Enhanced whitening cosmetic composition

Abstract

The present invention provides an enhanced whitening cosmetic composition comprising (A) concentrated birch sap and (B) one or more substances selected from arbutin, tranexamic acid, niacinamide, glabridin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate and ascorbyl tetraisopalmitate, wherein the concentrated birch sap is concentrated at a multiple of about 1.05-6 times, preferably about 1.1-5 times, and more preferably about 1.2-4 times.

Description

Technical Field

[0001] The present invention relates to an enhanced whitening cosmetic composition comprising (A) concentrated birch sap and (B) one or more substances selected from the group consisting of arbutin, tranexamic acid, niacinamide, glabridin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate and ascorbyl tetraisopalmitate, wherein the concentrated birch sap is concentrated at a multiple of about 1.05 to 6 times, preferably about 1.1 to 5 times, and more preferably about 1.2 to 4 times. Background Art

[0002] Birch is a deciduous tree in the Betulaceae family. There are currently approximately 100 species worldwide, primarily distributed in the northern and cold temperate zones. Of these, approximately 29 species are found in my country, primarily in Northeast China, Northwest China, North China, and Southwest China. Birches mostly grow in remote mountainous areas with minimal human intervention and free from industrial pollution. Birch sap (also known as birch sap) is the fresh sap that flows out of birch bark when it is scratched or a hole drilled into the trunk. It is colorless or light yellow, free of sediment and impurities, and has a light birch fragrance. Birch sap contains a large amount of sugars, amino acids, vitamins, biotin, cytokinins, trace minerals, aromatic oils, betulin, saponins, and other compounds, and has excellent skin-care benefits such as moisturizing and whitening. Summary of the Invention

[0003] In one aspect, the present invention relates to use of a combination of (A) concentrated birch sap and (B) one or more selected from arbutin, tranexamic acid, niacinamide, glabridin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate, and ascorbyl tetraisopalmitate in a whitening cosmetic composition, wherein the concentrated birch sap is concentrated at a multiple of about 1.05-6 times, preferably about 1.1-5 times, and more preferably about 1.2-4 times.

[0004] In another aspect, the present invention provides an enhanced whitening cosmetic composition comprising (A) concentrated birch sap, and (B) one or more substances selected from the group consisting of arbutin, tranexamic acid, niacinamide, glabridin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate, and ascorbyl tetraisopalmitate, wherein the concentrated birch sap is concentrated at a multiple of about 1.05-6 times, preferably about 1.1-5 times, and more preferably about 1.2-4 times.

[0005] Unexpectedly, the present inventors discovered that compared with the use of concentrated birch sap, arbutin, tranexamic acid, niacinamide, glabridin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate or ascorbyl tetraisopalmitate alone, the combination of concentrated birch sap with arbutin, tranexamic acid, niacinamide, glabridin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate and / or ascorbyl tetraisopalmitate has significantly better whitening effect, which is much higher than the combined effect of the two functions. It is manifested in the ability to inhibit the synthesis and activity of tyrosinase, inhibit the synthesis and transport of melanin, reduce dull skin tone, and make the skin whiter and brighter, which indicates that a synergistic effect occurs between them.

[0006] The birch sap used in the present invention is obtained from the genus Betula (Betulaceae), and can come from four species: Betula alba, Betula pubescens, Betula pendula, and Betula platyphylla. The birch sap is collected by drilling holes at the base of birch trunks between thawing and leafing in early spring. It is colorless, transparent, and free of sediment and debris, and has a refreshing birch fragrance and is rich in nutrients. The birch sap can be commercially obtained and used as is, for example, from Daxing'anling Chaoyue Wild Berry Development Co., Ltd.

[0007] The concentrated birch sap in the present invention is obtained by concentrating the commercially available product. Concentration methods are known in the art, such as heating concentration, low-temperature vacuum concentration, and membrane concentration. In the present invention, concentration is preferably performed by low-temperature freeze concentration or membrane concentration. For example, commercially available birch sap stock solution is fed into a low-temperature drying device, cooled to -40°C to -70°C, and vacuumed to 0.1-30 Pa for low-temperature vacuum concentration, thereby obtaining concentrated birch sap of varying concentration ratios.

[0008] Furthermore, the inventors have discovered that the whitening effect of concentrated birch sap is not linearly correlated with its concentration level, but rather increases and then decreases with increasing concentration ratio. Therefore, controlling the concentration ratio of birch sap is crucial. In the present invention, the concentration ratio of birch sap is controlled to be approximately 1.05-6 times, preferably approximately 1.1-5 times, and more preferably approximately 1.2-4 times.

[0009] The content of the concentrated birch sap is about 10-98% by weight, preferably about 20-98% by weight, more preferably about 30-97% by weight, based on the total weight of the whitening cosmetic composition.

[0010] The component (B) arbutin, tranexamic acid, nicotinamide, glabridin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate or ascorbyl tetraisopalmitate are all known in the art and can be commercially obtained and used in the present invention as they are.

[0011] The total content of component (B) is about 0.0005-30 wt%, preferably about 0.001-10 wt%, more preferably about 0.1-5 wt%, most preferably about 0.5-3 wt%, based on the total weight of the whitening cosmetic composition.

[0012] The whitening cosmetic composition does not contain any added water, but does not exclude the moisture inherently contained in the various components.

[0013] Preferably, the whitening cosmetic composition does not contain chelating agents such as EDTA salt, sodium polyphosphate, sodium metaphosphate, gluconic acid, etc.

[0014] In addition to components (A) and (B) described above, the whitening cosmetic composition may optionally include component (C), an ingredient commonly used in skin care cosmetic compositions. Examples of component (C) include, but are not limited to, vehicles, active ingredients, and excipients. These ingredients are known in the art, and those skilled in the art can select the type and amount of component (C) as needed. For example, the content of component (C) is generally about 0-70% by weight, based on the total weight of the whitening cosmetic composition.

[0015] The vehicle includes, for example, a diluent, a dispersant or a carrier, and examples thereof include, but are not limited to, ethanol, dipropylene glycol, butylene glycol, etc. The content of the vehicle in the cosmetic composition is known in the art, for example, it generally accounts for 0.5-20% of the total weight of component (C).

[0016] Such active ingredients include, for example, emollients, moisturizers, whitening active ingredients, and the like.

[0017] Examples of the emollient include, but are not limited to, one or more of olive oil, macadamia nut oil, sweet almond oil, grape seed oil, avocado oil, corn oil, sesame oil, soybean oil, peanut oil, meadowfoam seed oil, safflower seed oil, rosa canina fruit oil, argania spinosa kernel oil, jojoba seed oil, sunflower seed oil, palm oil, squalane, ethylhexyl palmitate, isopropyl myristate, hydrogenated polyisobutene, isohexadecane, isododecane, diethylhexyl carbonate, dicaprylyl carbonate, isopropyl lauroyl sarcosinate, isononyl isononanoate, hydrogenated polydecene, triethylhexanoin, cetyl ethylhexanoate, bis-diethoxydiglycol cyclohexane 1,4-dicarboxylate, caprylic / capric triglyceride, oleyl erucate, octyldodecyl myristate, octyldodecanol, dimethicone, caprylyl methicone, cetyl dimethicone, cyclopentasiloxane, and the like. Examples of solid emollients include, but are not limited to, cetyl alcohol, stearyl alcohol, cetearyl alcohol, behenyl alcohol, batyl alcohol, lauric acid, myristic acid, palmitic acid, stearic acid, beeswax, candelilla wax, carnauba wax, lanolin, ozokerite, jojoba seed wax, paraffin, microcrystalline wax, hydrogenated rice bran wax, hydrogenated coconut oil glycerides, glyceryl behenate / eicosate, myristyl myristate, bis-diglyceryl polyacyl adipate-2, shea butter, Murumuru seed butter, etc. The content of the emollient in the cosmetic composition is known in the art, for example, it generally accounts for 1-50% of the total weight of component (C).

[0018] Examples of the moisturizing agent include, but are not limited to, one or more of glycerin, diglycerin, butylene glycol, propylene glycol, 1,3-propanediol, dipropylene glycol, 1,2-pentanediol, polyethylene glycol-8, polyethylene glycol-32, methyl gluceth-10, methyl gluceth-20, PEG / PPG-17 / 6 copolymer, glycereth-7, glycereth-26, glyceryl glucoside, PPG-10 methyl gluceth, PPG-20 methyl gluceth, PEG / PPG / polybutylene glycol-8 / 5 / 3 glycerol, sucrose, trehalose, rhamnose, mannose, raffinose, betaine, erythritol, xylitol, urea, glycereth-5 lactate, sodium hyaluronate, hydrolyzed sodium hyaluronate, acetylated sodium hyaluronate, sodium polyglutamate, hydrolyzed sclerotium gum, budding pullulan polysaccharide, tremella polysaccharide, and sour bean seed polysaccharide. The content of the moisturizing agent in the cosmetic composition is known in the art, for example, it generally accounts for 1-30% by weight of the total weight of component (C).

[0019] The whitening active ingredients include, but are not limited to, kojic acid, ascorbyl glucoside, arbutin, tranexamic acid, niacinamide, phytosterols, phytosterol / behenyl alcohol / octyldecyl lauroyl glutamate, phenylethyl resorcinol, turmeric root extract, birch bark extract, ceramide 2, ceramide 3, acetyl phytosphingosine, resveratrol, palmyra palm bark extract, coleus forskohlii root extract, pepper seed extract, ubiquinone, cholesterol, cholesterol stearate, ascorbic acid, ascorbyl dipalmitate, tocopherol (vitamin E), tocopheryl acetate, bisabolol, ascorbyl tetraisopalmitate, pyridoxine dioctanoate, pyridoxine dipalmitate, retinyl palmitate, phytosterol / octyldodecanol lauroyl glutamate, bis-behenyl alcohol / isostearyl alcohol / phytosteryl dimer linoleyl dimer linoleate, phytosteryl macadamia nut oleate, various peptides, various plant extracts, etc. One or more. The content of the whitening active ingredient in the cosmetic composition is known in the art, for example, it generally accounts for 0.01-50% of the total weight of component (C).

[0020] The auxiliary materials include, for example, emulsifiers, thickeners, preservatives, flavors, and the like.

[0021] Examples of the emulsifier include, but are not limited to, cetearyl olivate, sorbitan olivate, polysorbate 60, polysorbate 80, methyl glucose sesquistearate, PEG-20 methyl glucose sesquistearate, PEG-40 hydrogenated castor oil, PPG-26-buteth-26, PEG-4 polyglyceryl-2 stearate, PEG-60 hydrogenated castor oil, steareth-2, steareth-21, PPG-13-decyltetradeceth-24, cetearyl glucoside, PEG-100 stearate, glycerin. Stearate, glyceryl stearate SE, coco-glucoside, ceteareth-25, PEG-40 stearate, polyglyceryl-3 methylglucose distearate, glyceryl stearate citrate, polyglyceryl-10 stearate, polyglyceryl-10 myristate, polyglyceryl-10 dioleate, polyglyceryl-10 laurate, polyglyceryl-10 isostearate, polyglyceryl-10 oleate, polyglyceryl-10 diisostearate, polyglyceryl-6 laurate, polyglyceryl-6 myristate, sucrose stearate, sucrose polystearate, etc. One or more of the following. The content of the emulsifier in the cosmetic composition is known in the art, for example, it generally accounts for 0.5-10% of the total weight of component (C).

[0022] Examples of the thickener include, but are not limited to, one or more of carbomers, acrylic acid (esters) and their derivatives, xanthan gum, gum arabic, polyethylene glycol-14M, polyethylene glycol-90M, succinoglycan, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, and other polymers. The content of the thickener in the cosmetic composition is known in the art, and for example, it generally accounts for 0.1-10% of the total weight of component (C).

[0023] Examples of the preservative include, but are not limited to, one or more of methylparaben, ethylparaben, propylparaben, phenoxyethanol, benzyl alcohol, phenylethyl alcohol, bis(hydroxymethyl)imidazolidinyl urea, potassium sorbate, sodium benzoate, chlorphenesin, sodium dehydroacetate, etc. The content of the preservative in the cosmetic composition is known in the art, for example, it generally accounts for 0.01-30% of the total weight of component (C).

[0024] The whitening cosmetic composition of the present invention can be prepared by any suitable method known in the art. For example, it can be prepared using equipment commonly used in the cosmetics field, such as dissolution tanks, emulsifying pots, dispersers, and delivery pumps. During preparation, the water-soluble substance is first put into the water phase dissolution kettle, and the oil-soluble substance is put into the oil phase dissolution kettle. The temperature of the two kettles is heated to about 80°C. For raw materials that are easy to agglomerate, they can be pre-dispersed with a disperser. After the dissolution is completed, the oil phase and the water phase are transported to the emulsifying pot and homogenized and emulsified for about 5-15 minutes. After the emulsification is completed, the temperature of the material body is lowered to room temperature, and optional flavors, preservatives, etc. are added, and the pH of the product is adjusted as needed. The product can be filled and shipped only after all relevant test indicators are qualified.

[0025] The above preparation method can be deleted or adjusted according to the dosage form requirements. As needed, the whitening cosmetic composition can be made into various dosage forms such as ointment, cream, emulsion, essence, etc. Example

[0026] The present invention will be further described in detail below with reference to the examples. However, it should be understood that these examples and comparative examples are merely provided to illustrate the present invention in more detail and should not be construed as limiting the scope of the appended claims in any form.

[0027] Example 1 :Effects on the expression of genes related to melanin synthesis and transport

[0028] In this example, the effects of birch sap at different concentrations, arbutin, tranexamic acid, and their combination on the expression of genes related to melanin synthesis and transport were tested and compared.

[0029] 1. Birch sap concentration

[0030] The fresh birch sap stock solution purchased from Daxinganling Chaoyue Wild Berry Development Co., Ltd. was input into the low-temperature drying equipment, cooled to -65℃, vacuumed to 0.1Pa, and concentrated to 2 times and 8 times respectively.

[0031] 2. Testing

[0032] Experimental instruments: fluorescence quantitative PCR instrument (Roche), clean bench (Sujing), carbon dioxide incubator (Binder), microplate reader (BIO-TEK), micro-oscillator.

[0033] Experimental reagents and consumables: human primary melanocytes, 6-well plates, melanocyte culture medium, RNA extraction kit, reverse transcription kit, Trizol lysis buffer, etc.

[0034] Sample loading information: The loading amount of a single raw material is one whole portion of the raw material; the compound raw material is half a portion of birch sap raw material plus half a portion of 0.1% other active raw materials.

[0035] The steps for melanocyte-based gene expression analysis are as follows:

[0036] (1) Seeding: Seed cells into 6-well plates at a seeding density of 5E5 / well and incubate overnight in a 37°C, 5% CO2 incubator;

[0037] (2) Drug administration: When the cell plating rate in the 6-well plate reaches about 60%, add the test substance of each group, with 6 replicate wells for each group;

[0038] (3) Sample collection: After 24 h in a 37°C, 5% CO2 incubator, discard the culture medium, add 1 mL of Trizol to each well, pipette and lyse the cells, and then collect the samples;

[0039] (4) PCR detection: RNA was extracted, reverse transcribed into cDNA, and then fluorescence quantitative PCR was performed;

[0040] (5) Analysis: Using 2 -△△CT Methods The results were calculated and statistically analyzed using the T-Test method.

[0041] The test results are shown in the following table:

[0042]

[0043] The above results show that the combination of 2x concentrated birch sap and arbutin or tranexamic acid significantly outperformed birch sap concentrate alone, 2x concentrated birch sap with arbutin or tranexamic acid, and the combination of birch sap concentrate with arbutin or tranexamic acid in inhibiting the transcription of melanin synthesis and transport genes. The transcription of melanin synthesis-related genes TYR and PMEL17, as well as melanin transport-related genes Rab-27a and MyosinVa, was significantly inhibited. When birch sap was concentrated to 8x, the effect of combining it with other active ingredients was significantly weakened, even falling short of the effect of the combination of birch sap concentrate and other active ingredients.

[0044] Example 2: Effects on the expression of melanin synthesis and transport-related proteins

[0045] In this example, the effects of birch sap at different concentrations, its nicotinamide, glabridin, and their combination on the expression of proteins related to melanin synthesis and transport were tested and compared.

[0046] 1. Birch sap concentration

[0047] The fresh birch sap stock solution purchased from Daxinganling Chaoyue Wild Berry Development Co., Ltd. was input into the low-temperature drying equipment, cooled to -65℃, vacuumed to 0.1Pa, and concentrated to 2 times and 8 times respectively.

[0048] 2. Testing

[0049] Experimental instruments: clean bench (Sujing), plate washer (BIO-RAD), microplate reader (BIO-TEK), carbon dioxide incubator (Binder)

[0050] Experimental reagents and consumables: human primary melanocytes, 12-well plates, melanocyte culture medium, ELISA detection kits for different indicators, etc.

[0051] Sample loading information: The loading amount of a single raw material is one whole portion of the raw material; the compound raw material is half a portion of birch sap raw material plus half a portion of 0.1% other active raw materials.

[0052] The test steps are as follows:

[0053] (1) Seeding: The cells were seeded into 12-well culture plates at a seeding density of 2E5 / well and cultured in a 37°C, 5% CO2 incubator. The culture medium was changed every two days.

[0054] (2) Drug administration: When the cell fusion reaches more than 60% again, add different groups of test substances, with 6 replicate wells for each group;

[0055] (3) Sample collection: After 48 h in a 37°C, 5% CO2 incubator, discard the culture medium, add 1 mL of Trizol to each well, pipette and lyse the cells, and then collect the samples;

[0056] (4) Detection: Measure the indicators according to the ELISA kit method;

[0057] (5) Analysis: T-Test method was used for statistical analysis.

[0058] The test results are shown in the following table.

[0059]

[0060] The above results show that the combination of 2x concentrated birch sap and niacinamide or glabridin is significantly more effective in inhibiting melanin synthesis and transporter protein expression than birch sap concentrate alone, 2x concentrated birch sap with niacinamide or glabridin, and significantly better than the combination of birch sap concentrate and niacinamide or glabridin. The expression levels of melanin synthesis-related proteins TYR, TYR1, and TYR2, as well as the melanin transport-related protein Rab-27a, were all significantly reduced. When birch sap was concentrated to 8x, the effect of combining it with other active ingredients was significantly weakened, even less than the effect of the combination of birch sap concentrate and other active ingredients.

[0061] Example 3 :Effects on melanin production in melanocytes

[0062] In this example, the effects of birch sap at different concentrations and ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate or ascorbyl tetraisopalmitate, and their combination on melanin production in melanocytes were tested and compared.

[0063] 1. Birch sap concentration

[0064] The fresh birch sap stock solution purchased from Daxinganling Chaoyue Wild Berry Development Co., Ltd. was input into the low-temperature drying equipment, cooled to -65℃, vacuumed to 0.1Pa, and concentrated to 2 times and 8 times respectively.

[0065] 2. Testing

[0066] Experimental instruments: clean bench (Sujing), carbon dioxide incubator (Binder), water bath, microplate reader (BIO-TEK).

[0067] Experimental reagents and consumables: human primary melanocytes, 12-well plates, melanocyte culture medium, NaOH lysis solution.

[0068] Sample loading information: The loading amount of a single raw material is one whole portion of the raw material; the compound raw material is half a portion of birch sap raw material plus half a portion of 0.1% other active raw materials.

[0069] Experimental methods:

[0070] (1) Inoculation: The cells were seeded into 12-well culture plates at a density of 2E5 / well and cultured in a 37°C, 5% CO2 incubator. The culture medium was changed every two days.

[0071] (2) Drug administration: When the cell fusion reaches more than 60% again, different groups of test substances are added, and a negative control group (no drug) is set up at the same time. Each group has 6 replicate wells.

[0072] (3) Sample collection: After 48 hours in a 37°C, 5% CO2 incubator, discard the culture medium, wash three times with PBS, then add 100 μl of 1 mol / L NaOH, and incubate in an 80°C water bath for 1 hour.

[0073] (4) Detection: After the water bath, centrifuge at 10,000 rpm for 10 minutes, aspirate the supernatant, and measure the absorbance (A) at 460 nm using a microplate reader. Calculate the melanin inhibition rate according to the following formula: Melanin inhibition rate (%) = (A negative control group - A treatment group) / A negative control group * 100%

[0074] (5) Analysis: T-Test method was used for statistical analysis.

[0075] sample Melanin inhibition rate % Birch sap concentrate 10.6％±1.2％ 2x concentrated birch sap 23.6％±2.2％ 8 times concentrated birch sap 12.3％±1.3％ ascorbic acid 3.7％±1.7％ Ascorbyl Glucoside 5.3％±1.9％ Ascorbyl dipalmitate 8.2％±1.2％ Ascorbyl Tetraisopalmitate 3.4％±1.1％ Birch sap extract + ascorbic acid 16.4％±2.2％ Birch sap extract + ascorbyl glucoside 17.7％±1.9％ Birch sap extract + ascorbyl dipalmitate 15.3％±1.4％ Birch sap extract + ascorbyl tetraisopalmitate 15.9％±1.6％ 2x concentrated birch sap + ascorbic acid 25.7％±1.5％ 2x concentrated birch sap + ascorbyl glucoside 28.2％±2.3％ 2x concentrated birch sap + ascorbyl dipalmitate 27.6％±1.2％ 2x concentrated birch sap + ascorbyl tetraisopalmitate 24.8％±1.6％ 8x concentrated birch sap + ascorbic acid 14.6％±1.2％ 8x concentrated birch sap + ascorbyl glucoside 15.1％±1.5％ 8x concentrated birch sap + ascorbyl dipalmitate 13.9％±1.8％ 8x concentrated birch sap + ascorbyl tetraisopalmitate 15.4％±0.9％

[0076] The above results show that in terms of inhibiting melanin production by melanocytes, the combination of 2x concentrated birch sap with ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate, or ascorbyl tetraisopalmitate was significantly more effective than the use of birch sap concentrate alone, 2x concentrated birch sap and ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate, or ascorbyl tetraisopalmitate alone. It was also significantly better than the combination of birch sap concentrate with ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate, or ascorbyl tetraisopalmitate, significantly increasing the inhibition rate of melanin production by melanocytes. When birch sap was concentrated to 8x, the effect of combining it with other active ingredients was significantly weakened, even falling short of the effect of the combination of birch sap concentrate and other active ingredients.

[0077] Example 4 :Effects on melanin production in a 3D melanocyte model

[0078] In this example, the effects of birch sap and ascorbic acid at different concentrations, as well as their combination, on melanin production in a 3D melanocyte model were tested and compared.

[0079] 1. Birch sap concentration

[0080] The fresh birch sap stock solution purchased from Daxinganling Chaoyue Wild Berry Development Co., Ltd. was input into the low-temperature drying equipment, cooled to -65℃, vacuumed to 0.1Pa, and concentrated to 2 times and 8 times respectively.

[0081] 2. Test Method

[0082] Experimental instruments: clean bench (Sujing), carbon dioxide incubator (Binder), UVB irradiator, water bath, microplate reader (BIO-TEK).

[0083] Experimental reagents and consumables: 3D melanin skin model (laboratory-made), model culture medium, NaOH lysis solution.

[0084] Sample loading information: The loading amount of a single raw material is one whole portion of the raw material; the compound raw material is half a portion of birch sap raw material plus half a portion of 0.1% other active raw materials.

[0085] Experimental methods:

[0086] (1) 3D model construction: 3D skin model is constructed using keratinocytes and melanocytes.

[0087] (2) Modeling and drug administration: On day 0 of the model’s ex-factory, UVB irradiation treatment (UVB: 50 mJ / cm 2 ), and then a certain amount of samples were coated on the corresponding model surface, and the model control group was only coated with model culture medium. Each group had 6 replicates, and the samples were coated once a day for a total of 4 days.

[0088] (3) Sampling and testing: After the sample treatment is completed, the model is removed, washed three times with PBS, and placed in a centrifuge tube. Then, 100 μl of 1 mol / L NaOH is added and the mixture is incubated in a water bath at 80 degrees for 1 hour. After the water bath, the mixture is centrifuged at 10,000 rpm for 10 minutes. The supernatant is aspirated and the absorbance (A) is measured at 460 nm using a microplate reader. The melanin inhibition rate is calculated according to the following formula:

[0089] Melanin inhibition rate (%) = (A model control group - A drug group) / A model control group x 100%

[0090] (4) Analysis: T-Test method was used for statistical analysis.

[0091] The test results are shown in the following table.

[0092] sample Melanin inhibition rate % Birch sap concentrate 7.7％±0.6％ 2x concentrated birch sap 18.3％±1.1％ 8 times concentrated birch sap 8.5％±0.7％ ascorbic acid 4.5％±0.8％ Birch sap extract + ascorbic acid 14.6％±1.2％ 2x concentrated birch sap + ascorbic acid 24.2％±1.8％ 8x concentrated birch sap + ascorbic acid 12.9％±1.3％

[0093] The results show that the combination of 2x concentrated birch sap and ascorbic acid significantly outperformed birch sap concentrate, 2x concentrated birch sap and ascorbic acid alone, and significantly outperformed the combination of birch sap concentrate and ascorbic acid. The inhibition rate of melanin in the 3D skin model was significantly increased. However, when birch sap was concentrated to 8x, the effect of combining it with other active ingredients was significantly reduced, even falling short of the effect of the combination of birch sap concentrate and other active ingredients.

[0094] Example 5 : Preparation of whitening essence milk composition

[0095] The formula of the whitening essence composition is shown in the following table:

[0096]

[0097]

[0098] The above-mentioned whitening essence composition is prepared as follows:

[0099] 1. Heat phases A and B to 80°C and dissolve evenly;

[0100] 2. Maintaining the temperature at 80°C, slowly add phase B to phase A while stirring. Stir for 10 minutes, then homogenize at 10,000 rpm for 5 minutes.

[0101] 3. After defoaming, slowly stir and cool to 60 degrees. Add the pre-dispersed phase C to phase AB and homogenize at 10000 rpm / min for 3 minutes;

[0102] 4. Add phase D to phase ABC, stir and cool to 40 degrees before discharging.

[0103] Using a half-face comparison test method, 20 volunteers were tested before and after 8 weeks of use:

[0104] 1) Use the CK-Skincolor instrument to measure the whiteness value L* of the facial skin;

[0105] 2) The melanin index of the skin at the same location was measured using a Maxmeter MX18 reflectance spectrometer.

[0106] 3) VISIA-CR was used to collect facial images of the subjects under different light sources at different time periods. IPP software was used to analyze the skin gloss, whiteness value L*, and visible spot area of ​​the same measurement area on the subjects' faces at different test time points.

[0107] The results showed that using a whitening essence composition containing a combination of 1.5 times concentrated birch juice and arbutin for 8 weeks can increase the facial skin brightness L* value by 5.23%, reduce melanin content by 17.46%, and increase skin brightness by 20.37%. The area of ​​facial pigmentation was significantly reduced in 16 out of 20 subjects.

[0108] The technical solutions of the above-described embodiments are preferred implementations of the present invention. Several improvements and changes may be made without departing from the principles of the present invention. These improvements and changes should also be considered to be within the scope of protection of the present invention.

Claims

1. Use of a combination of (A) concentrated birch sap and B) one or more selected from arbutin, niacinamide, glabridin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate, and ascorbyl tetraisopalmitate in preparing a whitening cosmetic composition, wherein the concentrated birch sap is concentrated 1.2-4 times, and wherein the whitening cosmetic composition does not contain any added water.

2. A whitening cosmetic composition comprising (A) concentrated birch sap, and (B) one or more substances selected from the group consisting of arbutin, niacinamide, glabridin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate, and ascorbyl tetraisopalmitate, wherein the concentrated birch sap is concentrated to a multiple of 1.2 to 4 times, and wherein the whitening cosmetic composition does not contain any added water.

3. The whitening cosmetic composition according to claim 2, wherein the content of the concentrated birch sap of component (A) is 10 to 98% by weight based on the total weight of the whitening cosmetic composition.

4. The whitening cosmetic composition according to any one of claims 2 to 3, wherein the content of component (B) is 0.0005 to 30% by weight, based on the total weight of the whitening cosmetic composition.

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