CN114796046B

CN114796046B - Whitening and freckle-removing antioxidant composition and application thereof

Info

Publication number: CN114796046B
Application number: CN202210345175.0A
Authority: CN
Inventors: 姚玲娣; 谢水林; 聂舟; 潘晓燕; 陈家欢; 吴忠利; 王晓慧
Original assignee: Guangzhou Rui Sen Biotechnology Co ltd
Current assignee: Guangzhou Rui Sen Biotechnology Co ltd
Priority date: 2022-03-31
Filing date: 2022-03-31
Publication date: 2023-07-07
Anticipated expiration: 2042-03-31
Also published as: CN114796046A

Abstract

The invention relates to a whitening and spot-fading antioxidant composition and application thereof, wherein the whitening and spot-fading antioxidant composition comprises the following components: n-acetylneuraminic acid, tranexamic acid, hop extract and lotus embryo extract. The four active ingredients are creatively matched for whitening, freckle-fading and oxidation resistance, the four active ingredients complement each other, the four active ingredients can be synergistic, and all-round and multi-angle inhibition of melanin generation or transfer is realized by different ways or mechanisms respectively, so that the whitening, freckle-fading and oxidation resistance effect of the product is remarkable and long-acting.

Description

Whitening and freckle-removing antioxidant composition and application thereof

Technical Field

The invention belongs to the technical field of cosmetics, relates to a whitening and freckle-fading antioxidant composition and application thereof, and in particular relates to a whitening and freckle-fading antioxidant composition and essence with whitening and freckle-fading antioxidant effects.

Background

The whitening is always the unchanged theme in the beauty market, and huge market demands are always made. Whitening, freckle removing, yellow removing, black fading and the like become main requirements of beautifying and whitening functions. The intensity of the skin color is regulated by a plurality of factors, and mainly depends on the content and distribution of melanin. Melanin is an amino acid derivative formed by a series of chemical reactions of tyrosine or 3, 4-dihydroxyphenylalanine, which is often present in a polymeric manner. Melanin is synthesized by melanocytes in basal layers of human epidermis, and when ultraviolet light is irradiated on the skin, the skin is in a 'self-protection' state, activates tyrosinase activity, catalyzes oxidation of tyrosine or 3, 4-dihydroxyphenylalanine to form melanin, and protects our skin cells. Melanin moves layer by layer through cell metabolism, and forms freckle, sunburn, black spot, etc. on skin epidermis.

Enzymes mainly involved in melanin synthesis include tyrosinase, dopachrome tautomerase and dihydroxyindole carboxylic acid oxidase, wherein tyrosinase belongs to oxidoreductase, is a main rate-limiting enzyme for melanin synthesis, and the activity of tyrosinase is used for determining the quantity of melanin formation. Tyrosinase has the characteristics of monophenolase and diphenolase, namely has the functions of oxygenase and oxidase. During melanin synthesis, it is able to catalyze the hydroxylation of L-tyrosine to levodopa (monophenolase activity); the second step oxidizes levodopa to produce dopaquinone (diphenolase activity), which is unstable in nature and eventually produces melanin after various complex non-enzymatic reactions.

The whitening oral products such as the whitening pill, the whitening tablet, the anti-saccharification oral liquid and the like have non-negligible side effects: the whitening tablets have side effects, and if the tablets are taken excessively, thrombus is at risk; the important principle of the whitening tablet is to promote skin metabolism melanin, but the whitening tablet contains excessive vitamin c, if the symptoms of abdominal pain, diarrhea and blood deficiency appear after long-time taking, hyperuricemia probably occurs, and thus kidney stones are accelerated, and the kidney is greatly influenced.

The patent CN202110818300.0 discloses a whitening and moisturizing essence emulsion and a preparation method thereof, wherein the whitening and moisturizing essence emulsion comprises the following raw materials, by weight, 2-5 parts of water, 3-6 parts of glycerin, 5-8 parts of cucumber juice, 4-6 parts of essence, 2-5 parts of carbomer, 5-8 parts of mink oil, 2-4 parts of petrolatum, 4-6 parts of triethanolamine, 2-5 parts of glycerol stearate, 4-6 parts of an antioxidant, 4-6 parts of anti-inflammatory light cosmetic water, 4-6 parts of honey water, 8-10 parts of dish grass cleaning liquid medicine, 4-6 parts of vitamins, 8-10 parts of ginseng extract and 1-3 parts of pilose antler extract. The invention has stronger water supplementing capability, but the whitening effect is not proved by specific data, and the spot-fading effect is not mentioned.

Patent CN201710391557.6 discloses a whitening and freckle-removing composition and a cosmetic, wherein the whitening and freckle-removing composition comprises the following components in parts by weight: 0.01-15 parts of raw material for inhibiting tyrosinase activity or converting eumelanin into light melanin; 0.1-15 parts of raw materials for inhibiting tyrosinase expression; 0.01-10 parts of raw materials for increasing the melanocyte stimulating hormone receptor activity of melanocytes; 0.1-8 parts of liquid crystal emulsifier; the whitening and freckle-removing composition fully exerts the synergistic effect of all the components, can effectively improve the darkness of skin and lighten the complexion.

However, the whitening and freckle-removing effects of the product disclosed by the prior art are not very remarkable and long-acting, so that the development of the product which is simple in preparation method, remarkable in whitening and freckle-removing effects and long-acting is very significant.

Disclosure of Invention

Aiming at the defects of the prior art, the invention aims to provide a whitening and freckle-fading antioxidant composition and application thereof, in particular to a whitening and freckle-fading antioxidant composition and essence with whitening and freckle-fading antioxidant effects.

In order to achieve the aim of the invention, the invention adopts the following technical scheme:

in a first aspect, the present invention provides a whitening, spot-lightening and antioxidant composition comprising: n-acetylneuraminic acid, tranexamic acid, hop extract and lotus embryo extract.

N-acetylneuraminic Acid, also called Sialic Acid (SA for short), is a naturally occurring amino sugar, and has the effects of resisting aging, brightening skin, reducing fine wrinkles of the canthus and the like when applied to cosmetics; and it is very soluble in water. Biochemical derivatives of sialic acid are also commonly used in the synthesis of drugs.

Tranexamic acid is also known as trans-p-aminomethylcyclohexane carboxylic acid, anti-fibrinolytic cyclic acid, tranexamic acid, and Xuekuning. Tranexamic acid is used as a skin conditioner, a moisturizer, and a whitening agent in cosmetics. It has the factor group for inhibiting melanin enhancement, so that it can completely block the path of melanin formation due to UV irradiation, and can prevent the melanin from thickening and enlarging, and can effectively prevent skin pigmentation.

The flos Lupuli (HUMULUS LUPULUS) flower extract is rich in lupulone, tannin, volatile oil, humulone-II, gamma-dehydrocalamine, astragalin, isoquercitrin, rutin-3-rhamnosyldiglucoside, quercetin-3-rhamnosyldiglucoside, etc. Inhibition of elastase, promotion of brain amide formation and antioxidant properties indicate that it can be used to prevent skin aging and wrinkle; leukocyte subsequent inhibition and activation of PPAR has been shown to be useful in preventing skin damage and skin inflammation, inhibiting inflammatory pigmentation reactions; has strong bactericidal, antibacterial, enzyme inhibiting and antiseptic effects, and can be used for oral cavity to remove halitosis and relieve itching of scalp.

The Nelumbo NUCIFERA embryo bud extract contains plumula Nelumbinis extract, isoliensinine, plumula Nelumbinis extract, nuciferine, and demethylated linderane; and flavonoid such as luteolin, hyperoside, rutin, etc. The extract has effect in stimulating collagen and elastin formation, and can be used for preparing antiaging and wrinkle-preventing cosmetics. The alkaloid contained in the lotus embryo bud has the function of scavenging oxygen free radicals, and the oxygen free radicals react with polyunsaturated fatty acids to cause various oxidative damages to organisms.

Enzymes mainly involved in melanin synthesis include tyrosinase, dopachrome tautomerase and dihydroxyindole carboxylic acid oxidase, wherein tyrosinase belongs to oxidoreductase, is a main rate-limiting enzyme for melanin synthesis, and the activity of tyrosinase is used for determining the quantity of melanin formation. Tyrosinase is a copper-containing aerobic enzyme, and oxygen radicals are necessary to participate in the reaction process of converting tyrosine into melanin, so that the removal of the oxygen radicals can block the catalytic reaction of tyrosinase, and the intensity of tyrosine oxidation reaction is reduced.

The four active ingredients are creatively matched for whitening, freckle-fading and oxidation resistance, the four active ingredients complement each other, the four active ingredients can be synergistic, and all-round and multi-angle inhibition of melanin generation or transfer is realized by different ways or mechanisms respectively, so that the whitening, freckle-fading and oxidation resistance effect of the product is remarkable and long-acting.

Preferably, the whitening and freckle-removing antioxidant composition comprises the following components in parts by weight: 0.01-2 parts of N-acetylneuraminic acid, 0.05-2 parts of tranexamic acid, 0.1-4 parts of hop extract and 1-7 parts of lotus embryo extract.

The parts by weight of the N-acetylneuraminic acid may be 0.01 part, 0.05 part, 0.1 part, 0.3 part, 0.5 part, 0.8 part, 1 part, 1.2 part, 1.5 part, 2 parts, etc.

The tranexamic acid may be 0.05 part, 0.1 part, 0.3 part, 0.5 part, 0.8 part, 1 part, 1.2 part, 1.5 part, 2 parts, etc.

The hop extract may be 0.1 part, 0.5 part, 1 part, 1.5 parts, 2 parts, 2.3 parts, 2.5 parts, 3 parts, 3.5 parts, 4 parts, etc. by weight.

The lotus embryo bud extract can be 1 part, 1.5 parts, 2 parts, 2.5 parts, 3 parts, 3.5 parts, 4 parts, 5 parts, 6 parts, 7 parts and the like by weight.

Other specific point values in the numerical ranges are selectable, and will not be described in detail herein.

The hop (HUMULUS LUPULUS) extract or the Nelumbo NUCIFERA embryo extract according to the present invention may be obtained by using commercially available materials or by self-preparing. The hop extract prepared by the method has better effect when being used for the product.

Preferably, the hops extract is prepared by a preparation method comprising the steps of:

(1) Mixing hops with ethanol water solution, extracting with ethanol, concentrating the extractive solution until no ethanol smell;

(2) Extracting the concentrated solution obtained in the step (1) with an organic solvent;

(3) Purifying and drying the extracted aqueous solution obtained in the step (2).

Preferably, the concentration of the aqueous ethanol solution of step (1) is 80-95%, e.g. 80%, 82%, 85%, 87%, 90%, 92%, 95%, etc.

Preferably, the mass ratio of the aqueous ethanol solution to hops of step (1) is 8-15 times, e.g. 8-fold, 9-fold, 10-fold, 11-fold, 12-fold, 13-fold, 14-fold, 15-fold, etc.

Preferably, the organic solvent of step (2) comprises any one or a combination of at least two of petroleum ether, pentane, hexane or heptane.

Preferably, the purification in step (3) is performed by eluting with an aqueous ethanol solution using a column of a polyamide resin.

Preferably, the elution is carried out by gradient elution from low concentration to high concentration with 25-60% ethanol aqueous solution. For example, the eluate is eluted with 25%, 40% and 60% ethanol aqueous solution in this order, and the 60% ethanol eluate is collected.

In a second aspect, the invention provides a use of the whitening and spot-lightening antioxidant composition according to the first aspect in the preparation of a cosmetic.

Preferably, the cosmetic comprises essence, essential oil, lotion, face cream, facial mask, eye cream, facial cleanser.

In a third aspect, the invention provides an essence with whitening, freckle-fading and oxidation-resisting effects, which comprises the following components: the whitening and freckle-removing antioxidant composition, the humectant, the thickener, the antibacterial preservative and the water.

Preferably, the essence comprises the following components in parts by weight: 1-15 parts of the whitening and freckle-fading antioxidant composition, 0.1-10 parts of a humectant, 0.1-5 parts of a thickening agent, 0.01-1 part of an antibacterial preservative and water.

The weight parts of the whitening and spot-fading antioxidant composition according to the first aspect may be 1 part, 3 parts, 5 parts, 8 parts, 10 parts, 12 parts, 14 parts, 15 parts, etc.

The humectant may be 0.1 part, 0.3 part, 0.5 part, 0.8 part, 1 part, 2 parts, 4 parts, 5 parts, 7 parts, 8 parts, 10 parts, etc.

The weight parts of the thickener may be 0.1 part, 0.3 part, 0.5 part, 0.8 part, 1 part, 2 parts, 4 parts, 5 parts, etc.

The weight parts of the antibacterial preservative may be 0.01 part, 0.03 part, 0.05 part, 0.08 part, 0.1 part, 0.2 part, 0.4 part, 0.5 part, 0.7 part, 0.8 part, 1 part, etc.

Preferably, the humectant comprises any one or a combination of at least two of jojoba esters, sodium hyaluronate, methyl propylene glycol, chlorella extract, dipotassium glycyrrhizinate, squalane, betaine or 1, 2-pentanediol.

A combination of squalane, dipotassium glycyrrhizinate and 1, 2-pentanediol is preferred.

Preferably, the thickener comprises any one or a combination of at least two of hydroxypropyl guar, cetyl esters, glyceryl tribhenate, cellulose gum or carboxymethyl hydroxyethyl cellulose.

Preferably, the antibacterial preservative comprises any one or a combination of at least two of methylparaben, 1, 2-hexanediol, octylglycol, octanoyl hydroxamic acid, or 1, 2-pentanediol.

Compared with the prior art, the invention has the following beneficial effects:

the composition disclosed by the invention has the advantages that four components are combined, the component formula is reasonable, the active components complement each other, the synergistic effect can be achieved, the generation or transfer of melanin is inhibited in all directions and multiple angles through different ways or mechanisms, and the whitening, freckle removing and oxidation resisting effects of the product are obvious and long-acting. The composition is applied to cosmetics, so that the prepared product has high safety performance and obvious long-acting whitening, freckle removing and oxidation resisting effects.

Detailed Description

In order to further describe the technical means adopted by the present invention and the effects thereof, the following describes the technical scheme of the present invention in combination with the preferred embodiments of the present invention, but the present invention is not limited to the scope of the embodiments.

The N-acetylneuraminic acid referred to in the following examples, comparative examples, application examples and comparative application examples is a product of model N-Acetylneuraminic acid available from Setaria green biotechnology Co., ltd. Of Wu Hanzhong; tranexamic acid is a product of model tranexamic acid purchased from the company of the company Hunan Dongting medicine Co; the hop extract was obtained from Kepler biotechnology Co., ltd. Shaanxi under the model KPL-0048 (except examples 4-5); the lotus embryo extract is a product of model LIENSININE available from macrobiotechnology limited of south genie.

Example 1

The embodiment provides a whitening and freckle-fading antioxidant composition (I), which comprises the following components in parts by weight: 1 part of N-acetylneuraminic acid, 0.5 part of tranexamic acid, 2.5 parts of hop extract, 3 parts of lotus embryo extract and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Example 2

The embodiment provides a whitening and freckle-fading antioxidant composition (II), which comprises the following components in parts by weight: 0.5 part of N-acetylneuraminic acid, 0.9 part of tranexamic acid, 1.6 parts of hop extract, 4 parts of lotus embryo bud extract and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Example 3

The embodiment provides a whitening and freckle-fading antioxidant composition (III), which comprises the following components in parts by weight: 2 parts of N-acetylneuraminic acid, 0.5 part of tranexamic acid, 3.5 parts of hop extract, 1 part of lotus embryo extract and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Example 4

This example provides a whitening, spot-lightening and antioxidant composition (IV) which differs from example 1 only in that the hops extract is prepared by:

(1) Mixing hops with 10 times of 85% ethanol water solution, extracting with ethanol for 2 times, mixing extractive solutions, and concentrating under reduced pressure at 80deg.C until no ethanol smell;

(2) Extracting the concentrated solution obtained in the step (1) with petroleum ether for 3 times, and collecting an extracted aqueous solution;

(3) Passing the extracted aqueous solution obtained in the step (2) through a polyamide resin column, sequentially carrying out gradient elution by using 25%, 40% and 60% ethanol aqueous solutions, and collecting the eluent with the concentration of 60%; concentrating the eluent under reduced pressure, and drying.

Example 5

This example provides a whitening, spot-reducing and antioxidant composition (v) which differs from example 1 only in that the hops extract is prepared as follows:

(1) Mixing hops with 10 times of 70% ethanol water solution, extracting with ethanol for 2 times, mixing extractive solutions, and concentrating under reduced pressure at 80deg.C until no ethanol smell;

Comparative example 1

This comparative example provides a composition (A) differing from example 1 only in the absence of N-acetylneuraminic acid component, the reduced fraction of which was added to tranexamic acid, hops extract and lotus embryo extract in the original ratio, with the other conditions remaining unchanged.

Comparative example 2

This comparative example provides a composition (B) differing from example 1 only in the absence of the tranexamic acid component, the reduced fraction being added to the N-acetylneuraminic acid, hop extract and lotus embryo extract in the ratio of the original fractions, all the other conditions remaining unchanged.

Comparative example 3

This comparative example provides a composition (C) which differs from example 1 only in the lack of hops extract components, the reduced fraction being added to the N-acetylneuraminic acid, tranexamic acid and lotus embryo extract in the ratio of the original fractions, all other conditions remaining unchanged.

Comparative example 4

This comparative example provides a composition (D) differing from example 1 only in the lack of the component of the lotus embryo extract, the reduced fraction being added to the N-acetylneuraminic acid, tranexamic acid and hops extract in the ratio of the original fractions, all other conditions remaining unchanged.

Comparative example 5

The comparative example provides a composition (E) which comprises the following components in parts by weight: 7 parts of N-acetylneuraminic acid and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Comparative example 6

The comparative example provides a composition (F) which comprises the following components in parts by weight: 7 parts of tranexamic acid and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Comparative example 7

The comparative example provides a composition (G) which comprises the following components in parts by weight: 7 parts of hops extract and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Comparative example 8

The comparative example provides a composition (H) which comprises the following components in parts by weight: 7 parts of lotus embryo extract and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Application example 1

The application example provides essence with whitening, freckle-fading and antioxidation effects, which comprises the following components in parts by weight: 14 parts of whitening and spot-lightening antioxidant composition (I), 5 parts of squalane, 3 parts of dipotassium glycyrrhizinate, 0.5 part of 1, 2-pentanediol, 0.8 part of cetyl ester, 0.3 part of octanediol and 76.4 parts of water. The components are mixed and dissolved uniformly at 45 ℃.

Application example 2

The application example provides essence with whitening, freckle-fading and antioxidation effects, which comprises the following components in parts by weight: 14 parts of whitening and spot-lightening antioxidant composition (II), 5 parts of sodium hyaluronate, 3 parts of methyl propylene glycol, 0.5 part of 1, 2-pentanediol, 0.8 part of hydroxypropyl guar, 0.3 part of methylparaben and 76.4 parts of water. The components are mixed and dissolved uniformly at 45 ℃.

Application example 3

The application example provides essence with whitening, freckle-fading and antioxidation effects, which comprises the following components in parts by weight: 14 parts of whitening and spot-lightening antioxidant composition (III), 5 parts of chlorella extract, 3 parts of squalane, 0.5 part of methyl propylene glycol, 0.8 part of glyceryl tribehenate, 0.3 part of methylparaben and 76.4 parts of water. The components are mixed and dissolved uniformly at 45 ℃.

Application examples 4 to 5

The application example provides two essences with the effects of whitening, fading and resisting oxidation, which are different from application example 1 only in that the whitening, fading and resisting oxidation composition (I) is replaced by a whitening, fading and resisting oxidation composition (IV) and a whitening, fading and resisting oxidation composition (V) in equal amounts, and other conditions are kept unchanged.

Comparative application examples 1 to 8

The present application example provides eight kinds of essence, which differ from application example 1 only in that the whitening and spot-fading antioxidant composition (i) was replaced with the whitening and spot-fading antioxidant compositions (a to H) in equal amounts, and the other conditions were kept unchanged.

Application example 6

The application example provides essence with whitening and spot-fading and antioxidation effects, which is different from application example 1 only in that 5 parts of squalane, 3 parts of dipotassium glycyrrhizinate and 0.5 part of 1, 2-pentanediol are replaced by 7.3 parts of dipotassium glycyrrhizinate and 1.2 parts of 1, 2-pentanediol, and other conditions are kept unchanged.

Application example 7

The application example provides essence with the effects of whitening, fading spots and resisting oxidation, which is different from the application example 1 only in that 5 parts of squalane, 3 parts of dipotassium glycyrrhizinate and 0.5 part of 1, 2-pentanediol are replaced by 5.3 parts of squalane and 3.2 parts of dipotassium glycyrrhizinate, and other conditions are kept unchanged.

Application example 8

The application example provides essence with the effects of whitening, fading spots and resisting oxidation, which is different from the application example 1 only in that 5 parts of squalane, 3 parts of dipotassium glycyrrhizinate and 0.5 part of 1, 2-pentanediol are replaced by 7.5 parts of squalane and 1, 2-pentanediol, and other conditions are kept unchanged.

Test example 1

The essences prepared in application examples 1 to 8 and comparative application examples 1 to 8 were subjected to safety test.

The specific method comprises the following steps: putting the test object into a patch tester, using the dosage of about 0.020-0.025g, attaching the patch tester with the test object to the forearm flexor side of a subject by using a non-irritating adhesive tape, and uniformly attaching the patch tester to the skin by using the palm light pressure for 24 hours. After removing the spot tester for 30min, the skin reaction is observed after the indentation disappears. If the result is negative, the spot test is observed again 24h and 48h after the spot test.

Evaluation criteria: level 0: a negative reaction; stage 1: suspicious reactions, only weak erythema; 2 stages: weak positive response, erythema, infiltration, edema, and possibly papules; 3 stages: strong positive reaction, erythema, infiltration, edema, papule, and reaction beyond the test area; 4 stages: very strong positive response, marked erythema, severe infiltration, edema, blepharospermia, and response beyond the test area.

The results show that the skin reactions of the subjects are negative, which indicates that the composition and the essence related to the invention are mild, safe and non-irritating.

Test example 2

Tyrosinase activity inhibition experiments were performed on the compositions prepared in examples 1 to 5 and comparative examples 1 to 8.

Test instrument and reagents:

the main instrument is as follows: spectronics GENESYS-5, thermo Inc. of America.

The main reagent comprises: tyrosinase powder with enzyme activity of 25000U, sigma company in U.S.; l-tyrosine, analytically pure, shanghai JCBIO; ascorbic acid, analytically pure, shanghai nationality drug.

Preparing a solution: 7.8g of sodium dihydrogen phosphate and 17.91g of disodium hydrogen phosphate are weighed, dissolved by distilled water to a volume of 500mL, and phosphate buffer solution with pH of 6.8 and 0.1mol/L is prepared; accurately measuring 0.431mL of hydrochloric acid with the mass fraction of 36% -38%, and preparing 0.1mol/L hydrochloric acid by using distilled water to reach a constant volume of 50 mL; weighing 0.05g L-tyrosine, dissolving in 35mL of 0.1mol/L hydrochloric acid, and adding 65mL of PBS buffer solution with pH of 6.8 to obtain an L-tyrosine solution with mass fraction of 0.05%; dissolving 25000U tyrosinase in 250mL pure water to prepare tyrosinase solution with the enzyme activity of 100U/mL, subpackaging into 1.5mL EP pipes, and storing each 1mL in a refrigerator at-40 ℃; each sample and anti-cyclic acid was diluted with PBS buffer to a mass fraction concentration of 5%.

The specific method comprises the following steps: the sample adding systems of each group are shown in the following table, PBS buffer solution, L-tyrosine solution and each sample solution are mixed and put into a water bath with constant temperature of 37 ℃ for 10-15min; adding tyrosinase into the reaction solution, shaking uniformly, accurately timing, and stopping the reaction for 15min; the plates were spotted sequentially on 96-well plates, absorbance was measured with an enzyme-labeled instrument, and inhibition ratios were calculated.

Reagent(s)	C1/mL	C2/mL	S1/mL	S2/mL
					PBS	4	5	2	3
Sample of	0	0	2	2
					L-tyrosine	2	2	2	2
Tyrosinase solution	1	0	1	0

The formula of tyrosinase inhibition rate is shown as follows:

tyrosinase inhibition rate = [ (A1-A2) - (A3-A4) ]/(A1-A2) ×100%

Wherein A1, A2, A3 and A4 are absorbance values of C1, C2, S1 and S2, respectively.

The test results are shown in table 1:

TABLE 1

Group of	Tyrosinase inhibition rate (%)
		Example 1	87.36％
Example 2	85.23％
		Example 3	86.47％
Example 4	91.15％
		Example 5	90.02％
Comparative example 1	81.26％
		Comparative example 2	75.46％
Comparative example 3	83.11％
		Comparative example 4	82.83％
Comparative example 5	70.36％
		Comparative example 6	76.79％
Comparative example 7	73.90％
		Comparative example 8	70.54％

As can be seen from the data in table 1: the overall tyrosinase inhibition rates of examples 1-5 were higher than those of comparative examples 1-8, indicating that the tyrosinase inhibition effect of examples 4-5 was slightly better than examples 1-3, when either component was absent or only a single component was present in the composition.

Test example 3

The compositions prepared in examples 1-5 and comparative examples 1-8 were subjected to DPPH radical scavenging test.

Laboratory instrument and reagent:

The main reagent comprises: DPPH, analytically pure, tianjin metallocene; methanol, analytically pure, tianjin metallocene; ascorbic acid, analytically pure, shanghai nationality drug.

Preparing a solution: first, DPPH 1mg is dissolved in about 20mL of methanol, and the solution is subjected to ultrasonic treatment for 5min and is fully shaken to ensure that the upper part and the lower part are uniform. Taking 1mL of the DPPH solution, and measuring A value at 519nm to ensure that A=1.2-1.3; and preparing various sample solutions: the compositions of examples 1-5 and comparative examples 1-8 were diluted with methanol to prepare a composition having a mass fraction of 1%.

The specific method comprises the following steps: the sample addition systems for each group are shown in the following table, the reaction solution was shaken and then placed in a water bath at 37℃for 15 minutes, and then taken out, and the absorbance value of the solution was measured by an ultraviolet-visible spectrophotometer.

Reagent(s)	C1/mL	C2/mL	C3/mL
				DPPH solution	2	2	0
Sample solution	0	2	2
				Anhydrous methanol	2	0	2

The calculation formula of the DPPH free radical clearance is shown as follows:

DPPH radical scavenging = 1- (A2-A3)/a1×100%

Wherein A1, A2 and A3 are absorbance values of C1, C2 and C3, respectively.

The test results are shown in table 2:

TABLE 2

As can be seen from the data in table 2: the overall DPPH radical scavenging rate of examples 1-5 was higher than that of comparative examples 1-8, indicating that the DPPH radical scavenging effect was reduced when either component was absent or only a single component was present in the composition, wherein the DPPH radical scavenging effect of examples 4-5 was slightly better than that of examples 1-3.

Test example 4

Whitening effect tests were performed on the essences prepared in application examples 1 to 8 and comparative application examples 1 to 8.

The specific method comprises the following steps: after use, 10 volunteers (5 men and 5 women) were selected for each subject at ages 20-50 years and each male and female, and a multifunctional skin tester (model: MPA 580) manufactured by Courage Khazaka, germany was used. The whitening effect of the test subjects was evaluated by testing the ITA value (averaged) of each group of volunteers at week 0, week 4 using the essences prepared in application examples 1 to 8 and comparative application examples 1 to 8, respectively, and applying the same to facial skin 2 times daily for 4 weeks, the ITA test values (averaged) are shown in table 3:

TABLE 3 Table 3

Group of	0 week	4 weeks of
			Application example 1	39	66
Application example 2	42	65
			Application example 3	46	59
Application example 4	44	70
			Application example 5	40	63
Application example 6	41	67
			Application example 7	44	68
Application example 8	40	66
			Comparative application example 1	39	59
Comparative application example 2	42	52
			Comparative application example 3	43	60
Comparative application example 4	41	56
			Comparative application example 5	40	49
Comparative application example 6	41	51
			Comparative application example 7	40	46
Comparative application example 8	42	49

As can be seen from the data in table 3: the overall whitening effect of application examples 1-8 was higher than that of application examples 1-8, indicating that the whitening effect was reduced when either component was absent or only a single component was present in the composition, wherein the whitening effect of examples 4-5 was slightly better than examples 1-3.

Test example 5

The essence prepared in application examples 1 to 8 was subjected to a moisturizing effect test.

The specific method comprises the following steps: and under the environment of 24-26 ℃ and 50% relative humidity, selecting each half of men and women with ages of 20-50, and carrying out a post-use test on 10 volunteers (5 men and 5 women) corresponding to each tested object, wherein before the test, the test subjects need to uniformly clean the inner sides of the forearms of the two hands with clear water. Marking test areas on the left and right forearms of the subject after washing, wherein the interval between the test areas is 1cm, and each test area is 5×5cm ² . The essences prepared in application examples 1 to 8 were applied respectively, and the test sample amount was 0.2g. The measurement of the moisture content and the moisture content increase rate (average) of the test site were performed using a Corneometer after the subject was allowed to sit for 30 minutes in a constant environment are shown in table 4.

TABLE 4 Table 4

Group of	Moisture content increase Rate (%)
		Application example 1	33.63％
Application example 2	32.45％
		Application example 3	29.74％
Application example 4	35.97％
		Application example 5	33.50％
Application example 6	31.26％
		Application example 7	28.64％
Application example 8	29.13％

As can be seen from the data in table 4: the essence has excellent moisturizing effect, and has better moisturizing effect when the humectant component is a combination of squalane, dipotassium glycyrrhizinate and 1, 2-pentanediol.

Test example 6

Skin improvement satisfaction scores were performed on the essences prepared in application examples 1 to 8 and comparative application examples 1 to 8.

The specific method comprises the following steps: 160 volunteers, aged 25-45 years, women, were selected and divided into 16 groups. The essences prepared in application examples 1 to 8 and comparative application examples 1 to 8 were applied to facial skin 2 times a day for 12 weeks, respectively, and the skin care product was evaluated according to its skin improvement condition and scored. The scoring criteria are shown in the following table:

scoring of	Evaluation definition
		1≤X＜3	General skin improvement effect
3≤X＜4	The skin becomes tender and smooth, and has good whitening and freckle-removing effects
		4≤X≤5	The skin is obviously fine, smooth and tender, and the whitening and freckle-removing effects are quite obvious

The scoring results (average) are shown in table 5:

TABLE 5

As can be seen from the data in table 5: the combination and essence of the invention have good whitening and freckle-fading effects, and the scores of application examples 1-8 are higher overall than those of comparative application examples 1-8, which indicates that the whitening and freckle-fading effects are reduced when any one component is absent or only a single component is absent in the composition, wherein the whitening and freckle-fading effects of application examples 4-5 are slightly better than those of comparative application examples 1-3.

The applicant states that the present invention is described by way of the above examples as a whitening and spot-lightening antioxidant composition and its use, but the present invention is not limited to, i.e., does not mean that the present invention must be practiced in dependence upon the above examples. It should be apparent to those skilled in the art that any modification of the present invention, equivalent substitution of raw materials for the product of the present invention, addition of auxiliary components, selection of specific modes, etc., falls within the scope of the present invention and the scope of disclosure.

The preferred embodiments of the present invention have been described in detail above, but the present invention is not limited to the specific details of the above embodiments, and various simple modifications can be made to the technical solution of the present invention within the scope of the technical concept of the present invention, and all the simple modifications belong to the protection scope of the present invention.

In addition, the specific features described in the above embodiments may be combined in any suitable manner, and in order to avoid unnecessary repetition, various possible combinations are not described further.

Claims

1. The whitening and freckle-removing antioxidant composition is characterized by comprising the following components in parts by weight: 0.01-2 parts of N-acetylneuraminic acid, 0.05-2 parts of tranexamic acid, 0.1-4 parts of hop extract and 1-7 parts of lotus embryo extract.

2. The whitening, spot-lightening and antioxidant composition of claim 1 wherein the hops extract is prepared by a process comprising the steps of:

3. The whitening and spot-fading antioxidant composition as set forth in claim 2, wherein the concentration of the aqueous ethanol solution in step (1) is 80-95%.

4. The whitening and spot-fading antioxidant composition as set forth in claim 2, wherein the mass ratio of the aqueous ethanol solution to hops in the step (1) is 8-15 times.

5. The whitening and spot-fading antioxidant composition as set forth in claim 2, wherein the organic solvent of step (2) comprises any one or a combination of at least two of petroleum ether, pentane, hexane or heptane.

6. The whitening and spot-reducing antioxidant composition according to claim 2, wherein the purification in step (3) is performed by eluting with an aqueous ethanol solution using a column of a polyamide resin.

7. The whitening and spot-reducing antioxidant composition of claim 6, wherein the elution is a gradient elution from low concentration to high concentration with 25-60% aqueous ethanol.

8. Use of the whitening, spot-reducing and antioxidant composition according to any one of claims 1 to 7 for the preparation of cosmetics.

9. The use according to claim 8, wherein the cosmetic comprises a serum, an essential oil, an emulsion, a cream, a mask, an eye cream, a facial cleanser.

10. An essence with whitening, freckle-fading and oxidation-resisting effects is characterized by comprising the following components: the whitening and spot-reducing antioxidant composition of any of claims 1-7, a humectant, a thickener, an antibacterial preservative, and water.

11. The essence with whitening, freckle-fading and oxidation-resisting effects as claimed in claim 10, wherein the essence comprises the following components in parts by weight: the whitening and spot-fading antioxidant composition of any one of claims 1-7, wherein the composition comprises 1-15 parts of a humectant 0.1-10 parts of a thickener 0.1-5 parts of an antibacterial preservative 0.01-1 part of water.

12. The essence with whitening, spot-fading and oxidation-resisting effects according to claim 10, wherein the humectant comprises any one or a combination of at least two of jojoba esters, sodium hyaluronate, methyl propylene glycol, chlorella extract, dipotassium glycyrrhizinate, squalane, betaine or 1, 2-pentanediol.

13. The essence with whitening, spot-fading and oxidation-resisting effects according to claim 10, wherein the humectant is a combination of squalane, dipotassium glycyrrhizinate and 1, 2-pentanediol.

14. The essence with whitening, spot-fading and oxidation-resisting effects according to claim 10, wherein the antibacterial preservative comprises any one or a combination of at least two of methylparaben, 1, 2-hexanediol, octanoyl glycol, octanoyl hydroxamic acid or 1, 2-pentanediol.