Stable composition capable of whitening skin and removing yellow smell as well as preparation method, cosmetic and application of stable composition

Abstract

The invention provides a whitening and yellow-smell-removing stable composition and a preparation method thereof, cosmetics and application, and belongs to the technical field of cosmetics, and the whitening and yellow-smell-removing stable composition is composed of a resorcinol derivative, ethyl ascorbic acid, bakuchiol and a solvent. Through in-vitro tyrosinase activity determination and stability test determination, the three components have a synergistic effect on inhibition of tyrosinase activity, and the dosage of the whitening agent can be reduced on the premise of achieving the same whitening effect, so that the irritation risk of the high-concentration whitening agent is reduced, and the whitening effect is improved. The color stability of the composition of the resorcinol derivative and the ethyl ascorbic acid is improved, the problem of discoloration of the product is solved, and unnecessary stabilizers are prevented from being additionally added in a cosmetic formula. The whitening and yellow smell removing composition is used for cosmetics, can reduce the skin yellowing condition, and has the effect of removing yellow smell.

Description

Technical Field

[0001] The present invention relates to the technical field of cosmetics, and in particular to a whitening and yellowing-removing stable composition, a preparation method thereof, cosmetics and applications thereof. Background Art

[0002] Ideal skin is characterized by a smooth, delicate surface, uniform color, and the absence of noticeable surface blemishes. However, due to factors such as UV radiation, environmental pollutants, and unhealthy lifestyle habits (such as irregular sleep and rest), skin often experiences increased pigmentation, leading to a dull complexion and even the formation of dark spots and other undesirable conditions.

[0003] Melanin is a protein found in the basal layer of everyone's skin. Ultraviolet radiation triggers a series of stress changes within the skin, sending signals to melanocytes within the skin, triggering the production of melanin. Tyrosinase, in turn, converts dopa into dopaquinone and melanosomes, which are then transported along the dendrites of the melanocytes to the surrounding keratinocytes. Melanin then migrates through layers of cellular metabolism to the epidermis, causing skin problems such as darkening and uneven skin tone. Melanin production in the skin is fundamentally a process in which tyrosine in the skin is gradually oxidized by tyrosinase to form melanin. Melanin is the most significant factor affecting skin fairness, and inhibiting melanin production is crucial for whitening products.

[0004] The vast majority of commercially available whitening agents work by inhibiting melanin production, with tyrosinase inhibition being a key development target. Currently, whitening ingredients that have dominated the market include resorcinol and its derivatives, ascorbic acid and its derivatives, and others.

[0005] The whitening active ingredients added to existing whitening skin care products are single, and the whitening effect of a single whitening ingredient is poor. Resorcinol and its derivatives, ascorbic acid and its derivatives as whitening agents all have a certain inhibitory effect on tyrosinase, but there are the following problems: First, they are prone to oxidative discoloration and are easily degraded or reacted by light, temperature and the external environment, producing colored products, causing the product to change color during storage, and ultimately causing the skin care product to lose its activity, giving the product a loss of sensory pleasure in appearance and use, thus limiting its application in cosmetics; second, the concentration of these whitening agents decreases after permeation through the skin, and the amount added needs to be higher than the effective concentration, but high concentrations of whitening agents are prone to cause skin irritation on the skin surface. The existing technology uses a combination of multiple whitening agents to reduce the amount of single whitening agent added, but does not fundamentally solve the problem; third, the existing whitening agent combination is usually just a simple addition of efficacy, lacking a synergistic effect.

[0006] Therefore, there is a need for a stable and efficient whitening stable composition that can more effectively inhibit tyrosinase, reduce melanin production, and have a stable appearance. Summary of the Invention

[0007] In view of the deficiencies in the prior art, the present invention discloses a whitening and yellowing-removing stable composition, a preparation method thereof, a cosmetic and applications thereof.

[0008] In one aspect, the present invention provides a whitening and yellowing-removing stabilizing composition, which is composed of a resorcinol derivative, ethyl ascorbic acid, bakuchiol, and a solvent.

[0009] Resorcinol derivatives and ethyl ascorbic acid are both known whitening agents in cosmetics. Their combination has been shown to inhibit tyrosinase activity. However, their current application in cosmetics is limited by their instability. Resorcinols are easily oxidized in water to quinones, resulting in a reddish-brown color. This can lead to discoloration during storage and a decrease in the content of whitening active ingredients, compromising the product's appearance and aesthetic appeal. Ascorbic acid is also susceptible to discoloration. Its chemical structure is relatively unstable and susceptible to changes in light, heat, oxygen, and other factors. This instability is a key factor contributing to its oxidative discoloration. Combining resorcinol derivatives with ethyl ascorbic acid exacerbates color instability in the cosmetic composition, causing the color to shift from red to deep red, resulting in discoloration. Therefore, maintaining color stability in cosmetic compositions containing resorcinol derivatives and ethyl ascorbic acid is challenging.

[0010] The research and development team of the present invention unexpectedly discovered that by adding bakuchiol to the composition of resorcinol derivatives and ethyl ascorbic acid, after in vitro tyrosinase activity assay and stability test, the three not only play a synergistic role in inhibiting tyrosinase activity, but also can reduce the dosage of whitening agent while achieving the same whitening effect, thereby reducing the irritation risk of high-concentration whitening agents, and improve the color stability of the composition containing resorcinol derivatives and ethyl ascorbic acid, solving the problem of product discoloration and avoiding the addition of unnecessary stabilizers in cosmetic formulas.

[0011] The stability of the combination of resorcinol derivatives, ethyl ascorbic acid, and bakuchiol stems from the fact that resorcinol derivatives, due to their p-π conjugated structure, have a high electron cloud density and are easily oxidized to meta-benzoquinone structures, causing discoloration. Ethyl ascorbic acid may form a complex with meta-benzoquinone through intermolecular hydrogen bonding, leading to a darker color. Furthermore, when ethyl ascorbic acid is oxidized, it easily produces peroxides, which also accelerate the oxidative discoloration of the resorcinol derivatives. The research and development team speculates that the unique structure of bakuchiol provides electrons through the dissociation of the phenolic hydroxyl group, preventing the conversion of resorcinol derivatives to quinone structures, thereby improving stability.

[0012] Furthermore, the whitening and yellowing-removing stable composition comprises, by weight percentage, 0.1-10% resorcinol derivative, 0.2-50% ethyl ascorbic acid, 0.1-20% bakuchiol, and the remainder solvent. If the ratio of the composition falls below the lower limit, the whitening effect may not be achieved. If it exceeds the upper limit, it may cause skin irritation, reduce stability, and increase product costs.

[0013] Furthermore, the whitening and yellowing-removing stabilizing composition comprises, by weight percentage, 1 to 10% of a resorcinol derivative, 1 to 10% of ethyl ascorbic acid, 2 to 10% of bakuchiol, and the remainder being a solvent.

[0014] Exemplarily, the whitening and yellowing stabilizing composition consists of 5% resorcinol derivatives, 5% ethyl ascorbic acid, 5% bakuchiol and 85% solvent, or 2.5% resorcinol derivatives, 2.5% ethyl ascorbic acid, 5% bakuchiol and 90% solvent, or 4% resorcinol derivatives, 4% ethyl ascorbic acid, 2% bakuchiol and 90% solvent; or 1% resorcinol derivatives, 1% ethyl ascorbic acid, 3% bakuchiol and 95% solvent.

[0015] Furthermore, the resorcinol derivative includes one or more of 4-hexylresorcinol, phenethylresorcinol, dimethoxytolyl-4-propylresorcinol, and 4-butylresorcinol, preferably 4-hexylresorcinol. The embodiments of the present invention provide relevant components of the composition.

[0016] Furthermore, the ethyl ascorbic acid is one or both of 3-O-ethyl ascorbic acid and 2-O-ethyl ascorbic acid, preferably 3-O-ethyl ascorbic acid. The embodiments of the present invention provide relevant components of the composition.

[0017] Furthermore, the solvent includes one or more of 1,3-butanediol, 1,3-propylene glycol, propylene glycol, 1,2-pentanediol, ethanol, and water.

[0018] In another aspect, the present invention also provides a method for preparing a whitening and yellowing-removing stable composition. The components of the composition are mixed in a solvent in appropriate proportions and stirred evenly to obtain the whitening and yellowing-removing stable composition. The stirring speed is 50 to 100 rpm and the temperature is room temperature (20 to 25°C). This method is simple, easy to operate, and suitable for large-scale production.

[0019] For example, at room temperature, 5 g of 4-hexylresorcinol, 5 g of 3-O-ethyl ascorbic acid, and 5 g of bakuchiol were mixed, and the remainder was added with 85 g of ethanol and water (the mass ratio of ethanol to water was 35:65), and stirred evenly at a stirring speed of 50 rpm to obtain a whitening and yellowing-removing stable composition.

[0020] For example, at room temperature, 2.5 g of 4-hexylresorcinol, 2.5 g of 3-O-ethyl ascorbic acid, and 2.5 g of bakuchiol are mixed, and the remainder is added with 92.5 g of ethanol and water (the mass ratio of ethanol to water is 35:65), and stirred evenly at a stirring speed of 75 rpm to obtain a whitening and yellowing-removing stable composition.

[0021] On the other hand, the present invention also provides an application of a whitening and yellowing-removing stable composition in the preparation of anti-aging cosmetics. The amount of the whitening and yellowing-removing stable composition in the cosmetics is 0.01 to 10%.

[0022] On the other hand, the present invention also provides a cosmetic product comprising a whitening and yellowing-removing stable composition. The composition of a resorcinol derivative, ethyl ascorbic acid, and bakuchiol used in cosmetics can also reduce skin yellowing and have a yellowing-removing effect.

[0023] The cosmetic comprises, by weight percentage, 0.01-10% of a whitening and yellowing-removing stabilizing composition, 0-20% of a moisturizing agent, 0-1% of a thickening agent, 0-10% of an emulsifier, 0-20% of a moisturizing agent, 0-0.1% of a chelating agent, 0-1% of a preservative, 0-0.2% of a pH regulator, and the balance being water.

[0024] The moisturizing agents include glycerin, dipropylene glycol, betaine, glyceryl glucoside, methyl gluceth-20, glycereth-26, trehalose, sucrose, mannitol, rhamnose, xylitol, urea, polyethylene glycol-8, polyethylene glycol-32, methyl gluceth-10, PEG / PPG-17 / 6 copolymer, sodium polyglutamate, budding pullulan polysaccharide, tremella polysaccharide, sodium polyglutamate, PPG-10 methyl glucose ether, panthenol and PPG-20 methyl glucose ether.

[0025] The thickeners include carbomer, xanthan gum, hydroxyethyl cellulose, hydroxypropyl cellulose, Sphingomonas fermentation product extract, acrylic acid (esters) / C10-30 alkyl acrylate crosspolymer, ammonium acryloyldimethyltaurate / VP copolymer, sodium polyacryloyldimethyltaurate, sodium polyacrylate grafted starch, acrylates, glucomannan, sclerotium gum, crispus extract, sodium polyacrylate, etc.

[0026] The emulsifiers include PEG-100 stearate, glyceryl stearate, cetearyl olivate, sorbitan olivate, sorbitan oleate, glyceryl stearate citrate, cetyl potassium phosphate, sodium stearoyl glutamate, cetearyl glucoside, bis-PEG / PPG-20 / 5PEG / PPG-20 / 5 dimethicone, methoxy PEG / PPG-25 / 4 dimethicone, C14-22 alcohol, C12-20 alkyl glucoside, steareth-2, steareth-21, sorbitan stearate, polysorbate-20, polysorbate-60, polysorbate-80, trideceth-6, stearyl alcohol, cetyl alcohol, myristyl alcohol, arachidyl alcohol, behenyl alcohol, and the like.

[0027] The emollients include stearic acid, squalane, squalene, jojoba seed oil, coconut oil-caprylate / caprate, shea butter, hydrogenated coconut glycerides, white meadowfoam seed oil, baobab seed oil, phytosteryl oleate, camellia seed oil, olive fruit oil, egg yolk oil, myristyl myristate, caprylic / capric triglyceride, hydrogenated polyisobutene, hydrogenated polydecene, isohexadecane, octyldodecanol, isononyl isononanoate, butylene glycol dicaprylate / dicaprate, isopropyl palmitate, isooctyl palmitate, isopropyl palmitate, ethylhexylglycerin, C18-21 alkane, C11-13 isoparaffin, bis-diglyceryl polyacyl adipate-2, mineral oil, petrolatum, dimethicone, cyclopentasiloxane, cyclohexasiloxane, dimethiconol, dimethicone crosspolymer, and the like.

[0028] The chelating agent is disodium EDTA, ethylenediamine disuccinic acid (EDDS), pentasodium diethylenetriamine pentaacetic acid, etc.

[0029] The preservatives are phenoxyethanol, benzyl alcohol, phenylethyl alcohol, methylparaben, propylparaben, benzyl alcohol, phenylethyl alcohol, potassium sorbate, sodium benzoate, chlorphenesin, 1,2-hexanediol, caprylyl glycol and p-hydroxyacetophenone.

[0030] The pH regulator is sodium hydroxide, potassium hydroxide, citric acid and citrate / citric acid buffer, which can be used to adjust the pH of the whitening and yellowing-removing stable composition of the present invention to 5-8, preferably 5-6.

[0031] Furthermore, the cosmetics include any one of lotion, essence, emulsion, cream, spray, eye cream, mask, gel, BB cream, sunscreen, and cleanser. The cosmetics of the whitening and yellowing-removing stable composition of the present invention are suitable for multiple scenarios and multiple dosage forms.

[0032] Compared with the prior art, the present invention has the following beneficial effects:

[0033] 1. The present invention provides a whitening and yellowing-removing stable composition, which is composed of a resorcinol derivative, ethyl ascorbic acid, bakuchiol and a solvent. The whitening and yellowing-removing stable composition can play a synergistic and additive role in inhibiting tyrosinase activity and has a whitening effect; and the whitening and yellowing-removing stable composition has good stability and is not easy to change color.

[0034] 2. The present invention provides a method for preparing a whitening and yellowing-removing stable composition, which has a simple preparation process, is easy to operate, and is suitable for large-scale production.

[0035] 3. The present invention provides an application of a whitening and yellowing-removing stable composition in the preparation of cosmetics. The prepared cosmetics have good stability while having whitening and yellowing-removing effects and are not easy to change color in appearance.

[0036] 4. The present invention provides a cosmetic with a whitening and yellowing-removing stable composition, which is suitable for use in cosmetics in multiple scenarios and multiple dosage forms, and can be easily added to various toiletries, creams, and lotions. BRIEF DESCRIPTION OF THE DRAWINGS

[0037] The accompanying drawings, which constitute part of this application, are intended to provide a further understanding of the present invention. The exemplary embodiments of the present invention and their descriptions are intended to explain the present invention and do not constitute an undue limitation of the present invention. In the accompanying drawings:

[0038] Figure 1 A graph showing the comparative results of stability tests of the whitening and yellowing-removing stable composition 1 of the present invention and the control group 1;

[0039] Figure 2 A graph showing the comparative results of stability tests of cosmetic application example 1 of the present invention and cosmetic comparative example 1 is shown;

[0040] Figure 3 A diagram showing the human efficacy test of application example 1 of the cosmetics of the present invention;

[0041] Figure 4 A diagram showing the human efficacy test of Comparative Example 2 of the cosmetics of the present invention is shown. DETAILED DESCRIPTION

[0042] The following is a clear and complete description of the technical solutions in the embodiments of the present invention. Obviously, the embodiments described are only part of the embodiments of the present invention, not all of them. All other embodiments derived by persons of ordinary skill in the art based on the embodiments of the present invention without creative effort are within the scope of protection of the present invention.

[0043] To facilitate understanding of the present invention, the present invention will be described in more detail below, with preferred embodiments of the present invention provided. However, it should be understood that these embodiments are provided for further explanation only and are not intended to limit the present invention in any manner, i.e., they do not limit the scope of protection of the present invention.

[0044] "Comprising" or "including" is intended to indicate that compositions (e.g., media) and methods include the recited elements, but do not exclude other elements. When used to define compositions and methods, "consisting essentially of" means excluding other elements that have any significance for the combination for the stated purpose. Thus, a composition consisting essentially of the elements defined herein does not exclude other materials or steps that do not materially affect the basic and novel characteristics of the claimed application. "Consisting of" means excluding trace elements and substantial method steps of other components. Embodiments defined by each of these transition terms are within the scope of this application.

[0045] Unless otherwise specified, the raw materials and equipment used in this application are all commonly used in the art and are commercially available. Unless otherwise specified, the methods used in this application are all conventional methods in the art.

[0046] 4-Hexylresorcinol

[0047] The whitening and yellowing-removing stabilizing composition of the present invention comprises 4-hexylresorcinol.

[0048] The molecular structure of 4-hexylresorcinol is as follows:

[0049]

[0050] 4-Hexylresorcinol can be used without particular limitation as long as it is 4-hexylresorcinol commonly used in cosmetics.

[0051] As 4-hexylresorcinol, a commercially available product can be used.

[0052] 3-O-ethyl ascorbic acid

[0053] The whitening and yellowing-removing stabilizing composition of the present invention comprises 3-O-ethyl ascorbic acid.

[0054] The molecular structure of 3-O-ethyl ascorbic acid is as follows:

[0055]

[0056] 3-O-ethyl ascorbic acid can be used without particular limitation as long as it is 3-O-ethyl ascorbic acid commonly used in cosmetics.

[0057] As 3-O-ethylascorbic acid, a commercially available product can be used.

[0058] Bakuchiol

[0059] The whitening and yellowing-removing stable composition of the present invention comprises bakuchiol.

[0060] The molecular structure of bakuchiol is as follows:

[0061]

[0062] Bakuchiol is a monoterpenoid compound extracted, purified, and isolated from the seeds of the natural leguminous plant Psoralea corylifolia. Existing research suggests that bakuchiol can inhibit the expression of metalloproteinases, promote cell proliferation, and stimulate collagen production, thereby playing a role in skin anti-aging. However, bakuchiol has not been shown to have a synergistic whitening effect.

[0063] Bakuchiol can be used without particular limitation as long as it is bakuchiol commonly used in cosmetics.

[0064] As bakuchiol, a commercial product may be used, or it may be prepared at home.

[0065] Example 1 Preparation of a whitening and yellowing-removing stable composition

[0066] Whitening and yellowing stabilizing composition 1

[0067] 5 g of 4-hexylresorcinol, 5 g of 3-O-ethyl ascorbic acid, and 5 g of bakuchiol were mixed, and the remainder was added with 85 g of ethanol and water (the mass ratio of ethanol to water was 35:65), and stirred evenly to obtain a whitening and yellowing-removing stable composition 1.

[0068] Whitening and yellowing stabilizing composition 2

[0069] 2.5 g of 4-hexylresorcinol, 2.5 g of 3-O-ethyl ascorbic acid, and 5 g of bakuchiol were mixed, and the remainder was added with 90 g of ethanol and water (the mass ratio of ethanol to water was 35:65), and stirred evenly to obtain a whitening and yellowing-removing stable composition 2.

[0070] Whitening and yellowing stabilizing composition 3

[0071] 4 g of 4-hexylresorcinol, 4 g of 3-O-ethyl ascorbic acid, and 2 g of bakuchiol were mixed, and the remainder was added with 90 g of ethanol and water (the mass ratio of ethanol to water was 35:65), and stirred evenly to obtain a whitening and yellowing-removing stable composition 3.

[0072] Whitening and yellowing stabilizing composition 4

[0073] 10 g of 4-hexylresorcinol, 10 g of 3-O-ethyl ascorbic acid, and 10 g of bakuchiol were mixed, and 70 g of 1,3-butanediol was added to the remainder, and the mixture was stirred evenly to obtain a whitening and yellowing-removing stable composition 4.

[0074] Whitening and yellowing stabilizing composition 5

[0075] 3 g of 4-hexylresorcinol, 5 g of 3-O-ethyl ascorbic acid, and 5 g of bakuchiol were mixed, and 87 g of 1,3-butanediol was added to the remainder, and the mixture was stirred evenly to obtain a whitening and yellowing-removing stable composition 5.

[0076] Whitening and yellowing stabilizing composition 6

[0077] 1 g of 4-hexylresorcinol, 1 g of 3-O-ethyl ascorbic acid, and 3 g of bakuchiol were mixed, and 96 g of 1,3-butanediol was added to the remainder, and the mixture was stirred evenly to obtain a whitening and yellowing-removing stable composition 6.

[0078] Example 2 Preparation of control group samples

[0079] Control group 1

[0080] 5 g of 4-hexylresorcinol and 5 g of 3-O-ethylascorbic acid were mixed, and 90 g of ethanol and water (the mass ratio of ethanol to water was 35:65) were added to the remainder, and stirred evenly to obtain a control group 1 sample.

[0081] Control group 2

[0082] 10 g of 4-hexylresorcinol and 10 g of 3-O-ethylascorbic acid were mixed, and 80 g of 1,3-butanediol was added to the remainder, and the mixture was stirred evenly to obtain a control group 2 sample.

[0083] Test Example 1 In vitro tyrosinase activity assay

[0084] Experimental Group 1

[0085] The ethanol solution of the whitening and yellowing stabilizing composition 1 (the mass ratio of ethanol to water is 35:65) was first diluted 20 times with a 35% ethanol solution (the mass ratio of ethanol to water is 35:65), and then diluted 1000 times stepwise with PBS buffer to obtain experimental group 1.

[0086] Experimental Group 2

[0087] A 0.25% 4-hexylresorcinol and 3-O-ethylascorbic acid mixture (mass ratio 1:1) in ethanol (mass ratio of ethanol to water is 35:65) was serially diluted 1000-fold with PBS buffer to obtain experimental group 2.

[0088] Experimental Group 3

[0089] A 0.25% bakuchiol ethanol solution (ethanol to water mass ratio of 35:65) was diluted 1000 times with PBS buffer to obtain experimental group 3.

[0090] The experimental procedure for in vitro tyrosinase activity assay is as follows: according to the ratio in Table 1, L-dopa is used as the substrate, tyrosinase and different concentrations of test active substances (sample groups) prepared in experimental groups 1 to 3 are added, and then the assay plate is incubated at 37°C for 30 minutes. The assay is detected at a wavelength of 475 nm using a microplate reader, and PBS buffer is used as the blank group. The percentage of inhibition of tyrosinase activity is calculated.

[0091] Table 1 In vitro tyrosinase activity assay

[0092]

[0093] Among them, L-dopa is the substrate, kojic acid is the tyrosinase inhibitor, and the sample volume unit is μL;

[0094] Inhibition rate calculation formula:

[0095]

[0096] The results of in vitro tyrosinase activity assays are shown in Table 2. The tyrosinase activity test results for each group in Table 2 indicate that, compared to the blank control, the addition of the 4-hexylresorcinol and 3-O-ethylascorbic acid combination inhibited tyrosinase activity to a certain extent. Bakuchiol also exhibited a moderate inhibitory effect on tyrosinase. Under the same concentration conditions, a comparison revealed that the 4-hexylresorcinol and 3-O-ethylascorbic acid combination had similar inhibitory effects on tyrosinase as bakuchiol.

[0097] When bakuchiol was combined with 4-hexylresorcinol and 3-O-ethylascorbic acid (experimental group 1), the inhibition rate of tyrosinase activity was significantly increased compared to the blank control group. The inhibition rate of tyrosinase was increased by about 1.5 times compared to experimental group 2 (4-hexylresorcinol and 3-O-ethylascorbic acid combination). This shows that the combination of bakuchiol, 4-hexylresorcinol and 3-O-ethylascorbic acid synergistically improves the inhibition rate of tyrosinase activity.

[0098] Table 2 Tyrosinase inhibition test results of the composition

[0099]

[0100]

[0101] Test Example 2 Stability Test of Whitening and Yellowing Stable Composition

[0102] Different whitening and yellowing-removing stable compositions prepared according to Example 1 are shown in Table 3, which are used to investigate the improvement effect of bakuchiol on the stability of the compositions.

[0103] Table 3 Composition composition of stability test

[0104]

[0105] The whitening and yellowing-removing stable composition solution prepared above was subjected to stability tests at room temperature and heat resistance. The specific test conditions were as follows:

[0106] The test conditions at room temperature are: 25±1℃, constant temperature and dark, 30 days;

[0107] Heat resistance test conditions: 45±1℃, constant temperature and dark environment, 30d;

[0108] The test results are shown in Table 4 and Appendix Figure 1 As shown, the results show that the whitening and yellowing stabilizing composition containing 4-hexylresorcinol, 3-O-ethyl ascorbic acid and bakuchiol can significantly improve the color stability and improve the high-temperature discoloration of the two compounds 4-hexylresorcinol and 3-O-ethyl ascorbic acid.

[0109] When the composition contains both 4-hexylresorcinol and 3-O-ethylascorbic acid as whitening agents, they accelerate the oxidation process, causing instability in the cosmetic composition and severe discoloration at high temperatures, with the color changing to red to dark red. However, adding bakuchiol to the 4-hexylresorcinol and 3-O-ethylascorbic acid composition significantly improves color stability at high temperatures.

[0110] Therefore, the test results show that the present invention provides a stable active ingredient composition with whitening and yellowing-removing effects, and after long-term stability testing, it can still maintain color stability.

[0111] Table 4 Stability test of whitening and yellowing stable composition

[0112] sample Normal temperature test Heat resistance test Whitening and yellowing stabilizing composition 1 No significant changes were found No significant changes were found Whitening and yellowing stabilizing composition 2 No significant changes were found No significant changes were found Whitening and yellowing stabilizing composition 3 No significant changes were found No significant changes were found Whitening and yellowing stabilizing composition 4 No significant changes were found No significant changes were found Whitening and yellowing stabilizing composition 5 No significant changes were found No significant changes were found Whitening and yellowing stabilizing composition 6 No significant changes were found No significant changes were found Control group 1 No significant changes were found Severe discoloration Control group 2 No significant changes were found Severe discoloration

[0113] Example 3 Preparation of cosmetics containing a whitening and yellowing-removing stable composition

[0114] The present invention also provides a cosmetic application and preparation method thereof comprising the whitening and yellowing-removing stable composition 4 of Example 1. Since the whitening and yellowing-removing stable composition has an excellent tyrosinase inhibitory effect, the prepared cosmetic also has a whitening effect.

[0115] Cosmetic application example 1

[0116] In the cosmetic application example, the components and contents are as follows:

[0117] 3 parts of whitening and yellowing stabilizing composition 4;

[0118] 7 parts moisturizer: 5 parts glycerin, 2 parts glyceryl glucoside;

[0119] 0.4 parts thickener: 0.1 parts xanthan gum, 0.3 parts ammonium acryloyldimethyltaurate / VP copolymer (commercially available Aristoflex AVC);

[0120] 1 part emulsifier: 1 part Tween 80;

[0121] 5 parts oil-based emollients: 1 part stearic acid, 3 parts caprylic / capric triglyceride, 1 part dimethicone;

[0122] 0.9 parts of preservatives: 0.4 parts of p-hydroxyacetophenone, 0.5 parts of 1,2-hexanediol;

[0123] 0.1 part chelating agent: 0.1 part disodium EDTA;

[0124] 0.02 parts of pH regulator, the balance water to 100 parts.

[0125] Cosmetic Comparative Example 1

[0126] In the cosmetic comparative example 1, the control composition is the sample of the control group 1, that is, the bakuchiol in the whitening and yellowing stabilizing composition 4 is replaced with an equal amount of solvent, and the other components and contents of the formula are the same as those in the cosmetic application example 1.

[0127] Cosmetic Comparative Example 2

[0128] Cosmetic Comparative Example 2 does not contain the whitening and yellowing-removing stabilizing composition 4 in Cosmetic Application Example 1, and the other components and contents of the formula are the same as those in Cosmetic Application Example 1.

[0129] According to the components and contents in Table 5, an oil-in-water whitening emulsion containing the whitening and yellowing-removing stable composition was prepared.

[0130] Table 5 Composition of cosmetic ingredients containing whitening and yellowing-removing stable composition

[0131]

[0132] The specific preparation methods of the cosmetic application examples and the cosmetic comparative examples are as follows:

[0133] Step 1: Mix phase A, heat to 75-80°C, and stir until dispersed evenly without particles;

[0134] Step 2: Mix phase B, heat to 75-80°C, and stir until there are no particles;

[0135] Step 3: Quickly pump phase B into phase A, homogenize at 3000 rpm / min for 10 minutes at high temperature, keep stirring for 5 minutes, and then start cooling;

[0136] Step 4: Stir and cool the ingredients in step 3 to 40±2℃, add pre-mixed phase C and phase D, stir well, and cool.

[0137] According to some embodiments of the present invention, the prepared cosmetics include but are not limited to lotions, lotions, creams, facial masks, gels, essences, sprays, sunscreens, and BB creams. In this way, different types of cosmetics can be prepared as needed.

[0138] Test Example 3: Stability test of cosmetics containing whitening and yellowing-removing stable composition

[0139] Cosmetic Application Example 1 and Cosmetic Comparative Example 1 prepared according to Example 3 were subjected to room temperature and heat resistance stability tests. The specific test conditions were:

[0140] Normal temperature test conditions: 25±1℃, constant temperature and dark, 60 days;

[0141] Heat resistance test conditions: 45±1℃, constant temperature and dark environment, 60 days.

[0142] The test results are shown in Table 6 and Appendix Figure 2 shown.

[0143] Table 6 Product stability test

[0144]

[0145] According to Table 6 and Appendix Figure 2 As shown, compared with the cosmetic comparative example 1 containing only two ingredients, 4-hexylresorcinol and 3-O-ethylascorbic acid, the cosmetic application example 1 containing the whitening and yellowing stabilizing composition comprising 4-hexylresorcinol, 3-O-ethylascorbic acid and bakuchiol according to the present invention can significantly improve the color stability of the product under normal temperature and heat-resistant conditions, and the prepared cosmetic has excellent stability.

[0146] Test Example 4: Human Efficacy Test

[0147] The cosmetic application example 1 and the cosmetic comparative example 2 prepared according to Example 3 were subjected to human efficacy tests to evaluate whether the cosmetics had whitening, brightening and yellowing removal effects.

[0148] Test time point: D0, immediate (10 min).

[0149] Test site: inner arm, blank matrix control, before and after control test.

[0150] Subjects: A total of 3 valid subjects completed the assessment, aged 28 to 38 years old, and met the subject voluntary inclusion and exclusion criteria.

[0151] How to use: After cleaning the test area, take an appropriate amount of the product and apply it to the inside of the arm at random, and massage gently until absorbed.

[0152] The specific test steps are as follows:

[0153] 1) The subjects cleaned the forearms of both hands uniformly by wiping them clean with dry tissue paper and sat quietly in a laboratory at a temperature of 21±1°C and a relative humidity of 50±10% for 10 minutes.

[0154] 2) Select two areas of the forearm on one side of the subject at random, each area measuring 2 cm x 2 cm, with a 1 cm interval between the areas. Use the test sample and a blank control.

[0155] 3) Skin color measuring instrument CL400 is used to detect skin color: the higher the L* value, the brighter the skin; the higher the b value, the yellower the skin color.

[0156] 4) Data statistics: Compare the differences between the same parts of the subjects before and after using the samples, with the statistical method significance level p<0.05.

[0157] The test results are shown in Table 7, where the evaluation parameter change rate is the average of the change rates of three healthy subjects.

[0158] Table 7 Human efficacy evaluation results

[0159]

[0160] The results of the evaluation before and after the use of cosmetic application example 1 and cosmetic comparative example 2 by 3 healthy subjects (Table 7) and the attached Figure 3 Cosmetic application example 1 and attached Figure 4 The pictures of the typical subjects of Cosmetic Comparative Example 2 before and after using the product show that under the evaluation conditions, the human efficacy evaluation results in Table 7 show that the skin brightness and dull yellow condition are improved after use, and Cosmetic Application Example 1 is better than Cosmetic Comparative Example 2. Figure 3It can be seen that the skin is whitened after use and the skin has a significant effect of removing yellow gas. Therefore, the cosmetics prepared by the composition of the specific embodiment of the present invention have the effects of whitening and removing yellow gas after use.

[0161] In summary, the whitening and yellowing-removing stable composition of the present invention, composed of a resorcinol derivative, ethyl ascorbic acid, bakuchiol, and a solvent, can synergistically inhibit tyrosinase activity, resulting in a whitening effect. Furthermore, the whitening and yellowing-removing stable composition exhibits excellent stability and is not prone to discoloration, thus avoiding the need for unnecessary stabilizers in cosmetic formulations. The whitening and yellowing-removing stable composition of the present invention can also be used in cosmetics to reduce skin yellowing and achieve a yellowing-removing effect.

[0162] The above is only a preferred embodiment of the present invention and is not intended to limit the present invention. Any modifications, equivalent substitutions, etc. made within the spirit and principles of the present invention shall be included in the scope of protection of the present invention. For those skilled in the art, various modifications and improvements can be made without departing from the concept of the present invention, and these shall fall within the scope of protection of the present invention. Therefore, the scope of protection of the patent for this invention shall be based on the appended claims.

Claims

1. A whitening and yellowing stable composition, characterized in that: It is composed of resorcinol derivatives, ethyl ascorbic acid, bakuchiol and solvent.

2. A whitening and yellowing stable composition according to claim 1, characterized in that: The whitening and yellowing-removing stable composition comprises, by weight percentage, 0.1 to 10% of a resorcinol derivative, 0.2 to 50% of ethyl ascorbic acid, 0.1 to 20% of bakuchiol, and the remainder being a solvent.

3. A whitening and yellowing stable composition according to claim 1, characterized in that: The whitening and yellowing-removing stable composition comprises, by weight percentage, 1 to 10% of a resorcinol derivative, 1 to 10% of ethyl ascorbic acid, 2 to 10% of bakuchiol, and the remainder being a solvent.

4. A whitening and yellowing stable composition according to claim 1, characterized in that: The resorcinol derivatives include one or more of 4-hexylresorcinol, phenethylresorcinol, dimethoxytolyl-4-propylresorcinol, and 4-butylresorcinol, preferably 4-hexylresorcinol.

5. A whitening and yellowing stable composition according to claim 1, characterized in that: The ethyl ascorbic acid is one or both of 3-O-ethyl ascorbic acid and 2-O-ethyl ascorbic acid, preferably 3-O-ethyl ascorbic acid.

6. A whitening and yellowing stable composition according to claim 1, characterized in that: The solvent includes one or more of 1,3-butanediol, 1,3-propylene glycol, propylene glycol, 1,2-pentanediol, ethanol, and water.

7. A method for preparing the whitening and yellowing-removing stable composition according to any one of claims 1 to 6, characterized in that: The components of the composition are mixed in a solvent in proportion and stirred evenly to obtain a whitening and yellowing-removing stable composition.

8. Use of the whitening and yellowing-removing stable composition according to any one of claims 1 to 6 in the preparation of cosmetics, characterized in that: The amount of the whitening and yellowing-removing stable composition used in the preparation of cosmetics is 0.01-10%.

9. A cosmetic comprising the whitening and yellowing-removing stable composition according to any one of claims 1 to 6, characterized in that: The cosmetic comprises, by mass percentage, 0.01-10% of a whitening and de-yellowing stabilizing composition, 0-20% of a moisturizing agent, 0-1% of a thickening agent, 0-10% of an emulsifier, 0-20% of a skin moisturizer, 0-1% of a preservative, 0-0.1% of a chelating agent, 0-0.2% of a pH regulator, and the remainder is water.

10. The cosmetic composition of the whitening and yellowing-removing stable composition according to claim 9, characterized in that: The cosmetics include any one of lotion, essence, emulsion, cream, spray, eye cream, mask, gel, BB cream, sunscreen, and cleanser.

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