Transdermal composition with whitening and freckle removing effects and preparation method thereof

Abstract

The invention provides a transdermal composition with whitening and freckle removing effects and a preparation method thereof, and belongs to the technical field of cosmetics. The transdermal composition comprises whitening and freckle-removing functional components. The whitening and freckle-removing functional components comprise nicotinamide, arbutin, glycerol and water, and further comprise a plant extract and a fermentation extract. The plant extract comprises a silybum marianum extract, a sarcandra glabra extract and a radix paeoniae rubra extract. The fermentation extract is obtained by fermenting a soybean seed coat extract, a sargassum pallidum extract and a red bean extract through a compound fermentation inoculant. And the compound fermentation inoculant comprises bacillus alvei, lactobacillus rhamnosus and streptomyces olivaceus. The transdermal composition prepared by the invention not only has good whitening and freckle-removing effects and transdermal property, but also can keep the appearance state when the external temperature changes.

Description

Technical Field

[0001] The invention belongs to the technical field of cosmetics, and specifically relates to a transdermal composition with whitening and freckle removal effects and a preparation method thereof. Background Art

[0002] Whitening and anti-freckle compositions generally refer to formulas composed of one or more ingredients that have the function of whitening and reducing skin pigmentation. Such compositions are intended to reduce spots, freckles and other pigmentation phenomena on the skin through different mechanisms to achieve the effect of whitening the skin. These ingredients can be extracts from natural sources, or chemically synthesized active substances, or a combination of the two.

[0003] Currently commonly used whitening and freckle-removing ingredients include arbutin, niacinamide, resveratrol, green tea extract, etc. Among them, arbutin can inhibit the activity of tyrosinase and reduce the production of melanin; niacinamide can reduce the transfer of melanin to the stratum corneum, thereby helping to alleviate the problems of pigmentation and uneven skin tone; resveratrol has an antioxidant effect, which helps to protect the skin from damage and indirectly supports the whitening effect; green tea extract contains antioxidant ingredients such as catechins, which can reduce UV damage and prevent excessive accumulation of melanin.

[0004] Although the above ingredients can achieve the effect of whitening and removing freckles, the whitening and removing freckles effect is very limited in actual use. The specific disadvantages are as follows:

[0005] (1) Niacinamide and arbutin have large molecular weights and may not be able to penetrate deep into the skin. Transdermal absorption is also slow, resulting in their inability to achieve their own whitening and freckle removal effects during actual use;

[0006] (2) Niacinamide and arbutin are prone to deterioration when the temperature changes, affecting the appearance and stability of cosmetics.

[0007] (3) Niacinamide or arbutin alone have limited whitening and freckle removal effects, and the design of cosmetic ingredients is unreasonable. Summary of the invention

[0008] The purpose of the present invention is to provide a transdermal composition with whitening and freckle removal effects and a preparation method thereof, so as to solve the problems of poor transdermal effect, unreasonable component design and susceptibility to external environmental influences of the above-mentioned whitening and freckle removal compositions.

[0009] In order to achieve the above object, the present invention provides the following technical solutions:

[0010] The first aspect of the present invention provides a transdermal composition with whitening and freckle removal effects. The raw materials of the transdermal composition include whitening and freckle removal functional ingredients. The whitening and freckle removal functional ingredients include niacinamide, arbutin, glycerin and water in a mass ratio of (0.2-0.4): (0.5-0.8): (0.1-0.3): (3-5).

[0011] Preferably, the whitening and freckle-removing effective ingredients include niacinamide, arbutin, glycerin and water in a mass ratio of (0.3-0.4):(0.6-0.8):(0.2-0.3):(4-5).

[0012] Preferably, the whitening and freckle-removing effective ingredients include niacinamide, arbutin, glycerin and water in a mass ratio of 0.3:0.7:0.2:4.5.

[0013] Preferably, the raw materials of the transdermal composition also include moisturizers, emulsifiers, fillers, thickeners, transdermal absorption enhancers and water; the whitening and anti-freckle ingredients also include plant extracts and fermented extracts;

[0014] The transdermal composition comprises the following raw materials in terms of mass percentage:

[0015] 10-15% whitening and freckle removing ingredients, 5-40% emollient, 0.5-30% emulsifier, 0.1-20% filler, 0.1-10% thickener, 1-3% transdermal absorption enhancer and the balance water;

[0016] The whitening and anti-freckle ingredients include niacinamide, arbutin, glycerin, water, plant extracts and fermented extracts according to the mass ratio of (0.2-0.4): (0.5-0.8): (0.1-0.3): (5-10): (3-5): 1;

[0017] The plant extracts include milk thistle extract, coral grass extract and red peony root extract in a mass ratio of (1.5-3.5):(0.5-1):1;

[0018] The fermented extract is obtained by fermenting soybean seed coat extract, giant algae extract and sea red bean extract in a mass ratio of (0.8-1): (3-4): 1 through a composite fermentation agent;

[0019] The composite fermentation bacterial agent includes Bacillus alvei, Lactobacillus murinus and Streptomyces oliveri in a mass ratio of (6-10):(2.5-4):1.

[0020] In order to solve the problem that the whitening and freckle removal composition in the prior art has poor actual use effect, the commonly used nicotinamide and arbutin in the prior art are designed as ingredients, and the synergistic effect between multiple substances is utilized to improve the whitening and freckle removal effect of the composition. The whitening and freckle removal effect ingredients in the present invention include four substances, namely nicotinamide, arbutin, plant extract and fermented extract. These four substances can synergistically act with the skin to improve the whitening and freckle removal effect. Analysis of the reasons: Nicotinamide can inhibit the formation of melanin and reduce pigmentation. Nicotinamide also has anti-inflammatory properties and can help reduce pigmentation caused by skin inflammation. Arbutin prevents the synthesis of melanin by inhibiting the activity of tyrosinase. Milk thistle, coral grass and Sichuan red peony in plant extracts contain a variety of antioxidant ingredients, such as polyphenol compounds, which can scavenge free radicals and reduce the damage of oxidative stress to the skin. They can also regulate the metabolism of skin cells and promote healthy cell renewal. Soybean seed coat, large-leaf seaweed and sea red bean in the fermented extract can not only provide strong antioxidant protection, but also work together through multiple mechanisms to promote the moisturizing, repairing and whitening effects of the skin. When the four substances in the present invention are used simultaneously according to the proportion, niacinamide and arbutin can jointly inhibit the production of melanin, the antioxidant properties of the plant extract can protect the skin from damage and reduce inflammatory reactions, and the fermented extract provides additional nutritional support to promote skin health. This multi-faceted protection and repair mechanism makes the composition perform well in whitening and freckle removal, and the interaction of the four substances can further enhance the whitening effect.

[0021] The present invention uses a variety of plant extracts such as milk thistle extract, coral extract, Sichuan red peony extract, soybean seed coat extract, large leaf seaweed extract and sea red bean extract. Although it can further improve the whitening and freckle removal effect, it is found that when the external temperature environment changes, the appearance of the prepared composition is prone to change, affecting subsequent use. The reason for the analysis may be that the plant extract contains a variety of substances, and the physical and chemical properties of different components are quite different. Some components may be more sensitive to temperature changes, and precipitation and discoloration may occur with the change of time and temperature, and the emulsification system will also be destroyed. In response to this problem, the present invention ferments three kinds of extracts of soybean seed coat extract, large leaf seaweed extract and sea red bean extract with composite strains, which can not only maintain its whitening and freckle removal effect, but also improve its appearance stability. The reason for the analysis is that during the fermentation process, microorganisms can convert complex organic molecules into simpler small molecules, and these converted components are often more stable and are not easily affected by temperature changes. In addition, by fermentation, the content of certain unstable components can be reduced, and the stability of the entire extract can be improved. The surfactant that may be produced during the microbial fermentation process helps to improve the stability of the emulsification system and reduce the destruction of the emulsification system caused by temperature changes. The fermentation product may also have some emulsifying properties, which helps to maintain the uniformity of the emulsified system and prevent oil-water separation. The present invention can achieve the stability of the emulsified system when the temperature changes through the mixed fermentation process of the composite fermentation bacteria.

[0022] Preferably, the emollient is one or more of caprylic capric triglyceride, squalane, avocado oil, shea butter, jojoba oil, glycerin, butylene glycol, hexylene glycol, pentylene glycol, dimethicone, dimethiconol, PEG-11 methyl ether dimethicone, phytosterol, phytosterol / octyldodecyl lauroyl glutamate, hydrogenated polyisobutene, rapeseed oil, polydecene, soybean oil, olive oil, isododecane, isohexadecane, stearyl alcohol, and behenyl alcohol.

[0023] Preferably, the emulsifier is olive oil PEG-7 esters, PEG-8 caprylic / capric glycerides, sorbitan olivate, polysorbate-20, laureth-23, PEG-40 stearate, steareth-21, a mixture of palmityl alcohol and PEG-75 stearate and glyceryl stearate and steareth-20, polysorbate-80, soy lecithin PC60, a mixture of glyceryl stearate and PEG-75 stearate, poloxamer 407, PEG-30 dipolyhydroxystearate, and ceteareth-25. One or more.

[0024] Preferably, the filler is one or more of titanium dioxide, mica, boron nitride, polymethylsilsesquioxane, diatomaceous earth, kaolin, cellulose acetate, aluminum starch octyl succinate, talc, barium sulfate, and volcanic ash.

[0025] Preferably, the thickener is one or more of hydroxyethyl cellulose, xanthan gum, carbomer, polymer EMT-10, polyacrylate crosspolymer-6, sodium acrylate / sodium acryloyldimethyl taurate copolymer, acryloyldimethyl taurate amine / VP copolymer, acrylate / C10-30 alkyl acrylate crosspolymer, polyvinyl alcohol, gum arabic, and hydroxypropyl starch phosphate.

[0026] Preferably, the transdermal absorption enhancer comprises peppermint oil, laurocapram and N-acetylproline pentanol ester in a mass ratio of (2-4):(8-10):1.

[0027] To improve the whitening and freckle removal effect of the whitening and freckle removal composition, it is necessary not only to pay attention to the composition design of the composition so that it can maximize the efficacy of the composition, but also to consider the absorbability of the skin so that the added whitening and freckle removal functional components can penetrate deep into the skin and have a good transdermal effect. The present invention specifically limits the type and proportion of the transdermal absorption enhancer, thereby improving the transdermal property of the product. Analysis of the reasons: Peppermint oil, laurocapram and N-acetylproline pentanol ester can synergistically improve the transdermal absorption of whitening and freckle removal functional components, wherein the cool feeling of peppermint oil can temporarily increase the temperature of the skin, promote local blood circulation, and facilitate nicotinamide, arbutin and other components to penetrate the stratum corneum faster and enter the deep layer of the skin. Laurocapram can effectively promote the transdermal absorption of the active ingredients in plant extracts and fermented extracts because it can increase the lipophilicity of these ingredients, making them easier to pass through the skin barrier. N-acetylproline pentanol ester can increase the hydration of the skin, loosen the stratum corneum of the skin, and help water-soluble components such as nicotinamide and arbutin to better penetrate into the skin. When these three transdermal absorption enhancers are mixed in a certain proportion, they can complement each other to form an effective enhancement system.

[0028] Preferably, the preparation method of the fermentation extract is:

[0029] S11: mixing soybean seed coat extract, giant algae extract and red bean extract according to a certain proportion to obtain a mixture;

[0030] S12: adding a composite fermentation agent to the mixture, wherein the inoculation amount of the composite fermentation agent is 6-8wt%, then adding water, wherein the mass of the added water is 15-20 times that of the mixture, continuously introducing oxygen, and fermenting at 28-32° C. for 5-7 days to obtain a fermentation liquid;

[0031] S13: filtering the fermentation liquid to obtain a filtrate, sterilizing the filtrate at 100-110° C. for 30-60 min, then centrifuging the filtrate, collecting the supernatant, and freeze-drying to obtain a fermentation extract.

[0032] The second aspect of the present invention provides a method for preparing a transdermal composition having whitening and freckle removal effects, comprising the following steps:

[0033] S1: Wetting and dispersing the thickener in water to obtain a mixed solution;

[0034] S2: adding emollient and filler to the mixed solution of step S1, heating to 60-80°C, and homogenizing at 2500-3500 r / min for 3-5 minutes to completely disperse them;

[0035] S3: Add an emulsifier to step S2, homogenize at 2500-3500 r / min for 3-5 minutes to fully emulsify the mixture, add whitening and anti-freckle ingredients and a transdermal absorption accelerator while stirring and cooling to obtain a transdermal composition.

[0036] Compared with the prior art, the advantages and beneficial effects of the present invention are:

[0037] 1. The present invention contains niacinamide, arbutin, plant extracts and fermented extracts, which have multiple whitening and freckle-removing effects, and achieves multi-effect synergistic effects through scientific proportions. This synergistic effect can not only improve the whitening and freckle-removing effects, but also enhance the skin's self-repairing ability and overall health status.

[0038] 2. The present invention uses fermentation technology to process plant extracts, which can improve the stability of the active ingredients in the extracts and reduce changes in the appearance of the composition caused by external factors such as temperature. In addition, the small molecules produced during the fermentation process are more easily absorbed by the skin and are also more stable.

[0039] 3. In the present invention, peppermint oil, laurocapram and N-acetylproline pentanol ester are used as transdermal absorption enhancers. These ingredients can effectively promote the transdermal absorption of whitening and anti-freckle ingredients, thereby improving their bioavailability, so that the effective ingredients can reach the deep layers of the skin more quickly and deeply to exert their effects.

[0040] 4. The ingredients used in the composition of the present invention are all substances existing in nature or obtained through biological fermentation. Compared with chemically synthesized ingredients, these natural ingredients are generally considered to be safer, milder, less irritating to the skin, and suitable for long-term use. DETAILED DESCRIPTION

[0041] The technical solutions in the embodiments of the present invention are described clearly and completely below. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.

[0042] Example 1

[0043] This embodiment provides a transdermal composition with whitening and freckle removal effects, and the composition is shown in Table 1.

[0044] Table 1 Composition ingredients

[0045]

[0046]

[0047] The transdermal absorption enhancer includes peppermint oil, laurocapram and N-acetylproline pentanol ester in a mass ratio of 3:9:1.

[0048] The whitening and anti-freckle ingredients include niacinamide, arbutin, glycerin, water, plant extracts and fermented extracts in a mass ratio of 0.3:0.7:0.2:7:4:1;

[0049] The plant extracts include milk thistle extract, coral grass extract and red peony root extract in a mass ratio of 2:0.8:1;

[0050] Milk thistle extract was purchased from Hunan Langlin Biological Resources Co., Ltd.;

[0051] Coralleaf sarmentosa extract was purchased from Lanzhou Waterless Biotechnology Co., Ltd.;

[0052] Sichuan red peony root extract was purchased from Xi'an Yunuo Bioengineering Co., Ltd.;

[0053] The preparation method of the fermentation extract is:

[0054] S11: mixing soybean seed coat extract, giant kelp extract and red bean extract in proportion to obtain a mixture; the mass ratio of soybean seed coat extract, giant kelp extract and red bean extract is 0.9:3.5:1;

[0055] Soybean seed coat extract was purchased from Shaanxi Guanchen Biotechnology Co., Ltd.;

[0056] Macrophylla sutchuenensis extract was purchased from Ningxia Vanilla Biotechnology Co., Ltd.;

[0057] Sea red bean extract was purchased from Lanzhou Waterless Biotechnology Co., Ltd.;

[0058] S12: adding a composite fermentation agent to the mixture, wherein the inoculation amount of the composite fermentation agent is 7wt%, then adding water, wherein the mass of the added water is 18 times that of the mixture, continuously introducing oxygen, and fermenting at 30° C. for 6 days to obtain a fermentation liquid;

[0059] The composite fermentation agent includes Bacillus alvei, Lactobacillus murinus and Streptomyces olivetica in a mass ratio of 8:3:1;

[0060] Bacillus alvei was purchased from Shanghai Chen Microbiology Technology Co., Ltd., model number GDMCC 800145;

[0061] Lactobacillus murinus was purchased from Shanghai Chen Microbiology Technology Co., Ltd., model number CICC 23144;

[0062] Streptomyces oliveri was purchased from Shanghai Chen Microbiology Technology Co., Ltd., model number CICC 11001;

[0063] S13: filtering the fermentation broth to obtain a filtrate, sterilizing the filtrate at 105° C. for 40 min, and then centrifuging the filtrate to collect the supernatant, and freeze-drying to obtain a fermentation extract.

[0064] A method for preparing a transdermal composition having whitening and freckle removal effects comprises the following steps:

[0065] S1: Wetting and dispersing the thickener in water to obtain a mixed solution;

[0066] S2: adding emollient and filler to the mixed solution of step S1, heating to 65°C, and homogenizing at 3000r / min for 3min to make them dispersed completely;

[0067] S3: Add an emulsifier to step S2, homogenize at 3000 r / min for 5 minutes to fully emulsify the mixture, add whitening and anti-freckle ingredients and a transdermal absorption accelerator while stirring and cooling to obtain a transdermal composition.

[0068] Example 2

[0069] The difference between this embodiment and embodiment 1 is: the composition and addition amount of the whitening and freckle-removing functional component. The mass percentage of the whitening and freckle-removing functional component in the composition of this embodiment is 12%.

[0070] In this embodiment, the whitening and anti-freckle effective ingredients include niacinamide, arbutin, glycerin, water, plant extracts and fermented extracts in a mass ratio of 0.2:0.6:0.3:8:4:1;

[0071] The plant extracts include milk thistle extract, coral grass extract and red peony root extract in a mass ratio of 2.2:0.6:1;

[0072] The preparation method of the fermentation extract is:

[0073] S11: mixing soybean seed coat extract, giant kelp extract and red bean extract in proportion to obtain a mixture; the mass ratio of soybean seed coat extract, giant kelp extract and red bean extract is 0.8:3.8:1;

[0074] S12: adding a composite fermentation agent to the mixture, wherein the inoculation amount of the composite fermentation agent is 8%, then adding water, wherein the amount of water added is 20 times of the mixture, continuously introducing oxygen, and fermenting at 28° C. for 7 days to obtain a fermentation liquid;

[0075] The composite fermentation agent includes Bacillus alvei, Lactobacillus murinus and Streptomyces olivetica in a mass ratio of 8.5:3:1;

[0076] S13: filtering the fermentation broth to obtain a filtrate, sterilizing the filtrate at 105° C. for 30 min, and then centrifuging the filtrate to collect the supernatant, and freeze-drying to obtain a fermentation extract.

[0077] Comparative Example 1

[0078] The difference between this comparative example and Example 1 is that the mass ratio of the plant extracts is different, and the added ratio of the coral grass extract is increased.

[0079] In this comparative example, the mass ratio of milk thistle extract, coral grass extract and red peony root extract is 2:2:1.

[0080] Comparative Example 2

[0081] The difference between this comparative example and Example 1 is that the mass ratios of soybean seed coat extract, giant algae extract and red bean extract in the fermented extract are different, and the addition ratio of soybean seed coat extract is increased.

[0082] In this comparative example, the mass ratio of soybean seed coat extract, giant algae extract and red bean extract is 2:3.5:1.

[0083] Comparative Example 3

[0084] The difference between this comparative example and Example 1 is that the mass ratio of the composite fermentation bacteria used in the preparation process of the fermentation extract is different, and the addition ratio of Lactobacillus murinus is increased.

[0085] In this comparative example, the mass ratio of Bacillus alvei, Lactobacillus murinus and Streptomyces oliveri is 8:6:1.

[0086] Comparative Example 4

[0087] The difference between this comparative example and Example 1 is that the types of composite fermentation bacteria are different. In this comparative example, Bacillus alvei is replaced by Bacillus licheniformis. Bacillus licheniformis is purchased from Shanghai Chen Microbiology Technology Co., Ltd., model number GDMCC1.182.

[0088] Comparative Example 5

[0089] The difference between this comparative example and Example 1 is that the types of composite fermentation bacteria are different. In this comparative example, Lactobacillus murinus is replaced by Lactobacillus plantarum, which is purchased from Shanghai Chen Microbiology Technology Co., Ltd., model number CICC 23135.

[0090] Comparative Example 6

[0091] The difference between this comparative example and Example 1 is that the types of composite fermentation bacteria are different. In this comparative example, Streptomyces oliveti is replaced by Streptomyces griseus. Streptomyces griseus is purchased from Shanghai Chen Microbiology Technology Co., Ltd., model number CICC 11002.

[0092] Comparative Example 7

[0093] The difference between this comparative example and Example 1 is that the mass ratio of the whitening and freckle-removing effective ingredients is different, and the added ratio of arbutin is increased.

[0094] The whitening and freckle-removing effective ingredients in this comparative example include niacinamide, arbutin, glycerin, water, plant extract and fermentation extract in a mass ratio of 0.3:1.5:0.2:7:4:1.

[0095] Comparative Example 8

[0096] The difference between this comparative example and Example 1 is that the ingredients of the whitening and freckle-removing functional components are different, and no fermentation extract is added in this comparative example.

[0097] The whitening and freckle-removing effective ingredients in this comparative example include niacinamide, arbutin, glycerin, water and plant extracts in a mass ratio of 0.3:0.7:0.2:7:4.

[0098] Comparative Example 9

[0099] The difference between this comparative example and Example 1 is that the ingredients of the whitening and freckle-removing functional components are different, and no plant extract is added in this comparative example.

[0100] The whitening and freckle-removing effective ingredients in this comparative example include niacinamide, arbutin, glycerin, water and fermentation extract in a mass ratio of 0.3:0.7:0.2:7:1.

[0101] Comparative Example 10

[0102] The difference between this comparative example and Example 1 is that the ingredients of the whitening and anti-freckle functional components are different. In this comparative example, no fermented extract is added, and unfermented soybean seed coat extract, giant algae extract and red bean extract are directly added to the whitening and anti-freckle functional components.

[0103] The whitening and freckle-removing effective ingredients in this comparative example include niacinamide, arbutin, glycerin, water, plant extracts and plant raw materials in a mass ratio of 0.3:0.7:0.2:7:4:1; the plant raw materials soybean seed coat extract, giant algae extract and red bean extract have a mass ratio of 0.9:3.5:1.

[0104] Comparative Example 11

[0105] The difference between this comparative example and Example 1 is that the mass ratio of the transdermal absorption enhancer is different.

[0106] In this comparative example, the transdermal absorption enhancer includes peppermint oil, laurocapram and N-acetylproline pentanol ester in a mass ratio of 8:9:1.

[0107] Performance Testing

[0108] (1) Safety testing

[0109] Test samples: transdermal compositions prepared in Examples and Comparative Examples;

[0110] Test method: Use a third-party testing agency to test safety. Select an area not exceeding 50mm 2 , a suitable patch with a depth of about 1mm, add about 0.02g of the test substance into the patch tester by the closed patch test method. The patch tester is attached to the curved side of the subject's forearm, and the test substance is removed after 24 hours. The skin reaction is observed 48 hours after removal, and the results are recorded according to the skin reaction grading standards in the "Technical Regulations on Cosmetic Safety 2015". The test results are shown in Table 2.

[0111] The skin reaction grading standards are as follows:

[0112] Grade 0: negative reaction;

[0113] Grade 1: Suspicious reaction; only slight erythema;

[0114] Grade 2: weak positive reaction (erythema reaction); erythema, infiltration, edema, and papules may be present;

[0115] Grade 3: Strong positive reaction (herpes reaction); erythema, infiltration, edema, papules, herpes; the reaction may extend beyond the test area;

[0116] Grade 4: Very strong reaction (confluent herpes reaction); obvious erythema, severe infiltration, edema, confluent herpes, and the reaction exceeds the test area.

[0117] Table 2 Safety test results

[0118]

[0119]

[0120] It can be seen from Table 2 that the compositions prepared in the examples and comparative examples are relatively safe and can be used for subsequent experiments.

[0121] (2) Stability test

[0122] Test samples: transdermal compositions prepared in Examples and Comparative Examples;

[0123] Test method: The transdermal compositions prepared in the examples and comparative examples were placed under conditions of 45°C away from light, 25°C away from light, -15°C away from light, 45°C and -15°C cycle, and 25°C light, and the appearance was observed after three months. The 45°C and -15°C cycle specifically refers to placing the transdermal composition under 45°C away from light for 3 days, and then placing it under -15°C away from light for 3 days, and so on.

[0124] After the above experiment, the appearance test results are expressed as 1, 2, 3 and 4, where 1 means no obvious change in appearance, 2 means precipitation of trace substances, 3 means precipitation of a small amount of substances, and 4 means precipitation of a large amount of substances. The test results are shown in Table 3.

[0125] Table 3 Stability test results

[0126]

[0127]

[0128] As can be seen from Table 3, the transdermal compositions prepared in Examples 1-2 did not show any significant changes in appearance after three months under high and low temperature conditions or under light exposure, while the appearances of Comparative Examples 1-11 all deteriorated and precipitated to varying degrees, indicating that the compositions prepared in the present invention have good stability.

[0129] (3) Freckle removal effect test

[0130] Test samples: transdermal compositions prepared in Examples and Comparative Examples;

[0131] Volunteer selection: 260 testers with an average age of 25-35 years old; healthy skin without damage, with many spots on the face; 20 test subjects for each embodiment and comparative example, and the average value of the test results was taken.

[0132] Test method: Use the sample twice a day, morning and evening, for 12 weeks. Apply 0.5g of the transdermal composition to the entire face of the volunteer. Use a Mexameter melanin tester to test the melanin index of a fixed spot before and after using the transdermal composition. The test results are shown in Table 4.

[0133] Melanin reduction rate = (melanin index before using the transdermal composition - melanin index after using the transdermal composition) / melanin index before using the transdermal composition × 100%.

[0134] Table 4. Test results of freckle removal effect

[0135]

[0136]

[0137] (4) Whitening effect test

[0138] Test samples: transdermal compositions prepared in Examples and Comparative Examples;

[0139] Selection of subjects: 260 testers with an average age of 25-35 years old; healthy skin without damage; 20 testers for each embodiment and comparative example, and the average value of the test results was taken.

[0140] Test method: Apply the sample on the face twice a day, morning and night. Apply 0.5g of the test sample on one side of the face at random, and do not use the test sample on the other side of the face as a control group. Test the skin before using the sample (D0) and 56 days after using the sample (D56).

[0141] The test items are:

[0142] 1) Skin melanin meter Mexameter@MX18 is used to detect skin melanin;

[0143] 2) Skin color measuring instrument Colorimeter@CL200 is used to detect skin glossiness.

[0144] The test results are shown in Table 5. The melanin level in the control group increased and the skin glossiness decreased.

[0145] Melanin reduction rate = (melanin index before using the transdermal composition - melanin index after using the transdermal composition) / melanin index before using the transdermal composition × 100%.

[0146] Skin glossiness improvement rate=(skin glossiness after using the transdermal composition-skin glossiness before using the transdermal composition) / skin glossiness before using the transdermal composition×100%.

[0147] Table 5 Whitening effect test results

[0148] Melanin reduction rate % Skin glossiness improvement rate% Example 1 28.1 25.5 Example 2 25.5 23.6 Comparative Example 1 17.6 14.2 Comparative Example 2 16.8 13.6 Comparative Example 3 14.2 12.5 Comparative Example 4 12.5 10.8 Comparative Example 5 13.4 11.5 Comparative Example 6 12.0 12.7 Comparative Example 7 10.8 9.2 Comparative Example 8 8.7 7.5 Comparative Example 9 7.9 6.9 Comparative Example 10 11.6 10.1 Comparative Example 11 15.4 12.5 Control group -8.5 -6.6

[0149] It can be seen from the above performance test results that the transdermal compositions of Examples 1-2 have good whitening and freckle removal effects and good appearance stability, especially the comprehensive performance of Example 1 is the most outstanding, which is mainly because the whitening and freckle removal functional ingredients are designed in the present invention and a specific proportion of plant extracts and fermentation extracts are added.

[0150] However, the comparative examples are significantly inferior to the embodiments in the corresponding performance tests because they do not adopt the necessary technical solutions. In comparative example 1, the mass ratio of the plant extracts is changed. It can be seen that the stability and whitening and freckle removal effects of the composition have decreased to a certain extent, proving that the mass ratio of the plant extracts has a certain degree of influence on the improvement of the comprehensive performance of the composition. In comparative example 2, the ratio of the plant raw materials in the fermented extract is changed. From the results, it can be seen that the stability and whitening and freckle removal effects of the composition are affected, indicating that the raw material ratio in the fermented extract has a certain degree of influence on the improvement of the comprehensive performance of the composition. In comparative example 3, the mass ratio of the composite fermentation agent in the fermented extract is changed. From the results, it can be seen that the stability and whitening and freckle removal effects of the composition are further affected, indicating that the ratio of the composite fermentation agent has a significant effect on the comprehensive performance of the transdermal composition of the present invention. Comparative examples 4 to 6 respectively change the type of a bacterial agent in the composite fermentation agent. From the results, it can be seen that it has a significant effect on the stability and whitening and freckle removal effects of the transdermal composition, and both are significantly reduced. In Comparative Example 7, the ratio of the four substances in the whitening and freckle-removing functional ingredients was changed, and in Comparative Examples 8 and 9, no fermented extract and plant extract were added, respectively. From the results, it can be seen that the stability and whitening and freckle-removing effect of the transdermal composition prepared therefrom decreased, indicating that the four whitening and freckle-removing functional ingredients in the present invention have a synergistic effect, and only when the four substances are combined in a specific ratio can a synergistic effect be produced, thereby maximizing the comprehensive effect of the transdermal composition. In Comparative Example 10, the soybean seed coat extract, the large leaf seaweed extract, and the sea red bean extract were not fermented. From the results, it can be seen that the stability of the transdermal composition prepared therefrom decreased significantly, and the whitening and freckle-removing effect also decreased significantly, indicating that the special arrangement of the present invention to ferment these four raw materials can improve the stability of the transdermal composition and further improve the whitening and freckle-removing effect. Comparative Example 11 changes the mass ratio of the transdermal absorption enhancer. From the results, it can be seen that the whitening and freckle removal effect of the prepared transdermal composition is significantly reduced, indicating that the four whitening and freckle removal functional components in the present invention can only achieve the maximum skin absorption effect in a specific ratio of the transdermal absorption enhancer. The whitening and freckle removal functional components and the transdermal absorption enhancer in the present invention can synergistically improve the transdermal permeability and whitening and freckle removal effect of the transdermal composition. The above experimental results further prove the importance of the technical solution defined in the present invention for its technical effect.

[0151] The above is a preferred embodiment of the present invention. It should be pointed out that for ordinary technicians in this technical field, several improvements and modifications can be made without departing from the principles of the present invention. These improvements and modifications should also be regarded as the scope of protection of the present invention.

Claims

1. A transdermal composition with whitening and freckle removal effects, characterized in that: The raw materials of the transdermal composition include whitening and freckle-removing effective ingredients, which include niacinamide, arbutin, glycerin and water in a mass ratio of (0.2-0.4): (0.5-0.8): (0.1-0.3): (5-10).

2. A transdermal composition with whitening and freckle removal effects according to claim 1, characterized in that: The whitening and freckle-removing effective ingredients include niacinamide, arbutin, glycerin and water in the mass ratio of (0.3-0.4):(0.6-0.8):(0.2-0.3):(5-8).

3. A transdermal composition with whitening and freckle removal effects according to claim 2, characterized in that: The whitening and anti-freckle ingredients include niacinamide, arbutin, glycerin and water in a mass ratio of 0.3:0.7:0.2:

7.

4. A transdermal composition with whitening and freckle removal effects according to claim 1, characterized in that: The raw materials of the transdermal composition also include moisturizers, emulsifiers, fillers, thickeners, transdermal absorption accelerators and water; the whitening and anti-freckle ingredients also include plant extracts and fermented extracts; The transdermal composition comprises the following raw materials in terms of mass percentage: 10-15% whitening and freckle removing ingredients, 5-40% emollient, 0.5-30% emulsifier, 0.1-20% filler, 0.1-10% thickener, 1-3% transdermal absorption enhancer and the balance water; The whitening and anti-freckle ingredients include niacinamide, arbutin, glycerin, water, plant extracts and fermented extracts according to the mass ratio of (0.2-0.4): (0.5-0.8): (0.1-0.3): (5-10): (3-5): 1; The plant extracts include milk thistle extract, coral grass extract and red peony root extract in a mass ratio of (1.5-3.5):(0.5-1):1; The fermented extract is obtained by fermenting soybean seed coat extract, giant algae extract and sea red bean extract in a mass ratio of (0.8-1): (3-4): 1 through a composite fermentation agent; The composite fermentation bacterial agent includes Bacillus alvei, Lactobacillus murinus and Streptomyces oliveri in a mass ratio of (6-10):(2.5-4):

1.

5. A transdermal composition with whitening and freckle removal effects according to claim 4, characterized in that: The emollient is one or more of caprylic capric triglyceride, squalane, avocado oil, shea butter, jojoba oil, glycerin, butylene glycol, hexylene glycol, pentylene glycol, dimethicone, dimethiconol, PEG-11 methyl ether dimethicone, phytosterol, phytosteryl / octyldodecyl lauroyl glutamate, hydrogenated polyisobutene, rapeseed oil, polydecene, soybean oil, olive oil, isododecane, isohexadecane, stearyl alcohol, and behenyl alcohol; The emulsifier is one or more of olive oil PEG-7 esters, PEG-8 caprylic / capric glycerides, sorbitan olivate, polysorbate-20, laureth-23, PEG-40 stearate, steareth-21, a mixture of palmityl alcohol and PEG-75 stearate and glyceryl stearate and steareth-20, polysorbate-80, soy lecithin PC60, a mixture of glyceryl stearate and PEG-75 stearate, poloxamer 407, PEG-30 dipolyhydroxystearate, and ceteareth-25; The filler is one or more of titanium dioxide, mica, boron nitride, polymethylsilsesquioxane, diatomaceous earth, kaolin, cellulose acetate, aluminum starch octyl succinate, talc, barium sulfate, and volcanic ash; The thickener is one or more of hydroxyethyl cellulose, xanthan gum, carbomer, polymer EMT-10, polyacrylate crosspolymer-6, sodium acrylate / sodium acryloyldimethyl taurate copolymer, acryloyldimethyl taurate amine / VP copolymer, acrylate / C10-30 alkyl acrylate crosspolymer, polyvinyl alcohol, gum arabic, and hydroxypropyl starch phosphate.

6. A transdermal composition with whitening and freckle removal effects according to claim 4, characterized in that: The transdermal absorption enhancer includes peppermint oil, laurocapram and N-acetylproline pentanol ester in a mass ratio of (2-4):(8-10):

1.

7. A transdermal composition with whitening and freckle removal effects according to claim 4, characterized in that: The preparation method of the fermentation extract is: S11: mixing soybean seed coat extract, giant algae extract and red bean extract according to a certain proportion to obtain a mixture; S12: adding a composite fermentation agent to the mixture, wherein the inoculation amount of the composite fermentation agent is 6-8wt%, then adding water, wherein the mass of the added water is 15-20 times that of the mixture, continuously introducing oxygen, and fermenting at 28-32° C. for 5-7 days to obtain a fermentation liquid; S13: filtering the fermentation liquid to obtain a filtrate, sterilizing the filtrate at 100-110° C. for 30-60 min, then centrifuging the filtrate, collecting the supernatant, and freeze-drying to obtain a fermentation extract.

8. A method for preparing a transdermal composition having whitening and freckle removal effects according to any one of claims 1 to 7, characterized in that: The following steps are involved: S1: Wetting and dispersing the thickener in water to obtain a mixed solution; S2: adding emollient and filler to the mixed solution of step S1, heating to 60-80°C, and homogenizing at 2500-3500 r / min for 3-5 minutes to fully disperse them; S3: Add an emulsifier to step S2, homogenize at 2500-3500 r / min for 3-5 min to fully emulsify the mixture, add whitening and anti-freckle ingredients and a transdermal absorption accelerator while stirring and cooling to obtain a transdermal composition.

Images