A whitening and freckle-removing composition, its preparation method and application
By adding isosorbic dimethyl ether and hydrolyzed glucosaminoglycan as penetration additives to the whitening and freckle removal composition, the problem that the existing whitening and freckle removal composition is not fast and efficient enough, and 99% inhibition of melanin in zebrafish embryos was achieved, which significantly improved the whitening and freckle removal effect.
Patent Information
- Application Number
- CN202311324749.7
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2023-10-12
- Publication Date
- 2025-06-10
- Estimated Expiration
- 2043-10-12
AI Technical Summary
The existing whitening and freckle removal composition containing flower wood bark extract and 4-butyl resorcinol has not been fast and efficient enough to whiten and remove freckles.
By adding isosorbic dimethyl ether and hydrolyzed glucosaminoglycan as penetration aids, it helps the carmine bark extract and methyl 2,5-dihydroxybenzoate to quickly and accurately reach the base layer of human skin, thereby achieving a rapid and efficient whitening and freckle removal effect.
99% inhibition of melanin in zebrafish embryos was achieved, which significantly improved the rapid and efficient whitening and freckle removal.
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Figure CN117100662B_ABST
Abstract
Description
Technical Field
[0001] The present invention relates to the field of cosmetics, and more specifically, to a whitening and freckle-removing composition and a preparation method and application thereof. Background Art
[0002] In the cosmetics market, people's demand for whitening and freckle-removing products is increasing day by day. At the same time, whitening and freckle-removing products have also become a mainstream therapeutic skin care product, because people are no longer satisfied with covering up facial melanin with foundation and concealer.
[0003] Melanin is one of the important factors that affect people's skin color. Eumelanin is a type of melanin. Under the action of enzymes such as tyrosinase, tyrosine in melanocyte tissue is gradually converted into eumelanin through intermediates such as dopa, dopaquinone, dopachrome and dihydroxyindole. It exists in the basal layer of everyone's skin. If eumelanin grows too fast and is unevenly distributed, it will cause local skin to be too dark or pigmented. Therefore, whitening and freckle removal products that inhibit tyrosinase activity can effectively reduce the production of melanin, thereby truly achieving whitening and freckle removal.
[0004] The whitening and freckle-removing composition of Chinese patent CN114948824A adopts the tamarisk bark extract and the resorcinol derivative 4-butylresorcinol, both of which can inhibit the activity of tyrosinase, to achieve the whitening effect through synergistic enhancement. However, even so, the whitening and freckle-removing effect of the whitening and freckle-removing composition is still not fast and efficient enough, so it is very necessary to modify the whitening and freckle-removing composition containing the tamarisk bark extract and 4-butylresorcinol.
[0005] Therefore, it is of great significance to modify the whitening and anti-freckle composition containing the Pterocarpus tataricus bark extract and 4-butylresorcinol to obtain a new whitening and anti-freckle composition with rapid and efficient whitening and anti-freckle effects. Summary of the invention
[0006] The primary purpose of the present invention is to solve the problem that the whitening and freckle-removing effect of the whitening and freckle-removing composition containing the Pterocarpus tataricus bark extract and 4-butylresorcinol is not fast and efficient enough, and to provide a whitening and freckle-removing composition.
[0007] Another object of the present invention is to provide a method for preparing the whitening and freckle-removing composition.
[0008] Another object of the present invention is to provide a whitening and freckle-removing composition for use in the preparation of cosmetics or skin care products.
[0009] In order to achieve the above object, the present invention adopts the following technical solutions:
[0010] A whitening and freckle-removing composition, comprising the following components by weight:
[0011] 6-10 parts of rosewood bark extract, 18-22 parts of methyl 2,5-dihydroxybenzoate, and 68-76 parts of a penetration aid;
[0012] The penetration aid comprises isosorbide dimethyl ether and hydrolyzed glycosaminoglycan in a weight ratio of 1:(0.2-0.8).
[0013] In the whitening and freckle-removing composition of the present invention, the whitening raw material pterocarpa bark extract and the resorcinol derivative methyl 2,5-dihydroxybenzoate can both achieve the effect of whitening and freckle-removing by inhibiting the activity of tyrosinase; and the penetration aid containing dimethyl isosorbide and hydrolyzed glycosaminoglycan can help the whitening raw material pterocarpa bark extract and methyl 2,5-dihydroxybenzoate to quickly and accurately reach the basal layer of human skin, thereby achieving a fast and efficient whitening and freckle-removing effect. Among penetration aids, dimethyl isosorbide penetrates the skin by dissolving free fat in the skin, thereby opening a channel for the rosewood bark extract and methyl 2,5-dihydroxybenzoate to reach the basal layer of human skin; hydrolyzed glycosaminoglycan forms a complex with the water-insoluble rosewood bark extract and methyl 2,5-dihydroxybenzoate through hydrogen bonds and intermolecular forces. At the same time, the hydrolyzed glycosaminoglycan and dimethyl isosorbide are both water-soluble substances and can be miscible. With the help of the skin channel opened by dimethyl isosorbide, the complex formed by hydrolyzed glycosaminoglycan, rosewood bark extract and methyl 2,5-dihydroxybenzoate is quickly and accurately delivered to the basal layer of human skin, thereby achieving a fast and efficient whitening and freckle removal effect.
[0014] In addition, hydrolyzed glycosaminoglycan, a hydrolysis product of glucosaminoglycan that fills the cells between the epidermal layers of the skin, can help dimethyl isosorbide to quickly penetrate the epidermis to reach the basal layer and accelerate the dissolution of free fat in the skin, quickly open the channels, and further achieve a fast and efficient whitening and freckle removal effect after being miscible with dimethyl isosorbide.
[0015] Preferably, the penetration aid comprises isosorbide dimethyl ether and hydrolyzed glycosaminoglycan in a weight ratio of 1:(0.4-0.6).
[0016] Further preferably, the penetration aid comprises isosorbide dimethyl ether and hydrolyzed glycosaminoglycan in a weight ratio of 1:0.5.
[0017] Preferably, a whitening and freckle-removing composition comprises the following components, calculated by weight:
[0018] 8 parts of Pterocarpus tatarinowii bark extract, 20 parts of methyl 2,5-dihydroxybenzoate, and 72 parts of a penetration aid.
[0019] The bark extract of Ormosia henryi Prain used in the present invention is an aqueous extract, which can be obtained commercially or prepared by conventional methods in the art.
[0020] A method for preparing a whitening and freckle-removing composition comprises the following steps:
[0021] Mix the bark extract of Ormosia henryi Prain, methyl 2,5-dihydroxybenzoate and a penetration aid to obtain the whitening and freckle-removing composition.
[0022] Preferably, the method for preparing the whitening and freckle-removing composition comprises the following steps:
[0023] Weigh the bark extract of Ormosia henryi Prain, methyl 2,5-dihydroxybenzoate and a penetration aid, stir and heat to obtain the whitening and freckle-removing composition.
[0024] Further preferably, the heating temperature is 50-55 °C.
[0025] The application of the above-mentioned whitening and freckle-removing composition in the preparation of cosmetics or skin care products should also be within the protection scope of the present invention.
[0026] Preferably, the application of the whitening and freckle-removing composition in the preparation of cosmetics or skin care products includes diluting the whitening and freckle-removing composition with a liquid.
[0027] Further, the liquid is water.
[0028] Compared with the prior art, the beneficial effects of the present invention are as follows:
[0029] In the whitening and freckle-removing composition of the present invention, the whitening raw material, the bark extract of Ormosia henryi Prain and the resorcinol derivative, methyl 2,5-dihydroxybenzoate, can both achieve the effect of whitening and freckle-removing by inhibiting the activity of tyrosinase; while the penetration aid containing isosorbide dimethyl ether and hydrolyzed glucosaminoglycan can help the whitening raw materials, the bark extract of Ormosia henryi Prain and methyl 2,5-dihydroxybenzoate, reach the basal layer of human skin quickly and accurately, so as to achieve a fast and efficient whitening and freckle-removing effect. The zebrafish experiment shows that the inhibitory rate of the whitening and freckle-removing composition of the present invention on the melanin of zebrafish embryos can reach 99%. Description of the Drawings
[0030] Figure 1 It is the whitening effect diagram of zebrafish under different treatment conditions. Among them, Figure 1 A is the whitening effect diagram of zebrafish in the blank control group, Figure 1 B is the whitening effect diagram of zebrafish after being treated with kojic acid, Figure 1 C is the whitening effect diagram of zebrafish after being treated with the whitening and freckle-removing composition of Example 1. Detailed Embodiments
[0031] The present invention will be further described below in conjunction with embodiments. These embodiments are only used to illustrate the present invention and not to limit the scope of the present invention. For the experimental methods without specific conditions in the following embodiments, they are generally carried out according to the conventional conditions in the art or according to the conditions recommended by the manufacturer; the raw materials, reagents, etc. used, unless otherwise specified, are all raw materials and reagents that can be obtained from commercial channels such as the conventional market. Any non-substantial changes and substitutions made by those skilled in the art based on the present invention fall within the scope of protection required by the present invention.
[0032] The reagents used in the present invention are as follows:
[0033] Hydrolyzed Opuntia ficus-indica flower extract, SILAB-FRANCE;
[0034] Hydrolyzed Candida extract, SILAB-FRANCE;
[0035] Ormosia henryi bark extract, PTE90, Synsil Organic Inc.
[0036] Example 1
[0037] This example provides a whitening and freckle-removing composition, which includes the following components by weight:
[0038] 8 parts of Ormosia henryi bark extract, 20 parts of methyl 2,5-dihydroxybenzoate, and 72 parts of penetration aid;
[0039] The penetration aid contains dimethyl isosorbide and hydrolyzed glucosaminoglycan with a weight ratio of 1:0.5.
[0040] A preparation method of a whitening and freckle-removing composition includes the following steps:
[0041] Weigh the Ormosia henryi bark extract, methyl 2,5-dihydroxybenzoate, and penetration aid, and heat them with stirring to 55 °C until they are completely dissolved and dispersed, thus obtaining the whitening and freckle-removing composition.
[0042] Examples 2-5 and Comparative Examples 1-2
[0043] Examples 2-5 and Comparative Examples 1-2 provide different whitening and freckle-removing compositions and their preparation methods, all referring to Example 1. The differences between Examples 2-5 and Comparative Examples 1-2 and Example 1 are only the weight ratios of dimethyl isosorbide and hydrolyzed glucosaminoglycan in the penetration aid, as shown in Table 1 specifically:
[0044] Table 1 Weight ratios of dimethyl isosorbide and hydrolyzed glucosaminoglycan in Examples 1-5 and Comparative Examples 1-2
[0045]
[0046] Examples 6 - 11 and Comparative Examples 3 - 8
[0047] Examples 6 - 11 and Comparative Examples 3 - 8 provide different whitening and freckle - removing compositions and their preparation methods. All refer to Example 1. The differences between Examples 6 - 11 and Comparative Examples 3 - 8 and Example 1 are only the weight parts of the bark extract of Ormosia henryi, methyl 2,5 - dihydroxybenzoate, and the penetration aid. Calculated by weight parts, the details are shown in Table 2 as follows:
[0048] Table 2 Weight Parts of Each Component in Example 1, Examples 6 - 11 and Comparative Examples 3 - 8
[0049]
[0050]
[0051] Comparative Example 9
[0052] This comparative example provides a whitening and freckle - removing composition. The difference from Example 1 is only that the penetration aid only contains isosorbide dimethyl ether. Specifically, calculated by weight parts, it includes the following components:
[0053] 8 parts of the bark extract of Ormosia henryi, 20 parts of methyl 2,5 - dihydroxybenzoate, 72 parts of the penetration aid;
[0054] The penetration aid is isosorbide dimethyl ether.
[0055] A preparation method of a whitening and freckle - removing composition refers to Example 1.
[0056] Comparative Example 10
[0057] This comparative example provides a whitening and freckle - removing composition. The difference from Example 1 is only that the penetration aid only contains hydrolyzed glucosaminoglycan. Specifically, calculated by weight parts, it includes the following components:
[0058] 8 parts of the bark extract of Ormosia henryi, 20 parts of methyl 2,5 - dihydroxybenzoate, 72 parts of the penetration aid;
[0059] The penetration aid is hydrolyzed glucosaminoglycan.
[0060] A preparation method of a whitening and freckle - removing composition refers to Example 1.
[0061] Comparative Example 11
[0062] This comparative example provides a whitening and freckle - removing composition. The difference from Example 1 is only that 4 - butylresorcinol is used instead of methyl 2,5 - dihydroxybenzoate. Specifically, calculated by weight parts, it includes the following components:
[0063] 8 parts of Pterocarpus tatarinowii bark extract, 20 parts of 4-butylresorcinol, and 72 parts of a penetration aid;
[0064] The penetration aid comprises isosorbide dimethyl ether and hydrolyzed glycosaminoglycan in a weight ratio of 1:0.5.
[0065] A preparation method of a whitening and freckle-removing composition, see Example 1.
[0066] Comparative Example 12
[0067] This comparative example provides a whitening and freckle-removing composition, which differs from Example 1 only in that 2,5-dihydroxybenzoic acid is used instead of methyl 2,5-dihydroxybenzoate. Specifically, the composition comprises the following components, calculated by weight:
[0068] 8 parts of Pterocarpus tataricus bark extract, 20 parts of 2,5-dihydroxybenzoic acid, and 72 parts of a penetration aid;
[0069] The penetration aid comprises isosorbide dimethyl ether and hydrolyzed glycosaminoglycan in a weight ratio of 1:0.5.
[0070] A preparation method of a whitening and freckle-removing composition, see Example 1.
[0071] Comparative Example 13
[0072] This comparative example provides a whitening and freckle-removing composition, which differs from Example 1 only in that 2,5-dihydroxybenzoic acid methyl ester is replaced by phenethyl resorcinol. Specifically, the composition comprises the following components in parts by weight:
[0073] 8 parts of Pterocarpus tatarinowii bark extract, 20 parts of phenethyl resorcinol, and 72 parts of a penetration aid;
[0074] The penetration aid comprises isosorbide dimethyl ether and hydrolyzed glycosaminoglycan in a weight ratio of 1:0.5.
[0075] A preparation method of a whitening and freckle-removing composition, see Example 1.
[0076] Performance Testing
[0077] 1. Zebrafish experiment for rapid whitening and freckle removal
[0078] The whitening and freckle-removing compositions of each example and comparative example were respectively diluted with water to prepare a sample solution of 1 g / L, and 8-hour-old zebrafish embryos were exposed to the sample solution. Then, when the melanin inhibition rate reached 99%, the treatment time of different sample solutions on 8-hour-old zebrafish embryos was measured; the longest treatment time of different sample solutions on 8-hour-old zebrafish embryos was 96 hours. If the melanin inhibition rate still did not reach 99% when the treatment time was 96 hours, the melanin inhibition rate when the treatment time of the sample solution on 8-hour-old zebrafish embryos was 96 hours was recorded.
[0079] Melanin inhibition rate (%) = (S1 - S2) / S1 × 100%;
[0080] Among them, S1 refers to the melanin signal intensity of zebrafish embryos before treatment with the sample solution; S2 refers to the melanin signal intensity of zebrafish embryos after treatment with the sample solution for a period of time; the melanin signal intensity of zebrafish embryos was measured by the following method: the zebrafish embryos were photographed with a dissection microscope and the pictures were saved, and then the Image-J Pro advanced image processing software was used for analysis and data collection to obtain the melanin signal intensity of the whole body of the zebrafish embryos.
[0081] The experimental results are shown in the following table:
[0082] Table 3 Rapid whitening and freckle-removing results of the whitening and freckle-removing compositions of Examples 1-5 and Comparative Examples 1-2
[0083]
[0084]
[0085] As can be seen from Table 3, when the weight ratio of dimethyl isosorbide and hydrolyzed glucosaminoglycan in the penetration enhancer is 1:(0.2 - 0.8), the whitening and freckle-removing composition of the present invention has the effect of rapid whitening and freckle removal.
[0086] Table 4 Rapid whitening and freckle-removing results of the whitening and freckle-removing compositions of Examples 1, 6-11 and Comparative Examples 3-8
[0087]
[0088] As can be seen from Table 4, the whitening and freckle-removing composition of the present invention has the effect of rapid whitening and freckle removal.
[0089] Table 5 Rapid whitening and freckle-removing results of the whitening and freckle-removing compositions of Example 1 and Comparative Examples 9-13
[0090]
[0091]
[0092] As can be seen from Table 5, compared with the mixture of isosorbide dimethyl ether and hydrolyzed glucosaminoglycan, when only isosorbide dimethyl ether or hydrolyzed glucosaminoglycan is used as the penetration enhancer, the rapid whitening and freckle-removing efficacy of the whitening and freckle-removing composition will decrease; when 4-butylresorcinol, 2,5-dihydroxybenzoic acid, or phenethylresorcinol is used instead of methyl 2,5-dihydroxybenzoate of the present invention, the rapid whitening and freckle-removing efficacy of the whitening and freckle-removing composition will also decrease.
[0093] 2. Zebrafish Experiment for Highly Effective Whitening and Freckle Removal
[0094] The whitening and freckle-removing compositions of each example and comparative example were respectively diluted with water to prepare a sample solution of 1 g / L, and 8-hour-old zebrafish embryos were exposed to the sample solution for 36 hours, and then the melanin inhibition rate was measured;
[0095] Water was used instead of the sample solution as the blank control group; 4-butylresorcinol, resveratrol, glabridin, diglucosyl gallic acid, salicylic acid, hydrolyzed prickly pear flower extract, tetraisopalmitate ascorbate, azelaic amide, 1-methylhydantoin-2-imide, citric acid, ferulic acid, glycolic acid, glucosyl hesperidin, α-arbutin, hydrolyzed candida extract, 3-O-ethyl ascorbic acid, and kojic acid were respectively diluted with water to prepare solutions of 1 g / L, which were used as the positive control groups;
[0096] Melanin inhibition rate (%) = (S1 - S3) / S1 × 100%;
[0097] Wherein, S1 refers to the melanin signal intensity of the zebrafish embryo before treatment with the sample solution; S3 refers to the melanin signal intensity of the zebrafish embryo after 36 hours of treatment with the sample solution; the melanin signal intensity of the zebrafish embryo was measured by the following method: the zebrafish embryo was photographed with a dissection microscope and the picture was saved, and then the Image-J Pro advanced image processing software was used for analysis and data collection to obtain the melanin signal intensity of the whole body of the zebrafish embryo.
[0098] The experimental results are shown in Table 6:
[0099] Table 6 Results of Highly Effective Whitening and Freckle Removal of Whitening and Freckle-Removing Compositions of Each Example and Comparative Example
[0100]
[0101]
[0102] Figure 1 is the zebrafish whitening effect diagram under different treatment conditions, wherein, Figure 1 A is the zebrafish whitening effect diagram of the blank control group, Figure 1 B is the zebrafish whitening effect diagram after treatment with kojic acid,Figure 1 C is the whitening effect diagram of zebrafish after being treated with the whitening and freckle removing composition of Example 1.
[0103] From Table 6 and Figure 1 it can be seen that the whitening and freckle removing composition of the present invention has an efficient whitening and freckle removing effect.
[0104] Obviously, the above-mentioned embodiments of the present invention are merely examples for clearly illustrating the present invention, rather than limitations on the implementation manners of the present invention. For those of ordinary skill in the art, other different forms of changes or modifications can be made on the basis of the above description. It is not necessary and impossible to enumerate all the implementation manners here. Any modifications, equivalent replacements, improvements, etc. made within the spirit and principle of the present invention shall be included in the protection scope of the claims of the present invention.
Claims
1. A whitening and freckle-removing composition, It is characterized in that Calculated by weight, it includes the following ingredients: 6-10 parts of rosewood bark extract, 18-22 parts of methyl 2,5-dihydroxybenzoate, and 68-76 parts of a penetration aid; The penetration aid comprises isosorbide dimethyl ether and hydrolyzed glycosaminoglycan in a weight ratio of 1:(0.4-0.6).
2. The whitening and anti-freckle composition according to claim 1, It is characterized in that The penetration aid comprises isosorbide dimethyl ether and hydrolyzed glycosaminoglycan in a weight ratio of 1:0.
5.
3. The whitening and anti-freckle composition according to claim 1, It is characterized in that Calculated by weight, it includes the following ingredients: 8 parts of Pterocarpus tatarinowii bark extract, 20 parts of methyl 2,5-dihydroxybenzoate, and 72 parts of a penetration aid.
4. A method for preparing the whitening and anti-freckle composition according to any one of claims 1 to 3, It is characterized in that The steps include: The extract of Pterocarpus tatarinowii bark, methyl 2,5-dihydroxybenzoate and a penetration aid are mixed to obtain a whitening and freckle-removing composition.
5. The preparation method of the whitening and anti-freckle composition according to claim 4, It is characterized in that The steps include: The extract of Pterocarpus tatarinowii bark, methyl 2,5-dihydroxybenzoate and a penetration aid are weighed, stirred and heated to obtain a whitening and freckle-removing composition.
6. The preparation method of the whitening and freckle-removing composition according to claim 5, It is characterized in that The heating temperature is 50-55°C.
7. Use of the whitening and anti-freckle composition according to any one of claims 1 to 3 in the preparation of cosmetics or skin care products.
8. The use according to claim 7, It is characterized in that The method comprises diluting the whitening and anti-freckle composition with a liquid.
9. The use according to claim 8, It is characterized in that The liquid is water.
Citation Information
Patent Citations
Novel gentianic acid derivative 2-hydroxy-5-substituted long-chain fat acyloxymethyl benzoates, preparation method for novel gentianic acid derivative and application of novel gentianic acid derivative
CN102531904A
Penetration-promoting cosmetic composition and preparation method thereof
CN112716819A
Whitening and freckle-removing composition
CN114948824A