CN114042001A - Whitening composition with synergistic effect and application thereof - Google Patents

Whitening composition with synergistic effect and application thereof Download PDF

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CN114042001A
CN114042001A CN202111211140.XA CN202111211140A CN114042001A CN 114042001 A CN114042001 A CN 114042001A CN 202111211140 A CN202111211140 A CN 202111211140A CN 114042001 A CN114042001 A CN 114042001A
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whitening
parts
resveratrol
ethyl ether
composition
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孙亚娟
杨成
梅杰
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Shenzhen Lantern Science Co ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/347Phenols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/676Ascorbic acid, i.e. vitamin C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59Mixtures
    • A61K2800/592Mixtures of compounds complementing their respective functions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59Mixtures
    • A61K2800/592Mixtures of compounds complementing their respective functions
    • A61K2800/5922At least two compounds being classified in the same subclass of A61K8/18
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74Biological properties of particular ingredients
    • A61K2800/78Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782Enzyme inhibitors; Enzyme antagonists

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  • Cosmetics (AREA)

Abstract

The invention belongs to the technical field of cosmetics and discloses a whitening composition with a synergistic effect and application thereof. The whitening composition comprises the following components in parts by weight: 0.5-3 parts of 4-butyl resorcinol, 3-12 parts of resveratrol and 5-25 parts of ascorbic acid ethyl ether. The whitening composition provided by the invention contains whitening active substances such as 4-butyl resorcinol, resveratrol and ascorbic acid ethyl ether, so that the tyrosinase activity can be effectively inhibited, melanin can be effectively reduced, and the whitening effect can be exerted through a whitening mechanism with double channels of inhibiting the tyrosinase activity and reducing the melanin.

Description

Whitening composition with synergistic effect and application thereof
Technical Field
The invention belongs to the technical field of cosmetics, and particularly relates to a whitening composition with a synergistic effect and application thereof.
Background
Whitening is one of the most extensive fields for skin care of modern Chinese women, and meanwhile, whitening cosmetics also become one of the fastest branches of the development of the cosmetic industry in China, and the market scale is increased by more than 20% every year. The core component of the whitening product is a whitening agent which is contacted with the skin of a human body, released and absorbed through the skin and acts on melanocytes and color spots in the using process of the whitening cosmetic. At present, the action mechanism of the whitening agent is mainly three aspects: 1. inhibiting and hindering the production and transfer of melanin in melanocytes; 2. reducing melanin in the horny layer to lighten the color; 3. accelerate the metabolism of melanin and make the existing pigment deposition part fall off. Among them, the 3 rd mechanism is often used in whitening products in a "brushing acid" manner, artificially promoting exfoliation of keratin, easily breaking skin barrier and causing sensitive skin. Therefore, the design of general whitening agents and whitening products is always spread around melanin and melanocytes.
The human melanin is generated by melanocyte, the key factor of melanin synthesis is tyrosinase, and the inhibition of tyrosinase activity is the most important link for reducing melanin generation; the whitening effect can be achieved by introducing antioxidant to reduce melanin into colorless substance. 4-butyl resorcinol, based on its small molecular structure and high permeability, readily enters the active center of tyrosinase, has a strong ability to inhibit tyrosinase activity, but is accompanied by strong skin irritation. Resveratrol has certain ability of inhibiting tyrosinase activity, is a polyphenol substance, has certain antioxidant ability, has obvious inhibition effect on cell growth at high concentration, and shows certain cytotoxicity. The ascorbyl ethyl ether is a hydrophilic and oleophilic amphiphilic substance, has high transdermal absorption capacity and stability and strong oxidation resistance, can also penetrate into a corium layer to promote the formation of collagen and improve the skin elasticity, but needs high dosage when being used for a whitening product alone.
Because different whitening agents have different whitening mechanisms and whitening effects, multiple whitening agents are compounded and combined, and the utilization of the synergistic interaction capacity among the whitening agents is a necessary way to reduce the dosage of the whitening agents, improve the whitening efficiency and reduce the production cost.
Disclosure of Invention
The first aspect of the present invention is directed to a whitening composition.
In a second aspect, the present invention is directed to a method for preparing the whitening composition of the first aspect of the present invention.
The third aspect of the present invention is directed to the use of the whitening composition of the first aspect of the present invention in the preparation of products.
In a fourth aspect, the present invention is directed to a cosmetic.
The fifth aspect of the invention aims to provide a whitening cream.
In order to achieve the purpose, the technical scheme adopted by the invention is as follows:
in a first aspect of the present invention, there is provided a whitening composition comprising the following components in parts by weight: 0.5-3 parts of 4-butyl resorcinol, 3-12 parts of resveratrol and 5-25 parts of ascorbic acid ethyl ether.
Preferably, the whitening composition comprises the following components in parts by weight: 0.5-2 parts of 4-butyl resorcinol, 4-12 parts of resveratrol and 5-20 parts of ascorbic acid ethyl ether.
Further preferably, the whitening composition comprises the following components in parts by weight: 1-2 parts of 4-butyl resorcinol, 4-8 parts of resveratrol and 5-10 parts of ascorbic acid ethyl ether.
Preferably, the whitening composition further comprises 56-80 parts of alcohol.
Further preferably, the whitening composition further comprises 56-70 parts of alcohol.
Still more preferably, the whitening composition further comprises 56-68 parts of alcohol.
Preferably, the alcohols include one or more of ethanol, isopropanol, glycerol, n-butanol, 1, 3-butanediol, and pentanol.
Preferably, the whitening composition further comprises 9-20 parts of water.
In a second aspect of the present invention, there is provided a method for preparing the whitening composition of the first aspect of the present invention, comprising the steps of: mixing 4-butylresorcinol, resveratrol, ascorbic acid ethyl ether, alcohols and water to obtain the whitening composition.
In a third aspect of the present invention, there is provided a use of the whitening composition of the first aspect of the present invention in the manufacture of a product.
Preferably, the product is used for:
(1) inhibiting tyrosinase activity, and/or
(2) Reduce melanin.
In a fourth aspect of the present invention, there is provided a cosmetic comprising the whitening composition of the first aspect of the present invention.
Preferably, the whitening composition accounts for 3-10% of the cosmetic by mass.
More preferably, the whitening composition is 5 to 10 percent by weight of the cosmetic.
More preferably, the whitening composition is 5 to 8 percent by weight of the cosmetic.
Preferably, the cosmetic includes an aqueous type cosmetic, a gel type cosmetic, an emulsion type cosmetic or a cream type cosmetic.
Further preferably, the cosmetic is a cream-type cosmetic.
In a fifth aspect of the present invention, there is provided a whitening cream comprising the whitening composition of the first aspect of the present invention and a cosmetically acceptable adjuvant.
Preferably, the mass percentage content of the 4-butyl resorcinol in the whitening cream is 0.04-0.2%.
Further preferably, the mass percentage of the 4-butyl resorcinol in the whitening cream is 0.05-0.2%.
More preferably, the mass percentage of the 4-butyl resorcinol in the whitening cream is 0.05-0.15%.
Preferably, the resveratrol in the whitening cream is 0.2-0.9% by mass.
Further preferably, the resveratrol in the whitening cream is 0.2-0.7% by mass.
More preferably, the resveratrol in the whitening cream is 0.2-0.6% by mass.
Preferably, the content of the ascorbic acid ethyl ether in the whitening cream is 0.5-3% by mass.
Further preferably, the content of the ascorbic acid ethyl ether in the whitening cream is 0.5-2% by mass.
More preferably, the content of the ascorbic acid ethyl ether in the whitening cream is 0.5-1.5% by mass.
The invention has the beneficial effects that: 1. the whitening composition provided by the invention contains whitening active substances such as 4-butyl resorcinol, resveratrol and ascorbic acid ethyl ether, so that the tyrosinase activity can be effectively inhibited, melanin can be reduced, and the whitening effect can be exerted by a whitening mechanism with double channels of inhibiting the tyrosinase activity and reducing the melanin; 2. the whitening composition provided by the invention has a good synergistic effect, can achieve a good whitening effect by using a lower-content whitening composition, greatly reduces the use amount of each whitening active substance in cosmetics, and can effectively reduce the discomfort caused by the whitening active substances to the skin; 3. the whitening composition provided by the invention is used in whitening cream, the prepared whitening cream can effectively inhibit tyrosinase activity, reduce the generation of melanin, reduce the existing melanin in the horny layer of the skin, lighten the color of the skin, further improve the whiteness of the skin and the brightness of the skin complexion, and simultaneously enhance the elasticity of the skin, and the whitening cream is mild, non-irritant, safe and effective; 4. the whitening combination formula is optimized by combining a biochemical test, a cell test and a human body test, so that the optimal use concentration of each whitening active ingredient is obtained, and the safety and low irritation of the whitening composition are ensured while the whitening effect is ensured; 5. the whitening composition provided by the invention can be applied to various product forms of whitening cosmetics, and has the characteristics of simple preparation method, wide application and capability of meeting market demands.
Drawings
FIG. 1 is a statistical chart of the results of the effect of 4-butylresorcinol on tyrosinase activity at various concentrations.
FIG. 2 is a statistical chart of the results of the effect of different concentrations of resveratrol on tyrosinase activity.
FIG. 3 is a graph showing the results of the effect of various concentrations of ascorbic acid ethyl ether on tyrosinase activity.
FIG. 4 is a statistical chart showing the effect of different concentrations of 4-butylresorcinol on the viability of mouse melanoma cells B16-F10.
FIG. 5 is a statistical chart of the results of the effect of resveratrol at different concentrations on the viability of mouse melanoma cells B16-F10.
FIG. 6 is a statistical chart of the results of the effect of different concentrations of ascorbyl ethyl ether on the viability of mouse melanoma cells B16-F10.
Figure 7 is a graph of the inhibitory effect of the whitening active compound combination composition of example 2 on tyrosinase.
FIG. 8 is a statistical chart showing the results of the melanin change values of the skin after applying the whitening cream in the example of application.
Fig. 9 is a result statistical chart of the brightness change value of skin color after the whitening cream in the smearing application example.
FIG. 10 is a statistical chart showing the results of the change in skin elasticity after application of the whitening cream in the example of the application.
Detailed Description
The present invention will now be described in detail with reference to specific examples, but the scope of the present invention is not limited thereto.
The materials, reagents and the like used in the present examples are commercially available materials and reagents unless otherwise specified.
Example 14 tyrosinase activity inhibiting ability of butyl Resorcinol, resveratrol and ascorbic acid Ethyl Ether and its cytotoxicity
1. Tyrosinase activity inhibition assay
Tyrosinase activity inhibition experiments were performed in 96-well plates, and the experiments were divided into two groups, experiment group: add 40. mu.L of the sample to be tested (0.1. mu. mol/L, 0.2. mu. mol/L, 0.5. mu. mol/L, 1. mu. mol/L and 2. mu. mol/L of 4-butylresorcinol; 3. mu. mol/L, 5. mu. mol/L, 10. mu. mol/L, 15. mu. mol/L and 30. mu. mol/L of resveratrol; 0.4mmol/L, 0.8mmol/L, 1.6mmol/L, 2mmol/L and 4mmol/L of ethyl ether ascorbate) and 60. mu.L of 250U/mL tyrosinase, control: add 40. mu.L 80mM PBS (pH6.8) and 60. mu.L 250U/mL tyrosinase, each treatment 3 more wells; incubating the 96-well plate at room temperature (20-25 ℃) for 10min, and measuring the absorbance value at 475nm wavelength of an enzyme-labeling instrument; adding 100 mu L of 6.0mM tyrosine into each hole, shaking, uniformly mixing, placing in an incubator at 37 ℃ for reaction for 30min, measuring the absorbance value at the wavelength of 475nm by using an enzyme-labeling instrument, and calculating the inhibition rate of the tyrosinase activity by using the following formula: the inhibition rate (%) [1- (As-Asb)/(Ac-Acb) ] × 100%, wherein As is the absorbance of the solution after the experimental group reacts with tyrosine, Ac is the absorbance of the solution after the control group reacts with tyrosine, Acb is the absorbance of the solution without tyrosine added to the experimental group, and Asb is the absorbance of the solution without tyrosine added to the control group.
The inhibition efficiency of each whitening active substance on the tyrosinase activity is obtained by observing the inhibition capacity of 4-butyl resorcinol, resveratrol and ascorbic acid ethyl ether on the tyrosinase activity. The lower the concentration of active required to achieve the same inhibition rate, the greater the ability of the active to inhibit tyrosinase. As can be seen from FIGS. 1 to 3, the better the inhibition effect on tyrosinase activity with increasing concentrations of 4-butylresorcinol, resveratrol and ascorbyl ethyl ether; to inhibit tyrosinase activity by 30% (EC)30) EC of 4-butylresorcinol on tyrosinase Activity as an evaluation index30EC of resveratrol on tyrosinase Activity of 0.35. mu. mol/L30EC of 10. mu. mol/L, ascorbyl ethyl ether on tyrosinase activity30The content of the active substances is 2mmol/L, and the inhibition abilities of the three whitening active substances on the tyrosinase activity are 4-butyl resorcinol, resveratrol and ascorbic acid ethyl ether in sequence from strong to weak.
2. Cytotoxicity test experiment
Culturing mouse melanoma cells B16-F10, after the cells enter logarithmic growth phase, digesting with trypsin, dispersing the cells with DMEM medium, counting the cells with a hemocytometer, and diluting the cell concentration with DMEM medium to 10 × 104Per mL; the diluted cell suspension was added to a 96-well plate at 100. mu.L per well, i.e., 1X 104One/well, placed at 37 ℃ in 5% CO2Culturing for 24 hours in an incubator; the medium was removed from the 96-well plate, washed 3 times with PBS and 100. mu.L of the test sample was added to each well(experimental group: 0.0625. mu. mol/L, 0.25. mu. mol/L, 1. mu. mol/L, 2.5. mu. mol/L and 5. mu. mol/L of 4-butylresorcinol, 5. mu. mol/L, 10. mu. mol/L, 20. mu. mol/L, 40. mu. mol/L and 50. mu. mol/L of resveratrol, 1mmol/L, 2mmol/L, 7.5mmol/L, 15mmol/L and 30mmol/L of ethyl ether ascorbate; control group: DMEM medium), 3 duplicate wells were treated each; the 96-well plate was placed at 37 ℃ in 5% CO2Culturing for 24 hours in an incubator; removing the culture medium from the 96-well plate, washing with PBS 3 times, adding 100 mu L of 0.5mg/mL thiazole blue into each well, and continuing to incubate for 4h in the incubator at 37 ℃; removing supernatant from 96-well plate, adding 150 μ L dimethyl sulfoxide into each well, shaking at 37 deg.C for 10min, and measuring absorbance at 490nm with enzyme-labeling instrument; the cell viability of mouse melanoma cells B16-F10 was calculated using the following formula: cell viability (%) — absorbance value of test sample/absorbance value of control group × 100%.
The mouse melanoma cells B16-F10 are taken as research objects, and the influence of different addition concentrations of 4-butyl resorcinol, resveratrol and ascorbyl ethyl ether on the vitality of the mouse melanoma cells B16-F10 is examined. By taking the mouse melanoma cell B16-F10 cell activity of 80% as an evaluation index, the toxicity of each whitening active substance to human skin cells can be obtained. When the cell viability of the mouse melanoma cells B16-F10 is more than 80%, the active matter is non-toxic or basically non-toxic to human cells under the using concentration; when the cell activity of mouse melanoma cells B16-F10 is less than 80%, the active matter is toxic to human cells at the use concentration, and the content of the active matter needs to be controlled when the active matter is applied to cosmetics; the lower the concentration of active substance required to render the cell viability of mouse melanoma cells B16-F10 less than 80%, indicates that the more toxic the active substance is to human cells and that more careful use should be made. As can be seen from FIGS. 4 to 6, 4-butylresorcinol at a concentration of less than 1. mu. mol/L was substantially non-toxic to mouse melanoma cells B16-F10 and had a cell viability of greater than 80%, and at a concentration of 2.5. mu. mol/L, began to exert a toxic effect on mouse melanoma cells B16-F10; 5 mu mol/L-40 mu mol/L resveratrol has no toxicity to mouse melanoma cells B16-F10, and when the concentration reaches 50 mu mol/L, resveratrol starts to produce toxic action to mouse melanoma cells B16-F10; 1 mmol/L-15 mmol/L of ascorbic acid ethyl ether has no toxicity to mouse melanoma cells B16-F10, and starts to produce toxic effect on mouse melanoma cells B16-F10 when the concentration reaches 30 mmol/L; it can be seen that the cytotoxicity is, in order from strong to weak: 4-butyl resorcinol, resveratrol and ascorbic acid ethyl ether, and therefore, the cytotoxicity result of the whitening active substance provided by the invention is consistent with the variation trend of the highest dosage of the whitening active substance specified in the catalogue of used cosmetic raw materials (2021 edition).
By comparing the results of the tyrosinase inhibition ability and cytotoxicity test of 4-butylresorcinol, resveratrol and ascorbic acid ethyl ether (table 1), it can be seen that the concentration of the 4-butylresorcinol, resveratrol and ascorbic acid ethyl ether is low, the whitening efficiency is high, and simultaneously the EC is low30The difference between the concentration and the cytotoxicity concentration is more than 5 times, so that the flexible regulation of the 4-butyl resorcinol, the resveratrol and the ascorbic acid ethyl ether in the cosmetic formula is facilitated.
TABLE 1 EC of three substances on tyrosinase30And results of cytotoxicity test
Active substance EC30 Cytotoxicity
4-butylresorcinol 0.35μmol/L 2.5μmol/L
Resveratrol 10μmol/L 50μmol/L
Ascorbic acid ethyl ether 2mmol/L 30mmol/L
Example 24 synergistic Effect of three whitening actives butyl Resorcinol, resveratrol and ascorbic acid Ethyl Ether
The whitening active substances 4-butylresorcinol, resveratrol and ascorbic acid ethyl ether are compounded to investigate whether the three whitening active substances have a synergistic effect, the compound composition condition is shown in table 2, and the EC of each whitening active substance is determined30The test result designs the use concentration of each whitening active substance, and the maximum concentration of the whitening active substance does not exceed the cytotoxic concentration of the whitening active substance.
Table 2 combination table for compounding three kinds of whitening active substances
Figure BDA0003308900890000071
By observing the synergistic interaction among the whitening active substances (4-butyl resorcinol, resveratrol and ascorbic acid ethyl ether), compounding the 4-butyl resorcinol, the resveratrol and the ascorbic acid ethyl ether at different concentrations, and detecting the inhibition effect of the compounded composition on the tyrosinase activity, wherein the inhibition effect of the compounded composition on the tyrosinase activity is in negative correlation with the color of a reaction system (the volume ratio of the compounded composition to the tyrosine to the tyrosinase is 2: 5: 3), namely, the darker the color is, the poorer the inhibition effect of the compounded composition on the tyrosinase activity is. By measuring the intensity of the characteristic absorption of melanin at 475nm (Abs)475nm) Characterization of the inhibitory Effect on tyrosinase Activity, wherein Abs contains only tyrosine and tyrosinase475nmIs 0.427.
By aiming at three beauty foodsThe white active substances are compounded, the inhibition effect of the compound composition of the three whitening active substances on the tyrosinase activity is obviously better than that of the compound composition of one or two active substances (table 2), and especially, the inhibition effect of the compound composition of the number 13 on the tyrosinase activity (Abs)475nm0.426 reduction) is obviously better than the sum of the inhibition effect (Abs) of the compound composition containing only 4-butylresorcinol and resveratrol (number 8) and the compound composition containing only ascorbyl ethyl ether (number 5) on the tyrosinase activity475nm0.419 reduction (0.419 ═ 0.427-0.058+ 0.427-0.377)); inhibitory Effect of combination composition No. 14 on tyrosinase Activity (Abs)475nm0.426 reduction) is obviously better than the sum of the inhibition effect of the compound composition (number 7) only containing the 4-butyl resorcinol and the resveratrol and the compound composition (number 5) only containing the ascorbyl ethyl ether on the tyrosinase activity (Abs)475nm0.40 reduction (0.40 ═ 0.427-0.077+ 0.427-0.377)); inhibitory Effect of combination composition No. 15 on tyrosinase Activity (Abs)475nm0.417 reduction) is obviously better than the sum of the inhibition effect of the compound composition (number 7) only containing the 4-butyl resorcinol and the resveratrol and the compound composition (number 5) only containing the ascorbyl ethyl ether on the tyrosinase activity (Abs)475nmA reduction of 0.40 (0.40-0.427-0.077 +0.427-0.377)), it can be seen that the three whitening actives in the combination compositions numbered 13, 14 and 15 produce a synergistic effect; meanwhile, the inhibition effect of the compound composition (Abs) with the number of 13-18 on the tyrosinase activity475nmMinimum reduction of 0.417) is obviously better than the compound composition with the number of 7-12, 4-butyl resorcinol, resveratrol and ascorbic acid ethyl ether (Abs)475nmThe highest reduction is 0.409), further showing that the compound composition with the number of 13-18 has a remarkable synergistic effect.
The color of the reaction system of the compound composition is observed, the result is shown in fig. 7, the color of the reaction system of the single whitening active substance and the reaction system of the compound composition compounded in pairs is obviously darker, while the color of the reaction system of the compound composition of the three whitening active substances is lighter and almost colorless and visible, and the compound composition compounded by the three whitening active substances can effectively inhibit the activity of tyrosinase and has better whitening effect.
Example 3
A whitening composition with a synergistic effect comprises the following components in parts by weight: 1g of 4-butyl resorcinol, 4g of resveratrol, 10g of ascorbic acid ethyl ether, 68g of 1, 3-butanediol and 17g of water.
The preparation method of the whitening composition with the synergistic effect comprises the following steps:
dissolving 4-butylresorcinol and resveratrol completely with 1, 3-butanediol, adding ascorbic acid ethyl ether, stirring, adding water, stirring to dissolve all components completely to obtain whitening composition with synergistic effect.
Example 4
A whitening composition with a synergistic effect comprises the following components in parts by weight: 0.5g of 4-butyl resorcinol, 3g of resveratrol, 25g of ascorbic acid ethyl ether, 56g of 1, 3-butanediol and 15.5g of water.
The preparation method of the whitening composition with the synergistic effect comprises the following steps:
dissolving 4-butylresorcinol and resveratrol completely with 1, 3-butanediol, adding ascorbic acid ethyl ether, stirring, adding water, stirring to dissolve all components completely to obtain whitening composition with synergistic effect.
Example 5
A whitening composition with a synergistic effect comprises the following components in parts by weight: 2g of 4-butyl resorcinol, 12g of resveratrol, 20g of ascorbic acid ethyl ether, 56g of 1, 3-butanediol and 10g of water.
The preparation method of the whitening composition with the synergistic effect comprises the following steps:
dissolving 4-butylresorcinol and resveratrol completely with 1, 3-butanediol, adding ascorbic acid ethyl ether, stirring, adding water, stirring to dissolve all components completely to obtain whitening composition with synergistic effect.
Example 6
A whitening composition with a synergistic effect comprises the following components in parts by weight: 3g of 4-butyl resorcinol, 3g of resveratrol, 5g of ascorbic acid ethyl ether, 80g of 1, 3-butanediol and 9g of water.
The preparation method of the whitening composition with the synergistic effect comprises the following steps:
dissolving 4-butylresorcinol and resveratrol completely with 1, 3-butanediol, adding ascorbic acid ethyl ether, stirring, adding water, stirring to dissolve all components completely to obtain whitening composition with synergistic effect.
Comparative examples 1 to 7
The whitening compositions of comparative examples 1 to 7 have the components shown in table 3.
Table 3 ingredient table of whitening composition
Figure BDA0003308900890000091
Figure BDA0003308900890000101
Application examples
The whitening composition of example 3 and comparative examples 1 to 7 was used to prepare a whitening cream, the formula of which is shown in table 4, wherein the ingredients except 4-butylresorcinol, resveratrol and ascorbyl ethyl ether all have no whitening effect. According to the whitening test results of molecular level and cell level and the record of the highest dosage of active matters provided in the catalogue of used cosmetic raw materials (2021 edition), the highest content of each whitening active matter in the whitening cream prepared by the invention is 5 times lower than the record of the highest dosage, namely 4-butyl resorcinol is less than or equal to 0.4 wt%, and resveratrol is less than or equal to 1.0 wt%.
TABLE 4 whitening cream formula
Figure BDA0003308900890000102
Note: "whitening composition" is the whitening composition described in example 3 and comparative examples 1 to 7.
The preparation method of the whitening cream comprises the following steps:
preparation of an aqueous phase: mixing the components of the phase A, dissolving the components completely in a water bath at 85 ℃ and keeping the temperature constant to obtain a water phase;
preparing an oil phase: melting the components of phase B in water bath at 85 deg.C, stirring, and maintaining constant temperature to obtain oil phase;
mixing: adding the water phase into the oil phase, stirring uniformly, cooling to 45 ℃, adding the phase C, and stirring uniformly; and (3) cooling to below 40 ℃, adding the whitening composition, and uniformly stirring to obtain the whitening cream (the No. 1-8 whitening cream is prepared by respectively adding the whitening compositions in the embodiment 3 and the comparative examples 1-7).
Effects of the embodiment
1. Evaluation method for skin whitening effect of human body
Selecting 32 female volunteers with the ages of 30-50, keeping the skin healthy, having no dermatosis and allergy history, and carrying out an effect test; and (3) testing conditions are as follows: at the room temperature of 24 +/-2 ℃ and the relative humidity of 50 +/-5%, the volunteers sit still for 30min and then test related data, and the test results are averaged. The experimental process comprises the following steps: dividing volunteers into 4 groups at random, wherein each group comprises 8 persons, the first group is coated with No. 1 whitening cream at the inner side of the left arm, and the right arm is coated with No. 2 whitening cream at the same position; the second group is coated with 3# whitening cream at the inner side of the left arm, and is coated with 4# whitening cream at the same position of the right arm; the third group is coated with No. 5 whitening cream at the inner side of the left arm, and is coated with No. 6 whitening cream at the same position of the right arm; the fourth group is coated with 7# whitening cream at the inner side of the left arm, and is coated with 8# whitening cream at the same position of the right arm; the composition is applied twice a day, once in the morning and evening, and applied and then moderately massaged for 56 days, during which melanin content (German CK company MPA10-MX18), skin color brightness (German CK company MPA10-CL400), and skin elasticity (German CK company MPA 580-Cutomer) are tested on the applied position of arm of volunteer every two weeks.
The test was carried out by applying the melanin content, the skin tone and the skin elasticity to the inner arm position of the volunteer (test method refer to the instrument description), whichThe corresponding evaluation indexes are respectively as follows: a melanin change value (Δ M), a skin color lightness change value (Δ L), a skin elasticity change value (Δ R2); the calculation formulas of the melanin change value (Δ M), the skin color lightness change value (Δ L), and the skin elasticity change value (Δ R2) are as follows: Δ M ═ M0-M56,ΔL=L56-L0,ΔR2=R2(56)-R2(0)Wherein M is0Is the initial melanin measurement, M56Measured as melanin after 56 days, L56Measured as skin tone brightness after 56 days, L0Is an initial skin tone luminance measurement; r2(56)Is a skin elasticity measurement after 56 days, R2(0)Is the initial skin elasticity measurement. The skin melanin values show the most intuitive skin whitening effect, as shown in fig. 8, the whitening cream (1#) prepared by three whitening active substances of 4-butyl resorcinol, resveratrol and ascorbic acid ethyl ether can effectively reduce the melanin in the skin, and the reduction effect is obviously better than that of the whitening cream containing only one or two whitening active substances, so that the whitening effect can be effectively improved by adding the 4-butyl resorcinol, the resveratrol and the ascorbic acid ethyl ether into the whitening cream. The skin color brightness can endow the skin with the characteristic of shining people, the skin color brightness is increased while the skin whiteness is improved, the whitening cream is one of the characteristics of health whitening, and the whitening cream (1#) prepared by three whitening active substances of 4-butyl resorcinol, resveratrol and ascorbic acid ethyl ether has a good effect on improving the skin color and can obviously improve the skin color brightness (figure 9). Healthy skin should also have better elasticity, so that the whitening product has a "touch" effect, as shown in fig. 10, the 1# whitening cream has certain capability of enhancing skin elasticity.
In conclusion, the whitening composition compounded by adding the three whitening active substances, namely 4-butylresorcinol, resveratrol and ascorbyl ethyl ether, into the whitening cream can improve the whiteness, brightness and elasticity of skin at the same time, and compared with the whitening composition compounded by adding one or two whitening active substances, the whitening composition compounded by using the three whitening active substances has a better whitening effect.
2. Comparison with commercially available whitening cream
The whitening cream used in this experiment was 1# whitening cream prepared in the application examples, and commercially available whitening cream was a marume white love pure white spot-fading night cream (Guangdong marume Biotechnology Co., Ltd.). The experimental process comprises the following steps: selecting 8 female volunteers with the ages of 30-50, keeping the skin healthy, having no dermatosis and allergy history, and carrying out an effect test; a No. 1 whitening cream is smeared at the inner side fixed position of the left arm of a volunteer, a commercially available whitening cream is smeared at the same position of the right arm of the volunteer, the cream is used twice a day, once in the morning and evening, moderate massage is carried out after smearing, the cream is continuously used for 56 days, and the smearing position of the volunteer is tested for melanin content, skin color brightness and skin elasticity every two weeks.
The results are shown in table 5, and the effect of the # 1 whitening cream on reducing melanin and improving skin color brightness is obviously better than that of the commercially available whitening cream; the No. 1 whitening cream and the commercially available whitening cream have no obvious difference in improving the skin elasticity, so that the No. 1 whitening cream can effectively inhibit the activity of tyrosinase, reduce the generation of melanin in the skin, reduce the existing melanin in the horny layer of the skin, improve the whiteness and brightness of the skin and enhance the skin elasticity to a certain extent.
TABLE 5 comparison of whitening cream results
Index (I) Whitening cream 1# Commercially available product
ΔM 20.1 13.8
ΔL 1.3 0.7
ΔR2 0.137 0.145
The embodiments of the present invention have been described in detail with reference to the accompanying drawings, but the present invention is not limited to the above embodiments, and various changes can be made within the knowledge of those skilled in the art without departing from the gist of the present invention. Furthermore, the embodiments of the present invention and the features of the embodiments may be combined with each other without conflict.

Claims (10)

1. The whitening composition is characterized by comprising the following components in parts by weight: 0.5-3 parts of 4-butyl resorcinol, 3-12 parts of resveratrol and 5-25 parts of ascorbic acid ethyl ether.
2. The whitening composition of claim 1, comprising the following components in parts by weight: 0.5-2 parts of 4-butyl resorcinol, 4-12 parts of resveratrol and 5-20 parts of ascorbic acid ethyl ether.
3. The whitening composition of claim 2, comprising the following components in parts by weight: 1-2 parts of 4-butyl resorcinol, 4-8 parts of resveratrol and 5-10 parts of ascorbic acid ethyl ether.
4. The whitening composition of any one of claims 1 to 3, further comprising 56 to 80 parts of an alcohol.
5. A method of preparing the whitening composition of claim 4, comprising the steps of: mixing 4-butylresorcinol, resveratrol, ascorbic acid ethyl ether, alcohols and water to obtain the whitening composition.
6. Use of the whitening composition of any one of claims 1 to 4 in the preparation of a product.
7. Use according to claim 6, wherein the product is used for:
(1) inhibiting tyrosinase activity, and/or
(2) Reduce melanin.
8. A cosmetic comprising the whitening composition of any one of claims 1 to 4;
preferably, the whitening composition accounts for 3-10% of the cosmetic by mass.
9. A whitening cream comprising the whitening composition of any one of claims 1 to 4 and a cosmetically acceptable adjuvant.
10. The whitening cream as recited in claim 9, wherein the content of 4-butyl resorcinol in the whitening cream is 0.04-0.2% by mass;
preferably, the mass percentage content of the resveratrol in the whitening cream is 0.2-0.9%;
preferably, the content of the ascorbic acid ethyl ether in the whitening cream is 0.5-3% by mass.
CN202111211140.XA 2021-10-18 2021-10-18 Whitening composition with synergistic effect and application thereof Pending CN114042001A (en)

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CN115501151A (en) * 2022-10-10 2022-12-23 广东工业大学 Tearable potato soft mask powder with whitening effect and preparation method thereof
WO2023191610A1 (en) * 2022-03-31 2023-10-05 Winnox Cosmeceutics Sdn. Bhd. Composition and method for treating skin pigmentation disorders

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CN111743851A (en) * 2020-07-09 2020-10-09 广州市胜梅化妆品有限公司 Whitening and spot-fading composition and application thereof
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WO2023191610A1 (en) * 2022-03-31 2023-10-05 Winnox Cosmeceutics Sdn. Bhd. Composition and method for treating skin pigmentation disorders
CN115501151A (en) * 2022-10-10 2022-12-23 广东工业大学 Tearable potato soft mask powder with whitening effect and preparation method thereof
CN115501151B (en) * 2022-10-10 2024-01-16 广东工业大学 Tear-off potato soft film powder with whitening effect and preparation method thereof

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Application publication date: 20220215