing whitening agent, and in combination with these when applied to the human skin when applied to the human skin clinical experiment was able to see the actual effect.

Hereinafter, the present invention will be described in more detail by the following examples and experimental examples. However, these Examples and Experimental Examples are only for helping understanding of the present invention, but the present invention is not limited thereto.

Experimental Example 1 Whitening Effect Test Using Skin Melanin Cell Culture

1. Skin-derived melanocytes derived from humans are maintained in MGM (Melanocyte Growth Media; Clonetics) medium in 37 ° C., pH 7.3, 5% CO ₂ incubator.

2. For the test, a predetermined number of cells (2 × 10 ⁶ cells) were cultured in a 75T culture flask to confirm cell adhesion, and then, a constant concentration of test substance was added to the cell culture solution for 2 to 3 days. do.

3. Remove the culture, wash with phosphate buffered saline (PBS) and add trypsin solution to harvest the cells.

4. After pelleting the cells by centrifugation, observe the color, dissolve in 1N NaOH and measure the absorbance at 475nm wavelength.

5. Calculate the amount of melanin using the absorbance obtained from the melanin standard and correct this value with the total protein amount of melanocytes and express it as the amount of melanin per protein. Melanin production inhibition rate (%) is calculated as follows:

% Melanogenesis inhibition = [(A-B) / A] × 100

A: the amount of melanin / protein of the control group (control: melanocytes grown in culture medium without processing the raw material)

B: amount of melanin / protein amount of cells treated with each sample

The results of testing the rate of melanogenesis inhibition at the cellular level of about 10 kinds of water-soluble whitening substances are shown in Table 1 below.

Based on the results obtained in the above experiments, after selecting a suitable whitening material in groups A to E, the optimum composition and blending ratio that can exhibit a synergistic whitening effect was tested, and the degree of whitening effect with the existing whitening agent was also tested. Experimental method is the same as above.

(1) Product Name: Whitegenic 1 (Sederma, France)

(2) A brand name: Whitegenic 2 (made by Exymol, Monaco)

(3) A brand name: White Zen 3 (Sero company, France)

(4) Guavaphenone: Guava Phenone (Bizen Chemical Co., Ltd., Japan)

(5) A brand name: White Zen 4 (Sapporo company, Japan)

As shown in Tables 2a and 2b, the water-soluble whitening compositions (Examples 1 and 2, 5 and 6) according to the present invention had a higher rate of inhibition of melanin production than the whitening compositions (Comparative Examples 1 to 5) in which any of them were missing. In particular, in the case of using a conventionally known group B whitening agent (Examples 3 and 4), the melanin production inhibition rate was further improved. In light of Examples 1 to 6, the blending ratio in which the water-soluble whitening composition according to the present invention can give an optimal synergistic effect is A: C: D: E = 5: 0.5-4: 0.1-3: 1-8.

Experimental Example 2 Inhibitory Effect of Tyrosinase with Dopa-Oxidase Activity

Experimental Method: Human skin-derived melanocytes were obtained after maintaining the culture in MGM (Melanocyte Growth Media; Clonetics) medium at 37 ° C., pH 7.3, 5% CO ₂ incubator for 2 days. Tyrosinase inhibitory effect is obtained by applying each sample to cells and reading the absorbance change after 3 hours at 490 nm to determine the dopa-oxidase activity. The result is shown in FIG.

In FIG. 1, sample P represents purified water, sample A is comparative example 1, sample T is example 1, and sample S is example 3. FIG.

As can be seen in Figure 1, the dopa-oxidase activity is more than three times in the case of Example 1, the water-soluble mixed whitening composition according to the present invention than the case of arbutin, a whitening B-stage agonist, using the conventional whitening agent arbutin as an auxiliary For Example 3 it can be seen that the effect of tyrosinase was significantly reduced by 4.5 times or more.

Experimental Example 3 Melanin Production Rate and Synthesis Rate Change Effect Test

Experimental Method: Human skin-derived melanocytes were obtained after incubation for 2 days at 37 ° C., pH 7.3, 5% CO ₂ incubator in MGM (Melanocyte Growth Media, Clonetics) medium. Each sample was applied to the cells and aged for 5 days, and then the amount of melanin produced was extracted to determine the changed amount of melanin for each sample.

(Sample P: Purified water, Sample A: Comparative Example 1, Sample T: Example 1, Sample S: Example 3)

(Sample P: Purified water, Sample A: Comparative Example 1, Sample T: Example 1, Sample S: Example 3)

As shown in the results of Table 3 above, when using only arbutin belonging to the existing group B alone (Comparative Example 1), the remaining melanin amounted to 35%, Example 1 and a water-soluble whitening composition and adjuvants according to the present invention In Example 3 using rho arbutin in parallel, the residual melanin was about 30% and 25%, respectively.

Melanin synthesis rate was also significantly reduced compared to the conventional whitening agent in Examples 1 and 3, especially in Example 3 using the conventional whitening agent can be seen that the melanin synthesis rate is further reduced (see Table 4).

Experimental Example 4 Changes in Epidermal Tissue Containing Melanosite of Type IV (Tissue Study)

Experimental Method: 1) Experiment was performed using a Reconstructed epidermis model containing melanocytes from Skin Ethic. 2) This epidermal model is grown in fresh medium for 24 hours and then treated with each sample for 7 days. 3) This epidermal model is cut and stained with H & R (Hematoxylin & Eosin) to observe melanin pigment particles.

2 and 3 are tissue change diagrams when cultured with Sample P (purified water) and Sample S (Example 3). In the drawings, B means Stratum Basale, SC means Stratum Corneum, and MG means Melanin Pigment Granules.

As shown in the above organization chart, it can be seen that in the case of Example 3, melanocytes were hardly seen as compared to the control group.

Experimental Example 5 Skin Irritant Test

In order to confirm the skin irritation of the water-soluble whitening composition according to the present invention, a patch test using skin of a normal person was performed. The results are shown in Table 5 below.

The stimulus index was evaluated by the following equation, and the stimulus judgment was as follows:

Stimulus index = {Σ (Evaluation standard value × number of corresponding evaluation value)} / (Total subject × highest evaluation standard value) × 100

Stimulus judgment degree => 1.9 or less: minimum stimulation, 2.0 to 2.9: mild stimulation,

3.0 to 3.9: moderate stimulation, 4.0 or higher: severe stimulation

As can be seen from the results of Table 5, when the arbutin and kojic acid are used in combination as the water-soluble whitening composition and adjuvant according to the present invention, it can be seen that there is almost no intradermal irritation.

Experimental Example 6 Phase Stability Experiment

In order to test the phase stability of the water-soluble whitening composition according to the present invention, the change in room temperature, 40 ° C. and sunlight was observed, and the results are shown in Table 6 below.

(◎: No change, ○: Light change, ▲: High change, ★: Full change)

As shown in Table 6, in the case of Comparative Example 1 and Comparative Example 5, discoloration occurs rapidly under each condition, whereas in Example 1 and Example 3, discoloration hardly occurred.

Cosmetic compositions for the purpose of skin whitening containing 0.1 to 50% by weight of the water-soluble mixed whitening composition obtained in the present invention, for example, a lotion and an emulsion can be prepared by the following method.

Experimental Example 7 Application of Lotion

By the composition ratio shown in Table 7 1 to 4 times After dissolving the aqueous part and the alcohol parts 5 to 9 with an azimixer at room temperature, respectively, the alcohol parts are solubilized by gradually introducing the aqueous part into the aqueous part. After all the alcohol parts are added and mixed for another 10 to 20 minutes to complete the preparation of the lotion.

Experimental Example 8 Application of Emulsion

By the composition ratio shown in Table 8 1 to 5 times After completely dissolving the water phase part and 6-10 times oil phase parts to 75-80 ° C., the oil phase part was slowly added to the water phase part, and then emulsified at 75-80 ° C. at 3000 rpm for 5 minutes. Neutralization agent 11 is added during the emulsification to neutralize it. After completion of the first emulsification, cool and inject 12 ~ 13 No. 12 ~ 13 at 50 ~ 55 ℃ and then emulsify for 2 minutes at 3000 rpm of homomixer, then cool and finish at 27 ~ 30 ℃ to complete the preparation of emulsion. .

In order to determine the efficacy and effects on the compositions of Examples 9 and 10 and Comparative Examples 6 and 7, the following experiment was carried out.

[Experiment 9] Clinical results of whitening effect on human body

Experimental method: 15 healthy women over 18 years old applied the emulsion of Comparative Examples 8, 9 and 7, 8 to the face twice a day for 1 month using a colorimeter (Minolta CR2002) To determine the effect. L *, a *, b * color system is used to display color. In this experiment, L * value (brightness) was mainly used as an index. The L * values range from black (L * = 0) to white (L * = 100) and ΔL * was obtained from the difference of L * 28 one month after L * 0 when the sample was applied, and is shown in Table 9 below.

As shown in Table 9, Example 9 containing the water-soluble whitening composition according to the present invention and Example 10 using arbutin as an adjuvant in parallel with the water-soluble whitening composition are relatively much better than the comparative examples 6 and 7. It can be seen that.

As described above, the present invention relates to a water-soluble whitening composition having excellent skin whitening effect and a cosmetic composition for skin whitening containing the same. More specifically, the water-soluble whitening composition of the present invention is a citrus ounce oil peel extract; Aminoethylphosphonic acid; At least one of Walderian Indica leaf extract and guavaphenone; And a hydrolyzed yeast aqueous solution. In addition, the whitening composition according to the present invention can further enhance the effect when used in combination with a conventional whitening agent such as arbutin, kojic acid, eric acid or rucinol.

The water-soluble whitening composition of the present invention and the cosmetic composition for skin whitening containing the same not only provide an excellent synergistic whitening effect even in a small amount, but also overcome problems such as time-dependent changes that may occur during the manufacturing process or storage of the product, and It has no effect such as irritation.

Claims (6)

Citrus oil oil peel extract; Aminoethylphosphonic acid; At least one of Walderian Indica leaf extract and guavaphenone; And a hydrolyzed yeast aqueous solution. The composition according to claim 1, wherein the compounding ratio of each component is 5: 0.5 to 4: 0.1 to 3: 1 to 8 by weight. A cosmetic composition for skin whitening, comprising the water-soluble whitening composition according to claim 1. The composition of claim 3, wherein the composition is prepared by further containing at least one member selected from the group consisting of arbutin, kojic acid, eric acid, and rucinol. The composition according to claim 4, wherein the compounding ratio of the water-soluble whitening composition and the auxiliary component is 0.1 to 10.0: 1 by weight. The composition according to any one of claims 3 to 5, wherein the water-soluble whitening composition is contained in the cosmetic composition in an amount of 0.1 to 50% by weight.