A composition and its preparation method and application

Abstract

The present invention belongs to the technical field of daily chemical products, and discloses a composition, a preparation method thereof and an application thereof. The composition includes vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol and diglucosyl gallic acid. The present invention adopts vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol and diglucosyl gallic acid with clear whitening and antioxidant mechanisms, and exerts a synergistic effect, acts on the skin from multiple dimensions, has good whitening and antioxidant effects, is mild and non-irritating, and has stable performance (no physical and chemical changes occur, and no discoloration, taste change, or stratification occurs).

Description

Technical Field

[0001] The invention belongs to the technical field of daily chemical products, and particularly relates to a composition and a preparation method and application thereof. Background Art

[0002] At present, the cosmetics with whitening and antioxidant effects on the market have the following problems: 1. Adding a variety of traditional Chinese medicines with whitening and antioxidant effects. Due to the complex composition of traditional Chinese medicines, the whitening and antioxidant mechanisms are unclear, which easily brings unknown risks, and the whitening and antioxidant effects are relatively weak; 2. Since many whitening ingredients cannot be directly added to cosmetics, direct addition is prone to deterioration, discoloration, and taste changes, so most of them need to be pre-emulsified to increase their stability. Encapsulation will cause the effective ingredients to not fully play their role, and the whitening effect is relatively weak. Summary of the invention

[0003] The present invention aims to solve at least one of the technical problems existing in the above-mentioned prior art. To this end, the present invention proposes a composition and a preparation method and application thereof, which uses a combination of multiple components with clear whitening and anti-oxidation mechanisms to exert a synergistic effect, acts on the skin from multiple dimensions, has good whitening and anti-oxidation effects, and is mild and non-irritating.

[0004] The first aspect of the present invention provides a composition comprising vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol, and diglucosyl gallic acid.

[0005] The present invention adopts a variety of components with clear whitening and anti-oxidation mechanisms as follows:

[0006] Vitamin C is a safe and effective skin whitening agent. Vitamin C participates in the metabolism of tyrosinase in the body, promotes the oxidative decomposition of tyrosinase in the body, and reduces the conversion of tyrosine into melanin. It also has potential anti-inflammatory activity, which can promote wound healing and prevent excessive pigmentation after inflammation.

[0007] As a derivative of vitamin C, 3-o-ethyl ascorbic acid not only has a stable structure, but also can be absorbed through the skin and has high bioavailability.

[0008] Paeonol can inhibit intracellular O 2- The production of free radicals can whiten the skin, reduce the discoloration of pigments deposited in the skin, and remove blood stasis and spots; it also has anti-inflammatory, anti-swelling and analgesic, anti-allergic and antiviral effects.

[0009] Salicylic acid is a fat-soluble organic acid that can dissolve the constituent substances between keratinocytes. Therefore, it has the advantages of reducing the adhesion of keratinocytes, accelerating the shedding and renewal of epidermal cells, stimulating dermal collagen synthesis and tissue repair, and mild anti-inflammatory effects. At the same time, it improves skin texture and has the advantages of fast effect and good efficacy.

[0010] Diglucosyl gallic acid has the effects of scavenging free radicals, inhibiting tyrosinase activity, and preventing melanin transfer.

[0011] The present invention adopts a compound of multiple components including vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol and diglucosyl gallic acid with clear whitening and antioxidant mechanisms to exert a synergistic effect, act on the skin from multiple dimensions, have good whitening and antioxidant effects, and are mild and non-irritating.

[0012] Preferably, based on weight parts, it includes 1-25 parts of vitamin C, 0.01-1 parts of salicylic acid, 0.1-1.5 parts of 3-o-ethyl ascorbic acid, 0.01-0.5 parts of paeonol, and 0.001-0.5 parts of diglucosyl gallic acid.

[0013] Preferably, based on weight parts, it includes 10-25 parts of vitamin C, 0.2-1 parts of salicylic acid, 0.2-1.5 parts of 3-o-ethyl ascorbic acid, 0.1-0.5 parts of paeonol, and 0.01-0.5 parts of diglucosyl gallic acid.

[0014] Preferably, polyols are also included.

[0015] Preferably, the polyol includes at least one of ethoxydiglycol, dipropylene glycol, glycerol, butylene glycol, and 1,3-propylene glycol.

[0016] Preferably, the polyol includes at least two of ethoxydiglycol, dipropylene glycol, glycerol, butylene glycol, and 1,3-propylene glycol.

[0017] The second aspect of the present invention provides a method for preparing the composition of the present invention, comprising the following steps:

[0018] The vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol and diglucosyl gallic acid are mixed and stirred to obtain the composition.

[0019] Preferably, the method for preparing the composition of the present invention comprises the following steps:

[0020] Add paeonol to part of the polyol, heat to 50-80° C., stir until completely dissolved, and cool to 40-45° C. to obtain a mixed solution 1;

[0021] Add vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, and diglucosyl gallic acid to the remaining polyol and water, and stir until completely dissolved to obtain a mixed solution 2;

[0022] The mixed solution 1 and the mixed solution 2 are mixed and stirred to obtain the composition.

[0023] The third aspect of the present invention provides use of the composition of the present invention in preparing cosmetics or external skin preparations.

[0024] Preferably, the addition amount of the composition is 0.01 to 95 wt%.

[0025] Preferably, the addition amount of the composition is 70 to 95 wt%.

[0026] Preferably, the addition amount of the composition is 70 to 90 wt%.

[0027] Preferably, the dosage form of the cosmetic comprises one of a cream, an emulsion, an aqueous solution, a gel, a facial mask or a lotion.

[0028] Compared with the prior art, the beneficial effects of the present invention are as follows:

[0029] The present invention adopts a compound of multiple components including vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol and diglucosyl gallic acid with clear whitening and antioxidant mechanisms to exert a synergistic effect, act on the skin from multiple dimensions, have good whitening and antioxidant effects, are mild and non-irritating, and have stable performance (no physical and chemical changes occur, and no discoloration, taste change, or stratification occurs).

[0030] The scavenging rate of the composition of the present invention on superoxide anion free radicals can reach 92.12%, the scavenging rate on hydroxyl free radicals can reach 87.58%, and the relative activity inhibition rate of the composition of the present invention with a mass concentration of 5% on tyrosinase can reach 98.51%. DETAILED DESCRIPTION

[0031] In order to make the technical scheme of the present invention more clearly understood by those skilled in the art, the following embodiments are listed for illustration. It should be pointed out that the following embodiments do not limit the protection scope of the present invention.

[0032] Unless otherwise specified, the raw materials, reagents and devices used in the following examples can be obtained from conventional commercial sources or by existing known methods.

[0033] Example 1

[0034] A composition comprises, by weight, 12 parts of vitamin C, 0.2 parts of salicylic acid, 1 part of 3-o-ethyl ascorbic acid, 0.2 parts of paeonol, 0.1 parts of diglucosyl gallic acid, 50 parts of ethoxydiglycol, 25 parts of dipropylene glycol and 11.5 parts of deionized water.

[0035] The preparation method of the composition of this embodiment comprises the following steps:

[0036] Add paeonol to dipropylene glycol, heat to 65°C, stir until completely dissolved, and cool to 40°C to obtain a mixed solution 1;

[0037] Add vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, and diglucosyl gallic acid to ethoxydiglycol and deionized water, and stir until completely dissolved to obtain a mixed solution 2;

[0038] The mixed solution 1 and the mixed solution 2 are mixed and stirred to obtain a composition.

[0039] Example 2

[0040] A composition comprises, by weight, 1 part of vitamin C, 1 part of salicylic acid, 0.7 parts of 3-o-ethyl ascorbic acid, 0.5 parts of paeonol, 0.3 parts of diglucosyl gallic acid, 35 parts of glycerol, 35 parts of 1,3-propylene glycol and 26.5 parts of deionized water.

[0041] The preparation method of the composition of this embodiment comprises the following steps:

[0042] Add paeonol to 1,3-propylene glycol, heat to 50°C, stir until completely dissolved, and cool to 40°C to obtain a mixed solution 1;

[0043] Add vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, and diglucosyl gallic acid to glycerol and deionized water, and stir until completely dissolved to obtain a mixed solution 2;

[0044] The mixed solution 1 and the mixed solution 2 are mixed and stirred to obtain a composition.

[0045] Example 3

[0046] A composition comprises, by weight, 25 parts of vitamin C, 0.4 parts of salicylic acid, 0.2 parts of 3-o-ethyl ascorbic acid, 0.01 parts of paeonol, 0.5 parts of diglucosyl gallic acid, 40 parts of ethoxydiglycol, 20 parts of butylene glycol and 13.89 parts of deionized water.

[0047] The preparation method of the composition of this embodiment comprises the following steps:

[0048] Add paeonol to butanediol, heat to 60°C, stir until completely dissolved, and cool to 45°C to obtain a mixed solution 1;

[0049] Add vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, and diglucosyl gallic acid to ethoxydiglycol and deionized water, and stir until completely dissolved to obtain a mixed solution 2;

[0050] The mixed solution 1 and the mixed solution 2 are mixed and stirred to obtain a composition.

[0051] Example 4

[0052] A composition comprises, by weight, 10 parts of vitamin C, 0.3 parts of salicylic acid, 1.5 parts of 3-o-ethyl ascorbic acid, 0.5 parts of paeonol, 0.01 parts of diglucosyl gallic acid, 30 parts of ethoxydiglycol, 20 parts of dipropylene glycol, 20 parts of glycerol and 17.69 parts of deionized water.

[0053] The preparation method of the composition of this embodiment comprises the following steps:

[0054] Add paeonol to dipropylene glycol, heat to 70°C, stir until completely dissolved, and cool to ℃ to obtain a mixed solution 1;

[0055] Add vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, and diglucosyl gallic acid to ethoxydiglycol and deionized water, and stir until completely dissolved to obtain a mixed solution 2;

[0056] The mixed solution 1 and the mixed solution 2 are mixed and stirred to obtain a composition.

[0057] Example 5

[0058] A composition comprises, by weight, 20 parts of vitamin C, 0.5 parts of salicylic acid, 0.5 parts of 3-o-ethyl ascorbic acid, 0.1 parts of paeonol, 0.001 parts of diglucosyl gallic acid, 10 parts of dipropylene glycol, 10 parts of glycerol, 20 parts of butylene glycol, 20 parts of 1,3-propylene glycol and 18.899 parts of deionized water.

[0059] The preparation method of the composition of this embodiment comprises the following steps:

[0060] Add paeonol to dipropylene glycol, heat to 75°C, stir until completely dissolved, and cool to 40°C to obtain a mixed solution 1;

[0061] Vitamin C, deionized salicylic acid, 3-o-ethyl ascorbic acid, and diglucosyl gallic acid are added to butanediol, glycerol, and deionized water, and stirred until completely dissolved to obtain a mixed solution 2;

[0062] The mixed solution 1 and the mixed solution 2 are mixed and stirred to obtain a composition.

[0063] Example 6

[0064] A composition comprises, by weight, 10 parts of vitamin C, 0.2 parts of salicylic acid, 1 part of 3-o-ethyl ascorbic acid, 0.05 parts of paeonol, 0.01 parts of diglucosyl gallic acid, 20 parts of ethoxydiglycol, 15 parts of dipropylene glycol, 10 parts of glycerol, 10 parts of butylene glycol, 15 parts of 1,3-propylene glycol and 18.74 parts of deionized water.

[0065] The preparation method of the composition of this embodiment comprises the following steps:

[0066] Add paeonol to dipropylene glycol, heat to 80°C, stir until completely dissolved, and cool to 45°C to obtain a mixed solution 1;

[0067] Add vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, and diglucosyl gallic acid to ethoxydiglycol, glycerol, butylene glycol, 1,3-propylene glycol, and deionized water, and stir until completely dissolved to obtain a mixed solution 2;

[0068] The mixed solution 1 and the mixed solution 2 are mixed and stirred to obtain a composition.

[0069] Comparative Example 1

[0070] The difference from Example 1 is that in Comparative Example 1, vitamin C is replaced by deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0071] Comparative Example 2

[0072] The difference from Example 1 is that in Comparative Example 2, salicylic acid is replaced by deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0073] Comparative Example 3

[0074] The difference from Example 1 is that in Comparative Example 3, 3-o-ethyl ascorbic acid is replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0075] Comparative Example 4

[0076] The difference from Example 1 is that in Comparative Example 4, paeonol is replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0077] Comparative Example 5

[0078] The difference from Example 1 is that in Comparative Example 5, diglucosyl gallic acid is replaced by deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0079] Comparative Example 6

[0080] The difference from Example 1 is that in Comparative Example 6, vitamin C and salicylic acid are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0081] Comparative Example 7

[0082] The difference from Example 1 is that in Comparative Example 7, vitamin C and 3-o-ethyl ascorbic acid are replaced by deionized water, and the other components, amounts and preparation method of the composition are the same as those in Example 1.

[0083] Comparative Example 8

[0084] The difference from Example 1 is that in Comparative Example 8, vitamin C and paeonol are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0085] Comparative Example 9

[0086] The difference from Example 1 is that in Comparative Example 9, vitamin C and diglucosyl gallic acid are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0087] Comparative Example 10

[0088] The difference from Example 1 is that in Comparative Example 10, 3-o-ethyl ascorbic acid and salicylic acid are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0089] Comparative Example 11

[0090] The difference from Example 1 is that in Comparative Example 11, 3-o-ethyl ascorbic acid and paeonol are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0091] Comparative Example 12

[0092] The difference from Example 1 is that in Comparative Example 12, 3-o-ethyl ascorbic acid and diglucosyl gallic acid are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0093] Comparative Example 13

[0094] The difference from Example 1 is that in Comparative Example 13, paeonol and salicylic acid are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0095] Comparative Example 14

[0096] The difference from Example 1 is that in Comparative Example 14, paeonol and diglucosyl gallic acid are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0097] Comparative Example 15

[0098] The difference from Example 1 is that in Comparative Example 15, diglucosyl gallic acid and salicylic acid are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0099] Comparative Example 16

[0100] The difference from Example 1 is that in Comparative Example 16, vitamin C, salicylic acid, and 3-o-ethyl ascorbic acid are replaced with deionized water, and the other components, amounts, and preparation method of the composition are the same as those in Example 1.

[0101] Comparative Example 17

[0102] The difference from Example 1 is that in Comparative Example 17, vitamin C, salicylic acid and paeonol are replaced with deionized water, and the other components, amounts and preparation method of the composition are the same as those in Example 1.

[0103] Comparative Example 18

[0104] The difference from Example 1 is that in Comparative Example 18, vitamin C, salicylic acid, and diglucosyl gallic acid are replaced with deionized water, and the other components, amounts, and preparation method of the composition are the same as those in Example 1.

[0105] Comparative Example 19

[0106] The difference from Example 1 is that in Comparative Example 19, vitamin C, paeonol and 3-o-ethyl ascorbic acid are replaced with deionized water, and the other components, amounts and preparation method of the composition are the same as those in Example 1.

[0107] Comparative Example 20

[0108] The difference from Example 1 is that in Comparative Example 20, vitamin C, diglucosyl gallic acid, and 3-o-ethyl ascorbic acid are replaced by deionized water, and the other components, amounts, and preparation method of the composition are the same as those in Example 1.

[0109] Comparative Example 21

[0110] The difference from Example 1 is that in Comparative Example 21, vitamin C, paeonol and diglucosyl gallic acid are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0111] Comparative Example 22

[0112] The difference from Example 1 is that in Comparative Example 22, salicylic acid, 3-o-ethyl ascorbic acid and paeonol are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0113] Comparative Example 23

[0114] The difference from Example 1 is that in Comparative Example 23, salicylic acid, 3-o-ethyl ascorbic acid and diglucosyl gallic acid are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0115] Comparative Example 24

[0116] The difference from Example 1 is that in Comparative Example 24, salicylic acid, diglucosyl gallic acid and paeonol are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0117] Comparative Example 25

[0118] The difference from Example 1 is that in Comparative Example 25, 3-o-ethyl ascorbic acid, diglucosyl gallic acid and paeonol are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0119] Comparative Example 26

[0120] The difference from Example 1 is that in Comparative Example 26, vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, and diglucosyl gallic acid are replaced with deionized water, and the other components, amounts, and preparation method of the composition are the same as those in Example 1.

[0121] Comparative Example 27

[0122] The difference from Example 1 is that in Comparative Example 27, vitamin C, salicylic acid, 3-o-ethyl ascorbic acid and paeonol are replaced with deionized water, and the other components, amounts and preparation method of the composition are the same as those in Example 1.

[0123] Comparative Example 28

[0124] The difference from Example 1 is that in Comparative Example 28, vitamin C, 3-o-ethyl ascorbic acid, diglucosyl gallic acid and paeonol are replaced with deionized water, and the other components, amounts and preparation method of the composition are the same as those in Example 1.

[0125] Comparative Example 29

[0126] The difference from Example 1 is that in Comparative Example 29, salicylic acid, 3-o-ethyl ascorbic acid, paeonol and diglucosyl gallic acid are replaced with deionized water, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0127] Comparative Example 30

[0128] The difference from Example 1 is that in Comparative Example 30, vitamin C, salicylic acid, diglucosyl gallic acid and paeonol are replaced with deionized water, and the other components, amounts and preparation method of the composition are the same as those in Example 1.

[0129] Comparative Example 31

[0130] The difference from Example 1 is that in Comparative Example 31, vitamin C is replaced with vitamin E, and the other components, amounts and preparation method of the composition are the same as those in Example 1.

[0131] Comparative Example 32

[0132] The difference from Example 1 is that in Comparative Example 32, 3-o-ethyl ascorbic acid is replaced with ascorbyl glucoside, and the other components, amounts and preparation method of the composition are the same as those in Example 1.

[0133] Comparative Example 33

[0134] The difference from Example 1 is that in Comparative Example 33, salicylic acid is replaced by lactobionic acid, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0135] Comparative Example 34

[0136] The difference from Example 1 is that in Comparative Example 34, paeonol is replaced by phloretin, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0137] Comparative Example 35

[0138] The difference from Example 1 is that in Comparative Example 35, diglucosyl gallic acid is replaced by ellagic acid, and other components, amounts and preparation method of the composition are the same as those in Example 1.

[0139] Test Example 1 Stability Test

[0140] 1.1 Experimental Principle

[0141] In order to maintain stable performance of the product during storage and use, prevent physical and chemical changes, and prevent discoloration, taste change, stratification, etc., high and low temperature storage stability tests should be carried out during formula design.

[0142] 1.2 Test Method

[0143] The compositions obtained in Examples 1 to 6 and Comparative Examples 1 to 35 were placed at high temperature (40±1)°C, low temperature (5±1)°C and room temperature (25±1)°C for 3 months. On the 1st, 3rd, 7th, 14th, 21st, 28th, 45th, 60th, 75th and 90th days, the high temperature or low temperature products were restored to room temperature (about 25°C) and the products were observed for obvious discoloration, taste change and delamination problems. If such problems occurred, they were deemed unqualified.

[0144] 1.3 Test Results

[0145] Table 1 Stability test results

[0146]

[0147]

[0148]

[0149] Note: “OK” means no obvious change, “×” means unqualified.

[0150] The data in Table 1 show that Comparative Examples 2, 10, 13, 15, 22, 23, 24, and 29 have obvious discoloration problems, indicating that the presence of salicylic acid is conducive to the stability of vitamin C. The stability of Comparative Example 33 is not problematic, indicating that the addition of acid can improve the stability of vitamin C. Comparative Example 31 is unstable and has a stratification phenomenon mainly because vitamin E is an oil-soluble raw material and is incompatible with the entire solvent system.

[0151] Test Example 2 Free Radical Scavenging Test

[0152] Examples 1 to 6 and Comparative Examples 1 to 35 were used as samples and the following tests were performed:

[0153] 2.1 Evaluation test of superoxide anion free radical scavenging ability

[0154] Take 4.5mL of 0.05mol / L, pH=8.2 Tris-HCl buffer solution and preheat it in a 25℃ water bath for 30min. Then add 1mL of sample and 0.4mL of 25mol / L pyrogallol solution, mix well, react in a 25℃ water bath for 5min, and add 1mL of 8mol / L HCl to terminate the reaction. Use Tris-HCl buffer solution as a reference and measure the absorbance at 299nm. Use 1mL of deionized water instead of sample for the blank control group.

[0155] The calculation formula of superoxide anion radical scavenging rate is as follows:

[0156] Superoxide anion radical scavenging rate (%) = [1-(A2 / A1)] × 100%;

[0157] Where A1 is the absorbance value of the blank control group, and A2 is the absorbance value of the sample group.

[0158] 2.2 Hydroxyl free radical scavenging ability evaluation test

[0159] In a 25mL cuvette, add 3mL of 2mmol / L FeSO4 and 3mL of 1mmol / L H2O2, shake well, then add 3mL of 6mmol / L salicylic acid, shake well, heat in a 37℃ water bath for 15min, take out and measure its absorbance; add 1mL of sample respectively, shake well, continue to heat in a water bath for 15min, take out and measure its absorbance. The blank control group uses 1mL of deionized water instead of sample.

[0160] The calculation formula of hydroxyl radical scavenging rate is as follows:

[0161] Hydroxyl radical scavenging rate (%) = [A0-Ax-(A0-Ax0)] / A0×100%;

[0162] Wherein, A0 is the absorbance value of the reaction system before adding the sample; Ax is the absorbance value of the system after the sample removes the hydroxyl free radicals; Ax0 is the absorbance value of the system after the blank control group removes the hydroxyl free radicals.

[0163] The test results of the above superoxide anion free radical scavenging rate and hydroxyl free radical scavenging rate are shown in Table 2.

[0164] Table 2 Free radical scavenging test results

[0165]

[0166]

[0167]

[0168] The superoxide anion radical scavenging rate and the hydroxyl radical scavenging rate reflect its antioxidant capacity to a certain extent. The higher the scavenging rate, the better the antioxidant degree and the better the anti-aging effect. Therefore, the anti-aging effect can be judged by studying the ability of the composition to scavenging superoxide anion radicals and hydroxyl radicals. From the results of Table 2, the superoxide anion radical scavenging rate and the hydroxyl radical scavenging rate of Examples 1-6 are significantly higher than those of Comparative Examples 1-35; Examples 1-6 use vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol and diglucosyl gallic acid to compound, and the antioxidant effect is significantly higher than any one, two, three or four of the compounds used in Comparative Examples 1-30. At the same time, even if other components with similar effects are used to replace Comparative Examples 31-35, the antioxidant effect is significantly lower than that of Examples 1-6. It can be seen that vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol and diglucosyl gallic acid in the composition of the present invention have a synergistic effect and have good antioxidant efficacy.

[0169] Test Example 3 Tyrosinase Activity Inhibition Test

[0170] 3.1 Experimental Purpose

[0171] By comparing with arbutin, a commonly used whitening ingredient in skin care products, the inhibitory effect of the composition of different concentrations on tyrosinase activity was tested, thereby examining the whitening effect of the composition of the present invention.

[0172] 3.2 Preparation of reference products

[0173] Prepare 1% arbutin solution.

[0174] The mass concentrations of the compositions prepared in Examples 1 to 6 and Comparative Examples 1 to 35 were diluted to 5%, 0.5%, 0.05%, respectively.

[0175] Three gradients.

[0176] 3.3 Experimental methods

[0177] The in vitro DOPA oxidation reaction method was used to digest the human epidermal melanocytes in the logarithmic growth phase with trypsin / EDTA solution, and the digestion was terminated with trypsin neutralization solution. After centrifugation, the melanocytes were diluted to 1×10 with MelM medium. 5 The diluted liquid was inoculated into a 96-well plate at a density of 100 μL / well. 4 / well. Overnight, when the cells adhere to the wall, the culture medium is aspirated, and 3 gradient combination solutions are added to the 96-well plate, 100 μL per well, and 3 replicates are set up for each concentration. A positive control group containing arbutin (melanocytes + melanocyte culture medium + arbutin 1%, 100 μL), a negative control group (melanocytes + melanocyte culture medium) and a blank control group (melanocyte culture medium alone) are set up, and 3 replicates are set up for each group. The 24-well plate is placed in an incubator at 37°C and 5% CO2 for 72 hours. After the drug treatment is completed, the supernatant is discarded and the melanocytes are washed 2-3 times with PBS solution. 100 μL of 1% TritonX-100 (prepared with PBS solution) is added to each well, and the plate is shaken at a low speed on an oscillator for 30 minutes. The 96-well plate is placed in a -20°C refrigerator for 1 hour, and then taken out and melted at room temperature to completely lyse the melanocytes. 100 μL of 0.1% L-DOPA solution (prepared in PBS) was added to each well, and the samples were incubated at 37° C. for 2 h. The absorbance of the samples was measured by an enzyme-labeled instrument at a wavelength of 490 nm.

[0178] Relative tyrosinase activity inhibition rate = (1-[(average absorbance of drug group-average absorbance of blank group) / (average absorbance of negative control group-average absorbance of blank group)]) × 100%.

[0179] 3.4 Experimental Results

[0180] The results of the tyrosinase activity inhibition test are shown in Table 3.

[0181] Table 3 Tyrosinase activity inhibition test results

[0182]

[0183]

[0184]

[0185] From the data in Table 3, it can be seen that compared with the negative control group, the positive control group, Examples 1-6 and Comparative Examples 1-35 at different concentrations all have an inhibitory effect on tyrosinase activity. By comparing the test results of Examples 1-6 and Comparative Examples 1-35, the relative inhibition rate of tyrosinase in the composition of Example 1-6 is significantly higher than that in Comparative Examples 1-35; Example 1-6 uses vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol and diglucosyl gallic acid to compound the five components, and the inhibitory effect on tyrosinase activity is significantly higher than any one, two, three or four of the compounds used in Comparative Examples 1-30. At the same time, even if other components with similar effects are used to replace Comparative Examples 31-35, the inhibitory effect on tyrosinase activity is also significantly lower than that of Example 1-6. It can be seen that vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol and diglucosyl gallic acid in the composition of the present invention have a synergistic effect and have a good whitening effect.

[0186] Test Example 4 Red blood cell hemolysis test

[0187] The irritation of the enzymatic extract was evaluated by the red blood cell hemolysis test. The red blood cell hemolysis test is one of the alternative methods to the rabbit eye irritation test (Draize test). The basic principle is to evaluate the damage of chemicals to eye tissue cells by measuring the amount of hemoglobin dissolved and the degree of denaturation. Internationally, the RBC test is mainly used to evaluate the eye irritation of chemicals such as cosmetics and raw materials. The irritation classification standards are shown in Table 4.

[0188] Table 4 ECVAM cosmetic product RBC test irritation classification standard

[0189] L / D Grading L / D>100 Non-irritating 10<L / D≤100 Slightly irritating 1<L / D≤10 Mild irritant 0.1<L / D≤1 Moderate irritation L / D≤0.1 Severe irritation

[0190] The results of the red blood cell hemolysis test on the compositions prepared in Examples 1-6 and Comparative Examples 1-35 are shown in Table 5, wherein HD50 is the sample concentration when 50% of red blood cells are hemolyzed, DI is the protein denaturation index, and L / D is the ratio of HD50 to DI.

[0191] Table 5 Red blood cell hemolysis test results

[0192]

[0193]

[0194] It can be seen from the test results in Table 5 that the L / D values ​​of the compositions prepared in Examples 1-6 are all greater than 100, indicating that the irritation classification of the compositions of the present invention is non-irritating and has the characteristics of being mild and non-irritating.

[0195] Application Example 1

[0196] An essence water, the formula of which is shown in Table 6.

[0197] Table 6 Essence water formula

[0198]

[0199]

[0200] The preparation method of the essence water comprises the following steps:

[0201] (1) Pre-dissolve the phase A components at 65°C until transparent, and then cool to below 40°C;

[0202] (2) Pre-disperse the components of phase B evenly and completely;

[0203] (3) Mix and stir the phase C components until they are evenly dispersed, add the phase A and phase B components into the phase C components and stir until they are evenly dispersed to obtain essence water.

[0204] Application Example 2

[0205] The difference from Application Example 1 is that in Application Example 2, the composition prepared in Example 1 is replaced by the composition prepared in Example 2, and the other components, amounts and preparation method of the essence water are the same as those in Application Example 1.

[0206] Application Example 3

[0207] The difference from Application Example 1 is that in Application Example 3, the composition prepared in Example 1 is replaced by the composition prepared in Example 3, and the other components, amounts and preparation method of the essence water are the same as those in Application Example 1.

[0208] Application Example 4

[0209] The difference from Application Example 1 is that in Application Example 4, the composition prepared in Example 1 is replaced by the composition prepared in Example 4, and the other components, amounts and preparation method of the essence water are the same as those in Application Example 1.

[0210] Application Example 5

[0211] The difference from Application Example 1 is that in Application Example 5, the composition prepared in Example 1 is replaced by the composition prepared in Example 5, and the other components, amounts and preparation method of the essence water are the same as those in Application Example 1.

[0212] Application Example 6

[0213] The difference from Application Example 1 is that in Application Example 6, the composition prepared in Example 1 is replaced by the composition prepared in Example 6, and the other components, amounts and preparation method of the essence water are the same as those in Application Example 1.

[0214] Considering that the stability of the composition of comparative example 31 is unqualified and human trials are required when it is applied to essence water, it was not subsequently applied to essence water for comparative tests.

[0215] Comparative application example 1

[0216] The difference from Application Example 1 is that in Comparative Application Example 1, the composition prepared in Example 1 is replaced by the composition prepared in Comparative Example 32, and the other components, amounts and preparation method of essence water are the same as those in Application Example 1.

[0217] Comparative Application Example 2

[0218] The difference from Application Example 1 is that in Comparative Application Example 2, the composition prepared in Example 1 is replaced by the composition prepared in Comparative Example 33, and the other components, amounts and preparation method of essence water are the same as those in Application Example 1.

[0219] Comparative Application Example 3

[0220] The difference from Application Example 1 is that in Comparative Application Example 3, the composition prepared in Example 1 is replaced by the composition prepared in Comparative Example 34, and the other components, amounts and preparation method of essence water are the same as those in Application Example 1.

[0221] Comparative Application Example 4

[0222] The difference from Application Example 1 is that in Comparative Application Example 4, the composition prepared in Example 1 is replaced by the composition prepared in Comparative Example 35, and the other components, amounts and preparation method of essence water are the same as those in Application Example 1.

[0223] Test Example 5 Irritation Test

[0224] The mildness sample data of different application examples and the main comparative application examples were analyzed through irritation scoring to further confirm the irritation of the product. 300 consumers were selected and divided into 10 groups. The irritation scores of the essence water prepared by the corresponding application examples 1-6 and comparative application examples 1-4 were respectively calculated at the beginning of use and after 1 week of use. Irritation scoring rules: 5-point system, 1 point-mild irritation, 2 points-moderately mild irritation, 3 points-moderate irritation, 4 points-moderately severe irritation, 5 points-severe irritation. The statistical results are shown in Table 7.

[0225] Table 7 Product mildness test results

[0226]

[0227]

[0228] It can be seen from the test data in Table 7 that Application Examples 1-6 and Comparative Application Examples 1-4 have low irritation and good overall mildness, and can be used for subsequent human efficacy tests.

[0229] Test Example 6 Whitening and Anti-aging Human Trial Evaluation Test

[0230] 300 subjects (healthy, normal skin, no history of cosmetic allergies, aged 35-45 years old) were selected and randomly divided into 10 groups. Half-face tests were randomly selected. Samples were used once a day in the morning and evening for 28 days. On the 14th and 28th days, they were seated in a test environment with a temperature of 20±2℃ and a humidity of 50±10% for 30 minutes. The facial skin color brightness (L) and skin elasticity were measured and recorded as D14 and D28 respectively. The L value has a significant difference. The larger the L value, the more the color tends to be white, and the smaller the L value, the more the color tends to be black. The skin elasticity characterization value R2 is used to indicate the size of the skin's ability to recover after being stretched in the test. The younger the skin and the better the elasticity of the skin, the larger the R2; conversely, the older the skin and the less elastic the skin, the smaller the R2. Specific statistical results are shown in Table 8.

[0231] Table 8 Human trial evaluation results

[0232]

[0233]

[0234] From the results in Table 8, it can be seen that after 28 days of testing, the subjects who used the essence water of application examples 1-6 had better improvements in L value and skin elasticity than those who used the essence water of comparative application examples 1-4. Among them, the L value of application example 1 increased by 4.15% after 28 days, and the skin elasticity characteristic value R2 increased by 19.98%, while the corresponding values ​​of comparative application examples 1-4 increased by 1.41% and 8.82% respectively. This further verifies that the present invention uses a compound of five components of vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol and diglucosyl gallic acid to play a synergistic role and has good whitening and anti-aging effects.

[0235] The preferred embodiments of the present invention are specifically described above, but the invention is not limited to the embodiments. Those skilled in the art may make various equivalent modifications or substitutions without violating the spirit of the invention. These equivalent modifications or substitutions are all included in the scope defined by the claims of this application.

Claims

1. A composition, characterized in that Composed of vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol, diglucosyl gallic acid, polyol and deionized water, wherein, by weight, the vitamin C is 1 to 25 parts, the salicylic acid is 0.01 to 1 part, the 3-o-ethyl ascorbic acid is 0.1 to 1.5 parts, the paeonol is 0.01 to 0.5 parts, and the diglucosyl gallic acid is 0.001 to 0.5 parts; The polyol is at least one of ethoxydiglycol, dipropylene glycol, glycerol, butylene glycol and 1,3-propylene glycol.

2. The method for preparing the composition according to claim 1, characterized in that: The following steps are involved: The vitamin C, salicylic acid, 3-o-ethyl ascorbic acid, paeonol, diglucosyl gallic acid, polyol and deionized water are mixed and stirred to obtain the composition.

3. Use of the composition according to claim 1 in the preparation of cosmetics or external skin preparations.

4. The use according to claim 3, characterized in that: The addition amount of the composition is 0.01 to 95 wt %.

5. The use according to claim 4, characterized in that: The addition amount of the composition is 70 to 95 wt %.

6. The use according to claim 3, characterized in that: The dosage form of the cosmetic is selected from cream, emulsion, water, gel, facial mask or lotion.

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