CN105307729A - Topical composition for preventing or decreasing skin pigmentation and/or lightening skin tone and use thereof - Google Patents

Topical composition for preventing or decreasing skin pigmentation and/or lightening skin tone and use thereof Download PDF

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CN105307729A
CN105307729A CN201380077852.4A CN201380077852A CN105307729A CN 105307729 A CN105307729 A CN 105307729A CN 201380077852 A CN201380077852 A CN 201380077852A CN 105307729 A CN105307729 A CN 105307729A
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straight
branched
alkyl
weight
hydrogen
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CN105307729B (en
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周亮
S.约伊林
L.鲍克斯
J.塞尼
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LOreal SA
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LOreal SA
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/676Ascorbic acid, i.e. vitamin C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • A61K31/375Ascorbic acid, i.e. vitamin C; Salts thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/65Paeoniaceae (Peony family), e.g. Chinese peony
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics 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
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin

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  • Alternative & Traditional Medicine (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cosmetics (AREA)

Abstract

The present invention relates to a topical composition comprising the combination of the extract of a plant in the family Paeoniaceae and at least one compound of formula (I), and use thereof for preventing or decreasing skin pigmentation and/or lightening skin tone, wherein R, R 2 and R 3 are as defined in the specification.

Description

For preventing or reducing cutaneous pigmentation and/or the topical composition of desalinating the colour of skin and uses thereof
Invention field
The present invention relates to a kind of topical composition for preventing or reduce cutaneous pigmentation and/or the desalination colour of skin.More particularly, the present invention relates to a kind of topical composition, described topical composition comprises the extract of Paeoniaceae plant and at least one according to the combination of the compound of the formula (I) of the application.The invention still further relates to this topical composition for preventing or reduce the purposes of cutaneous pigmentation and/or the desalination colour of skin.
Background of invention
Cutaneous pigmentation controls to remain one of key factor realizing Aisan's desired skin.Although L ' Oreal and other cosmetics companies successfully develop one group of active component with whitening effect, it can not meet the flourishing demand that consumer integrates " natural origin composition " and traditional medicine effectively.
In the prior art, for preventing or reducing cutaneous pigmentation and/or desalinate the speckle on the dark colour of skin or skin, use in whitening cosmetic compound and there is the active component that melanin generates inhibit activities.Such as, described by Ascorbic Acid and derivant, resorcinol derivatives and plant extract have had.
In the traditional medicine building on long herbal medicine and make up in use history, usually mention the medical herbs that can prevent or even reduce cutaneous pigmentation, among these medical herbs, Peony Root is especially emphasized because of its significant skin whitening effects.
The skin-whitening effect of Radix Paeoniae to realize via oral particularly by combining with other medical herbs.But world market all can be buied containing the manufactured goods for the Radix Paeoniae Alba extract of local application, and especially sells well at Asian market.In this regard, Chinese patent CN102247446 describes a kind of activity of restraint of tyrosinase and prevents the compositions of melanic generation, and described compositions contains at least one whitening medical herbs, as Radix Paeoniae (Paeonia sterniana Fletcher in Journ.), Radix Glycyrrhizae, Radix Ginseng etc.In addition, Japan Patent JP2002128657, JP2002265348 and Korean Patent KR20090130584 respectively describe several compositionss for skin-whitening beneficial effect, and described compositions contains some combinations of medicinal herbal extract, comprises Radix Paeoniae Alba extract.
But described whitening active ingredients has some defect/shortcomings when being applied in cosmetic composition, such as: in most of cosmetic composition, ascorbic acid is unstable, and is easy to oxidized; Or when preparing with effective dose, unhappy abnormal smells from the patient and color are made us in the usual generation in cosmetic composition of some plant extracts.
Therefore, also need for preventing or reducing cutaneous pigmentation and/or the desalination colour of skin and without the product of above-mentioned defect/shortcoming.
Summary of the invention
The present invention is intended to carry out check melanin significantly via the collaborative combination of whitening active ingredients and produces, and therefore also points out a kind of Pigmented solution with secure safety for the precaution and treatment colour of skin by this measure the present invention.
According to an aspect of the present invention, provide the topical composition of the combination of the compound of extract and at least one formula (I) comprising Paeoniaceae plant,
Wherein:
R 1and R 3different from each other or identical, independently selected from by hydrogen, straight or branched C 1-C 20acyl carbonyl, straight or branched C 2-C 20alkenyl carbonyl, straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition, is preferably selected from by hydrogen and straight or branched C 1-C 10the group of alkyl composition, is more preferably selected from by hydrogen and straight chain side chain C 1-C 4the group of alkyl composition, is most preferably hydrogen;
R 2be selected from by straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition, is preferably straight or branched C 1-C 10alkyl is more preferably straight or branched C 1-C 4alkyl or ethyl.
According to a further aspect in the invention, be provided for the cosmetic method preventing or reduce cutaneous pigmentation and/or the desalination colour of skin, described cosmetic method comprises applying according to topical composition of the present invention.
According to an aspect of the present invention, the extract of Paeoniaceae plant is provided and being combined in of the compound of at least one formula (I) produces for the purposes of preventing or reduce cutaneous pigmentation and/or desalinate in the topical composition of the colour of skin.
Wherein:
R 1and R 3different from each other or identical, independently selected from by hydrogen, straight or branched C 1-C 20acyl carbonyl, straight or branched C 2-C 20alkenyl carbonyl, straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition, is preferably selected from by hydrogen and straight or branched C 1-C 10the group of alkyl composition, is more preferably selected from by hydrogen and straight chain side chain C 1-C 4the group of alkyl composition, is most preferably hydrogen;
R 2be selected from by straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition, is preferably straight or branched C 1-C 10alkyl is more preferably straight or branched C 1-C 4alkyl or ethyl.
Topical composition according to the present invention can be used for prevention or reduces cutaneous pigmentation and/or the desalination colour of skin.
Accompanying drawing is sketched
Although description terminates with the claims explicitly pointing out the defending party to the application and regard as its subject matter of an invention, should believe that the present invention will obtain better understanding by reference to the accompanying drawings time, wherein:
Fig. 1 illustrates and uses normal human subject melanocyte external test to the measurement of the depigmentation activity (minimizing of melanin generation) that Peony Root extract, formula (I) compound and their combination are carried out.In FIG, WP represents " Peony Root extract ", the positive control that Lu Senuo (Lucinol) is depigmentation activity.
Detailed Description Of The Invention
The present inventor is surprised to find that Paeonia sterniana Fletcher in Journ. extract once combine with some known compounds (such as ascorbic acid derivates), then its depigmentation effect is significantly improved, and described compound itself does not show any depigmentation effect, but when paeoniflorin and identical Compound Phase in conjunction with time, its depigmentation effect there is no improvement.
the compound of formula (I)
The present invention comprises the compound of at least one formula (I).
Wherein:
R 1and R 3different from each other or identical, independently selected from by hydrogen, straight or branched C 1-C 20acyl carbonyl, straight or branched C 2-C 20alkenyl carbonyl, straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition; R 2be selected from by straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition.
Preferably, R 1and R 3different from each other or identical, independently selected from by hydrogen and straight or branched C 1-C 10the group of alkyl composition.
Preferably, R 2be selected from straight or branched C 1-C 10alkyl.
More preferably, R 1and R 3different from each other or identical, independently selected from by hydrogen and straight or branched C 1-C 4the group of alkyl composition.
More preferably, R 2be selected from by straight or branched C 1-C 4the group of alkyl composition.
Most preferably, R 1and R 3for hydrogen.
Most preferably, R 2for ethyl.
According to preferred embodiment, R 1and R 3independently selected from hydrogen, straight or branched C 1-C 6alkyl-carbonyl, straight or branched C 2-C 6alkenyl carbonyl, straight or branched C 1-C 6alkyl, straight or branched C 2-C 6thiazolinyl, straight or branched C 3-C 6alkynyl; R 2be selected from straight or branched C 1-C 6alkyl, straight or branched C 2-C 6thiazolinyl.
According to another preferred embodiment, R 1and R 3independently selected from hydrogen, straight or branched C 1-C 4alkyl-carbonyl, straight or branched C 2-C 4alkenyl carbonyl, straight or branched C 1-C 4, straight or branched C 2-C 4thiazolinyl, straight or branched C 3-C 4alkynyl; R 2be selected from straight or branched C 1-C 4alkyl, straight or branched C 2-C 4thiazolinyl.
According to another preferred embodiment, R 1and R 3for hydrogen, R 2for ethyl.
The compound of formula (I) commercially or can be synthesized by means known in the art.
The compound of formula (I) is with at least 0.04g/L, and preferably at least the amount of 0.25g/L is present in according in compositions of the present invention.
the extract of Paeoniaceae plant
Compositions of the present invention comprises the extract of Paeoniaceae plant.
According to the present invention, this extract derives from the spontaneous growth part (be preferably in the group being selected from and being made up of leaf, stem, root, flower, fruit and subterraneous stem one or more, be more preferably root) of plant and cultivates part (be preferably in the group selecting free cell, tissue, organ and whole plant composition one or more).
Described Paeoniaceae plant is the plant of Paeonia, it is preferably one or more that be selected from the group that is made up of Radix Paeoniae (PaeonialactifloraPall.), Paeoniaanomalassp.Veitchii (Lynch) D.Y.Hong, Paeonia suffruticosa, PaeoniaostiiT.Hong & J.X.Zhang, Paeonia papaveracea (Paeoniarockii), four paeonia szechuanica Fangs (Paeoniadecomposita) and P. delavayi (Paeoniadelavayi), and is more preferably Radix Paeoniae.
Extract of the present invention can conventionally obtain.The root of plant pulverized and washs, then carrying out alcohol extraction, liquid part leached and concentrates centrifugal to remove impurity.Extract is applied to resin column, and by water and ethanol progressively eluting to obtain final extract.This final extract be concentrated and spraying dry to obtain product.
Preferably extract is Peony Root extract.
In preferred embodiments, Peony Root extract is containing the paeoniflorin being no less than 40%.
Find: although not determined by paeoniflorin according to the whitening effect of the improvement of the application, as long as consider the whitening effect of improvement, then preferably higher paeoniflorin amount.
According to embodiment, in the combination of the extract of Paeoniaceae plant and the compound of at least one formula (I), the weight ratio of the compound of extract and at least one formula (I) is 1:0.003-1, is preferably 1:0.070-1, and is more preferably 1:0.25-1.
According to embodiment, this combination is present in described compositions with 0.05 % by weight to 20 % by weight relative to the gross weight of topical composition.
According to preferred embodiment, this combination is present in described compositions with 1 % by weight to 10 % by weight relative to the gross weight of topical composition.
According to another preferred embodiment, this combination is present in described compositions with 2 % by weight to 6 % by weight relative to the gross weight of topical composition.
Optionally, the remainder of compositions is the acceptable media of cosmetics.
According to embodiment, according to the compound of topical composition of the present invention also contained (II),
(II)
Wherein:
R 4be selected from by hydrogen, alkali metal ion, straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition;
R 5and R 6different from each other or identical, independently selected from by hydrogen, straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition.
Preferably, R 4be selected from by hydrogen and straight or branched C 1-C 10the group of alkyl composition.
Preferably, R 5and R 6different from each other or identical, independently selected from by hydrogen and straight or branched C 1-C 10the group of alkyl composition.
More preferably, R 4be selected from by hydrogen and straight or branched C 1-C 4the group of alkyl composition.
More preferably, R 5and R 6different from each other or identical, independently selected from by hydrogen and straight or branched C 1-C 4the group of alkyl composition.
Most preferably, R 4for hydrogen.
Most preferably, R 5and R 6in one be methyl, and another is hydrogen.
According to preferred embodiment, R 4be selected from by hydrogen, straight or branched C 1-C 10the group of alkyl composition; R 5and R 6different from each other or identical, independently selected from by hydrogen and straight or branched C 1-C 10the group of alkyl composition.
According to another preferred embodiment, R 4be selected from by hydrogen, straight or branched C 1-C 6the group of alkyl composition; R 5and R 6different from each other or identical, independently selected from by hydrogen and straight or branched C 1-C 6the group of alkyl composition.
According to another preferred embodiment, R 4be selected from by hydrogen, straight or branched C 1-C 4the group of alkyl composition; R 5and R 6different from each other or identical, independently selected from by hydrogen and straight or branched C 1-C 4the group of alkyl composition.
According to another preferred embodiment, R 4for hydrogen, R 5for methyl and R 6for hydrogen.
According to embodiment, the compound of formula (II) is selected from the straight or branched C of ferulic acid 1-C 10arrcostab.
According to embodiment, R 4be selected from ethyl and iso-octyl, R 5and R 6for hydrogen.
According to embodiment, formula (II) Compound Phase accounts for 0.01 % by weight-10% % by weight for the gross weight of topical composition, preferably accounts for 0.05 % by weight-5 % by weight, and more preferably accounts for 0.05 % by weight-3 % by weight.
the acceptable medium of health
Except the compound previously pointed out, also can comprise the upper acceptable medium of physiology according to compositions of the present invention.
Term " the upper acceptable medium of physiology " is intended to represent the medium being particularly useful for compositions according to the present invention being applied to skin.
The upper acceptable medium of physiology is generally made to adapt to be applied with thereon the character of the carrier of said composition and be adapted to said composition by packaged form.
aqueous phase
Aqueous phase can be comprised according to compositions of the present invention.
Aqueous phase comprises water.Be applicable to water of the present invention and can be floral water (floralwater), such as Centaurea cyanus water and/or mineral water, such as Vittel water, Lucas water or LaRochePosay water and/or spring water.
Aqueous phase also can comprise water miscible property organic solvent (at room temperature: 25 DEG C), such as, monohydric alcohol containing 2 to 6 carbon atoms, such as ethanol or isopropyl alcohol; Polyhydric alcohol, especially contains 2 to 20 carbon atoms, preferably contains 2 to 10 carbon atoms, and the polyhydric alcohol preferably containing 2 to 6 carbon atoms, such as glycerol, propylene glycol, butanediol, pentanediol, hexanediol, dipropylene glycol or diethylene glycol; The glycol ether glycol ethers of 3 to 16 carbon atoms (especially containing), such as single-, two-or tripropylene glycol (C1-C4) alkyl ether, list-, two-or triethylene glycol (C1-C4) alkyl ether, and their mixture.
Aqueous phase also can comprise stabilizing agent, such as sodium chloride, magnesium dichloride or magnesium sulfate.
Aqueous phase also can comprise any water solublity compatible with aqueous phase or water-dispersible compound, such as gellant, film forming polymer, thickening agent or surfactant, and their mixture.
Specifically, compositions of the present invention can comprise the gross weight relative to compositions, and content is 1 % by weight to 80 % by weight, especially 5 % by weight to 50 % by weight, and more particularly 10 % by weight to 45 % by weight aqueous phase.
fat phase
At least one liquid and/or hard fat phase can be comprised according to cosmetic composition of the present invention.
According to embodiment, compositions according to the present invention is Emulsion form.
Specifically, compositions of the present invention can comprise at least one liquid aliphatic phase, the oil that especially at least one is hereafter mentioned.
Term " oil " refers under room temperature (20-25 DEG C) and any fatty material of the form that is in a liquid state at atmosheric pressure.
Compositions of the present invention can comprise the gross weight relative to compositions, content in 1 % by weight to 90 % by weight, especially 5 % by weight to 80 % by weight, especially 10 % by weight to 70 % by weight, and more particularly 20 % by weight to 50 % by weight liquid aliphatic phase.
Be applicable to the fat prepared according to cosmetic composition of the present invention and can comprise alkyl oil, silicone oil, fluorocarbon oil or non-fluorocarbon oil mutually, or their mixture.
Described oil can be volatility or nonvolatile.
Described oil can be animal, plant, mineral or synthesis source.
Term " nonvolatile oil " refers to the oil be retained at room temperature and pressure on skin or keratin fiber.More particularly, nonvolatile oil has and is strictly less than 0.01mg/cm 2the evaporation rate of/min.
For measuring this evaporation rate, oil to be tested for 15g or oil mixture being placed in the crystallizing dish of diameter 7cm, described crystallizing dish being placed in and regulating (at 25 DEG C of temperature) and hygrometry to regulate the about 0.3m of (under the relative humidity 50%) through temperature 3large room in balance on.Liquid is allowed freely to evaporate under stirring, simultaneously by means of the fan (Papst-Motoren of the upright position of the top of the crystallizing dish be placed in containing described oil or described mixture, with reference to model 8550N, rotate with 2700rpm) ventilation is provided, fan blade towards crystallizing dish, distance crystallizing dish bottom 20cm.The quality of remaining oil in crystallizing dish is measured with regular time interval.Evaporation rate per unit area (cm 2) and the mg number of oil that evaporates of time per unit (minute) represent.
Term " ethereal oil " refers at room temperature and pressure, can with skin or lip contact after be less than in 1 hour any non-aqueous media evaporated.This ethereal oil is cosmetic ethereal oil, and it is at room temperature liquid.More particularly, ethereal oil has 0.01 and 200mg/cm 2the evaporation rate of (boundary point is included) between/min.
For the purposes of the present invention, term " silicone oil " refers to and comprises at least one silicon atom, and the oil of especially at least one Si-O base.
Term " fluorocarbon oil " refers to the oil comprising at least one fluorine atom.
Term " alkyl oil " refers to the main oil containing hydrogen and carbon atom.
Described oil optionally comprises oxygen, nitrogen, sulfur and/or phosphorus atoms such as in hydroxyl or acid group form.
ethereal oil
Ethereal oil is optional from containing 8 to 16 carbon atoms, and the especially alkyl oil of C8-C16 branched paraffin (having another name called isoparaffin), such as Fancol ID (has another name called 2,2,4,4,6-five methylheptane), isodecane and 2-Methylpentadecane, such as, with the oil that trade name Isopar or Permethyl sells.
The ethereal oil that can also use comprises volatile silicone, and such as volatile straight chain or cyclic silicone oil, especially has and be less than or equal to 8 centistokes (cSt) (8 × 10 -6m 2/ s) viscosity, and especially containing 2 to 10 silicon atoms and those silicone oils of particularly 2 to 7 silicon atoms, these silicone optionally comprise alkyl containing 1 to 10 carbon atom or alkoxyl.About volatile silicone oil used in the present invention, especially can mention that viscosity is the dimethicone of 5cSt and 6cSt, octamethylcy-clotetrasiloxane, decamethylcyclopentasiloxane, dodecamethylcyclohexasiloxane, seven methylhexyl trisiloxanes, seven Methyl Octyl trisiloxanes, hexamethyl disiloxane, octamethyltrisiloxane, decamethyl tetrasiloxane and ten dimethyl five siloxanes, and their mixture.
According to an embodiment, compositions of the present invention can comprise the gross weight relative to compositions, 1 % by weight to 80 % by weight, or even 5 % by weight to 70 % by weight, or even 10 % by weight to 60 % by weight, and especially 15 % by weight to 50 % by weight ethereal oil.
nonvolatile oil
Nonvolatile oil can especially be selected from nonvolatile hydrocarbon-based oils, fluorocarbon oil and/or silicone oil.
The nonvolatile hydrocarbon-based oils that can especially mention comprises:
The alkyl oil of-animal origin, such as perhydro-squalene,
The alkyl oil of-plant origin, such as vegetable stearin base ester, such as oleic acid vegetable stearin base ester, isostearic acid vegetable stearin base ester and glutamic acid lauroyl ester/glutamic acid octyldodecyl/glutamic acid vegetable stearin base ester (Ajinomoto, EldewPS203), the triglyceride formed by the fatty acid ester of glycerol, particularly wherein fatty acid can have at C4 to C36, the chain length especially in C18 to C36 scope, these oil may be straight or branched, and saturated or undersaturated, these oil especially can be D3-C7 or Trivent OCG, shea butter (sheaoil), alfalfa oil (alfalfaoil), poppy seed oil, Cucurbita maxima oil, millet oil, large wheat oil, quinoa oil, rye-seed oil, candlenut oil, passionflower oil, Adeps Bovis seu Bubali resin, aloe, Semen pruni armeniacae oil, Semen Persicae oil, Oleum Arachidis hypogaeae semen, argan oil (arganoil), American Avocado Tree oil, kopok oil, borage seed oil, Brassica oleracea L. var. botrytis L. oil, Flos Inulae oil, cameline oil, canola oil (canolaoil), carrot oil, safflower oil, oleum lini, Oleum Brassicae campestris, Oleum Gossypii semen, Oleum Cocois, pepo oil (marrowseedoil), wheat germ oil, Jojoba oil (jojobaoil), Bulbus Lilii oil, macadimia nut oil, Semen Maydis oil, Bai Manghua seed oil (meadowfoamoil), Herba Hyperici perforati oil (StJohn'sWortoil), rub noy oil (monoioil), hazelnut oil, almond oil, walnut oil, olive oil, Radix Oenotherae erythrosepalae oil, Petiolus Trachycarpi oil, seed of black currant oil, Chinese gooseberry seed oil, Oleum Vitis viniferae, pistachio nut oil, Cucurbita maxima oil, squash oil, musk rose oil, Oleum sesami, Oleum Glycines, Oleum helianthi, Oleum Ricini and watermelon oil, with and composition thereof, or substitute Trivent OCG/tricaprin, such as by those products of StearineriesDubois sold or by DynamitNobel company with title Miglyol810, 812 and 818 those products sold,
The straight or branched hydrocarbon in-mineral or synthesis source, such as liquid paraffin and its derivant, petroleum jelly, poly-certain herbaceous plants with big flowers alkene, polybutene, Parleam (such as Parleam) and squalane;
-synthesis ether containing 10 to 40 carbon atoms;
-synthetic ester, the oil of such as formula RaCOORb, wherein, carbon number object in chain R1 and R2 and be more than or equal to 10 condition under, the straight or branched fatty acid residue of Ra representative containing 1 to 40 carbon atom, and the hydrocarbyl chain of Rb representative containing 1 to 40 carbon atom, especially branched hydrocarbyl chain.Described ester especially can be selected from the fatty acid ester of alcohol, such as cetearyl stearyl; Isopropyl alcohol ester, such as isopropyl myristate, isopropyl palmitate; Ethyl palmitate, Palmic acid 2-ethyl hexyl ester, stearic acid isopropyl ester, IPIS, isostearic acid base isostearate, stearic misery fat; Hydroxylating ester, such as lactic acid iso stearyl ester, octyl hydroxystearate; Adipic acid diisopropyl ester; Heptanoate, and especially enanthic acid iso stearyl ester; Sad alcohol ester or sad polyol ester, decanoin or ricinoleate ester, such as propylene, cetyl octanoate, sad tridecyl ester; 4-bis-enanthic acid 2-ethyl hexyl ester, Palmic acid 2-ethyl hexyl ester, benzoic acid Arrcostab, two enanthic acid macrogol esters, propylene glycol 2-ethylhexanoate, and their mixture; Benzoic acid C12-C15 alcohol ester, lauric acid hexyl ester; Pivalate, such as Dermol 105, the different tridecane ester of neopentanoic acid, neopentanoic acid iso stearyl ester, Elefac I 205; Different pelargonate, such as different n-nonanoic acid different nonyl ester, different n-nonanoic acid different tridecane ester, different octyl pelargonate; Hydroxylating ester, such as lactic acid iso stearyl ester and malic acid two iso stearyl ester,
-polyol ester and pentaerythritol ester, such as dipentaerythritol base tetrahydroxy-stearic acid ester/dipentaerythritol base tetraoctyl stearate,
The ester of-dimer diol and the ester of diacid dimer, such as, by NipponFineChemical sold and LusplanDD-DA5 and LusplanDD-DA7 be described in patent application US2004-175338,
The copolymer of-dimer diol and diacid dimer and its ester, sub-oil base glycol (dilinoleyldiol) dimer/dilinoleic acid dimer copolymer of such as dimerization and its ester, such as Plandool-G,
The copolymer of-polyhydric alcohol and diacid dimer, and its ester, such as HailuscentISDA or dilinoleic acid/butanediol copolymer,
-have containing the side chain of 12 to 26 carbon atoms and/or unsaturated carbon back chain and be at room temperature the fatty alcohol of liquid, such as 2-octyldodecanol, isooctadecanol, oleyl alcohol, 2-hexyldecanol, 2-butyl capryl alcohol and 2-hendecyl-pentadecanol;
-C12-C22 higher fatty acids, such as oleic acid, linoleic acid or linolenic acid, and their mixture,
-dialkyl carbonate, two alkyl chains can be identical or different, the carbonic acid two decoyl ester such as sold with title CetiolCC by Cognis,
The oil of-high molecular weight, especially have about 400 within the scope of about 10000g/mol, especially about 650 to about 10000g/mol, and especially about 750 to about 7500g/mol, and more especially about 1000 to the molal weight within the scope of about 5000g/mol.As the oil of high molecular weight used in the present invention, especially can mention and be selected from following oil:
Lipophilic polymers,
There is the straight-chain fatty acid ester of total carbon number in 35 to 70 scopes,
Hydroxylating ester,
Aromatic ester,
C24-C28 branched chain fatty acid or aliphatic alcohol ester,
Silicone oil,
The oil of plant origin, and
Their mixture;
-optionally part alkyl oil and/or silicone fluorocarbon oil, such as, fluorosilicon oil, fluoropolyether and fluorosilicone as described in document EP-A-847752;
-silicone oil, the non-volatile dimethione of such as straight chain or ring-type (PDMS); Dimethione, it is included in the alkyl of position, silicone chains side or end, alkoxyl or phenyl, and these groups contain 2 to 24 carbon atoms; Phenyl silicones, such as phenyl gathers front three siloxanes, phenyl dimethicone, phenyl trimethicone siloxy diphenyl siloxane, diphenyl dimethicone, diphenyl methyl diphenyl trisiloxanes and 2-phenethyl trimethylsiloxysilicates, and
-their mixture.
According to a specific embodiments, the fat according to compositions of the present invention only can contain volatile compound mutually.
adjuvant
The extra adjuvant of the application being generally used for imagining also can be comprised according to compositions of the present invention.
Especially water can be mentioned; Organic solvent, especially C 1-C 6alcohol and C 2-C 10carboxylate; The carbon back oil of mineral, animal and/or plant origin and/or silicone oil; Wax, pigment, filler, coloring agent, surfactant, emulsifying agent, co-emulsifier; Gellant, thickening agent, antiseptic, spice, antibacterial, ceramide, odour absorbents, the antioxidant of cosmetic or dermatological activity agent, UV-screening agent, polymer, hydrophilic or lipophilic.
These extra adjuvant can 0.001 % by weight to 80 % by weight relative to the gross weight of compositions, and especially the ratio of 0.1 % by weight to 40 % by weight is present in compositions.These adjuvant can be introduced according to their character in the mutually fatty of compositions or aqueous phase, or introduce in lipid vesicle.Under any circumstance, these adjuvant and its ratio will be selected the adverse effect making the interpolation not being subject to according to the favourable character of compound of the present invention or being imagined indistinctively by those skilled in the art.
lid human relations form
This compositions can in any lid human relations form being generally used for cosmetic or pharmaceutical field, and especially be following form: optionally gelation water solution or water-alcoholic solutions; The dispersion of lotion type, optionally two-phase dispersion; Oil in water emulsion or water in oil emulsion or multiple Emulsion (such as W/O/W or O/W/O); Aqueous gel; Oil is by means of the dispersion of bead at aqueous phase, and these beads may be polymer nano-particle, such as nanosphere and Nano capsule, or the lipid vesicle being more preferably ion and/or nonionic type; Aqueous or oil-base gel.These compositionss are prepared according to common method.According to the present invention, preferably use the compositions in Emulsion form, especially oil in water emulsion form.
Described compositions can be more or less fluid, and can have the outward appearance of the cream of white or colour, unguentum, emulsion, washing liquid, serosity, paste, gel or mousse.Compositions is optionally used with aerosol form.Compositions can be also solid form, especially in rod shape form.
When compositions is Emulsion, the ratio of fatty phase, can in 5 % by weight to 80 % by weight scopes relative to the gross weight of compositions, and preferably 8 % by weight to 50 % by weight.Emulsifying agent and co-emulsifier, relative to the gross weight of compositions, in 0.3 % by weight to 30 % by weight scope, and preferably can exist with the ratio of 0.5 % by weight to 20 % by weight.
Compositions used according to the invention can form skin care compositions and methods, and in particular for clean, the protection of face, hands, foot, major anatomical fold or trunk, treatment or nursing cream (such as, day cream, late frost, makeup removing frost, vanishing cream or sunscreen cream); Foundation emulsion, cleaning lotion, protection or nursing body lotion or ultra light sun block lotion; Skin nursing washing liquid, gel or mousse (mousse), such as clean washing liquid.
According to an aspect of the present invention, be provided for the cosmetic method preventing or reduce cutaneous pigmentation and/or the desalination colour of skin, described cosmetic method comprises topical composition according to the present invention is applied to skin.
According to an aspect of the present invention, provide being combined in of the extract of Paeoniaceae plant and the compound of at least one formula (I) and produce for preventing or reducing the purposes in the topical composition of cutaneous pigmentation and/or the desalination colour of skin,
Wherein:
R 1and R 3different from each other or identical, independently selected from by hydrogen, straight or branched C 1-C 20acyl carbonyl, straight or branched C 2-C 20alkenyl carbonyl, straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition, is preferably selected from by hydrogen and straight or branched C 1-C 10the group of alkyl composition, is more preferably selected from by hydrogen and straight or branched C 1-C 4the group of alkyl composition, is most preferably hydrogen;
R 2be selected from by straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition, is preferably straight or branched C 1-C 10alkyl is more preferably straight or branched C 1-C 4alkyl or ethyl.
Except as otherwise noted, otherwise all numerical value of the amount, reaction condition etc. of expression composition used in description and claims be all interpreted as in all cases and modified by term " about ".
Therefore, unless indicated to the contrary, otherwise the numerical parameter described in following description and following claims is approximation, and it can change according to attempting character needed for the present invention obtains.
Although numerical range and the parameter of setting forth broad range of the present invention are approximation, as far as possible accurately record the numerical value described in particular instance.
But any numerical value is inherently containing some error, by their respective measurements, described error is inevitable finds that standard deviation causes.Following instance is intended to illustrate the present invention, but not therefore limited field.Percentage ratio provides based on weight.
Embodiment:
embodiment 1: preparation embodiment
Preparation following examples (invexp represents inventive embodiments):
Above-described embodiment is prepared according to following steps:
1. at the temperature of 75 DEG C, in water, add glycerol, propylene glycol, phenoxyethanol and sodium hydroxide, stir this mixture until homogenizing.
2. phase B is heated to the temperature of 75 DEG C, under turbine stirring, phase B is added into phase A; Speed: 2000rpm; Machine brand: TurboptestTM2004; Supplier: VMITurbotest.
3. the temperature of the mixture obtained in step 2 is cooled to 60 DEG C, under turbine stirring, phase C is added in mixture; Speed: 2000rpm; Machine brand: TurboptestTM2004; Supplier: VMITurbotest.
4. at the temperature of 25 DEG C, phase D is added in the mixture obtained in step 3, mixes each composition until homogenizing.Regulate the pH of phase D, until reach the pH of 4.3.
Embodiment 2: assessment embodiment
To embodiment for prevent or reduce cutaneous pigmentation and/or desalination the colour of skin effect assess.
Use normal human subject melanocyte external test carrys out compound (the wherein R to Peony Root extract, formula (I) 1and R 3for hydrogen, R 2for ethyl) and the measurement of depigmentation activity (minimizing of melanin generation) carried out of their combination as follows.
First, make normal human subject melanocyte grow and be distributed in 384 blocks of plates.After 24 hours, replace described culture medium with the medium containing raw material to be assessed (compound of Peony Root extract, formula (I) or their combination).By cell culture 72 hours, then finally measure optical density (OD), the melanic amount produced by melanocyte is measured in described final measurement.
As seen from Figure 1, the positive control (Lu Senuo) of 1g/L concentration suppresses to produce melanin (100% depigmentation is active) by melanocyte.In this model, independent formula (I) compound lower than 1g/L concentration does not show activity (0% depigmentation is active); And under same concentrations, independent Peony Root extract shows the medium depression effect (49% depigmentation is active) produced melanin.
Be also shown in by Fig. 1, the unexpected whitening effect significantly improved is observed: when the Peony Root extract of 1g/L mixes with the compound of the formula (I) of 0.25g/L between Peony Root extract and the compound of formula (I), the activity of Peony Root extract adds+49%, reach 72% depigmentation active, and the mode that this this whitening effect improved can rely on the dosage of the compound of formula (I) is extended.

Claims (10)

1. a topical composition, described topical composition comprises the combination of the extract of Paeoniaceae plant and the compound of at least one formula (I),
Wherein:
R 1and R 3different from each other or identical, independently selected from by hydrogen, straight or branched C 1-C 20acyl carbonyl, straight or branched C 2-C 20alkenyl carbonyl, straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition, is preferably selected from by hydrogen and straight or branched C 1-C 10the group of alkyl composition, is more preferably selected from by hydrogen and straight or branched C 1-C 4the group of alkyl composition, is most preferably hydrogen;
R 2be selected from by straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition, is preferably straight or branched C 1-C 10alkyl is more preferably straight or branched C 1-C 4alkyl or ethyl.
2. topical composition according to claim 1, wherein said extract derives from the spontaneous growth part of plant, is preferably one or more in the group being selected from and being made up of leaf, stem, root, flower, fruit and subterraneous stem, is more preferably root; And the cultivation part of plant, be preferably select free cell, tissue, organ and whole plant composition group in one or more.
3. topical composition according to claim 1 and 2, wherein said Paeoniaceae plant is Paeonia plant, be preferably in the group being selected from and being made up of Radix Paeoniae, Paeoniaanomalassp.Veitchii (Lynch) D.Y.Hong, Paeonia suffruticosa, PaeoniaostiiT.Hong & J.X.Zhang, Paeonia papaveracea, four paeonia szechuanica Fangs and P. delavayi one or more, and be more preferably Radix Paeoniae.
4. the topical composition according to any one of aforementioned claims 1 to 3, wherein in described combination, the weight ratio of the compound of described extract and described at least one formula (I) is 1:0.003-1, is preferably 1:0.070-1, and is more preferably 1:0.25-1.
5. the topical composition according to any one of aforementioned Claims 1-4, wherein said combination relative to the gross weight of described topical composition with 0.05 % by weight to 20 % by weight, preferably with 1 % by weight to 10 % by weight, and be more preferably present in described compositions with 2 % by weight to 6 % by weight, optionally remaining as the acceptable medium of health.
6. the topical composition according to any one of aforementioned claim 1 to 5, also comprises the extra adjuvant of at least one.
7. the topical composition according to any one of aforementioned claim 1 to 6, the also compound of contained (II),
(II)
Wherein:
R 4be selected from by hydrogen, alkali metal ion, straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition, is preferably selected from by hydrogen and straight or branched C 1-C 10alkyl (is preferably straight or branched C 1-C 4alkyl) group that forms is more preferably hydrogen;
R 5and R 6different from each other or identical, independently selected from by hydrogen, straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition, is preferably selected from by hydrogen and straight or branched C 1-C 10the group of alkyl composition, is preferably straight or branched C 1-C 4alkyl; Preferably R 5and R 6in one be methyl, and another is hydrogen.
8. the topical composition according to any one of aforementioned claim 1 to 7, the Compound Phase of wherein said formula (II) for the gross weight of described topical composition with 0.01 % by weight to 10 % by weight, preferably with 0.05 % by weight to 5 % by weight, and be more preferably present in described compositions with 0.05 % by weight to 3 % by weight.
9., for preventing or reduce a cosmetic method for cutaneous pigmentation and/or the desalination colour of skin, described cosmetic method comprises topical composition according to any one of claim 1 to 8 is applied to described skin.
10. the extract of Paeoniaceae plant and being combined in of the compound of at least one formula (I) produce for the purposes of preventing or reduce cutaneous pigmentation and/or desalinate in the topical composition of the colour of skin,
Wherein:
R 1and R 3different from each other or identical, independently selected from by hydrogen, straight or branched C 1-C 20acyl carbonyl, straight or branched C 2-C 20alkenyl carbonyl, straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition, is preferably selected from by hydrogen and straight or branched C 1-C 10the group of alkyl composition, is more preferably selected from by hydrogen and straight chain side chain C 1-C 4the group of alkyl composition, is most preferably hydrogen;
R 2be selected from by straight or branched C 1-C 20alkyl, straight or branched C 2-C 20thiazolinyl and straight or branched C 2-C 20the group of alkynyl composition, is preferably straight or branched C 1-C 10alkyl is more preferably straight or branched C 1-C 4alkyl or ethyl.
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