BRIGHTENING COSMETIC COMPOSITION COMPRISING SODIUM PYRUVATE AS ACTIVE INGREDIENT

Abstract

Provided is a brightening use of a composition including sodium pyruvate and one or more selected from the group consisting of urea and hydroxyethyl urea. Since the composition exhibits a synergistic brightening effect, even when a low concentration of sodium pyruvate is included, a brightening effect at the same level as when a high concentration of sodium pyruvate is used can be obtained. Therefore, the composition can be effectively applied in cosmetics, medicines, external preparations, and the like.

Claims

1.-14. (canceled)

15. A cosmetic composition for skin brightening, comprising sodium pyruvate and one or more selected from the group consisting of urea and hydroxyethyl urea.

16. The cosmetic composition of claim 15, wherein the sodium pyruvate is comprised in an amount of 0.001 to 2 wt % relative to the total weight of the composition.

17. The cosmetic composition of claim 15, wherein the sodium pyruvate is comprised in an amount of 0.001 to 0.5 wt % relative to the total weight of the composition.

18. The cosmetic composition of claim 15, wherein the cosmetic composition is in a formulation of a toner, an essence, a lotion, a cream, a pack, a gel, a powder, a foundation, or a cleanser.

19. A pharmaceutical composition for treating skin pigmentation, comprising sodium pyruvate and one or more selected from the group consisting of urea and hydroxyethyl urea.

20. The pharmaceutical composition of claim 19, wherein the sodium pyruvate is comprised in an amount of 0.001 to 2 wt % relative to the total weight of the composition.

21. The pharmaceutical composition of claim 19, wherein the sodium pyruvate is comprised in an amount of 0.001 to 0.5 wt % relative to the total weight of the composition.

22. The pharmaceutical composition of claim 19, wherein the skin pigmentation is one or more selected from the group consisting of chloasma, melanosis (melasma), freckles, age spots, and melanin pigmentation.

23. A method for skin brightening, wherein the method comprises treating the skin of a subject in need thereof with the cosmetic composition of claim 15.

24. The method for skin brightening of claim 23, wherein the sodium pyruvate is comprised in an amount of 0.001 to 2 wt % relative to the total weight of the composition.

25. The method for skin brightening of claim 23, wherein the sodium pyruvate is comprised in an amount of 0.001 to 0.5 wt % relative to the total weight of the composition.

26. A method of treating skin pigmentation, wherein the method comprises treating the skin of a subject in need thereof with the pharmaceutical composition of claim 19.

27. The method of treating skin pigmentation of claim 26, wherein the sodium pyruvate is comprised in an amount of 0.001 to 2 wt % relative to the total weight of the composition.

28. The method of treating skin pigmentation of claim 26, wherein the sodium pyruvate is comprised in an amount of 0.001 to 0.5 wt % relative to the total weight of the composition.

Description

DESCRIPTION OF DRAWINGS

[0020] FIG. 1 is a graph for confirming the brightening efficacy of sodium pyruvate, urea, and hydroxyethyl urea according to Experimental Example 1.

MODES OF THE INVENTION

[0021] Hereinafter, the present invention will be described in detail.

[0022] One aspect of the present invention provides a brightening cosmetic composition which comprises sodium pyruvate and one or more selected from the group consisting of urea and hydroxyethyl urea.

[0023] Another aspect of the present invention provides a pharmaceutical composition for treating pigmentation, which comprises sodium pyruvate and one or more selected from the group consisting of urea and hydroxyethyl urea.

[0024] Still another aspect of the present invention provides a brightening composition for an external preparation for skin, which comprises sodium pyruvate and one or more selected from the group consisting of urea and hydroxyethyl urea.

[0025] Yet another aspect of the present invention provides a brightening method and pigmentation treatment method using a composition comprising sodium pyruvate and one or more selected from the group consisting of urea and hydroxyethyl urea, a use of the composition to prepare a brightening cosmetic, a use of the composition to prepare a therapeutic agent for pigmentation, and a use of the composition to prepare an external preparation for skin brightening.

[0026] Yet another aspect of the present invention provides a brightening method which comprises treating skin with a composition comprising sodium pyruvate and one or more selected from the group consisting of urea and hydroxyethyl urea.

[0027] Yet another aspect of the present invention provides a method of treating pigmentation, which comprises treating skin with the composition

[0028] Yet another aspect of the present invention provides a use of a composition comprising sodium pyruvate and one or more selected from the group consisting of urea and hydroxyethyl urea to prepare a brightening cosmetic.

[0029] Yet another aspect of the present invention provides a use of the composition to prepare a therapeutic agent for pigmentation.

[0030] Yet another aspect of the present invention provides a use of the composition to prepare an external preparation for skin brightening.

[0031] In the present invention, “sodium pyruvate” is represented by the following Chemical Formula 1 and is another salt form of pyruvic acid which is one of the α-keto acids.

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[0032] Since pyruvate is an intermediate in several metabolic pathways, sodium pyruvate is widely used to provide more energy in many experiments related to cell culture. According to previous studies, pyruvic acid not only inhibits melasma, solar lentigine, acne, and warts, but also promotes collagen synthesis and enhances skin elasticity. However, since these effects result from the chemical exfoliation of a high concentration (50 to 100%) of pyruvic acid, a stinging or hot sensation may be felt while using pyruvic acid, and may be accompanied by excessive exfoliation or inflammatory blisters.

[0033] In the present invention, “urea” is one of the natural moisturizing factors (NMFs) and is capable of imparting an excellent moisturizing effect to the skin. Urea softens the skin, is also called carbamide, and is used as an external preparation for skin due to having keratolytic and antibacterial properties. Depending on the concentration, low-concentration products (10% or less) may be used for xeroderma, and high-concentration products (20 to 40%) may be used as keratolytic agents.

[0034] In the present invention, “hydroxyethyl urea” can help maintain moisturizing power and skin elasticity in cosmetics, so it is used in a moisturizer and may also be used as a hair conditioner.

[0035] According to the present invention, the problems caused when a high concentration of sodium pyruvate that exhibits melanogenesis inhibitory efficacy is used can be resolved, a brightening effect superior to that when a high concentration is used can be exhibited even when a low concentration of sodium pyruvate is used in combination with one or more selected from the group consisting of urea and hydroxyethyl urea, and a degradation of the feeling of use of a product, which is caused by using a large amount of thickener, can be reduced.

[0036] Urea and hydroxyethyl urea by themselves do hardly exhibit a brightening effect. However, when used along with sodium pyruvate, they can enhance the brightening effect of sodium pyruvate.

[0037] Specifically, the composition of the present invention comprises all of a combination of sodium pyruvate and urea, a combination of sodium pyruvate and hydroxyethyl urea, and a combination of sodium pyruvate, urea, and hydroxyethyl urea.

[0038] The composition may comprise sodium pyruvate in an amount of 0.001 to 2% (w/w) with respect to the total weight of the composition. More preferably, sodium pyruvate may be comprised in an amount of 0.005 to 1% (w/w). Even more preferably, sodium pyruvate may be comprised in an amount of 0.01 to 0.5% (w/w), and most preferably, 0.01 to 0.1% (w/w). When the composition of the present invention comprises sodium pyruvate in an amount of less than 0.001%, a sufficient brightening effect may not be expected. Also, when sodium pyruvate is used along with a thickener, there is a problem of poor formulation stability, but when sodium pyruvate is used along with one or more of urea and hydroxyethyl urea, it is not necessary to excessively increase the concentration for brightening.

[0039] The composition may comprise urea in an amount of 0.001 to 5% (w/w) with respect to the total weight of the composition. More preferably, urea may be comprised in an amount of 0.005 to 3% (w/w). Even more preferably, urea may be comprised in an amount of 0.01 to 2% (w/w). When the content of urea does not satisfy the above range, the brightening efficacy of sodium pyruvate may not be sufficiently enhanced, and when a large amount of urea is used, problems such as odor and discoloration may occur due to ammonia gas.

[0040] The composition may comprise hydroxyethyl urea in an amount of 0.001 to 10% (w/w) with respect to the total weight of the composition. More preferably, hydroxyethyl urea may be comprised in an amount of 0.005 to 6% (w/w). Even more preferably, hydroxyethyl urea may be comprised in an amount of 0.01 to 4% (w/w). When the content of hydroxyethyl urea does not satisfy the above range, the brightening efficacy of sodium pyruvate may not be sufficiently enhanced, and when a large amount of hydroxyethyl urea is used, a pH in a formulation may be increased to affect formulation stability.

[0041] In the present invention, a “skin brightening effect” refers to brightening skin tone by inhibiting the synthesis of the melanin pigment, uniformizing skin tone or complexion, and improving chloasma, melanosis (melasma), freckles, age spots, or melanin pigmentation, which is caused by ultraviolet rays, hormones, or heredity, but the present invention is not limited thereto.

[0042] When the composition comprising sodium pyruvate and one or more selected from the group consisting of urea and hydroxyethyl urea is used as a cosmetic, cosmetics containing the above compounds and mixtures as active ingredients may be prepared in the form of a general emulsion formulation or a solubilized formulation. For example, the cosmetics may be in a formulation such as a toner such as a skin softening toner, a nutritional skin toner, or the like, a lotion such as a facial lotion, a body lotion, or the like, a cream such as a nourishing cream, a moisturizing cream, an eye cream, or the like, an essence, a cosmetic ointment, a spray, a gel, a pack, a sunscreen, a makeup base, a liquid-type, solid-type, or spray-type foundation, a powder, a makeup remover such as a cleansing cream, a cleansing lotion, or a cleansing oil, or a cleanser such as a cleansing foam, soap, a body wash, or the like.

[0043] In addition, the composition of the present invention may further contain an adjuvant typically used in the field of cosmetics, such as a lipid material, an organic solvent, a solubilizing agent, a concentrate, a gelating agent, an emollient, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, a surfactant, water, an ionic emulsifier, a non-ionic emulsifier, a filler, a sequestering agent, a chelating agent, a preservative, a vitamin, a blocking agent, a wetting agent, an essence oil, a dye, a pigment, a hydrophilic active agent, a lipophilic active agent, or a lipid vesicle.

[0044] In the present invention, a “pharmaceutical composition” may be administered orally or parenterally, and when the composition comprising sodium pyruvate and one or more selected from the group consisting of urea and hydroxyethyl urea is used as a pharmaceutical composition, it may be administered in a general pharmaceutical formulation, for example, in various oral and parenteral formulations for clinical administration. When formulated, the pharmaceutical composition may be prepared using a diluent or an excipient generally used in the art, such as a filler, an extending agent, a binding agent, a wetting agent, a disintegrant, a surfactant, and the like, but the present invention is not limited thereto.

[0045] A solid preparation for oral administration comprises a tablet, a pill, a powder, a granule, a capsule, and the like. Such a solid preparation may be prepared by mixing the pharmaceutical composition of the present invention with at least one or more excipients, for example, starch, calcium carbonate, sucrose or lactose, gelatin, and the like, but the present invention is not limited thereto.

[0046] In addition to simple excipient, lubricants such as magnesium stearate, talc, and the like are used. A liquid preparation for oral administration comprises a suspension, a liquid for internal use, an emulsion, a syrup, and the like. In this case, the liquid preparation for oral administration may comprise various excipients, for example, a wetting agent, a sweetening agent, a fragrance, a preservative, and the like, in addition to generally used simple diluents such as water and liquid paraffin, but the present invention is not limited thereto.

[0047] A preparation for parenteral administration comprises a sterile aqueous solution, a non-aqueous solvent, a suspension, an emulsion, a lyophilized preparation, a suppository, and the like. As the non-aqueous solvent and the suspension, propylene glycol, polyethylene glycol, a vegetable oil such as olive oil, and an injectable ester such as ethyl oleate may be used. As a base of the suppository, Witepsol, Macrogol, Tween 61, cocoa butter, laurin butter, glycerol gelatin, and the like may be used, but the present invention is not limited thereto.

[0048] In the present invention, pigmentation may be one or more selected from the group consisting of chloasma, melanosis (melasma), freckles, age spots, and melanin pigmentation, but the present invention is not limited thereto.

[0049] In the present invention, an “composition for an external preparation for skin” may be used as an external preparation for skin, but the present invention is not limited thereto. When the composition comprising sodium pyruvate and one or more selected from the group consisting of urea and hydroxyethyl urea is used as an external preparation for skin, an adjuvant typically used in the field of dermatology, such as a lipid material, an organic solvent, a solubilizing agent, a concentrate, a gelating agent, an emollient, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, a surfactant, water, an ionic emulsifier, a non-ionic emulsifier, a filler, a sequestering agent, a chelating agent, a preservative, a vitamin, a blocking agent, a wetting agent, an essence oil, a dye, a pigment, a hydrophilic active agent, lipophilic active agent, a lipid vesicle, and any other ingredients typically used in an external preparation for skin may be further contained. Also, the ingredients may be introduced in an amount generally used in the field of dermatology. When the composition is provided as an external preparation for skin, it may be in a formulation such as an ointment, a patch, a gel, a cream, and a spray, but the present invention is not limited thereto.

[0050] Hereinafter, the present invention will be described in detail with reference to the following experimental example. However, the following experimental example is merely presented to exemplify the present invention, and the scope of the present invention is not limited to the following experimental example. Also, the experimental example is provided only to promote understanding of the present invention, and the scope of the present invention is not limited to the experimental example in any sense.

EXAMPLES

Experimental Example 1. Melanogenesis Inhibitory Efficiency Test Results

[0051] In order to confirm melanogenesis inhibitory efficacy caused by sodium pyruvate, first, B16F10 cells were dispensed into a 6-well plate at 1×10.sup.5 cells/well and cultured in a DMEM medium containing 10% FBS and 1% penicillin/streptomycin under conditions of 37° C. and 5% CO.sub.2 for 24 hours. Subsequently, the cells were treated with sodium pyruvate and hydroxyethyl urea or urea according to each concentration, as shown in Table 1, along with 10 nM of α-MSH for 48 hours. The resulting cells were harvested, added to 100 μl of a lysis buffer (1N NaOH, 10% DMSO), and then allowed to react at 90° C. for 20 minutes, and melanin amounts were measured at 405 nm (EPOCH, Biotek). The melanin amount measurement results are as follows.

TABLE-US-00001 TABLE 1 Concentration of each Melanin Melanogenesis Experimental compositional ingredient (wt %) amount inhibitory groups SP* HEU* Urea (%) efficiency** Comparative (-) (-) (-) 100 0 Example 1 Comparative (-) 0.01 (-) 100 *** Example 2 Comparative (-) 0.1  (-) 100 *** Example 3 Comparative (-) (-) 0.01 100 *** Example 4 Comparative (-) (-) 0.1 100 *** Example 5 Comparative (-) 0.01 0.01 98 2 Example 6 Comparative (-) 0.1  0.1 97 3 Example 7 Comparative 0.01 (-) (-) 92 8 Example 8 Comparative 0.05 (-) (-) 82 18 Example 9 Comparative 0.1 (-) (-) 77 23 Example 10 Comparative 1 (-) (-) 64 36 Example 11 Example 1 0.01 0.01 (-) 83 17 Example 2 0.01 (-) 0.01 74 26 Example 3 0.01 0.01 0.01 60 40 Example 4 0.1 0.1  0.1 54 46 *SP: Sodium pyruvate *HEU: Hydroxyethyl urea **(Melanin amount upon no treatment − Melanin amount upon treatment)/(Melanin amount upon no treatment) × 100 *** 100 or more has no effect

[0052] As shown in Table 1, when urea or hydroxyethyl urea was used alone, a melanogenesis inhibitory effect was not shown (Comparative Examples 2, 3, 4 and 5). When both urea and hydroxyethyl urea were used, melanogenesis was inhibited at a very slight level of 3% (Comparative Examples 6 and 7). However, when sodium pyruvate was used together therewith, a melanogenesis inhibitory effect was shown, and it can be seen that urea or hydroxyethyl urea enhanced the brightening efficacy of sodium pyruvate (in the case of Examples 1, 2, 3 and 4, melanogenesis was inhibited at levels of 17%, 26%, 40%, and 46%, respectively). A combination of 0.01 wt % of sodium pyruvate, 0.01 wt % of urea, and 0.01 wt % of hydroxyethyl urea (Example 3) showed an inhibitory efficiency of 40%, which was about 11% higher than 36% shown when 1 wt % of sodium pyruvate was used alone (Comparative Example 11). This means that 100-fold-diluted sodium pyruvate in combination with one or more of urea and hydroxyethyl urea can exhibit a brightening effect similar to that of conventional sodium pyruvate. In addition, a combination of 0.1 wt % of sodium pyruvate, 0.1 wt % of urea, and 0.1 wt % of hydroxyethyl urea (Example 4) showed an inhibitory efficiency of 46%, which was about 27% higher than 36% shown when 1 wt % of sodium pyruvate was used alone (Comparative Example 11).

[0053] From these results, it can be seen that, when a low concentration of sodium pyruvate is comprised along with one or more selected from the group consisting of urea and hydroxyethyl urea, a brightening effect superior to that when a high concentration of sodium pyruvate is comprised is exhibited, and thus a sufficient brightening effect can be exhibited even at a low concentration of sodium pyruvate.