CN105307729B - For preventing or reducing cutaneous pigmentation and/or desalinate the topical composition and application thereof of the colour of skin - Google Patents

For preventing or reducing cutaneous pigmentation and/or desalinate the topical composition and application thereof of the colour of skin Download PDF

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Publication number
CN105307729B
CN105307729B CN201380077852.4A CN201380077852A CN105307729B CN 105307729 B CN105307729 B CN 105307729B CN 201380077852 A CN201380077852 A CN 201380077852A CN 105307729 B CN105307729 B CN 105307729B
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branched chain
chain
linear chain
oil
linear
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CN105307729A (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

Abstract

The present invention relates to a kind of topical compositions, the topical composition includes the combination of the extract of Paeoniaceae plant and the compound of at least one formula (I), and it is used to prevent or reduce cutaneous pigmentation and/or desalinates the purposes of the colour of skin, wherein R1, R2 and R3 as defined in the description.

Description

For preventing or reducing cutaneous pigmentation and/or desalinate the topical composition of the colour of skin And application thereof
Invention field
The present invention relates to a kind of topical compositions for preventing or reducing cutaneous pigmentation and/or desalinate the colour of skin.More In particular it relates to a kind of topical composition, the topical composition includes the extract and at least of Paeoniaceae plant A kind of combination of the compound of the formula (I) according to the application.The invention further relates to the topical compositions for preventing or reducing skin Skin pigmentation and/or the purposes for desalinating the colour of skin.
Background of invention
Cutaneous pigmentation control is still to realize one of the key factor of Asian's desired skin.Although L ' Oreal and Other cosmetics companies have successfully developed one group of active constituent with whitening effect, but it cannot effectively meet consumer The flourishing demand that " natural origin ingredient " and traditional medicine are integrated.
In the prior art, to prevent or reducing the spot on cutaneous pigmentation and/or the dark colour of skin of desalination or skin, in beauty The active constituent with melanin production inhibitory activity is used in albefaction cosmetic compositions.For example, Ascorbic Acid and its derivative Object, resorcinol derivatives and plant extracts have been described.
It can be prevented or very building on long herbal medicine and makeup using usually referring in the traditional medicine in history To the herbal medicine for reducing cutaneous pigmentation, among these herbal medicine, Peony Root due to its significant skin whitening effects especially by It emphasizes.
The skin-whitening effect of Chinese herbaceous peony is realized via taking orally particularly by combining with other herbal medicine.However, global city Field all commercially available manufactured goods containing the peony extract for local application, and especially sell well in Asian market.Herein Aspect, Chinese patent CN102247446 describe the group of a kind of activity for inhibiting tyrosinase and the generation that prevents melanin Object is closed, the composition contains at least one whitening herbal medicine, such as Chinese herbaceous peony (white flower Chinese herbaceous peony), Radix Glycyrrhizae, ginseng.In addition, Japanese Patent JP2002128657, JP2002265348 and Korean Patent KR20090130584 are respectively described to be had for skin-whitening Several compositions of beneficial effect, the composition contain some combinations of medicinal herbal extract, including peony extract.
However, the whitening active ingredients have some defect/disadvantages when being applied in cosmetic composition, such as: In most of cosmetic compositions, ascorbic acid is unstable, and is easily oxidised;It is some or when being prepared with effective dose Plant extracts generally produces unpleasant smell and color in cosmetic composition.
Therefore, it is also desirable to for preventing or reducing cutaneous pigmentation and/or the desalination colour of skin and without drawbacks described above/disadvantage Product.
Summary of the invention
The present invention is directed to inhibit melanin to generate significantly via the collaborative combination of whitening active ingredients, therefore pass through this The act present invention also indicates that a kind of for preventing and handling the pigmented solution with secure safety of the colour of skin.
According to an aspect of the invention, there is provided the change of the extract comprising Paeoniaceae plant and at least one formula (I) The combined topical composition of object is closed,
Wherein:
R1And R3It is different from each other or identical, independently selected from by hydrogen, linear chain or branched chain C1-C20Acyl carbonyl, linear chain or branched chain C2-C20Alkenyl carbonyl, linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20Alkynyl group At group, be preferably chosen from by hydrogen and linear chain or branched chain C1-C10The group of alkyl composition, is more preferably selected from by hydrogen and straight chain branch C1-C4The group of alkyl composition, most preferably hydrogen;
R2Selected from by linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20Alkynyl The group of composition, it is therefore preferable to linear chain or branched chain C1-C10Alkyl, more preferably linear chain or branched chain C1-C4Alkyl or ethyl.
According to another aspect of the present invention, it provides for preventing or reducing cutaneous pigmentation and/or desalinate the change of the colour of skin Cosmetic method, the cosmetic method include to apply topical composition according to the present invention.
According to an aspect of the invention, there is provided the compound of the extract of Paeoniaceae plant and at least one formula (I) Combination generate for prevent or reduce cutaneous pigmentation and/or desalinate the colour of skin topical composition in purposes.
Wherein:
R1And R3It is different from each other or identical, independently selected from by hydrogen, linear chain or branched chain C1-C20Acyl carbonyl, linear chain or branched chain C2-C20Alkenyl carbonyl, linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20Alkynyl group At group, be preferably chosen from by hydrogen and linear chain or branched chain C1-C10The group of alkyl composition, is more preferably selected from by hydrogen and straight chain branch C1-C4The group of alkyl composition, most preferably hydrogen;
R2Selected from by linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20Alkynyl The group of composition, it is therefore preferable to linear chain or branched chain C1-C10Alkyl, more preferably linear chain or branched chain C1-C4Alkyl or ethyl.
Topical composition according to the present invention can be used for preventing or reducing cutaneous pigmentation and/or the desalination colour of skin.
Brief description
Although specification is terminated with the claims for explicitly pointing out the theme that the defending party to the application is regarded as its invention, should It is believed that the present invention more preferably understands acquirement when in conjunction with attached drawing, in which:
Fig. 1 is illustrated using normal human subject melanocyte external test come to Chinese herbaceous peony root extract, formula (I) compound And the measurement of the depigmentation active (reduction of melanin yield) of their combination progress.In Fig. 1, WP indicates " Chinese herbaceous peony Root extract ", Lu Senuo (Lucinol) are the active positive control of depigmentation.
Detailed description of the invention
Present inventors discovered unexpectedly that once white flower peony extract is with some known compounds (such as Vitamin C Acid derivative) it combines, then its depigmentation effect significantly improves, and the compound itself does not show any depigmentation effect It answers, but when Paeoniflorin is combined with identical compound, depigmentation effect has no improvement.
The compound of formula (I)
The present invention includes the compound of at least one formula (I).
Wherein:
R1And R3It is different from each other or identical, independently selected from by hydrogen, linear chain or branched chain C1-C20Acyl carbonyl, linear chain or branched chain C2-C20Alkenyl carbonyl, linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20Alkynyl group At group;R2Selected from by linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20Alkynyl group At group.
Preferably, R1And R3It is different from each other or identical, independently selected from by hydrogen and linear chain or branched chain C1-C10Alkyl composition Group.
Preferably, R2Selected from linear chain or branched chain C1-C10Alkyl.
It is highly preferred that R1And R3It is different from each other or identical, independently selected from by hydrogen and linear chain or branched chain C1-C4Alkyl composition Group.
It is highly preferred that R2Selected from by linear chain or branched chain C1-C4The group of alkyl composition.
Most preferably, R1And R3For hydrogen.
Most preferably, R2For ethyl.
According to preferred embodiment, R1And R3Independently selected from hydrogen, linear chain or branched chain C1-C6Alkyl-carbonyl, linear chain or branched chain C2-C6Alkenyl carbonyl, linear chain or branched chain C1-C6Alkyl, linear chain or branched chain C2-C6Alkenyl, linear chain or branched chain C3-C6Alkynyl;R2It is selected from Linear chain or branched chain C1-C6Alkyl, linear chain or branched chain C2-C6Alkenyl.
According to another preferred embodiment, R1And R3Independently selected from hydrogen, linear chain or branched chain C1-C4Alkyl-carbonyl, straight chain or Branch C2-C4Alkenyl carbonyl, linear chain or branched chain C1-C4, linear chain or branched chain C2-C4Alkenyl, linear chain or branched chain C3-C4Alkynyl;R2It is selected from Linear chain or branched chain C1-C4Alkyl, linear chain or branched chain C2-C4Alkenyl.
According to another preferred embodiment, R1And R3For hydrogen, R2For ethyl.
The compound of formula (I) is commercially available or can be synthesized by means known in the art.
The compound of formula (I) is present according to the present invention group at least 0.04g/L, the preferably at least amount of 0.25g/L It closes in object.
The extract of Paeoniaceae plant
Composition of the invention includes the extract of Paeoniaceae plant.
According to the present invention, the extract derive from plant spontaneous growth part (preferably selected from by leaf, stem, root, flower, One of group of fruit and subterranean stem composition is a variety of, more preferably root) and part is cultivated (preferably selected from by thin One of group that born of the same parents, tissue, organ and entire plant form is a variety of).
The Paeoniaceae plant is the plant of Paeonia, is selected from by Chinese herbaceous peony (Paeonia lactiflora Pall.), Paeonia anomala ssp. Veitchii (Lynch) D. Y. Hong, tree peony, Paeonia ostii T. Hong J. X. Zhang, Paeonia papaveracea (Paeonia rockii), four paeonia szechuanica Fangs (Paeonia decomposita) and Yunnan One or more, and the more preferably Chinese herbaceous peony of the group of tree peony (Paeonia delavayi) composition.
Extract of the invention can be obtained conventionally.The root of plant is pulverized and washed, wine is then carried out Essence is extracted, and liquid portion is filtered out and is concentrated to be centrifuged to remove impurity.Extract is applied to resin column, and by water and Ethyl alcohol is gradually eluted to obtain final extract.This final extract is concentrated and is spray-dried to obtain product.
Preferably extract is Chinese herbaceous peony root extract.
In preferred embodiments, Chinese herbaceous peony root extract is containing the Paeoniflorin for being no less than 40%.
It has been found that: although not being determined by Paeoniflorin according to the improved whitening effect of the application, but as long as in view of changing Kind whitening effect, then preferably higher Paeoniflorin amount.
It is extracted in the combination of the compound of the extract and at least one formula (I) of Paeoniaceae plant according to embodiment The weight ratio of object and the compound of at least one formula (I) is 1:0.003-1, it is therefore preferable to 1:0.070-1, and more preferably 1:0.25-1。
According to embodiment, which is present in relative to the total weight of topical composition with 0.05 weight % to 20 weight % In the composition.
According to preferred embodiment, which exists relative to the total weight of topical composition with 1 weight % to 10 weight % In the composition.
According to another preferred embodiment, which is deposited relative to the total weight of topical composition with 2 weight % to 6 weight % It is in the composition.
Optionally, the rest part of composition is the acceptable medium of cosmetics.
According to embodiment, topical composition according to the present invention also includes the compound of formula (II),
(II)
Wherein:
R4Selected from by hydrogen, alkali metal ion, linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and straight chain or Branch C2-C20The group of alkynyl composition;
R5And R6It is different from each other or identical, independently selected from by hydrogen, linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2- C20Alkenyl and linear chain or branched chain C2-C20The group of alkynyl composition.
Preferably, R4Selected from by hydrogen and linear chain or branched chain C1-C10The group of alkyl composition.
Preferably, R5And R6It is different from each other or identical, independently selected from by hydrogen and linear chain or branched chain C1-C10Alkyl composition Group.
It is highly preferred that R4Selected from by hydrogen and linear chain or branched chain C1-C4The group of alkyl composition.
It is highly preferred that R5And R6It is different from each other or identical, independently selected from by hydrogen and linear chain or branched chain C1-C4Alkyl composition Group.
Most preferably, R4For hydrogen.
Most preferably, R5And R6In one be methyl, and another be hydrogen.
According to preferred embodiment, R4Selected from by hydrogen, linear chain or branched chain C1-C10The group of alkyl composition;R5And R6It is different from each other Or it is identical, independently selected from by hydrogen and linear chain or branched chain C1-C10The group of alkyl composition.
According to another preferred embodiment, R4Selected from by hydrogen, linear chain or branched chain C1-C6The group of alkyl composition;R5And R6Each other It is similar and different, independently selected from by hydrogen and linear chain or branched chain C1-C6The group of alkyl composition.
According to another preferred embodiment, R4Selected from by hydrogen, linear chain or branched chain C1-C4The group of alkyl composition;R5And R6Each other It is similar and different, independently selected from by hydrogen and linear chain or branched chain C1-C4The group of alkyl composition.
According to another preferred embodiment, R4For hydrogen, R5For methyl and R6For hydrogen.
According to embodiment, the compound of formula (II) is selected from the linear chain or branched chain C of ferulic acid1-C10Arrcostab.
According to embodiment, R4Selected from ethyl and iso-octyl, R5And R6For hydrogen.
According to embodiment, formula (II) compound accounts for 0.01 weight %-10% weight relative to the total weight of topical composition Amount %, 0.05 weight %-5 weight % is preferably comprised from, and more preferably accounts for 0.05 weight %-3 weight %.
The acceptable medium of body
In addition to the compound previously pointed out, composition according to the present invention also may include physiologically acceptable Jie Matter.
Term " physiologically acceptable medium ", which is intended to indicate that, to be particularly suitable for applying composition according to the present invention To the medium of skin.
Physiologically acceptable medium is generally set to adapt to the property for being applied with the carrier of the composition thereon and fit The form that should will be packaged in the composition.
Water phase
Composition according to the present invention may include water phase.
Water phase includes water.Be suitable for the invention water can for floral water (floral water), such as corn flower water and/or Mineral water, such as Vittel water, Lucas water or La Roche Posay water and/or spring.
Water phase also may include the miscible organic solvent of water (at room temperature: 25 DEG C), such as containing 2 to 6 carbon atoms Monohydric alcohol, such as ethyl alcohol or isopropanol;Polyalcohol especially contains 2 to 20 carbon atoms, preferably contains 2 to 10 carbon originals Son, and the polyalcohol preferably containing 2 to 6 carbon atoms, such as glycerol, propylene glycol, butanediol, pentanediol, hexylene glycol, two Propylene glycol or diethylene glycol;Glycol ether (glycol ether especially containing 3 to 16 carbon atoms), for example, it is mono-, two- or three Propylene glycol (C1-C4) alkyl ether, mono-, two- or triethylene glycol (C1-C4) alkyl ether and their mixture.
Water phase also may include stabilizer, such as sodium chloride, magnesium dichloride or magnesium sulfate.
Water phase also may include any water solubility compatible with water phase or water-dispersible compound, such as gelling agent, film forming Polymer, thickener or surfactant and their mixture.
Specifically, composition of the invention may include the total weight relative to composition, content is 1 weight % to 80 weights Measure %, especially 5 weight % to 50 weight %, and the water phase of more particularly 10 weight % to 45 weight %.
Fatty phase
Cosmetic composition according to the present invention may include at least one liquid and/or hard fat phase.
According to embodiment, composition according to the present invention is in emulsion form.
Specifically, composition of the invention may include at least one liquid aliphatic phase, especially at least a kind of hereafter institute The oil referred to.
Term " oil " refers to any fatty material for the form that is in a liquid state under room temperature (20-25 DEG C) and at atmosheric pressure.
Composition of the invention may include the total weight relative to composition, and content is in 1 weight % to 90 weight %, especially 5 Weight % to 80 weight %, especially 10 weight % are to 70 weight %, and the liquid aliphatic phase of more particularly 20 weight % to 50 weight %.
Fat suitable for preparing cosmetic composition according to the present invention mutually may include alkyl oil, silicone oil, fluorocarbon oil or Non- fluorocarbon oil or their mixture.
The oil can be volatility or non-volatile.
The oil can be animal, plant, mineral or synthesis source.
Term " nonvolatile oil " refers to the oil being retained on skin or keratin fiber at room temperature and pressure.More Specifically, nonvolatile oil has strictly less than 0.01mg/cm2The evaporation rate of/min.
To measure this evaporation rate, oil or oil mixture 15g to be tested are placed in the crystallising dish of diameter 7cm, by institute State the about 0.3m that crystallising dish is placed in temperature regulated (at a temperature of 25 DEG C) and hygrometry adjusts (under 50% relative humidity)3 Big room in balance on.Allow liquid it is without mixing it is lower freely evaporate, while by means of being placed in containing described oily or described mix (Papst-Motoren is revolved with reference to 8550 N of model with 2700rpm the fan of the upright position of the top of the crystallising dish of conjunction object Turn) ventilation, bottom 20cm of the fan blade towards crystallising dish, apart from crystallising dish are provided.It is spaced at regular times to measure crystallization The quality of remaining oil in ware.Evaporation rate per unit area (cm2) and per unit time (minute) evaporation oil mg number To indicate.
Term " ethereal oil " refers at room temperature and pressure, can with it is small less than 1 after skin or lip contact When interior evaporation any non-aqueous medium.The ethereal oil is cosmetic ethereal oil, is at room temperature liquid.More specifically It says, ethereal oil has in 0.01 and 200mg/cm2The evaporation rate of (boundary point is included) between/min.
For the purposes of the present invention, term " silicone oil " refers to comprising at least one silicon atom, and especially at least one The oil of Si-O base.
Term " fluorocarbon oil " refers to the oil comprising at least one fluorine atom.
Term " alkyl oil " refers to the oil for mainly containing hydrogen and carbon atom.
The oil is optionally including for example in hydroxyl or the oxygen of acid group form, nitrogen, sulphur and/or phosphorus atoms.
Ethereal oil
Ethereal oil can be selected from containing 8 to 16 carbon atoms, and especially C8-C16 branched paraffin (also known as different alkane Hydrocarbon) alkyl oil, such as Permethyl 99A (also known as 2,2,4,4,6- five methylheptanes), isodecane and isohexadecane, such as with quotient The oil that the name of an article Isopar or Permethyl are sold.
The ethereal oil that can also be used includes volatile silicone, such as volatile straight chain or ring shape silicone oil, especially With less than or equal to 8 centistokes (cSt) (8 × 10-6m2/ s) viscosity, and especially containing 2 to 10 silicon atoms and especially It is those of 2 to 7 silicon atoms silicone oil, these silicone optionally include alkyl or alkoxy containing 1 to 10 carbon atom. About volatile silicone oil for use in the present invention, it especially can be mentioned that viscosity is the dimethicone of 5cSt and 6cSt, eight first Basic ring tetrasiloxane, decamethylcyclopentasiloxane, dodecamethylcyclohexasiloxane, seven methylhexyl trisiloxanes, seven methyl are pungent Base trisiloxanes, hexamethyldisiloxane, five siloxanes of octamethyltrisiloxane, decamethyl tetrasiloxane and ten dimethyl, with And their mixture.
According to an embodiment, composition of the invention may include the total weight relative to composition, 1 weight % to 80 Weight %, or even 5 weight % to 70 weight %, or even 10 weight % to 60 weight %, and especially 15 weight % to 50 weight % Ethereal oil.
Nonvolatile oil
Nonvolatile oil can be especially selected from nonvolatile hydrocarbon-based oils, fluorocarbon oil and/or silicone oil.
The nonvolatile hydrocarbon-based oils that can especially refer to include:
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 plant Stearyl and glutamic acid lauroyl ester/glutamic acid octyldodecyl/glutamic acid vegetable stearin base ester (Ajinomoto, Eldew PS203), the triglycerides formed by the aliphatic ester of glycerol, especially wherein fatty acid can have in C4 to C36, Chain length within the scope of especially C18 to C36, these oil may be linear chain or branched chain and saturated or unsaturated;These oil are outstanding It can for D3-C7 or Trivent OCG, shea butter (shea oil), alfalfa oily (alfalfa oil), Poppy seed oil, winter squash oil, millet oil, big wheat oil, quinoa oil, rye-seed oil, candlenut oil, passionflower oil, sher butter, aloe, Sweet Almond Oil, peach-pit oil, peanut oil, argan oil (argan oil), avocado oil, kopok oil, Common Borage seed oil, flower coconut palm Rape oil, pot marigold oil, cameline oil, canola oil (canola oil), carrot oil, safflower oil, linseed oil, rapeseed oil, cottonseed Oil, coconut oil, pepo oily (marrow seed oil), wheat-germ oil, jojoba oil (jojoba oil), lily oil, Australia Macadamia nut oil, corn oil, white awns flower seed oil (meadowfoam oil), St. john's wort oily (St John ' s Wort oil) rub Noy oil (monoi oil), hazelnut oil, apricot kernel oil, walnut oil, olive oil, evening primrose oil, palm oil, 'Heijialun ' seed oil, macaque Peach seed oil, grape seed oil, pistachio nut oil, winter squash oil, squash oil, musk rose oil, sesame oil, soya-bean oil, sunflower oil, castor Sesame oil and watermelon seed oil and its mixture, or Trivent OCG/Triglyceride DDD of substitution, such as by Stearineries Dubois company sell those of product or by Dynamit Nobel company with title Miglyol 810 , 812 and 818 sell those of product,
The linear chain or branched chain hydrocarbon of 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 saualane;
Synthesis ether containing 10 to 40 carbon atoms;
Synthetic ester, such as the oil of formula RaCOORb, wherein carbon atom number purpose in chain R1 and R2 and be greater than or wait Under conditions of 10, Ra represent the linear chain or branched chain fatty acid residue containing 1 to 40 carbon atom, and Rb represent containing 1 to The hydrocarbyl chain of 40 carbon atoms, especially branched hydrocarbyl chain.The ester especially can be selected from the aliphatic ester of alcohol, such as cetearyl Stearyl;Isopropyl alcohol ester, such as isopropyl myristate, isopropyl palmitate;Ethyl palmitate, palmitinic acid 2- ethylhexyl Ester, stearic acid isopropyl ester, isopropyl isostearate, isostearic acid base isostearate, stearic misery rouge;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, decylate or ricinoleate ester, for example, propylene, cetyl octanoate, Sad tridecane base ester;Bis- enanthic acid 2- ethylhexyl of 4-, palmitinic acid 2- ethylhexyl, benzoic acid alkyl base ester, two enanthic acid are poly- Glycol ester, propylene glycol 2- ethylhexanoate and their mixture;Benzoic acid C12-C15 alcohol ester, lauric acid hexyl ester; Pivalate, such as the different tridecane ester of Dermol 105, neopentanoic acid, neopentanoic acid iso stearyl ester, neopentanoic acid octyldodecyl Base ester;Isononoate, such as the different tridecane ester of isononanoic acid isononyl ester, isononanoic acid, isononanoic acid monooctyl ester;Hydroxylating ester, such as cream Two iso stearyl ester of sour iso stearyl ester and malic acid,
Polyol ester and pentaerythritol ester, such as dipentaerythritol base tetrahydroxy-stearic acid ester/dipentaerythritol base four Isostearate,
The ester of dimer diol and the ester of diacid dimer, such as sold simultaneously by Nippon Fine Chemical company Lusplan DD-DA5 and the Lusplan DD-DA7 being described in patent application US 2004-175 338,
The copolymer and its ester of dimer diol and diacid dimer, such as dimerization Asia oil base glycol (dilinoleyl diol) dimer/dilinoleic acid dimerization composition copolymer and its ester, such as Plandool-G,
The copolymer and its ester of polyalcohol and diacid dimer, such as Hailuscent ISDA or dilinoleic acid/fourth Diol copolymer,
There is the branch for containing 12 to 26 carbon atoms and/or unsaturated carbon-based chain and be at room temperature the fat of liquid Alcohol, such as 2- octyldodecanol, isooctadecanol, oleyl alcohol, 2- hexyl decyl alcohol, 2- butyl octanol 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, such as by Cognis with title Cetiol CC The two decoyl ester of carbonic acid of sale,
The oil of high molecular weight especially has within the scope of about 400 to about 10000g/mol, and especially about 650 to about 10000g/mol, especially about 750 to about 7500g/mol, and rubbing within the scope of more particularly about 1000 to about 5000g/mol That quality.As the oil of high molecular weight for use in the present invention, oil selected from the following can be especially referred to:
Lipophilic polymers,
Straight-chain fatty acid ester with carbon number total in 35 to 70 ranges,
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 the fluorosilicon oil as described in document EP-A-847 752, Fluoropolyether and fluorosilicone;
Silicone oil, such as straight chain or cyclic annular non-volatile dimethione (PDMS);Dimethione, it includes Alkyl, alkoxy or the phenyl of silicone chains side position or end, these groups contain 2 to 24 carbon atoms;Phenyl silicones, such as The poly- front three siloxanes of phenyl, phenyl dimethicone, phenyl trimethicone siloxy diphenyl siloxane, the poly- silicon of diphenyl diformazan Oxygen alkane, diphenyl methyl diphenyl trisiloxanes and 2- phenethyl trimethylsiloxysilicates, and
Their mixture.
According to a specific embodiment, the fat of composition according to the present invention mutually can only contain volatile compound.
Adjuvant
Composition according to the present invention also may include the additional adjuvant of the application field commonly used in imagining.
It especially can be mentioned that water;Organic solvent, especially C1-C6Pure and mild C2-C10Carboxylate;Mineral, animal and/or plant come The carbon-based oil and/or silicone oil in source;Wax, pigment, filler, colorant, surfactant, emulsifier, co-emulsifier;Cosmetic or skin Skin disease activating agent, UV- smoke agent for shielding, polymer, hydrophilic or lipophilic gelling agent, thickener, preservative, fragrance, fungicide, mind Through amide, odour absorbents, antioxidant.
These additional adjuvants can be with 0.001 weight % to 80 weight %, and especially relative to the total weight of composition The ratio of 0.1 weight % to 40 weight % are present in composition.These adjuvants can introduce composition according to their nature Fat mutually or in water phase, or be introduced into lipid vesicle.Under any circumstance, these adjuvants and its ratio will be by this fields Technical staff's selection so that compound according to the present invention favorable property not by or indistinctively the addition imagined is not Benefit influences.
Galen form
This composition can be in any Galen form commonly used in makeup or pharmaceutical field, and is especially in following shape Formula: optionally gelling aqueous 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 by means of bead water phase dispersion, These beads may be polymer nano-particle, such as nanosphere and Nano capsule, or be more preferably ionically and/or non-ionically class The lipid vesicle of type;Aqueous or oil-base gel.These compositions are prepared according to common method.In accordance with the present invention it is preferred that using In the composition of emulsion form, especially oil in water emulsion form.
The composition can more or less be fluid, and can have white or colored creme, paste, lotion, washing lotion, The appearance of slurries, paste, gel or mousse.Composition is optionally applied with aerosol form.Composition can also be in solid shape Formula is especially in stick-like form.
When composition is emulsion, total weight of the ratio of fatty phase relative to composition can be in 5 weight % to 80 weight % In range, and preferably in 8 weight % to 50 weight %.The total weight of emulsifier and co-emulsifier relative to composition, can be with Within the scope of 0.3 weight % to 30 weight %, and preferably exist with the ratio of 0.5 weight % to 20 weight %.
Composition used according to the invention may make up skin care compositions and methods, and in particular for face, hand, foot, Cleaning, protection, treatment or the nursing creme of major anatomical fold or trunk are (for example, day cream, late frost, makeup removing frost, vanishing cream or anti- Shine frost);Foundation emulsion, cleaning lotion, protection or nursing body lotion or ultra light sun block lotion;Skin nursing washing lotion, gel or mousse (mousse), for example, cleaning washing lotion.
According to an aspect of the present invention, it provides for preventing or reducing cutaneous pigmentation and/or desalinate the change of the colour of skin Cosmetic method, the cosmetic method include that topical composition according to the present invention is applied to skin.
According to an aspect of the invention, there is provided the compound of the extract of Paeoniaceae plant and at least one formula (I) Combination production for prevent or reduce cutaneous pigmentation and/or desalinate the colour of skin topical composition in purposes,
Wherein:
R1And R3It is different from each other or identical, independently selected from by hydrogen, linear chain or branched chain C1-C20Acyl carbonyl, linear chain or branched chain C2-C20Alkenyl carbonyl, linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20Alkynyl group At group, be preferably chosen from by hydrogen and linear chain or branched chain C1-C10The group of alkyl composition, is more preferably selected from by hydrogen and straight chain or branch Chain C1-C4The group of alkyl composition, most preferably hydrogen;
R2Selected from by linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20Alkynyl The group of composition, it is therefore preferable to linear chain or branched chain C1-C10Alkyl, more preferably linear chain or branched chain C1-C4Alkyl or ethyl.
Unless otherwise specified, the amount of expression composition used in specification and claims, reaction condition etc. All numerical value be all interpreted as being modified by term " about " in all cases.
Therefore, unless indicated to the contrary, the otherwise numerical parameter described in following description and appended claim It, can be according to attempting to be changed by the required property that the present invention obtains for approximation.
Although illustrating the numberical range of broad range of the invention and parameter being approximation, record is special as accurately as possible Determine numerical value described in example.
However, any numerical value inherently contains certain errors, the error is inevitable by finding in their own measurement Standard deviation causes.Following instance is intended to illustrate the present invention, rather than therefore limits range.Percentage is provided based on weight.
Embodiment:
Embodiment 1: preparation embodiment
It prepares following embodiment (inv exp represents inventive embodiments):
Above-described embodiment is prepared according to the following steps:
1. 75 DEG C at a temperature of, add glycerol, propylene glycol, Phenoxyethanol and sodium hydroxide in water, stir the mixing Object is until homogeneous.
2. phase B to be heated to 75 DEG C of temperature, under turbine stirring, phase B is added to phase A;Speed: 2000 rpm;Machine Device brand: Turboptest TM 2004;Supplier: VMI Turbotest.
3. the temperature of the mixture obtained in step 2 is cooled to 60 DEG C, under turbine stirring, phase C is added to mixed It closes in object;Speed: 2000 rpm;Machine brand: Turboptest TM 2004;Supplier: VMI Turbotest.
4. 25 DEG C at a temperature of phase D is added in the mixture obtained in step 3, mix each ingredient until Matter.The pH of phase D is adjusted, until reaching 4.3 pH.
Embodiment 2: assessment embodiment
To being assessed for preventing or reducing cutaneous pigmentation and/or desalinate the effect of the colour of skin for embodiment.
Using normal human subject melanocyte external test come compound (the wherein R to Chinese herbaceous peony root extract, formula (I)1With R3For hydrogen, R2By ethyl) and the measurement of depigmentation active (reduction of melanin yield) that carries out of their combination is such as Under.
Firstly, growing normal human subject melanocyte and being distributed in 384 blocks of plates.After 24 hours, with containing to be evaluated The medium for estimating raw material (Chinese herbaceous peony root extract, the compound of formula (I) or their combination) replaces the culture medium.Cell is trained It educates 72 hours, then optical density (OD) is finally measured, the final measurement is to measure the black generated by melanocyte The amount of element.
As seen from Figure 1, the positive control (Lu Senuo) of 1g/L concentration inhibits to generate melanin (100% by melanocyte Depigmentation activity).In this model, individual formula (I) compound lower than 1g/L concentration does not show activity (0% depigmentation work Property);And under same concentrations, individual Chinese herbaceous peony root extract shows medium depression effect (49% decoloration generated to melanin Plain activity).
It is also shown by Fig. 1, observes the beauty unexpectedly significantly improved between Chinese herbaceous peony root extract and the compound of formula (I) Bai Xiaoying: when the Chinese herbaceous peony root extract of 1g/L is mixed with the compound of the formula (I) of 0.25g/L, the activity of Chinese herbaceous peony root extract + 49% is increased, reaches 72% depigmentation activity, and this improved whitening effect can rely on the agent of the compound of formula (I) The mode of amount is extended.

Claims (10)

1. a kind of topical composition, the topical composition includes the extract of Paeoniaceae plant and the change of at least one formula (I) The combination of object is closed,
Wherein:
R1And R3It is different from each other or identical, independently selected from by hydrogen, linear chain or branched chain C1-C20Acyl carbonyl, linear chain or branched chain C2- C20Alkenyl carbonyl, linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20Alkynyl composition Group;
R2Selected from by linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20Alkynyl composition Group.
2. topical composition according to claim 1, wherein the extract derive from plant spontaneous growth part and The cultivation part of plant.
3. topical composition according to claim 1 or 2, wherein the Paeoniaceae plant is Chinese herbaceous peony platymiscium.
4. topical composition according to claim 1 or 2, wherein in the combination, the extract and it is described at least A kind of weight ratio of the compound of formula (I) is 1:0.003-1.
5. topical composition according to claim 1 or 2, wherein gross weight of the combination relative to the topical composition Amount is present in the composition with 0.05 weight % to 20 weight %, remaining as the acceptable medium of body.
6. topical composition according to claim 1 or 2, also comprising at least one additional adjuvant.
7. topical composition according to claim 1 or 2 also includes the compound of formula (II),
(II)
Wherein:
R4Selected from by hydrogen, alkali metal ion, linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20The group of alkynyl composition;
R5And R6It is different from each other or identical, independently selected from by hydrogen, linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkene Base and linear chain or branched chain C2-C20The group of alkynyl composition.
8. topical composition according to claim 1 or 2, wherein the compound of the formula (II) is relative to the local group The total weight for closing object is present in the composition with 0.01 weight % to 10 weight %.
9. a kind of non-therapeutic cosmetic method for preventing or reducing cutaneous pigmentation and/or desalinate the colour of skin, described non-to control The property treated cosmetic method includes that topical composition according to any one of claim 1 to 8 is applied to the skin.
10. the combination of the extract of Paeoniaceae plant and the compound of at least one formula (I) is being generated for preventing or reducing skin Purposes in the topical composition of skin pigmentation and/or the desalination colour of skin,
Wherein:
R1And R3It is different from each other or identical, independently selected from by hydrogen, linear chain or branched chain C1-C20Acyl carbonyl, linear chain or branched chain C2- C20Alkenyl carbonyl, linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20Alkynyl composition Group;
R2Selected from by linear chain or branched chain C1-C20Alkyl, linear chain or branched chain C2-C20Alkenyl and linear chain or branched chain C2-C20Alkynyl composition Group.
CN201380077852.4A 2013-06-28 2013-06-28 For preventing or reducing cutaneous pigmentation and/or desalinate the topical composition and application thereof of the colour of skin Active CN105307729B (en)

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