WO2021017835A1 - Composition cosmétique de blanchiment améliorée - Google Patents

Composition cosmétique de blanchiment améliorée Download PDF

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Publication number
WO2021017835A1
WO2021017835A1 PCT/CN2020/102179 CN2020102179W WO2021017835A1 WO 2021017835 A1 WO2021017835 A1 WO 2021017835A1 CN 2020102179 W CN2020102179 W CN 2020102179W WO 2021017835 A1 WO2021017835 A1 WO 2021017835A1
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WO
WIPO (PCT)
Prior art keywords
birch sap
cosmetic composition
ascorbyl
whitening cosmetic
concentrated
Prior art date
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PCT/CN2020/102179
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English (en)
Chinese (zh)
Inventor
赵瑞丽
王莎莎
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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 WO2021017835A1 publication Critical patent/WO2021017835A1/fr

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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
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • 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
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated 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
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
    • 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
    • A61K8/60—Sugars; Derivatives thereof
    • A61K8/602—Glycosides, e.g. rutin
    • 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
    • A61K8/67—Vitamins
    • A61K8/673—Vitamin B group
    • A61K8/675—Vitamin B3 or vitamin B3 active, e.g. nicotinamide, nicotinic acid, nicotinyl aldehyde
    • 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
    • A61K8/67—Vitamins
    • A61K8/676—Ascorbic acid, i.e. vitamin C
    • 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
    • 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
    • A61K2800/74—Biological properties of particular ingredients
    • A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782—Enzyme inhibitors; Enzyme antagonists

Definitions

  • the present invention relates to an enhanced whitening cosmetic composition
  • an enhanced whitening cosmetic composition comprising (A) concentrated birch sap, and (B) selected from the group consisting of arbutin, tranexamic acid, nicotinamide, glycyrrhizin, ascorbic acid, ascorbyl glucoside, One or more of ascorbyl dipalmitate and ascorbyl tetraisopalmitate, wherein the concentration factor of the concentrated birch sap is about 1.05-6 times, preferably about 1.1-5 times, more preferably about 1.2 -4 times.
  • 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. Birch sap contains a lot of sugars, amino acids, vitamins, biotin, cytokinins, trace mineral elements, aromatic oils, betulin, saponins and other compounds. It has good moisturizing, whitening and other skin care effects.
  • the present invention relates to (A) concentrated birch sap and (B) selected from the group consisting of arbutin, tranexamic acid, nicotinamide, glycyrrhizin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate and tetraisoascorbate
  • concentration of the concentrated birch tree juice is about 1.05-6 times, preferably about 1.1-5 times, more preferably about 1.2 -4 times.
  • the present invention provides an enhanced whitening cosmetic composition
  • an enhanced whitening cosmetic composition comprising (A) concentrated birch sap, and (B) selected from the group consisting of arbutin, tranexamic acid, nicotinamide, glycyrrhizin, ascorbic acid, ascorbic acid One or more of glucoside, ascorbyl dipalmitate and ascorbyl tetraisopalmitate, wherein the concentration factor of the concentrated birch sap is about 1.05-6 times, preferably about 1.1-5 times, and more It is preferably about 1.2-4 times.
  • the present inventors found that the use of concentrated birch sap, arbutin, tranexamic acid, nicotinamide, glycyrrhizin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate or ascorbyl tetraisopalmitate alone Compared with esters, the combination of concentrated birch sap with arbutin, tranexamic acid, nicotinamide, glycyrrhizin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate and/or ascorbyl tetraisopalmitate has significantly better Its whitening effect is much higher than the superposition effect of the two functions. It can 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. A synergistic effect occurred between them.
  • 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, and no-drug sap that is artificially collected by drilling holes at the base of the trunk of the birch between thawing and 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.
  • controlling the concentration ratio of birch sap is critical.
  • controlling the concentration ratio of birch sap is about 1.05-6 times, preferably about 1.1-5 times, more preferably about 1.2-4 times.
  • the content of the concentrated birch tree 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.
  • the component (B) arbutin, tranexamic acid, nicotinamide, glycyrrhizin, ascorbic acid, ascorbyl glucoside, ascorbyl dipalmitate or ascorbyl tetraisopalmitate are all known in the art, and they are all known in the art. It is commercially available and used in the present invention as it is.
  • the total content of the component (B) is about 0.0005-30% by weight, preferably about 0.001-10% by weight, more preferably about 0.1-5% by weight, most preferably about 0.5-3% by weight, based on the whitening cosmetic combination The total weight of the object.
  • the whitening cosmetic composition does not contain any external water, but does not exclude the moisture inherently contained in each component.
  • the whitening cosmetic composition does not contain chelating agents such as EDTA salt, sodium polyphosphate, sodium metaphosphate, and gluconic acid.
  • chelating agents such as EDTA salt, sodium polyphosphate, sodium metaphosphate, and gluconic acid.
  • the whitening cosmetic composition may optionally include components (C) commonly used in skin care cosmetic compositions.
  • components (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) according to their needs.
  • the content of component (C) is usually about 0-70% by weight, based on the whitening The total weight of the cosmetic composition.
  • 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 (C).
  • 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 (C).
  • 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 (C).
  • preservatives examples include, but are not limited to, methyl paraben, ethyl paraben, propyl paraben, phenoxyethanol, benzyl alcohol, phenethyl alcohol, bis(hydroxymethyl)imidazolidinyl urea, potassium sorbate, One or more of sodium benzoate, chlorphenesin, sodium dehydroacetate, etc.
  • the content of the preservative in the cosmetic composition is known in the art, for example, it usually accounts for 0.01-30% of the total weight of component (C).
  • 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 When preparing, put 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.
  • a disperser 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. After the emulsification is completed, 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 whitening cosmetic composition can be made into various dosage forms such as creams, creams, emulsions, and essences.
  • Example 1 Effect on the expression of genes related to melanin synthesis and transport
  • Experimental reagents and consumables human primary melanocytes, 6-well plates, melanocyte culture medium, RNA extraction kit, reverse transcription kit, Trizol lysis solution, etc.
  • sample addition information the sample amount of a single raw material is a whole raw material; the compound raw material is half a birch sap raw material plus half a 0.1% other active raw material.
  • 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.
  • Example 2 Effect on the expression of melanin synthesis and transport related proteins
  • Experimental reagents and consumables human primary melanocytes, 12-well plates, melanocyte culture medium, ELISA test kits with different indicators, etc.
  • sample addition information the sample amount of a single raw material is a whole raw material; the compound raw material is half a birch sap raw material plus half a 0.1% other active raw material.
  • test steps are as follows:
  • Inoculation Inoculate in a 12-well culture plate at an inoculation density of 2E5/well, cultivate in a 37°C and 5% CO 2 incubator, and change the medium every two days;
  • T-Test method is used for statistical analysis.
  • Experimental reagents and consumables human primary melanocytes, 12-well plate, melanocyte culture medium, NaOH lysis solution.
  • sample addition information the sample amount of a single raw material is a whole raw material; the compound raw material is half a birch sap raw material plus half a 0.1% other active raw material.
  • Inoculation Inoculate in a 12-well culture plate at an inoculation density of 2E5/well, culture in a 37°C, 5% CO 2 incubator, and change the medium every two days.
  • melanin inhibition rate (% ) (A negative control group-A administration group)/A negative control group*100%
  • Experimental reagents and consumables 3D melanin skin model (made in the laboratory), model culture medium, NaOH lysis solution.
  • sample addition information the sample amount of a single raw material is a whole raw material; the compound raw material is half a birch sap raw material plus half a 0.1% other active raw material.
  • 3D model construction use keratinocytes and melanocytes to construct a 3D skin model.
  • UVB irradiation treatment (UVB: 50mJ/cm 2 ) 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 Coat the model culture medium, each group has 6 multiple holes, apply once a day, the total duration of action is 4 days.
  • Example 5 Preparation of whitening essence milk composition
  • the above whitening essence composition is prepared as follows:
  • the phases A and B are heated to 80°C to dissolve evenly;
  • phase D additive phase D to phase ABC, stir and lower the temperature to 40 degrees to discharge.
  • 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.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Dermatology (AREA)
  • Cosmetics (AREA)

Abstract

L'invention concerne une composition cosmétique de blanchiment améliorée, comprenant : (A) du jus de bouleau concentré ; et (B) une ou plusieurs substances choisies parmi l'arbutine, l'acide tranexamique, le nicotinamide, la glabridine, l'acide ascorbique, le glucoside d'ascorbyle, le dipalmitate de L-ascorbyle et le tétraisopalmitate d'ascorbyle, le facteur de concentration du jus de bouleau concentré étant compris entre 1,05 et 6.
PCT/CN2020/102179 2019-07-30 2020-07-15 Composition cosmétique de blanchiment améliorée WO2021017835A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201910694704.6A CN110731927A (zh) 2019-07-30 2019-07-30 增强的美白化妆品组合物
CN201910694704.6 2019-07-30

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WO2021017835A1 true WO2021017835A1 (fr) 2021-02-04

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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
CN110731922B (zh) * 2019-07-30 2022-08-02 浙江养生堂天然药物研究所有限公司 增强的防脱生发组合物
CN112370414A (zh) * 2020-08-24 2021-02-19 荣鼎(广东)生物科技有限公司 一种美藤果赋活雪颜精华液及其制备方法
CN112263496A (zh) * 2020-10-26 2021-01-26 广州环亚化妆品科技有限公司 一种美白剂、包含其的美白油凝胶及其制备方法
CN113975215A (zh) * 2021-11-18 2022-01-28 广州梵之容化妆品有限公司 一种美白霜及其制备方法
CN114588068B (zh) * 2022-03-29 2023-07-28 上海新高姿化妆品有限公司 具有皮肤美白淡斑功效的组合物

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