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WO2018196482A1 - 护肤化妆品组合物 - Google Patents

护肤化妆品组合物 Download PDF

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Publication number
WO2018196482A1
WO2018196482A1 PCT/CN2018/078208 CN2018078208W WO2018196482A1 WO 2018196482 A1 WO2018196482 A1 WO 2018196482A1 CN 2018078208 W CN2018078208 W CN 2018078208W WO 2018196482 A1 WO2018196482 A1 WO 2018196482A1
Authority
WO
WIPO (PCT)
Prior art keywords
composition
weight
skin care
birch
betulin
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/CN2018/078208
Other languages
English (en)
French (fr)
Inventor
郑小微
胡柳
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Yang Sheng Tang (shanghai) Cosmetic R & D Co Ltd
Original Assignee
Yang Sheng Tang (shanghai) Cosmetic R & D Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Yang Sheng Tang (shanghai) Cosmetic R & D Co Ltd filed Critical Yang Sheng Tang (shanghai) Cosmetic R & D Co Ltd
Priority to EP18792071.5A priority Critical patent/EP3510993A4/en
Priority to JP2019500558A priority patent/JP6608561B2/ja
Priority to US16/344,087 priority patent/US20190240134A1/en
Priority to EP22169439.1A priority patent/EP4062900A3/en
Priority to KR1020197010309A priority patent/KR102198054B1/ko
Publication of WO2018196482A1 publication Critical patent/WO2018196482A1/zh
Anticipated expiration legal-status Critical
Priority to US17/110,920 priority patent/US20210093535A1/en
Ceased legal-status Critical Current

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Classifications

    • 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
    • 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
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63—Steroids; Derivatives thereof
    • 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
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • 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
    • 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
    • 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
    • A61Q19/08—Anti-ageing preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/30—Characterized by the absence of a particular group of ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/30—Characterized by the absence of a particular group of ingredients
    • A61K2800/31—Anhydrous

Definitions

  • the present invention relates to a skin care cosmetic composition
  • a skin care cosmetic composition comprising birch juice, birch bark extract, and optional ingredients commonly used in skin care cosmetics, but does not comprise water which is usually added as a separate component.
  • Betulin also known as birch brain, is found in birch bark with a content of 10-35%. It is a very valuable natural product. It has anti-UV, anti-inflammatory, whitening and skin barriers. It is often used in cosmetics. In food and drug development, such as cosmetics Limi The Age of Innocenc, True Hydration 24H Gel Cream (GoodSkin Labs) and oOlution, but the above products are not satisfactory. At present, many drugs such as safflower extract, salvia miltiorrhiza extract, ginkgo biloba extract and other conventional oral and intravenous routes can significantly improve skin problems, but the topical effects cannot be achieved after topical application. Topical drugs are affected by many factors.
  • the present invention attempts to provide a technique for significantly improving the transdermal absorption rate of betulin in a product, thereby obtaining a function different from the prior art, which can better exert the effects of betulin, hydration, whitening and wrinkle resistance.
  • Skin care composition attempts to provide a technique for significantly improving the transdermal absorption rate of betulin in a product, thereby obtaining a function different from the prior art, which can better exert the effects of betulin, hydration, whitening and wrinkle resistance.
  • a skin care cosmetic composition in water The present inventors have surprisingly found that after topical application of the skin care cosmetic composition, the skin care cosmetic composition can significantly and effectively increase the transdermal absorption rate of the betulin in the skin compared to a similar formulation of added water, thereby enabling Good to play its moisturizing, whitening, anti-wrinkle and other effects.
  • the present invention has been completed based on the above findings.
  • the present invention provides a skin care cosmetic composition
  • a skin care cosmetic composition comprising (A) 30-99% by weight of birch sap, (B) 0.5 ppm-5% by weight of birch bark extract based on betulin, and (C)
  • a component commonly used in skin care cosmetics wherein the skin care cosmetic composition does not contain water which is usually added as a separate component.
  • the skin care cosmetic composition of the present invention has improved skin care effects such as moisturizing, whitening, and wrinkle resistance.
  • the skin care cosmetic composition of the present invention does not contain any added water, but does not exclude the moisture inherent in the birch juice used and the small or trace amount of water inevitably introduced in other ingredients.
  • a chelating agent such as EDTA salt, sodium polyphosphate, sodium metaphosphate or gluconic acid is not added to the skin care cosmetic composition of the present invention.
  • the present invention also relates to a method of increasing the transdermal absorption rate of betulin, comprising adding birch juice to a skin care cosmetic composition comprising birch bark extract but no water, wherein the birch bark extract It contains 0.05-99.95% by weight of betulin.
  • the method can significantly increase the transdermal absorption rate of betulin, thereby achieving a significantly improved skin care effect.
  • the invention also relates to the use of a combination of birch and birch bark extract in a skin care cosmetic composition comprising no water, wherein the birch bark extract comprises from 0.05 to 99.95% by weight of betulin.
  • the birch trees involved in the present invention belong to the birch family of birch, and can be derived from three varieties of Betula alba, Betula Pendula and Betula platyphylla.
  • the birch sap according to the present invention is a colorless, transparent, non-precipitating, non-mesh material which is obtained by drilling and arranging in the base of the trunk of the birch tree between the thawing and early spring leaves, and has a nutrient-rich juice of birch scent. .
  • the birch juice is commercially available and used as it is, for example, from Daxinganling Beyond Wild Berry Development Co., Ltd.
  • the skin care cosmetic composition of the present invention may comprise 30-99% by weight of birch juice, preferably 50-95% by weight, more preferably 60-90% by weight, based on the total weight of the composition.
  • the birch bark extract of the present invention is obtained by extracting one or more kinds of soft bark of birch, including but not limited to water, methanol, ethanol, diethyl ether, petroleum ether, chloroform, benzene and the like. Generally, the content of betulin in the extract may vary from 0.05 to 99.95%, depending on the solvent employed and the intended use.
  • the birch bark extract is usually in the form of a powder and is commercially available, for example, from Chengdu Jianteng Biotechnology Co., Ltd.
  • the skin care cosmetic composition of the present invention may comprise from 0.5 ppm to 5% by weight of birch bark extract, preferably from 0.001 to 3% by weight, more preferably from 0.01 to 2% by weight, based on the total weight of the composition, of betulin. Calculation.
  • the skin care cosmetic composition of the present invention also optionally contains the components commonly used in the component (C) skin care cosmetic, including vehicles, active ingredients, excipients and the like.
  • Component (C) is known in the art, and those skilled in the art can specifically select the type and amount thereof as needed.
  • component (C) is present in the composition of the invention in an amount of from 0 to 70% by weight.
  • the vehicle is, for example, a diluent, a dispersing agent or a carrier or the like. All of these vehicles are known in the art, and those skilled in the art can specifically select their type and amount as needed.
  • the vehicle includes, but is not limited to, ethanol, dipropylene glycol, butylene glycol, and the like.
  • the vehicle will comprise from 0.5% to 20% by weight based on the total weight of component (C).
  • the active ingredients include, for example, emollients, humectants, skin conditioners, and the like. All of these active ingredients are known in the art, and those skilled in the art can specifically select their type and amount as needed.
  • the emollient includes, but is 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, Dog tooth rose hip oil, thorn a dry tree seed oil, jojoba seed oil, sunflower seed oil, maurai palm oil, squalane, ethyl hexyl palmitate, isopropyl myristate, hydrogenated polyisobutylene, different ten Hexane, isododecane, diethylhexyl carbonate, dioctyl carbonate, isopropyl lauroyl sarcosinate, isodecyl isononanoate, hydrogenated polydecene, tris(ethylhexanoate) , cetyl ethylhexanoate, bis-diethoxydiglycol cyclohexane 1,
  • Solid emollients include, but are not limited to, cetyl alcohol, stearyl alcohol, cetearyl alcohol, behenyl alcohol, squalyl alcohol, lauric acid, myristic acid, palmitic acid, stearic acid, beeswax , candelilla wax, carnauba wax, lanolin, ozoke wax, jojoba seed wax, paraffin wax, microcrystalline wax, hydrogenated rice bran wax, hydrogenated coconut glyceride, glyceryl behenate/icoic acid ester, meat One or more of soybean croton myristate, bis-diglycerol polyacyl adipate-2, avocado, and sage.
  • the level of the emollient in the composition is known in the art. Usually, in the composition of the present invention, the emollient is from 1 to 50% by weight based on the total weight of the component (C).
  • the humectant includes, but is not limited to, glycerin, diglycerin, butylene glycol, propylene glycol, 1,3-propanediol, dipropylene glycol, 1,2-pentanediol, polyethylene glycol-8, polyethylene glycol Alcohol-32, methylglycol-10, methylglycol-20, PEG/PPG-17/6 copolymer, glycerol polyether-7, glycerol polyether-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, glycerol polyether-5 lactate, sodium hyaluronate, sodium polyglutamate, hydrolyzed nucle
  • the skin conditioning agent may include active ingredients for moisturizing, anti-wrinkle, ecchymosis, acne, oil control, etc., including but not limited to kojic acid, ascorbic acid, ascorbyl glucoside, arbutin, tranexamic acid, nicotinamide, Phytosterols, phytosterols/behenyl alcohol/octyl decyl laurate laurate glutamate, phenethyl resorcinol, turmeric root extract, birch bark extract, ceramide 2, ceramide 3, acetyl plant Sphingosine, resveratrol, flower bark extract, coleus, extract, pepper seed extract, ubiquinone, cholesterol, cholesterol stearate, ascorbyl dipalmitate, Tocopherol (vitamin E), tocopheryl acetate, bisabolol, ascorbyl tetraisopalmitate, pyridoxine dicaprylate, pyridoxine dip
  • excipients include, but are not limited to, emulsifiers, thickeners, preservatives, perfumes, and the like. All of these excipient ingredients are known in the art, and those skilled in the art can specifically select their type and amount as needed.
  • the emulsifier includes, but is not limited to, cetearyl oleate, sorbitan oligoate, polysorbate-60, polysorbate-80, methyl glucose stearate Ester, PEG-20 methylglucose sesquistearate, PEG-40 hydrogenated castor oil, PPG-26-butanol-26, PEG-4 polyglycerol-2 stearate, PEG-60 hydrogenation Castor oil, stearyl-2, stearyl-21, PPG-13-decyltetradecyl polyether-24, cetearyl glucoside, PEG-100 stearate, glycerol Stearate, glyceryl stearate SE, coco glucoside, ceteareth-25, PEG-40 stearate, polyglyceryl-3 methyl glucose distearate, Glyceryl stearate citrate, polyglyceryl-10 stearate, polyglycerol-10 myristate, polyglycerol
  • the thickeners include, but are not limited to, carbomers, acrylates and derivatives thereof, 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 amount of the thickening agent in the composition is known in the art.
  • the thickener accounts for 0.1 to 10% by weight based on the total weight of the component (C).
  • the preservative includes, but is not limited to, methylparaben, propylparaben, phenoxyethanol, benzyl alcohol, phenethyl alcohol, bis(hydroxymethyl)imidazolidinyl urea, potassium sorbate, sodium benzoate, chlorobenzene
  • the amount of the preservative in the composition is known in the art.
  • the preservative accounts for 0.01 to 2% by weight based on the total weight of the component (C).
  • the skin care cosmetic compositions of the present invention can be prepared by any suitable method known in the art. For example, it is prepared using equipment such as a dissolution tank, an emulsifying pot, a disperser, a transfer pump, and the like which are commonly used in the field of cosmetics.
  • the water-soluble substance is first put into the aqueous phase dissolution kettle, the oil-soluble substance is put into the oil phase dissolution kettle, and the temperature of the two kettles is heated to about 80 ° C, wherein for the agglomerated raw material, the disperser can be used first. Pre-dispersed.
  • the oil phase and the aqueous phase are transferred to an emulsification pot, and the mixture is homogenized and emulsified for about 5-15 minutes.
  • the temperature of the body is lowered to normal temperature, optional flavors, preservatives, etc. are added, and the pH of the product is adjusted as needed.
  • the relevant test indicators are all qualified before they can be filled and shipped.
  • the above preparation method can be deleted or adjusted according to the requirements of the dosage form, and the dosage forms such as cream, lotion, essence and cleansing can be prepared as needed.
  • the present invention provides a skin care composition having a formulation, preferably a toner, which exhibits excellent skin care benefits such as moisturizing, whitening and anti-wrinkle.
  • Example 1 Transdermal absorption rate of betulin in different systems
  • birch sap used in this article was purchased from Daxinganling Beyond Wild Berry Development Co., Ltd.
  • the birch bark extract used in this article was purchased from Chengdu Jianteng Biotechnology Co., Ltd.
  • Test method A commercially available depilated pig skin was cut into 2.5 cm x 2.5 cm pieces. 1 g of the above formula 1-4 was applied to each piece of pig skin, and placed in a constant temperature and humidity incubator at 30 ° C and a relative humidity (RH) of 50 ⁇ 5% for 24 hours. Six parallel experiments were performed in each group. After that, the pig skin was rinsed, chopped, and ultrasonically extracted with methanol for 30 minutes. The extracts were combined and concentrated to 5.0 ml under reduced pressure. Centrifuged, and the supernatant was filtered and filtered through a filter to be injected into high performance liquid chromatography. The test was carried out in the instrument, and the content of betulin was calculated by an external standard method. The test results are shown in Table 2 below.
  • Example 2 Liquid skin care composition of the present invention 1 vs. control liquid skin care composition 1-2
  • composition 1 of the present invention and the control composition 1-2 prepared above were used for experiments to examine their respective moisturizing effects.
  • Control composition 1 of the invention Control composition 1
  • Control composition 2 0 24.31% 25.76% 24.83% 7 47.12% abc 32.15% ac 38.52% ab 14 46.45% abc 33.47% ac 36.78% ab
  • the above results showed that the skin moisturizing performance of the composition 1 of the present invention was improved by 91% after 14 days of continuous use, the skin moisturizing performance of the control composition 1 was improved by 30%, and the skin moisturizing performance of the control composition 2 was improved by 48%. . Therefore, the composition 1 of the present invention has a better moisturizing effect than the control composition 1-2, thereby indicating that the birch and birch bark extracts exhibit a certain synergistic effect.
  • Example 3 Emulsion skin care composition of the present invention 2 vs. Control Emulsion Composition 3
  • phase A 1.
  • the glycerin, xanthan gum, sodium hyaluronate and acrylate/C10-30 alkanol acrylate crosspolymer in phase A are stirred and mixed uniformly in a container; the other materials of phase A are heated to At 80 ° C, the aforementioned pre-dispersed raw materials were further added; dissolved and uniformly mixed.
  • phase A Add phase A, phase B and phase C to the emulsion tank, heat at 80 ° C, and homogenize with 3000 rpm for 5 min; add arginine in phase D after the emulsification to adjust the pH.
  • the content of betulin in the birch bark extract, the composition 2 of the present invention, and the control composition 3 was measured in accordance with the test method in Example 1.
  • the test results were 40.2%, 0.201 g/100 g sample and 0.198 g/100 g sample, respectively.
  • composition prepared above was used for the test to compare the whitening effect.
  • the skin blackness value was >150.
  • the gender was random and the age distribution of each group was balanced.
  • the test site was selected as the test group, and the right arm was a blank group. Use the skin color test probe to obtain the skin LAB value (Colorimeter CL400) of the medial forearm of the arm before and after the sample is used. Above data points
  • Table 6 Average improvement in L value for Composition 2 and Control Composition 3 of the present invention
  • composition 2 of the invention Control composition 3 0 61.34 58.78 4 72.23 ab 65.34 8 75.45 ab 66.87
  • Example 4 Paste composition of the present invention 3 vs. control paste composition 4
  • phase A 1.
  • the glycerin, xanthan gum, sodium hyaluronate and acrylic acid/C10-30 alkanol acrylate crosslinked polymer in phase A are stirred and uniformly mixed in a container in advance; the other raw materials of phase A are heated to At 80 ° C, the aforementioned pre-dispersed raw materials were further added; dissolved and uniformly mixed.
  • phase A Add phase A, phase B and phase C to the emulsion tank, heat at 80 ° C, and homogenize with 3000 rpm for 5 min; add arginine in phase D after the emulsification to adjust the pH.
  • the content of betulin in the birch bark extract, the composition 3 of the present invention, and the control composition 4 was measured in accordance with the test method in Example 1. The results were 80.1%, 0.802 g/100 g sample and 0.799 g/100 g sample, respectively.
  • composition prepared above was used in a full face contrast test to evaluate the anti-aging effect.
  • the total amount of face is about 0.3g. Volunteers pick the right amount of samples according to the usual habit of applying cream cosmetics. Apply gently to the face until they are completely absorbed. Apply twice a day, twice. Leave at least 8 hours apart and ensure that the product stays on the skin for at least 6 hours. After using the product for 1 month and 2 months, the face was photographed separately, and then the elasticity value R2 of the facial skin cheek portion (COURAGE+KHAZAKA) was tested. The data were statistically analyzed by SPSS to evaluate the anti-aging effects of the two samples. Before and after data were analyzed by t-test, p ⁇ 0.05 was considered statistically significant. The test results are shown in Table 8 below.
  • Control composition 4 0 0.688 0.677 4 0.734 ab 0.687 8 0.765 ab 0.702

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Abstract

一种护肤化妆品组合物，其包含桦树汁、桦树皮提取物、和任选的护肤化妆品中常用的成分，但不包含通常作为单独组分添加的水。

Description

护肤化妆品组合物 技术领域
本发明涉及一种护肤化妆品组合物，其包含桦树汁、桦树皮提取物、和任选的护肤化妆品中常用的成分，但不包含通常作为单独组分添加的水。
背景技术
白桦脂醇又称桦木脑，在白桦树皮中含量高达10-35％，为非常有价值的天然产物，具有防紫外线、抗炎、美白、修复皮肤屏障等作用，因此常被应用于化妆品、食品和药物开发中，如在化妆品Limi The Age of Innocenc、True Hydration 24H Gel Cream(GoodSkin Labs)和oOlution中均有使用，但上述产品效果均不尽如人意。目前亦可见很多药物比如红花提取物、丹参提取物、银杏叶提取物等常规口服和静脉给药途径应用后可显著改善皮肤问题，但经局部外用后并不能达到同样效果的报道，可见局部外用药物受很多因素的影响。一般而言，不易透过皮肤的活性物将很难发挥相应药效，因此，如何使化妆品中的功能性成分按产品的有效性作用于皮肤表面或进入表皮或真皮，并在该部位积聚且发挥作用，是该领域技术人员亟待解决的问题。
为此，本发明尝试提供一种能显著提高产品中白桦脂醇透皮吸收率的技术，以获得一种区别于现有技术，能更好得发挥白桦脂醇保湿、美白、抗皱等功效的护肤组合物。
发明内容
本发明的目的在于提供一种能显著提高产品中白桦脂醇透皮吸收率的技术，从而获得一种区别于现有技术效果的护肤组合物，具体是一种通过以桦树汁完全取代配方中的水的护肤化妆品组合物。本发明令人意外地发现，局部外用该护肤化妆品组合物后，相较于外加水的类似配方，该护肤化妆品组合物可以显著有效地提高其中的白桦脂醇的透皮吸 收率，从而能更好得发挥其保湿、美白、抗皱等功效。本发明基于上述发现而得以完成。
因此，本发明提供了一种护肤化妆品组合物，其包含(A)30-99％重量的桦树汁，(B)以白桦脂醇计0.5ppm-5％重量的桦树皮提取物，和(C)任选的，护肤化妆品中常用的成分，其中，所述护肤化妆品组合物不包含通常作为单独组分添加的水。
本发明的护肤化妆品组合物具有改善的保湿、美白、抗皱等护肤功效。
本发明的护肤化妆品组合物不包含任何外加的水，但不排除所采用的桦树汁中固有的水分以及其它成分中不可避免引入的少量或痕量的水。
在优选的实施方案中，本发明的护肤化妆品组合物中不添加EDTA盐、多磷酸钠、偏磷酸钠、葡萄糖酸等螯合剂。
本发明还涉及一种增加白桦脂醇的透皮吸收率的方法，包括将桦树汁添加到包含桦树皮提取物但不包含水的护肤化妆品组合物中，其中所述桦树皮提取物中包含0.05-99.95％重量的白桦脂醇。所述方法可显著提高白桦脂醇的透皮吸收率，从而实现显著改善的护肤效果。
本发明也涉及桦树汁和桦树皮提取物的组合在不包含水的护肤化妆品组合物中的用途，其中所述桦树皮提取物中包含0.05-99.95％重量的白桦脂醇。
本发明中所涉及的桦树属于桦木科桦树属，可来自白桦(Betula alba)、垂枝桦(Betula Pendula)和亚洲白桦(Betula platyphylla)这三个品种。
本发明所述的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，例如了购自大兴安岭超越野生浆果开发有限责任公司。
本发明的护肤化妆品组合物可包含30-99％重量的桦树汁，优选50-95％重量，更优选60-90％重量，以所述组合物的总重量计算。
本发明所述桦树皮提取物为采用桦树的柔软树皮，经包括但不限于水、甲醇、乙醇、乙醚、石油醚、氯仿、苯等溶剂的一种或几种配合提取而得。通常，取决于所采用的溶剂以及打算的用途，所述提取物中白桦脂醇的含量可在0.05-99.95％之间变化。所述桦树皮提取物通常为粉末状，且可商购获得，例如可购自成都健腾生物技术有限公司。
本发明的护肤化妆品组合物可包含以白桦脂醇计0.5ppm-5％重量的桦树皮提取物，优选0.001-3％重量，更优选0.01-2％重量，以所述组合物的总重量计算。
本发明的护肤化妆品组合物还任选地包含组分(C)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(C)是本领域已知的，本领域技术人员可根据需要具体选择其类型和用量。通常，组分(C)在本发明组合物中的含量为0-70％重量。
所述媒介物例如是稀释剂、分散剂或载体等。所有这些媒介物都是本领域已知的，本领域技术人员可根据需要具体选择其类型和用量。例如，所述媒介物包括但不限于乙醇、双丙甘醇、丁二醇等。通常，在本发明组合物中，所述媒介物占组分(C)总重量的0.5-20％。
所述活性成分包括例如润肤剂、保湿剂、皮肤调理剂等。所有这些活性成分都是本领域已知的，本领域技术人员可根据需要具体选择其类型和用量。
例如，所述润肤剂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。本发明所述的固体润肤剂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，所述润肤剂占组分(C)总重量的1-50％重量。
例如，所述保湿剂包括但不限于甘油、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、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，所述保湿剂占组分(C)总重量的1-30％重量。
所述皮肤调理剂可包括用于具有保湿、抗皱、祛斑、祛痘、控油等功效的活性成分，包括但不限于曲酸、抗坏血酸、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。所述皮肤调理剂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，所述皮肤调理剂占组分(C)总重量的0.01-50％重量。
所述辅料包括但不限于乳化剂、增稠剂、防腐剂、香料等。所有这些辅料成分都是本领域已知的，本领域技术人员可根据需要具体选择其类型和用量。
例如，所述乳化剂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，所述乳化剂占组分(C)总重量的0.5-10％。
例如，所述增稠剂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，所述增稠剂占组分(C)总重量的0.1-10％重量。
例如，所述防腐剂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、脱氢乙酸钠等中的一种或多种。所述防腐剂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，所述防腐剂占组分(C)总重量的0.01-2％重量。
本发明的护肤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、洁面等剂型。
在一个优选的实施方案中，本发明提供一种具有下述配方的护肤组合物，优选爽肤水，该爽肤水显示出优异的保湿、美白和抗皱等护肤功效。
Figure PCTCN2018078208-appb-000001
实施例
下面通过具体的实施例、对照例进一步说明本发明，但是，应当理解为，这些实施例、对照例仅仅是用于更详细具体地说明之用，而不应理解为用于以任何形式限制本发明。
实施例1：在不同体系中白桦脂醇的透皮吸收率
在本实施例中，测试和对比白桦脂醇在含水体系与不含水体系中的透皮吸收率。具体测试配方见下表1。
表1
Figure PCTCN2018078208-appb-000002
注：
a:本文所用桦树汁均购自大兴安岭超越野生浆果开发有限责任公司
b：本文所用桦树皮提取物均购自成都健腾生物技术有限公司
*：由于白桦脂醇难溶于水，添加适量戊二醇有助于其溶解
上述配方如下制备：
1.将桦树皮提取物和戊二醇混合加热至80℃，搅拌溶解均匀。2.将白桦汁/水加热至80℃，然后加入步骤1所得混合物。
3.降温至40℃，出料。
测试方法:将市售去毛猪皮切割为2.5cm×2.5cm的小片。取1克上述配方1-4涂抹于每一片猪皮上，分别置于30℃、相对湿度(RH)50±5％的恒温恒湿培养箱中24h。每组进行6个平行实验。之后，将猪皮冲洗干净、剪碎，并用甲醇多次超声提取30分钟，合并提取液并减压浓缩定容至5.0ml，离心，取上层清液并用滤膜过滤后，注入高效液相色谱仪中进行测试，并用外标法计算白桦脂醇的含量。测试结果见下表2。
表2
Figure PCTCN2018078208-appb-000003
注*：经独立t检验，配方2、配方3和配方4与配方1相比，白桦脂醇透皮吸收量显著性降低(P＜0.01)
以上结果表明，与含水体系相比，在不含水而含桦树汁的本发明体系中，白桦脂醇的透皮吸收效果显著增强。
实施例2：本发明的液体护肤组合物1vs.对照液体护肤组合物1-2
上述组合物的配方如下表3所示。
表3
Figure PCTCN2018078208-appb-000004
上述组合物如下制备：
1.将B相混合加热至80℃，搅拌溶解均匀。
2.将A相中的原料加热至80℃，搅拌溶解均匀。
3.将溶解均匀的A相与B相混合，降温至40℃；再加入C相原料，搅拌均匀后出料。
将上述制备的本发明的组合物1和对照组合物1-2用于试验以考察它们各自的保湿效果。
招募了志愿者16名，在受试者右手前臂内侧用模板标识3cm*3cm区域，共有3个区域。测试期间不能饮食或剧烈活动，前臂暴露呈测试状态放置，保持放松。一个区域涂抹本发明的组合物1，第二个区域涂抹对照组合物1，第三个区域涂抹对照组合物2，将测试样品按照(2.0±0.1)mg/cm 2的用量进行涂布，要求受试者早晚(洗澡后)各涂抹一次。用仪器测定样品使用前0天(基准)和使用7天、14天的皮肤表皮水分含量，对每一个区域重复测试三次，取平均值。采用SPSS16.0软件进行统计分析，数据以平均值和标准偏差表示，前后数据采用t检验分析，p＜0.05认为有统计学意义。测试结果见下表4。
表4
天 本发明的组合物1 对照组合物1 对照组合物2
0 24.31％ 25.76％ 24.83％
7 47.12％ abc 32.15％ ac 38.52％ ab
14 46.45％ abc 33.47％ ac 36.78％ ab
注：a:与基准相比，具有显著差异(P＜0.01)
b：与对照1相比，具有显著差异(P＜0.01)
c:与对照2相比，具有显著差异(P＜0.01)
上述结果表明，在连续使用14天后，本发明的组合物1的皮肤保湿性能提高了91％，对照组合物1的皮肤保湿性能提高了30％，对照组 合物2的皮肤保湿性能提高了48％。因此，与对照组合物1-2相比，本发明的组合物1具有更好的保湿皮肤的效果，从而表明桦树汁和白桦树皮提取物显示了一定的协同增效作用。
实施例3：本发明的乳液护肤组合物2vs.对照乳液组合物3
上述组合物的配方见下表5所示。
表5
Figure PCTCN2018078208-appb-000005
上述组合物如下制备：
1.将A相中的甘油、黄原胶、透明质酸钠和丙烯酸(酯)类/C10- 30烷醇丙烯酸酯交联聚合物预先在容器中搅拌混合均匀；将A相其他原料加热至80℃，再加入前述预分散原料；溶解混合均匀。
2.将B相原料加热至80℃，溶解混合均匀。
3.将C相原料加热至80℃，溶解混合均匀。
4.将A相、B相和C相加入乳化罐中，保温在80℃，用3000rpm速度均质乳化5min；乳化完成后加入D相中的精氨酸，调节pH。
5.搅拌降温至40℃时加入D相中的苯氧乙醇，搅拌均匀后出料。
按照实施例1中的测试方法，对桦树皮提取物、本发明的组合物2和对照组合物3中白桦脂醇的含量进行测定。测试结果分别为40.2％、0.201g/100g样品和0.198g/100g样品。
将上述制备的组合物用于试验以进行美白效果的比较。
志愿者共计34人，每组16-18人，选择皮肤黑度值＞150者，性别随机，每组年龄分布均衡。测试部位选择双手手臂前臂内侧皮肤左侧手臂为测试组，右侧手臂为空白组。通过皮肤颜色测试探头获取使用样品前后的手臂前臂内侧皮肤LAB值(Colorimeter CL400)。以上数据分
别于“使用前”、“使用4周”、“使用8周”进行采集，通过SPSS对数据进行统计分析从而评价2个样品的长效美白功效。前后数据采用t检验分析，p＜0.05认为有统计学意义。测试结果见下表6。
表6：本发明组合物2和对照组合物3对L值的平均改善
周 本发明的组合物2 对照组合物3
0 61.34 58.78
4 72.23 ab 65.34
8 75.45 ab 66.87
注：a:与基准相比，具有显著差异(P＜0.01)
b：与对照组合物2相比，具有显著差异(P＜0.01)
以上结果表明，与对照组合物3相比，本发明的乳液护肤化妆品组合物2具有更好的改善皮肤色度(美白)的效果。
实施例4：本发明的膏状组合物3vs.对照膏状组合物4
上述组合物的配方见下表7所示。
表7
Figure PCTCN2018078208-appb-000006
上述组合物如下制备：
1.将A相中的甘油、黄原胶、透明质酸钠和丙烯酸(酯)类/C10-30烷醇丙烯酸酯交联聚合物预先在容器中搅拌混合均匀；将A相其他原料加热至80℃，再加入前述预分散原料；溶解混合均匀。
2.将B相原料加热至80℃，溶解混合均匀。
3.将C相原料加热至80℃，溶解混合均匀。
4.将A相、B相和C相加入乳化罐中，保温在80℃，用3000rpm速度均质乳化5min；乳化完成后加入D相中的精氨酸，调节pH。
5.搅拌降温至40℃时加入D相中的苯氧乙醇，搅拌均匀后出料。
按照实施例1中的测试方法，对桦树皮提取物、本发明的组合物3和对照组合物4中白桦脂醇的含量进行测定。结果分别为80.1％、0.802g/100g样品和0.799g/100g样品。
将上述制备的组合物用于全脸对比使用实验以评价抗衰老功效。
志愿者共计70人，每组35人，选择年龄＞40岁者，女性，每组年龄分布均衡。一组使用组合物3，一组使用对照4。按照2mg/cm 2的剂量，全脸使用量大约0.3g，志愿者按照平时使用膏霜型化妆品的使用习惯，挑取适量样品应用于面部轻轻按摩直至完全吸收，每天两次，两次涂抹间隔至少8小时，并确保产品停留在皮肤上至少6h。在使用产品1个月、2个月后，分别对面部进行拍照，然后测试面部皮肤脸颊部位的弹性值R2(德国CK(COURAGE+KHAZAKA))。通过SPSS对数据进行统计分析从而评价2个样品的抗衰老功效。前后数据采用t检验分析，p＜0.05认为有统计学意义。测试结果见下表8。
表8：本发明的组合物3和对照组合物3的抗衰老效果
周 本发明的组合物3 对照组合物4
0 0.688 0.677
4 0.734 ab 0.687
8 0.765 ab 0.702
注：a:与基准相比，具有显著差异(P＜0.01)
b：与对照3相比，具有显著差异(P＜0.01)
以上结果表明，与对照组合物4相比，本发明的膏状护肤化妆品组合物3具有更好的改善皮肤弹性的效果。

Claims (11)

  1. 一种护肤化妆品组合物，其包含：
    (A)30-99％重量的桦树汁，
    (B)以白桦脂醇计0.5ppm-5％重量的桦树皮提取物，和
    (C)任选的，护肤化妆品中常用的成分；
    其中，上述百分比含量基于所述组合物的总重量计算，和
    所述护肤化妆品组合物不包含通常作为单独组分添加的水。
  2. 权利要求1的护肤化妆品组合物，其中所述组合物不包含螯合剂。
  3. 权利要求1或2的护肤化妆品组合物，其中所述组合物包含50-95％重量或60-90％重量的桦树汁。
  4. 权利要求1-3任一项的护肤化妆品组合物，其中所述组合物包含0.001-3％重量或0.01-2％重量的桦树皮提取物。
  5. 权利要求1-4任一项的护肤化妆品组合物，其中所述桦树皮提取物中包含0.05-99.95％重量的白桦脂醇。
  6. 一种增加白桦脂醇的透皮吸收率的方法，包括将桦树汁添加到包含桦树皮提取物但不包含水的护肤化妆品组合物中，其中所述桦树皮提取物中包含0.05-99.95％重量的白桦脂醇。
  7. 权利要求6的方法，其中所述组合物包含30-99％重量的桦树汁和以白桦脂醇计0.5ppm-5％重量的桦树皮提取物，基于所述组合物的总重量计算。
  8. 权利要求6或7的方法，其中所述组合物不包含螯合剂。
  9. 桦树汁和桦树皮提取物的组合在不包含水的护肤化妆品组合物中的用途，其中所述桦树皮提取物中包含0.05-99.95％重量的白桦脂醇。
  10. 权利要求9的用途，其中30-99％重量的桦树汁与以白桦脂醇计0.5ppm-5％重量的桦树皮提取物进行组合，基于所述组合物的总重量计算。
  11. 权利要求9或10的用途，其中所述组合物不包含螯合剂。
PCT/CN2018/078208 2017-04-27 2018-03-07 护肤化妆品组合物 Ceased WO2018196482A1 (zh)

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