WO2021017877A1 - 美白化妆品组合物 - Google Patents

美白化妆品组合物 Download PDF

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Publication number
WO2021017877A1
WO2021017877A1 PCT/CN2020/102450 CN2020102450W WO2021017877A1 WO 2021017877 A1 WO2021017877 A1 WO 2021017877A1 CN 2020102450 W CN2020102450 W CN 2020102450W WO 2021017877 A1 WO2021017877 A1 WO 2021017877A1
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Prior art keywords
birch sap
cosmetic composition
whitening
phase
concentrated
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PCT/CN2020/102450
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English (en)
French (fr)
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王莎莎
张正方
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浙江养生堂天然药物研究所有限公司
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Publication of WO2021017877A1 publication Critical patent/WO2021017877A1/zh

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin

Definitions

  • the present invention relates to the use of concentrated birch sap in a whitening cosmetic composition, and a whitening cosmetic composition containing the concentrated birch sap.
  • Birch is a deciduous tree of the birch family. There are currently about 100 species in the world, mainly distributed in the northern temperate zone and the cold temperate zone. Among them, there are about 29 varieties in my country, mainly distributed in the northeast, northwest, north and southwest. Birch trees are mostly grown in remote mountainous areas with little human intervention and no industrial pollution. Birch sap (also called birch sap) is the fresh sap from the birch bark being cut or the trunk is drilled. It is colorless or light yellow, free of precipitation and impurities, and has a light birch fragrance. The birch sap contains a lot of sugars, amino acids, vitamins, biotin, cytokinins, trace mineral elements, aromatic oils, betulin, saponin and other compounds. It has good moisturizing, anti-inflammatory, anti-wrinkle and whitening properties. And other skin care effects.
  • the present invention provides a concentrated birch sap with a concentration factor of about 1.05-8 times, preferably about 1.1-4 times, and more preferably about 1.2-2 times.
  • the present invention relates to the use of concentrated birch sap in a whitening cosmetic composition, wherein the concentration of the concentrated birch sap is about 1.05-8 times, preferably about 1.1-4 times, more preferably about 1.2-2 Times.
  • the concentrated birch sap has good whitening and freckle removal effects, can inhibit the production and transport of melanin, reduce dull skin tone, and make skin whiter and brighter.
  • the birch sap involved in the present invention is obtained from the genus Betula, Betula alba, Betula pubescens, Betula Pendula and Asian white birch (Betula platyphylla). Varieties.
  • the birch sap is a colorless, transparent, no-sediment-free, and no-drug sap that is artificially collected by drilling holes at the base of the trunk of the birch from thawing to early spring.
  • the birch sap is commercially available and used as it is, for example, it can be purchased from Daxinganling Chaoyue Wild Berry Development Co., Ltd.
  • the concentrated birch sap in the present invention is obtained by concentrating the above-mentioned commercial products. Concentration methods are known in the art, such as heating concentration, low-temperature vacuum concentration, membrane concentration and the like. In the present invention, the concentration is preferably carried out by a low-temperature freeze concentration or membrane concentration process. For example, the commercially available birch juice stock solution is input into a low-temperature drying equipment, the temperature is lowered to -40°C to -70°C, and the vacuum is applied to 0.1-30Pa. Concentrated in vacuum at low temperature to obtain concentrated birch sap with different concentration times.
  • the inventors discovered that, compared with the unconcentrated birch sap, the concentrated birch sap has a significantly better whitening effect, which can inhibit the synthesis and activity of tyrosinase and inhibit melanin.
  • the synthesis and transfer of the skin reduces the dull skin tone and makes the skin whiter and brighter.
  • controlling the concentration ratio of birch sap is critical.
  • controlling the concentration ratio of birch sap is about 1.05-8 times, preferably about 1.1-4 times, more preferably about 1.1-2 times.
  • the present invention relates to a whitening cosmetic composition
  • a whitening cosmetic composition comprising the concentrated birch sap described in (A), wherein the concentration of the concentrated birch sap is about 1.05-8 times, preferably about 1.1-4 times, It is more preferably about 1.2-2 times.
  • the whitening cosmetic composition shows significant skin whitening effect.
  • the whitening cosmetic composition of the present invention does not contain chelating agents such as EDTA salt, sodium polyphosphate, sodium metaphosphate, and gluconic acid.
  • the whitening cosmetic composition of the present invention does not contain any added water, but does not exclude the moisture inherently contained in each component.
  • the content of the concentrated birch tree sap in the whitening cosmetic composition is about 18-98% by weight, preferably 20-95% by weight, more preferably 22-90% by weight, most preferably 30-90% by weight, based on the The total weight of the whitening cosmetic composition.
  • the whitening cosmetic composition optionally also contains (B) ingredients commonly used in skin care cosmetics, including vehicles, active ingredients, and auxiliary materials.
  • Component (B) is known in the art, and those skilled in the art can select its type and amount according to needs. For example, the content of component (B) is about 2-82% by weight, based on the total amount of the cosmetic composition. weight.
  • 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, and the like.
  • the content of the vehicle in the cosmetic composition is known in the art, for example, it usually accounts for 0.5-20% of the total weight of component (B).
  • the active ingredients include, for example, emollients, moisturizers, whitening active ingredients and the like.
  • emollient examples include, but are not limited to, olive oil, macadamia nut oil, sweet almond oil, grape seed oil, avocado oil, corn oil, sesame oil, soybean oil, peanut oil, white flower seed oil, safflower seed oil, Dogtooth rose hip oil, argan tree kernel oil, jojoba seed oil, sunflower seed oil, palm tree fruit oil, squalane, ethylhexyl palmitate, isopropyl myristate, hydrogenated polyisobutylene, isotene Hexane, isododecane, diethylhexyl carbonate, dioctyl carbonate, isopropyl lauroyl sarcosine, isononyl isononanoate, hydrogenated polydecene, glycerol tri(ethylhexanoate) , Cetyl alcohol ethyl hexanoate, bis-diethoxy diethylene glycol cyclohexane
  • solid emollients include, but are not limited to, cetyl alcohol, stearyl alcohol, cetearyl alcohol, behenyl alcohol, scylitol, lauric acid, myristic acid, palmitic acid, stearic acid, beeswax, candelilla Tree wax, carnauba wax, lanolin, ozokerite, jojoba seed wax, paraffin wax, microcrystalline wax, hydrogenated rice bran wax, hydrogenated coconut oil glycerides, glyceryl behenate/eicosanate, myristyl alcohol One or more of myristate, bis-diglyceride polyacyl adipate-2, shea butter, and muluxing palm seed butter.
  • the content of the emollient in the cosmetic composition is known in the art, for example, it usually accounts for 1-50% of the total weight of component (B).
  • moisturizer examples include, but are not limited to, glycerin, diglycerin, butylene glycol, propylene glycol, 1,3-propanediol, dipropylene glycol, 1,2-pentanediol, polyethylene glycol-8, polyethylene glycol Alcohol-32, methylglucitol-10, methylglucitol-20, PEG/PPG-17/6 copolymer, glycerol-7, glycerol-26, glycerol glucoside, PPG-10 methyl glucose ether, PPG-20 methyl glucose ether, PEG/PPG/polybutylene glycol-8/5/3 glycerin, sucrose, trehalose, rhamnose, mannose, raffinose, Betaine, erythritol, xylitol, urea, glyceryl polyether-5 lactate, sodium hyaluronate, hydrolyzed sodium hyaluronate, acetyl
  • the whitening active ingredients include, but are not limited to, kojic acid, ascorbyl glucoside, arbutin, tranexamic acid, nicotinamide, phytosterol, phytosterol/behenyl alcohol/octyldecanol lauroyl glutamate, benzene Ethyl resorcinol, turmeric root extract, birch bark extract, ceramide 2, ceramide 3, acetyl sphingosine, resveratrol, palm tree bark extract, coleus forskohlii Root extract, pepper seed extract, ubiquinone, cholesterol, cholesterol stearate, ascorbic acid, ascorbyl dipalmitate, tocopherol (vitamin E), tocopherol acetate, bisabolol, ascorbic acid Isopalmitate, pyridoxine dicaprylate, pyridoxine dipalmitate, retinyl palmitate, phytosterol/octyldodecanol
  • the auxiliary materials include, for example, emulsifiers, thickeners, preservatives, perfumes and the like.
  • emulsifier examples include, but are not limited to, cetearyl oleate, sorbitan oleate, polysorbate-60, polysorbate-80, methylglucose sesquistearic acid Ester, PEG-20 methyl glucose sesquistearate, PEG-40 hydrogenated castor oil, PPG-26-butanol-26, PEG-4 polyglycerol-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 Methyl Glucose Distearate, Glyceryl stearate citrate, polyglyceryl-10 stearate, polyglyceryl-10 myristate, polyglyce
  • the thickener examples include, but are not limited to, carbomers, acrylic acid (ester) and its derivatives, xanthan gum, gum arabic, polyethylene glycol-14M, polyethylene glycol-90M, succinyl poly One or more of high molecular polymers such as sugar, hydroxyethyl cellulose, hydroxypropyl cellulose, and hydroxypropyl methyl cellulose.
  • the content of the thickener in the cosmetic composition is known in the art, for example, it usually accounts for 0.1-10% of the total weight of the component (B).
  • preservatives examples include, but are not limited to, methylparaben, propylparaben, phenoxyethanol, benzyl alcohol, phenethyl alcohol, bis(hydroxymethyl)imidazolidinylurea, potassium sorbate, sodium benzoate, chlorobenzene Glycerol, sodium dehydroacetate, caprylic hydroxamic acid, 1,2-hexanediol, 1,2-pentanediol, p-hydroxyacetophenone, caprylyl glycol, glyceryl caprylate, undecylenic acid
  • the content of the preservative in the cosmetic composition is known in the art, for example, it usually accounts for 0.01-2% of the total weight of the component (B).
  • the whitening cosmetic composition of the present invention can be prepared by any suitable method known in the art.
  • it can be prepared by dissolving tanks, emulsifying pots, dispersers, and delivery pumps commonly used in the cosmetics field.
  • dissolving tanks emulsifying pots, dispersers, and delivery pumps commonly used in the cosmetics field.
  • the water-soluble substance into the water-phase dissolving kettle, and the oil-soluble substance into the oil-phase dissolving kettle, and heat the temperature of the two kettles to about 80°C.
  • the raw materials that are easy to agglomerate they can be mixed with a disperser first. Pre-dispersion. After the dissolution is completed, the oil phase and the water phase are transported to the emulsifying pot for homogenization and emulsification for about 5-15 minutes.
  • the temperature of the material body is reduced to normal temperature, optional flavors, preservatives, etc. are added, and the pH of the product is adjusted as necessary.
  • the products can be filled and shipped only after the relevant test indicators are qualified.
  • the above preparation methods can be deleted or adjusted according to the requirements of dosage forms, and dosage forms such as creams, creams, lotions, essences, etc. can be prepared as needed.
  • Example 1 The effect of birch sap stock and concentrated birch sap on the expression of melanin synthesis and transport related genes
  • the fresh white birch sap stock purchased from Daxinganling Chaoyue Wild Berry Development Co., Ltd. is fed into low-temperature drying equipment, cooled to -65°C, vacuumed to 0.1Pa, and concentrated to 1.05 times, 1.1 times, 1.2 times, 1.5 times, and 2 Times, 4 times, 8 times.
  • Experimental reagents and consumables human primary melanocytes, 6-well plates, melanocyte culture medium, RNA extraction kit, reverse transcription kit, Trizol lysis solution, etc.
  • Inoculation Inoculate cells into a 6-well plate at a seeding density of 5E5/well, and incubate overnight in a 37°C and 5% CO 2 incubator;
  • RNA is extracted, reverse transcribed to cDNA, and then subjected to fluorescence quantitative PCR detection;
  • the 2- ⁇ CT method is used for calculation of the results, and the T-Test method is used for statistical analysis.
  • the birch sap with a concentration of 1.1-4 times significantly inhibits the expression of genes related to melanin synthesis and transport, especially when the concentration is 1.1-2 times, the melanin
  • the expression levels of synthesis-related genes TYR, TYR1, TYR2, PMEL 17, MIFT M, MIFT B, and melanin transport-related genes Rab-27a and Myosin va were all significantly lower than birch sap.
  • Example 2 The effect of birch sap stock and concentrated birch sap on the expression of melanin synthesis and transport related proteins
  • the fresh white birch sap stock purchased from Daxinganling Chaoyue Wild Berry Development Co., Ltd. is fed into low-temperature drying equipment, cooled to -65°C, vacuumed to 0.1Pa, and concentrated to 1.05 times, 1.1 times, 1.2 times, 1.5 times, and 2 Times, 4 times, 8 times.
  • Experimental reagents and consumables human primary melanocytes, 12-well plates, melanocyte culture medium, ELISA test kits with different indicators, etc.
  • test steps are as follows:
  • Inoculation Inoculate in a 12-well culture plate at an inoculation density of 2E5/well, cultivate in an incubator at 37°C and 5% CO2, and change the medium every two days;
  • T-Test method is used for statistical analysis.
  • birch sap with a concentration of 1.1-4 times can significantly inhibit the expression of proteins related to melanin synthesis and transport, especially when the concentration is 1.1-2 times, melanin
  • the expression levels of synthesis-related proteins TYR, TYR1, TYR2, PMEL 17, MIFT M, MIFT B, and melanin transport related proteins Rab-27a and Myosin va are all significantly lower than birch sap.
  • Example 3 The effect of birch sap stock and concentrated birch sap on melanin production in melanocytes
  • the fresh white birch sap stock purchased from Daxinganling Chaoyue Wild Berry Development Co., Ltd. is fed into low-temperature drying equipment, cooled to -65°C, vacuumed to 0.1Pa, and concentrated to 1.05 times, 1.1 times, 1.2 times, 1.5 times, and 2 Times, 4 times, 8 times.
  • Experimental reagents and consumables human primary melanocytes, 12-well plate, melanocyte culture medium, NaOH lysis solution.
  • Inoculation Inoculate in a 12-well culture plate at an inoculation density of 2E5/well, culture in a 37°C, 5% CO2 incubator, and change the medium every two days.
  • melanin inhibition rate (% ) (A negative control group-A administration group)/A negative control group*100%
  • Example 4 The effect of birch sap stock and concentrated birch sap on melanin production in 3D melanocyte model
  • the fresh birch sap stock solution purchased from Daxinganling Chaoyue Wild Berry Development Co., Ltd. is fed into the reverse osmosis circulation device, the operating pressure is controlled at 0.5-5bar, and the operating temperature is controlled at 20-35°C, and circulated until the birch sap is respectively concentrated to 1.1 Times, 1.2 times, 1.5 times, 2 times, 4 times.
  • Experimental reagents and consumables 3D melanin skin model (made in the laboratory), model culture medium, NaOH lysis solution.
  • 3D model construction use keratinocytes and melanocytes to construct a 3D skin model.
  • UVB irradiation treatment (UVB: 50mJ/cm2) is carried out every day, and then a certain amount of samples are respectively coated on the corresponding model surface.
  • the model control group only Cloth model culture medium, each group of 6 replicate holes, smear once a day, the total duration of action is 4 days.
  • Example 5 Preparation of whitening essence milk composition
  • phase ingredient S S1 A 1.2 times concentrated birch sap 0 68.17 To water 68.17 0 To Sodium hyaluronate 0.03 0.03 To Xanthan gum 0.1 0.1 To Allantoin 0.1 0.1 To Methyl paraben 0.2 0.2 To PEG-11 methyl ether polydimethylsiloxane 0.1 0.1 To Panthenol 0.3 0.3 To Cetearyl olive oil and sorbitan olive oil 1 1 To glycerin 4 4 To Butanediol 5 5 To Acrylic (ester) type/vinyl isodecanoate cross-linked polymer 0.3 0.3 B Squalene 0.3 0.3 To Phytosterol/octyldodecanol lauroyl glutamate 0.3 0.3 To Tocopherol (Vitamin E) 0.2 0.2 0.2 To Triglyceride (ethylhexanoate) 3 3 C Polymethylsilsesquioxane 0.5 0.5 To
  • the above whitening essence composition is prepared as follows:
  • Phase A and Phase B are heated to 80°C to dissolve evenly;
  • phase AB After defoaming, slowly stir and cool to 60 degrees, add the pre-dispersed phase C to phase AB, and homogenize for 3 minutes at 10000RPM/min;
  • phase D additive phase D to phase ABC, stir and lower the temperature to 50 degrees;
  • VISIA-CR Using VISIA-CR to collect facial images of subjects under different light sources in different periods, use IPP software to analyze the skin glossiness, whiteness value L* and visible stain area of the same measurement area on the subject's face at different test time points.
  • the above-mentioned whitening cream composition is prepared as follows:
  • Phase A and Phase B are heated to 80°C to dissolve evenly;
  • phase B To phase A under stirring, after stirring for 10 minutes, homogenize at 10000RPM/min for 5 minutes;
  • phase C After defoaming, slowly stir and cool to 60 degrees, add phase C to phase AB, homogenize for 3 minutes at 10000PM/min;
  • Example 7 Whitening emulsion composition
  • the above skin care emulsion composition is prepared as follows:
  • Phase A and Phase B are heated to 80°C to dissolve evenly;
  • phase C After defoaming, slowly stir and cool down to 60 degrees, add phase C to phase AB;

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Abstract

浓缩的桦树汁在美白化妆品组合物中的用途，以及一种包含浓缩的桦树汁的美白化妆品组合物。

Description

美白化妆品组合物 技术领域
本发明涉及浓缩的桦树汁在美白化妆品组合物中的用途，以及一种包含浓缩的桦树汁的美白化妆品组合物。
背景技术
桦树为桦木科落叶乔木，目前全球大约有100个品种，主要分布于北温带和寒温带。其中，我国境内约有29个品种，主要分布在东北、西北、华北和西南等地。桦树大多生长于人为干涉较少、且没有工业污染的边远山区。桦树汁(也称桦树液)是桦树树皮被划开或树干钻孔流出的新鲜汁液，无色或浅黄色，无沉淀及杂质，具有淡淡的桦树清香。桦树汁内含大量的糖类、氨基酸、维生素、生物素、细胞分裂素、微量的矿质元素、芳香油、桦树醇、皂角甙等化合物，具有良好的保湿、抗炎、抗皱、美白等护肤功效。
发明内容
一方面，本发明提供一种浓缩的桦树汁，其浓缩倍数为约1.05-8倍，优选约1.1-4倍，更优选约1.2-2倍。
又一方面，本发明涉及浓缩的桦树汁在美白化妆品组合物中的用途，其中浓缩的桦树汁的浓缩倍数为约1.05-8倍，优选约1.1-4倍，更优选约1.2-2倍。所述浓缩的桦树汁具有良好的美白和祛斑功效，能够抑制黑色素的生成和转运，减少肤色暗沉，使皮肤变得更加白皙、明亮。
本发明中所涉及的桦树汁得自桦木科桦树属，其可来自白桦(Betula alba)、柔毛桦(Betula pubescens)、垂枝桦(Betula Pendula)和亚洲白桦(Betula platyphylla)这四个品种。所述桦树汁为在解冻至早春发叶之间，人工在桦树的树干基部钻孔收集而得的无色透明、无沉淀、无杂物，具有桦树清香营养丰富的汁液。所述桦树汁可商购获得并原样采用，例如可购自大兴安岭超越野生浆果开发有限责任公司。
本发明中的浓缩桦树汁是将上述商购产品浓缩得到的。浓缩方法是本领域已知的，例如加热浓缩、低温真空浓缩、膜浓缩等。在本发明中，优选通过低温冷冻浓缩或膜浓缩工艺进行浓缩，例如，将商购的桦树汁原液输入低温干燥设备，降温至-40℃至-70℃，抽真空至0.1-30Pa而进行低温真空浓缩，从而得到不同浓缩倍数的浓缩桦树汁。
意料不到地，本发明人发现，与未浓缩的桦树汁原液相比，浓缩桦树汁具有显著更好的美白功效，表现为能够抑制酪氨酸酶的合成及其活性，抑制黑色素的合成和转运，减少肤色暗沉，使皮肤变得更加白皙、明亮。
进一步地，本发明人还发现，浓缩桦树汁的美白功效与其浓缩程度并非简单的线性关系，而是随着浓缩倍数增加而呈现先增加后下降的趋势。因此，控制桦树汁的浓缩倍数是 关键的，在本发明中，控制桦树汁的浓缩倍数为约1.05-8倍，优选约1.1-4倍，更优选约1.1-2倍。
另一方面，本发明涉及一种美白化妆品组合物，其包含(A)所述浓缩的桦树汁，其中浓缩的桦树汁的浓缩倍数为约1.05-8倍，优选约1.1-4倍，更优选约1.2-2倍。所述美白化妆品组合物显示了显著的美白皮肤的功效。
在优选的实施方案中，本发明的美白化妆品组合物不包含EDTA盐、多磷酸钠、偏磷酸钠、葡萄糖酸等螯合剂。
在优选的实施方案中，本发明的美白化妆品组合物不包含任何外加的水，但不排除各组分中固有地包含的水分。
所述浓缩桦树汁在所述美白化妆品组合物中的含量为约18-98％重量，优选20-95％重量，更优选22-90％重量，最优选30-90％重量，基于所述美白化妆品组合物的总重量。
除了所述(A)浓缩的桦树汁外，所述美白化妆品组合物还任选地包含(B)护肤化妆品中常用的成分，其中包括媒介物、活性成分和辅料等。组分(B)是本领域已知的，本领域技术人员可根据需要选择其类型和用量，例如，组分(B)的含量为约2-82％重量，基于所述化妆品组合物的总重量。
所述媒介物包括例如稀释剂、分散剂或载体等，其实例包括但不限于乙醇、双丙甘醇、丁二醇等。所述媒介物在所述化妆品组合物中的含量是本领域已知的，例如，其通常占组分(B)总重量的0.5-20％。
所述活性成分包括例如润肤剂、保湿剂、美白活性成分等。
所述润肤剂的实例包括但不限于橄榄油、澳洲坚果油、甜杏仁油、葡萄籽油、鳄梨油、玉米油、芝麻油、大豆油、花生油、白池花籽油、红花籽油、狗牙蔷薇果油、刺阿干树仁油、霍霍巴籽油、向日葵籽油、毛瑞榈果油、角鲨烷、棕榈酸乙基己酯、肉豆蔻酸异丙酯、氢化聚异丁烯、异十六烷、异十二烷、碳酸二乙基己酯、碳酸二辛酯、月桂酰肌氨酸异丙酯、异壬酸异壬酯、氢化聚癸烯、甘油三(乙基己酸)酯、鲸蜡醇乙基己酸酯、双-二乙氧基二甘醇环己烷1,4-二羧酸酯、辛酸/癸酸甘油三酯、油醇芥酸酯、辛基十二醇肉豆蔻酸酯、辛基十二醇、聚二甲基硅氧烷、辛基聚甲基硅氧烷、鲸蜡基聚二甲基硅氧烷、环五聚二甲基硅氧烷等的一种或多种。固体润肤剂的实例包括但不限于鲸蜡醇、硬脂醇、鲸蜡硬脂醇、山嵛醇、鲨肝醇、月桂酸、肉豆蔻酸、棕榈酸、硬脂酸、蜂蜡、小烛树蜡、巴西棕榈蜡、羊毛脂、地蜡、霍霍巴籽蜡、石蜡、微晶蜡、氢化米糠蜡、氢化椰油甘油酯类、甘油山嵛酸酯/二十酸酯、肉豆蔻醇肉豆蔻酸酯、双-二甘油多酰基己二酸酯-2、牛油果树果脂、木鲁星果棕籽脂等中的一种或多种。所述润肤剂在所述化妆品组合物中的含量是本领域已知的，例如其通常占组分(B)总重量的1-50％。
所述保湿剂的实例包括但不限于甘油、双甘油、丁二醇、丙二醇、1,3-丙二醇、双丙甘醇、1,2-戊二醇、聚乙二醇-8、聚乙二醇-32、甲基葡糖醇聚醚-10、甲基葡糖醇聚醚-20、PEG/PPG-17/6共聚物、甘油聚醚-7、甘油聚醚-26、甘油葡糖苷、PPG-10甲基葡糖醚、PPG-20甲基葡糖醚、PEG/PPG/聚丁二醇-8/5/3甘油、蔗糖、海藻糖、鼠李糖、甘 露糖、棉子糖、甜菜碱、赤藓醇、木糖醇、尿素、甘油聚醚-5乳酸酯、透明质酸钠、水解透明质酸钠、乙酰化透明质酸钠、聚谷氨酸钠、水解小核菌胶、出芽短梗酶多糖、银耳多糖、酸豆籽多糖等中的一种或多种。所述保湿剂在所述化妆品组合物中的含量是本领域已知的，例如，其通常占组分(B)总重量的1-30％。
所述美白活性成分，包括但不限于曲酸、抗坏血酸葡糖苷、熊果苷、传明酸、烟酰胺、植物甾醇、植物甾醇/山嵛醇/辛基癸醇月桂酰谷氨酸酯、苯乙基间苯二酚、姜黄根提取物、白桦树皮提取物、神经酰胺2、神经酰胺3、乙酰植物鞘氨醇、白藜芦醇、花榈木树皮提取物、毛喉鞘蕊花根提取物、胡椒籽提取物、泛醌、胆甾醇、胆甾醇硬脂酸酯、抗坏血酸、抗坏血酸二棕榈酸酯、生育酚(维生素E)、生育酚乙酸酯、红没药醇、抗坏血酸四异棕榈酸酯、吡哆素二辛酸酯、吡哆素二棕榈酸酯、视黄醇棕榈酸酯、植物甾醇/辛基十二醇月桂酰谷氨酸酯、双-山嵛醇/异硬脂醇/植物甾醇二聚亚油醇二聚亚油酸酯、植物甾醇澳洲坚果油酸酯、各种肽类、各种植物提取物等中的一种或多种。所述美白成分在所述组合物中的含量是本领域已知的。通常，在本发明组合物中，所述美白活性成分占组分(B)总重量的0.01-30％重量。
所述辅料包括例如乳化剂、增稠剂、防腐剂、香料等。
所述乳化剂的实例包括但不限于鲸蜡硬脂醇橄榄油酸酯、山梨坦橄榄油酸酯、聚山梨醇酯-60、聚山梨醇酯-80、甲基葡糖倍半硬脂酸酯、PEG-20甲基葡糖倍半硬脂酸酯、PEG-40氢化蓖麻油、PPG-26-丁醇聚醚-26、PEG-4聚甘油-2硬脂酸酯、PEG-60氢化蓖麻油、硬脂醇聚醚-2、硬脂醇聚醚-21、PPG-13-癸基十四醇聚醚-24、鲸蜡硬脂基葡糖苷、PEG-100硬脂酸酯、甘油硬脂酸酯、甘油硬脂酸酯SE、椰油基葡糖苷、鲸蜡硬脂醇聚醚-25、PEG-40硬脂酸酯、聚甘油-3甲基葡糖二硬脂酸酯、甘油硬脂酸酯柠檬酸酯、聚甘油-10硬脂酸酯、聚甘油-10肉豆蔻酸酯、聚甘油-10二油酸酯、聚甘油-10月桂酸酯、聚甘油-10异硬脂酸酯、聚甘油-10油酸酯、聚甘油-10二异硬脂酸酯、聚甘油-6月桂酸酯、聚甘油-6肉豆蔻酸酯、蔗糖硬脂酸酯、蔗糖多硬脂酸酯等中的一种或多种。所述乳化剂在所述化妆品组合物中的含量是本领域已知的，例如，其通常占组分(B)总重量的0.5-10％。
所述增稠剂的实例包括但不限于卡波姆类、丙烯酸(酯)类及其衍生物、黄原胶、阿拉伯胶、聚乙二醇-14M、聚乙二醇-90M、琥珀酰聚糖、羟乙基纤维素、羟丙基纤维素、羟丙基甲基纤维素等高分子聚合物中的一种或多种。所述增稠剂在所述化妆品组合物中的含量是本领域已知的，例如，其通常占组分(B)总重量的0.1-10％。
所述防腐剂的实例包括但不限于羟苯甲酯、羟苯丙酯、苯氧乙醇、苯甲醇、苯乙醇、双(羟甲基)咪唑烷基脲、山梨酸钾、苯甲酸钠、氯苯甘醚、脱氢乙酸钠、辛酰羟肟酸、1,2-己二醇、1,2-戊二醇、对羟基苯乙酮、辛甘醇、甘油辛酸酯、十一碳烯酸甘油酯、山梨坦辛酸酯、乙基己基甘油、牡丹根提取物等中的一种或多种。所述防腐剂在所述化妆品组合物中的含量是本领域已知的，例如，其通常占组分(B)总重量的0.01-2％。
本发明的美白化妆品组合物可以通过本领域已知的任何合适的方法制备。例如，使用化妆品领域中常用的溶解槽、乳化锅、分散器、输送泵等设备制备。制备时先将水溶性物 质投入水相溶解釜，将油溶性物质投入油相溶解釜，将两个釜的温度加热至约80℃，其中对于易结块的原料，可先用分散器将其预分散。待溶解完成后将油相和水相输送至乳化锅中，均质乳化约5-15分钟。乳化完成后将料体温度降至常温，加入任选的香精、防腐剂等，并视需要调节产物的pH。相关检测指标都合格后方可灌装出货。以上制备方法可根据剂型要求进行删减或调整，可根据需要制备膏、霜、乳液、精华液等剂型。
实施例
以下结合实施例，对本发明进行进一步详细说明。但是，应当理解为，这些实施例、对比例仅仅是用于更详细地说明本发明，而不应理解为用于以任何形式限制本发明所附权利要求书的范围。
实施例1：桦树汁原液和浓缩桦树汁对黑色素合成、转运相关基因表达的影响
在本实施例中，测试和对比桦树汁原液和不同浓缩倍数的浓缩桦树汁对黑色素合成、转运相关基因表达的影响。
1.桦树汁的浓缩
将购自大兴安岭超越野生浆果开发有限责任公司的新鲜白桦树汁原液输入低温干燥设备，降温至-65℃，抽真空至0.1Pa，分别浓缩至1.05倍、1.1倍、1.2倍、1.5倍、2倍、4倍、8倍。
2.测试
实验仪器：荧光定量PCR仪(Roche)、超净工作台(苏净)、二氧化碳培养箱(Binder)、酶标仪(BIO-TEK)、微量振荡器。
实验试剂与耗材：人原代黑素细胞、6孔板、黑素细胞培养液、RNA提取试剂盒、反转录试剂盒、Trizol裂解液等。
基于黑素细胞的基因表达分析步骤如下：
(1)接种：以5E5/孔的接种密度，接种细胞至6孔板中，在37℃和5％CO 2培养箱中孵育过夜；
(2)给药：待6孔板中细胞铺板率达到60％左右时，加入各组别的受试物，每组设6个复孔；
(3)收样：在37℃和5％CO 2培养箱中24小时后，弃掉培养液，每孔加入1mL Trizol，吹打裂解细胞后，收样；
(4)PCR检测：提取RNA，反转录至cDNA后，进行荧光定量PCR检测；
(5)分析：采用2 -△△CT方法进行结果计算，采用T-Test方法进行统计分析。
测试结果如下表所示：
Figure PCTCN2020102450-appb-000001
Figure PCTCN2020102450-appb-000002
注：*表示与原汁相比为显著，P值小于0.05；**表示与原汁相比为极显著，P值小于0.01。
以上结果表明，与桦树汁原汁相比，浓缩倍数为1.1-4倍的桦树汁显著抑制了与黑色素合成及转运相关基因的表达，尤其是当浓缩倍数为1.1-2倍时，黑色素合成相关基因TYR、TYR1、TYR2、PMEL 17、MIFT M、MIFT B以及黑色素转运相关基因Rab-27a、Myosin va的表达量均非常显著地低于桦树汁原汁。
实施例2：桦树汁原液和浓缩桦树汁对黑色素合成、转运相关蛋白表达的影响
在本实施例中，测试和对比桦树汁原液和不同浓缩倍数的桦树汁对与黑色素合成和转运相关的蛋白表达的影响。
1.桦树汁的浓缩
将购自大兴安岭超越野生浆果开发有限责任公司的新鲜白桦树汁原液输入低温干燥设备，降温至-65℃，抽真空至0.1Pa，分别浓缩至1.05倍、1.1倍、1.2倍、1.5倍、2倍、4倍、8倍。
2.测试
实验仪器：超净工作台(苏净)、洗板机(BIO-RAD)、酶标仪(BIO-TEK)、二氧化碳培养箱(Binder)
实验试剂及耗材：人原代黑素细胞、12孔板、黑素细胞培养液、不同指标的ELISA检测试剂盒等。
测试步骤如下：
(1)接种：以2E5/孔的接种密度，接种于12孔培养板中，在37℃和5％CO2培养箱中培养，每两天换一次培养基；
(2)给药：待细胞融合再次达60％以上时，加入不同组别的受试物，每组设6个复孔；
(3)收样：在37℃和5％CO 2培养箱中48小时后，弃掉培养液，每孔加入1mL Trizol，吹打裂解细胞后，收样；
(4)检测：按照ELISA试剂盒的测定方法进行指标测定；
(5)分析：采用T-Test方法进行统计分析。
测试结果如下表所示。
Figure PCTCN2020102450-appb-000003
注：*表示与原汁相比为显著，P值小于0.05；**表示与原汁相比为极显著，P值小于0.01。
以上结果表明，与桦树汁原汁相比，浓缩倍数为1.1-4倍的桦树汁能够显著抑制与黑色素合成及转运相关蛋白的表达，尤其是当浓缩倍数为1.1-2倍时，黑色素合成相关蛋白TYR、TYR1、TYR2、PMEL 17、MIFT M、MIFT B以及黑色素转运相关蛋白Rab-27a、Myosin va的表达量均非常显著地低于桦树汁原汁。
实施例3：桦树汁原液和浓缩桦树汁对黑素细胞中黑色素生成的影响
在本实施例中，测试和对比桦树汁原液和不同浓缩倍数的桦树汁对黑素细胞中黑色素生成的影响。
1.桦树汁的浓缩
将购自大兴安岭超越野生浆果开发有限责任公司的新鲜白桦树汁原液输入低温干燥设备，降温至-65℃，抽真空至0.1Pa，分别浓缩至1.05倍、1.1倍、1.2倍、1.5倍、2倍、4倍、8倍。
2.测试
实验仪器：超净工作台(苏净)、二氧化碳培养箱(Binder)、水浴锅、酶标仪(BIO-TEK)。
实验试剂及耗材：人原代黑素细胞、12孔板、黑素细胞培养液、NaOH裂解液。
实验方法：
(1)接种：以2E5/孔的接种密度，接种于12孔培养板中，37℃，5％CO2培养箱培养，每两天换一次培养基。
(2)给药：待细胞融合再次达60％以上时，加入不同组别的受试物，同时设置阴性对照组(不加药)每组设6个复孔。
(3)收样：37℃，5％CO2培养箱48小时后，弃掉培养液，用PBS液洗3遍，然后加入100ul浓度1mol/L NaOH，80度水浴1小时。
(4)检测：水浴结束后在10000rpm条件下离心10分钟，吸取上清液用酶标仪在460nm下测定吸光值(A)，并根据下式计算黑素抑制率：黑素抑制率(％)＝(A阴性对照组-A给药组)/A阴性对照组*100％
(5)分析：T-Test方法进行统计分析。
测试结果如下表所示。
Figure PCTCN2020102450-appb-000004
注：*表示与原汁相比为显著，P值小于0.05；**表示与原汁相比为极显著，P值小于0.01。
以上测试结果表明，与桦树汁原液相比，浓缩倍数为1.1-4倍的桦树汁能够极显著地抑制黑素细胞中黑色素的生成。
实施例4：桦树汁原液和浓缩桦树汁对3D黑素细胞模型中黑色素生成的影响
在本实施例中，测试和对比桦树汁原液和不同浓缩倍数的桦树汁对3D黑素细胞模型中黑色素生成的影响。
1.桦树汁的浓缩
将购自大兴安岭超越野生浆果开发有限责任公司的新鲜白桦树汁原液输入反渗透循环装置，运行压力控制在0.5-5bar，运行温度控制在20-35℃，循环，直至桦树汁分别浓缩至1.1倍、1.2倍、1.5倍、2倍、4倍。
2.测试方法
实验仪器：超净工作台(苏净)、二氧化碳培养箱(Binder)、UVB辐照仪、水浴锅、酶标仪(BIO-TEK)。
实验试剂及耗材：3D黑素皮肤模型(实验室自制)，模型培养液、NaOH裂解液。
实验方法：
(1)3D模型构建：用角质细胞与黑素细胞构建3D皮肤模型。
(2)造模及给药：在模型出厂即0天时，每天进行UVB辐照处理(UVB：50mJ/cm2)，然后将一定量的样品分别涂布于相应的模型表面，模型对照组只涂布模型培养液，每组6 个复孔，每天涂抹一次，总作用时长4天。
(3)收样与检测：样品作用结束后，取出模型，用PBS清洗3次后置于离心管中，然后加入100ul浓度1mol/L NaOH，80度水浴1小时，水浴结束后在10000rpm条件下离心10分钟，吸取上清用酶标仪在460nm下测定吸光值(A)，并根据下式计算黑素抑制率：
黑素抑制率(％)＝(A模型对照组-A给药组)/A模型对照组*100％
(4)分析：T-Test方法进行统计分析。
测试结果如下表所示。
Figure PCTCN2020102450-appb-000005
注：*表示与原汁相比为显著，P值小于0.05；**表示与原汁相比为极显著，P值小于0.01。
以上测试结果表明，与桦树汁原液相比，浓缩倍数为1.1-4倍的桦树汁能够极显著地抑制3D黑素皮肤模型中黑色素的生成。
实施例5：美白精华乳组合物的制备
所述美白精华乳组合物的配方如下表所示：
相 成分 S S1
A 1.2倍浓缩桦树汁 0 68.17
  水 68.17 0
  透明质酸钠 0.03 0.03
  黄原胶 0.1 0.1
  尿囊素 0.1 0.1
  羟苯甲酯 0.2 0.2
  PEG-11甲醚聚二甲基硅氧烷 0.1 0.1
  泛醇 0.3 0.3
  鲸蜡硬脂醇橄榄油酸酯和山梨坦橄榄油酸酯 1 1
  甘油 4 4
  丁二醇 5 5
  丙烯酸(酯)类/异癸酸乙烯酯交联聚合物 0.3 0.3
B 鲨肝醇 0.3 0.3
  植物甾醇/辛基十二醇月桂酰谷氨酸酯 0.3 0.3
  生育酚(维生素E) 0.2 0.2
  甘油三(乙基己酸)酯 3 3
C 聚甲基硅倍半氧烷 0.5 0.5
  聚二甲基硅氧烷 1 1
D 氨丁三醇 0.4 0.4
E 抗坏血酸 2 2
  1.2倍浓缩桦树汁 0 13
  水 13 0
上述美白精华组合物如下制备：
1.A、B相分别加热至80度溶解均匀；
2.保持80度，搅拌下将B相缓慢加入A相，搅拌10分钟后，在10000RPM/分钟下均质5分钟；
3.消泡后缓慢搅拌降温至60度，将预先分散好的C相加入AB相中，在10000RPM/分钟下均质3分钟；
4.将D相加入ABC相中，搅拌下降温至50度；
5.将预先混合均匀的E相加入ABCD相中，搅拌均匀降温至40度即可出料。
采用半脸对照的测试方法，在使用产品前和使用产品8周后分别对20名志愿者进行如下测试：
1)利用Colorimeter仪器测定颜面部皮肤的L*；
2)利用Maxmeter MX18反射光谱仪测量相同位置皮肤的黑色素和红色素变化情况。
3)通过VISIA-CR采集受试者不同时期不同光源下的面部图形，利用IPP软件分析受试者面部不同测试时间点同一测量区域的皮肤光泽度、白度值L*和可见色斑面积。
结果显示，与美白精华组合物S相比，使用S1美白精华8周能够提升面部皮肤亮度L*值3.54％，降低黑色素含量15.86％，降低血红素含量19.8％，提升皮肤亮度18.53％。
实施例6：美白面霜组合物的制备
所述美白面霜组合物的配方如下表所示：
Figure PCTCN2020102450-appb-000006
Figure PCTCN2020102450-appb-000007
上述美白面霜组合物如下制备：
1.A、B相分别加热至80度溶解均匀；
2.保持80度，搅拌下将B相缓慢加入A相，搅拌10分钟后，在10000RPM/分钟下均质5分钟；
3.消泡后缓慢搅拌降温至60度，将C相加入AB相中，在10000PM/分钟下均质3分钟；
4.搅拌下降温至50度，将D相除氢氧化钾外的组分加入ABC相中，搅拌均匀后，用氢氧化钾调节体系的pH值在6.5-6.8；
5.将E相加入上述膏体中，搅拌降温至40度即可出料。
20名受试者使用上述配方的面霜4周后，对使用情况进行主观评估。结果有18人反映肤色暗沉得到明显改善，皮肤整体亮度和白皙度显著提升。其中有16人反映局部斑块明显淡化，肤色变得更加均匀。
实施例7：美白乳液组合物
所述美白乳液组合物的配方如下表所示：
Figure PCTCN2020102450-appb-000008
Figure PCTCN2020102450-appb-000009
上述护肤乳液组合物如下制备：
1.A、B相分别加热至80度溶解均匀；
2.保持80度，搅拌下将B相缓慢加入A相，搅拌10分钟后，在10000RPM/分钟下均质5分钟；
3.消泡后缓慢搅拌降温至60度，将C相加入AB相中；
4.搅拌下降温至50度，将预先混合均匀的D相加入ABC相中，搅拌均匀；
5.将E相加入上述膏体中，搅拌降温至40度即可出料。
以上所述实施例的技术方案是本发明优选实施方式，在不脱离本发明原理的前提下还可以进行若干改进和变换，这些改进和变化也应视为在本发明的保护范围内。

Claims (6)

  1. 一种浓缩的桦树汁，其浓缩倍数为1.05-8倍，优选1.1-4倍，更优选1.2-2倍。
  2. 浓缩的桦树汁在美白化妆品组合物中的用途，其中所述浓缩的桦树汁的浓缩倍数为1.05-8倍，优选1.1-4倍，更优选1.2-2倍。
  3. 一种美白化妆品组合物，其包含(A)浓缩的桦树汁，其中所述浓缩的桦树汁的浓缩倍数为1.05-8倍，优选1.1-4倍，更优选1.2-2倍。
  4. 权利要求3的美白化妆品组合物，其包含18-98％重量,优选20-95％重量，更优选22-90％重量,最优选30-90％重量的浓缩的桦树汁，基于所述美白化妆品组合物的总重量。
  5. 权利要求3或4的美白化妆品组合物，其中所述组合物不包含任何外加的水。
  6. 权利要求3-5任何一项的美白化妆品组合物，其中所述组合物还包含(B)护肤化妆品中常用的成分。
PCT/CN2020/102450 2019-07-30 2020-07-16 美白化妆品组合物 WO2021017877A1 (zh)

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CN110731925A (zh) * 2019-07-30 2020-01-31 浙江养生堂天然药物研究所有限公司 美白化妆品组合物
CN110731976B (zh) * 2019-07-30 2024-02-06 浙江养生堂天然药物研究所有限公司 防脱生发组合物
CN110731927A (zh) * 2019-07-30 2020-01-31 浙江养生堂天然药物研究所有限公司 增强的美白化妆品组合物
CN110731973A (zh) * 2019-07-30 2020-01-31 浙江养生堂天然药物研究所有限公司 具有抗炎功效的皮肤外用组合物
CN110876760B (zh) * 2019-11-28 2022-09-30 浙江养生堂天然药物研究所有限公司 具有促进伤口愈合和/或疤痕修复功效的皮肤外用组合物
CN112754010A (zh) * 2021-01-26 2021-05-07 呼伦贝尔市林海森林经营管理有限公司 一种桦树汁浓缩液的制备方法

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