CN101175469A - Regulation of mammalian keratinous tissue using personal care compositions comprising diethylhexyl syringylidene malonate - Google Patents

Regulation of mammalian keratinous tissue using personal care compositions comprising diethylhexyl syringylidene malonate Download PDF

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CN101175469A
CN101175469A CNA2006800169259A CN200680016925A CN101175469A CN 101175469 A CN101175469 A CN 101175469A CN A2006800169259 A CNA2006800169259 A CN A2006800169259A CN 200680016925 A CN200680016925 A CN 200680016925A CN 101175469 A CN101175469 A CN 101175469A
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skin
acid
active substance
personal care
compositions
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D·L·比赛特
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Procter and Gamble Ltd
Procter and Gamble Co
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Procter and Gamble Ltd
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Abstract

Personal care composition including a first skin and/or hair care active cetyl pyridinium chloride; and at least one additional skin and/or hair care active selected from the group consisting of tetrahydrocurcumin, sugar amine, vitamin B3, retinoids, hydroquinone, peptides, phytosterol, dialkanoyl hydroxyproline, hexamidine, salicylic acid, n-acyl amino acid compounds, sunscreen actives, water soluble vitamins, oil soluble vitamins, hesperedin, mustard seed extract, glycyrrhizic acid, glycyrrhetinic acid, carnosine, Butylated Hydroxytoluene (BHT) and Butylated Hydroxyanisole (BHA), ergothioneine, vanillin or its derivatives, diethylhexyl syrinylidene malonate, melanostatine, sterol esters, idebenone, dehydroacetic acid, Licohalcone A, creatine, creatinine, feverfew extract, yeast extract, beta glucans, alpha glucans, their salts, their derivatives, their precursors, and/or combinations thereof; and a dermatologically acceptable carrier. The invention further relates to methods for regulating the condition of mammalian keratinous tissue wherein the methods each comprise the step of topically applying to the keratinous tissue of a mammal needing such treatment, a safe and effective amount of the personal care composition of the invention.

Description

Use comprises the personal care composition of cetylpyridinium chloride and regulates mammiferous collenchyme
Technical field
The present invention relates to comprise the personal care composition of skin and hair-care active substance such as cetylpyridinium chloride.Described compositions can be used for regulating the mammiferous keratinous tissue conditions of the above-mentioned processing of needs, especially can be used for prevention, postpones and/or handle the uneven colour of skin, for example is used as blast skin or reduces Pigmented cosmetic agent.
Background of invention
Consumer at present obtainable many personal care products is intended to improve collenchyme such as skin, hair and refer to/health and the physical appearance of toenail.In these products, the overwhelming majority relates to delay, minimize or even eliminate a crease in the skin and the histology changes, described variations is typical relevant to the infringement of human skin with skin aging or environment.Yet, still need cosmetic agent by being used as blast skin or reducing Pigmented cosmetic agent and prevent, postpone and/or handle the uneven colour of skin.
Mammiferous collenchyme, especially Ren Lei skin and hair are subjected to the infringement of many external and intrinsic factor.Above-mentioned extrinsic factor comprises ultraviolet radiation, environmental pollution, wind, Exposure to Sunlight, infrared radiation, low humidity, deleterious surfactant, grinding agent etc.On the other hand, intrinsic factor comprise that other biochemistry in chronological age and the skin changes.No matter be extrinsic factor or intrinsic factor, they all cause producing tangible skin injury sign.Typical skin injury comprises the thinning of skin of the Lock-in along with the increase at age.Along with above-mentioned thinning of skin, cell and the blood vessel of supplying with skin are reducing.In addition, corium-epidermis junction is smooth day by day, and this causes the mechanical of this junction to die down." The Aging of Skin:Chronoaging Versus Photoaging " (the 3rd to page 4, nineteen ninety for Photodermatol.Photoimmunol.Photomed., the 7th volume) referring to for example Oikarinen.Visible other damage or variation comprise that microgroove, wrinkle, hyperpigmentation, sallow, sagging, black eye, swollen eye, pore increase, renewal rate slows down and abnormal desquamation or decortication on the aging or damaged skin.Other damage that causes owing to extrinsic factor and intrinsic factor comprises tangible dead bark (be exfoliation, peel off, coarse).For hair, except other problem, these extrinsic factor and intrinsic factor can cause bleaching hair, hair bifurcated, slim and frahile, coarse, trichomadesis, hair growth speed to slow down etc.Therefore, need to try hard to improve the product and the method for these keratinous tissue conditions.
The preferred embodiment general introduction
The applicant finds that the topical compositions that comprises some skin and hair-care active substance can be used for providing preventative and therapeutic treatment to keratinous tissue conditions, especially blast skin treatment.
According to a preferred embodiment of the present invention, a kind of personal care composition now is provided, described compositions comprises:
A) skin and/or hair-care active substance, described active substance is selected from the group of being made up of following material: cetylpyridinium chloride, Dodecyl trimethyl ammonium chloride, TPC, the cetyl dimethyl benzyl ammonium chloride, chlorination 1-cetyl pyridinium, the dimethyl stearyl benzyl ammonium chloride, hexadecyltrimethylammonium chloride, cetyl trimethyl ammonium bromide, octadecyl trimethyl ammonium chloride, domiphen bromide, chlorination N-myristyl-4-ethylpyridine, dodecyl dimethyl (2-phenoxy group ethyl) ammonium bromide, benzyl dimethyl stearyl chlorination ammonium, quaternized 5-amino-1,3-two (2-ethylhexyl)-5-methyl hexahydropyrimidine, alkyl benzyl dimethyl ammonium chloride, iso-octyl phenoxy group ethoxyethyl group benzyl dimethyl ammonium chloride, methyl iso-octyl phenoxy group ethoxyethyl group benzyl dimethyl ammonium chloride, and/or their combination;
B) at least a additional skin and/or hair-care active substance, described active substance is selected from the group of being made up of following material: tetrahydrocurcumin, osamine, vitamin B 3Retinoid, hydroquinone, peptide, plant sterol, two alkanoyl hydroxyprolines, primoline, salicylic acid, n-acyl amino acid compound, sunscreen actives, water soluble vitamins, fat soluble vitamin, hesperetin, the Semen Brassicae Junceae extract, glycyrrhizic acid, enoxolone, carnosine, Yoshinox BHT (BHT) and butylated hydroxyanisol (BHA), ergothioneine, the vanillin or derivatives thereof, Aden's perfume base malonic acid ethylhexyl, melanonostatin, sterol ester, idebenone, dehydroactic acid, licochalcone A, creatine, kreatinin, the Radix Agrimoniae extract, yeast extract, beta glucan, alpha-glucans, their salt, their derivant, their precursor and/or their combination; With
C) dermatological acceptable carrier.
The invention still further relates to the method that is used to regulate mammiferous keratinous tissue conditions, wherein each described method includes personal care composition of the present invention with safe and effective amount and locally applies to step on the mammiferous collenchyme that needs above-mentioned processing.The method that is used in the personal care composition marketization of regulating mammiferous keratinous tissue conditions also is provided.Also provide the method for implementing business activity, wherein to the information of consumer's transmission about personal care composition of the present invention.
Illustrative and embodiment preferred describes in detail
Except as otherwise noted, all percentage ratios used herein and ratio are all by the weight of total composition, and all measurements are all carried out at 25 ℃.
Compositions of the present invention can comprise, basically by or be grouped into by solvent described herein and nonessential one-tenth.Used herein " basically by ... form " be meant that described compositions or component can comprise supplementary element, as long as described supplementary element can not change the new characteristic of fundamental sum of claimed compositions of the present invention or method in itself.
Term used herein " collenchyme " is meant the horny layer that contains as mammal outermost layer guard cover, and it includes but not limited to skin, hair, toenail, fingernail, epidermis, hoof etc.
Term used herein " local application " is meant to be used compositions of the present invention or be applied on the surface of collenchyme.
Term used herein " dermatological is acceptable " is meant that described compositions or component are applicable to human collenchyme and contacts, and do not have unsuitable toxicity, incompatibility, unstability, atopic reaction etc.
Term used herein " safe and effective amount " is meant that the amount of chemical compound or compositions is enough to significantly produce positive beneficial effect, preferably produces positive collenchyme outward appearance or sensation beneficial effect.This beneficial effect comprises beneficial effect independently disclosed herein or combination, but this amount enough hang down again with avoid serious adverse (that is, and in the rational determination range of technical staff, provide rational effect by inches than).
Term used herein " hyperpigmentation after the inflammation " is meant the variation of the melanin content that reflects because of inflammation incident (as acne, scratch, sting, Exposure to Sunlight etc.), and is especially obvious to the experimenter of dark skin.
Term used herein " hyperpigmentation " is meant that wherein pigmentation is greater than the Pigmented skin area of skin adjacent domain (as eyespot, senile plaque etc.).
Term used herein " desquamation, decortication and/or renewal " is meant the outer layer of stratum corneum removal of (comprising horny layer).
Term used herein " oiliness and/or glossy appearance " is meant that the mammal skin with smooth appearance is tending towards demonstrating oils and fats, sebum and/or the perspiration from separately glandular secretion.
Term used herein " sagging " is meant the situation such as lax, sagging of skin, and described situation is by the proteic loss of skin elasticity, destruction, change and/or unusual the generation.
Term used herein " smooth " and " softening " are meant that the surface that changes collenchyme is to improve sense of touch.
Term used herein " sallow " is meant the protein glycation effect that together takes place owing to for example typical case and skin aging and lipofuscin gathers or peripheral blood flow minimizing effect, because of the loss of skin component, destruction, change and/or unusual so that situations such as the skin color that their variable colors (for example color jaundice) produce is greyish white, jaundice.
Compositions of the present invention can be used for local application, and can be used for regulating keratinous tissue conditions.Because intrinsic factor and/or extrinsic factor can bring out or cause the various situations of health, so usually need be, especially the human skin situation is regulated to keratinous tissue conditions.For example, " adjusting skin " comprises preventative adjusting and/or therapeutic regulation skin, and can comprise following one or more beneficial effects: thicken and (promptly construct epidermal area and/or skin corium and/or hypodermic layer such as the fat and the muscle of skin, and under suitable situation, structure refers to/horny layer of toenail and hair shaft) to reduce atrophy (as the atrophy of skin), increase curling of corium-epidermis border, plain dyschromasia of non-black such as eye pouch, the rash speckle (for example, by the inhomogeneous redness that causes as acne erythematosa) (hereinafter being referred to as erythema), sallow (canescence or yellow), the variable color that causes by telangiectasis or spider shape blood vessel, by melanin (as eyespot, senile plaque, inhomogeneous pigment calmness) (the lipofuscin for example of other chromophore and in the skin, protein cross those as occurring with saccharification, or the like) variable color that causes.Preventative adjusting skin used herein comprises delay, minimizes and/or prevents visible and/or palp skin discontinuity (for example, appreciable in irregular texture, microgroove, wrinkle, sagging, stretching vestige, honeycomb inflammation, swollen eye or the like skin or feel).Therapeutic regulation skin used herein comprises the discontinuity of improving (for example reduce, farthest reduce and/or eliminate) skin.Regulating skin comprises and improves skin appearance and/or sensation.
Term used herein " adjusting skin " be intended to comprise these signs adjusting and no matter the mechanism of the origin cause of formation.
The compositions of the present invention that comprises solvent and optional component thereof will be explained below.
Component
Compositions of the present invention can comprise the cetylpyridinium chloride (CPC) of safe and effective amount.The replacement form of hexadecylpyridinium chloride comprises quaternary compound, wherein one or two substituent carbon chain lengths (being typically alkyl) is about 8 to about 22 on the quaternary nitrogen, typical case about 10 is to about 18 carbon atoms, remain substituent group (being typically alkyl or benzyl) simultaneously and have carbon number still less, 1 to about 7 carbon atoms (being typically methyl or ethyl) according to appointment.These alkyl chains that substitute in the form can be straight or brancheds, and can be saturated or unsaturated.Dodecyl trimethyl ammonium chloride, TPC, the cetyl dimethyl benzyl ammonium chloride, chlorination 1-cetyl pyridinium, the dimethyl stearyl benzyl ammonium chloride, hexadecyltrimethylammonium chloride, cetyl trimethyl ammonium bromide, octadecyl trimethyl ammonium chloride, domiphen bromide, chlorination N-myristyl-4-ethylpyridine, dodecyl dimethyl (2-phenoxy group ethyl) ammonium bromide, benzyl dimethyl stearyl chlorination ammonium, quaternized 5-amino-1,3-two (2-ethylhexyl)-5-methyl hexahydropyrimidine, alkyl benzyl dimethyl ammonium chloride, iso-octyl phenoxy group ethoxyethyl group benzyl dimethyl ammonium chloride and methyl iso-octyl phenoxy group ethoxyethyl group benzyl dimethyl ammonium chloride are the examples of typical quaternary ammonium reagent.Other chemical compound is two-4-(R-amino)-1-pyridine alkane, and it is disclosed in United States Patent (USP) 4,206, in 215.The electronegative counter ion counterionsl gegenions of these quaternary compounds are typically chloride ion or bromide ion, but alternatively are fluorion, iodide ion, inferior sulfate radical, sulfate radical, carbonate etc.
The content of cetylpyridinium chloride or other quaternary compound counts about 0.005% to about 10% by the weight of described compositions, and more preferably from about 0.01% to about 5%, and more preferably from about 0.05% to about 2%.A discovery that never reckons with is, cetylpyridinium chloride is the inhibitor of some enzyme related in the pigmentation process, as tryrosinase.It is believed that other quaternary compound except that the chlorination cetyl pyridinium also can suppress enzyme related in the pigmentation process.The protein-tyrosine enzyme is that amino acid tyrosine is transformed into DOPA (Dihydroxyphenylalanine), further is transformed into other intermediate then and is aggregated to enzyme related in the dermal melanin process.The inhibition partially or completely of tryrosinase is delayed or stoped the formation of melanocyte respectively, and produce the more shallow colour of skin (for example, having reduced the degree of depth of hyperpigmentation speckle).
This paper provides the personal care composition that comprises cetylpyridinium chloride or other quaternary compound by local application to come the cosmetic treatments mammal skin to improve the method for colour of skin outward appearance.
Additional skin and/or hair-care active substance
In the preferred embodiment of the invention, at least some comprise at least a additional skin and/or the hair-care active substance of safe and effective amount.In a preferred embodiment, these skins and/or hair-care active substance are selected from the group of being made up of following material: tetrahydrocurcumin, osamine (for example comprising glycosamine and N-acetyl glucosamine), vitamin B 3(for example comprising nicotiamide); retinoid; peptide; plant sterol; two alkanoyl hydroxyprolines; primoline; salicylic acid; n-acyl amino acid compound; sunscreen actives; water soluble vitamins; fat soluble vitamin; hesperetin; the Semen Brassicae Junceae extract; glycyrrhizic acid; enoxolone; carnosine; Yoshinox BHT (BHT) and butylated hydroxyanisol (BHA); ergothioneine; the vanillin or derivatives thereof; Aden's perfume base malonic acid ethylhexyl; melanonostatin; sterol ester; fatty acid (especially polyunsaturated fatty acid); 1-oxygen-2-mercaptopyridine zinc (ZPT); antifungal; mercaptan compound is (as the N-acetylcysteine; glutathion; the thioglycol acid esters); solatene; ubiquinone; aminoacid; idebenone; dehydroactic acid; licochalcone A; creatine; kreatinin; the Radix Agrimoniae extract; yeast extract is (as Pitera ), beta glucan, alpha-glucans, Radix Agrimoniae extract, creatine, kreatinin, licochalcone A, their salt, their derivant, their precursor and/or their combination.A part of further describing in these additional activity materials hereinafter is provided.
Skin of the present invention and/or hair-care active substance can be used for blast skin.Blast skin can take place by number of mechanisms, comprises antioxidant mechanism, trypsin inhibitory action, antiinflammatory mechanism, nitric oxide scavenging action, tyrosinase inhibitory action etc.Therefore, exist these machine-processed chemical compounds to have the probability of blast skin.
1. tetrahydrocurcumin
The present invention comprises tetrahydrocurcumin (THC), its derivant such as ester or the ether and their combination of safe and effective amount.Preferably, described compositions comprises by the weight of described compositions about 0.01% to about 10%, and more preferably from about 0.1% to about 5%, even 0.2% to about 3% curcuminoid chemical compound more preferably from about.
Because many stimulations as contact ultraviolet and stimulus object, and cause producing oxygen-derived free radicals in skin.Above-mentioned free radical also can be used as ordinary cells or anabolic by-product and produces.Oxygen-derived free radicals can stimulate pigment cell's (melanocyte) to increase the generation of melanocyte.Curcuminoid (as THC) has antioxidant properties, thereby can before oxygen-derived free radicals stimulates melanocyte they be removed.
The protein-tyrosine enzyme is that amino acid tyrosine is transformed into DOPA (Dihydroxyphenylalanine), further is transformed into other intermediate then and is aggregated to enzyme related in the dermal melanin process.The inhibition partially or completely of tryrosinase is delayed or stoped the formation of melanocyte respectively, and produce the more shallow colour of skin (for example, having reduced the degree of depth of hyperpigmentation speckle).Curcuminoid (as THC) but also restraint of tyrosinase.
Other curcuminoid that can be used among the present invention comprises curcumin, tetrahydrochysene demethoxycurcumin, tetrahydrochysene bisdemethoxycurcumin, their derivant such as ester and ether and their combination.Curcuminoid (as THC) can have natural or synthetic source.Preferably, in the present invention, tetrahydrocurcumin can use separately, or unites use with the tetrahydrochysene demethoxycurcumin, and/or unites use with the tetrahydrochysene bisdemethoxycurcumin.Preferred derivant is an ester, especially tetrahydrocurcumin diacetate esters, and/or the combination of itself and tetrahydrocurcumin, and/or the combination of itself and tetrahydrochysene demethoxycurcumin, and/or the combination of itself and tetrahydrochysene bisdemethoxycurcumin, and/or combination, especially tetrahydrochysene demethoxycurcumin diacetate esters and/or the tetrahydrochysene bisdemethoxycurcumin diacetate esters of itself and ester.
Figure S2006800169259D00071
2. osamine (amino sugar)
Compositions of the present invention not necessarily comprises the osamine of safe and effective amount, and it is also referred to as amino sugar.The osamine chemical compound that can be used among the present invention is described in PCT announcement WO 02/076423 and the United States Patent (USP) 6,159,485.
Said composition preferably comprises by the weight of described compositions about 0.01% to about 15%, and more preferably from about 0.1% to about 10%, even 0.5% to about 5% osamine more preferably from about.
Osamine derives from synthetic or natural, and the mixture (for example being derived from the natural extract or the mixture of synthetic) that can be used as pure compound or chemical compound uses.Glycosamine is present in many Crustaceans and also usually can derive from fungal source.Term used herein " osamine " comprises the isomer and the tautomer of above-mentioned substance and salt (as HCl salt) thereof, and commercially available from SigmaChemical Co..
The example that can be used for osamine of the present invention comprises glycosamine, N-acetyl glucosamine, glucosamine sulfate, mannosamine, N-acetylmannosamine, galactosamine, N-acetyl group galactosamine, their isomer (as stereoisomer) and their salt (as HCl salt).What preferably can be used for this paper is glycosamine, especially D-glycosamine and N-acetyl glucosamine, especially N-acetyl group-D-glycosamine.
3. vitamin B 3
Compositions of the present invention can comprise the vitamin B of safe and effective amount 3Chemical compound.Vitamin B 3Chemical compound especially can be used for regulating skin, as United States Patent (USP) 5,939, described in 082.Preferably, described compositions comprises by the weight of described compositions about 0.01% to about 50%, and more preferably from about 0.1% to about 20%, even more preferably from about 0.5% to about 10%, also more preferably from about 1% to about 7%, even 2% to about 5% vitamin B more preferably from about 3Chemical compound.
" vitamin B used herein 3Chemical compound " be meant chemical compound with following formula structure:
Wherein R is-CONH 2(being nicotinamide) ,-COOH (being nicotinic acid) or-CH 2OH (being nicotinyl alcohol); Its derivant; Salt with any aforesaid compound.
Aforementioned vitamin B 3The exemplary derivant of chemical compound comprises nicotinate, and described ester comprises the non-vasodilation ester (as tocopheryl nicotinate, myristyl nicotinate) of nicotinic acid.
Suitable vitamin B 3Examples for compounds be well known in the art and can be from a plurality of sources (as Sigma Chemical Company, ICN Biomedicals, Inc. and AldrichChemical Company) commercially available.Preferably can be used for the vitamin B among the present invention 3Chemical compound is a nicotiamide.
4. retinoid
Compositions of the present invention can comprise the retinoid of safe and effective amount, so that resulting composition can be used to regulate keratinous tissue conditions safely and effectively, is preferred for regulating the vision and/or the sense of touch discontinuity of skin, more preferably is used to regulate signs of skin aging.Described compositions preferably comprises by the weight of described compositions about 0.001% to about 10%, and more preferably from about 0.005% to about 2%, even more preferably from about 0.01% to about 1%, also 0.01% to about 0.5% retinoid more preferably from about.Best working concentration in the compositions will depend on required concrete retinoid, because their effect has sizable difference.
" retinoid " used herein comprises the chemical compound with bioactive all natural and/or synthetic vitamin A analog of vitamin A in the skin or similar retinol, and the geometric isomer of these chemical compounds and stereoisomer.Retinoid is preferably selected from retinol, retinol ester (for example, the C of retinol 2-C 22Arrcostab comprises retinyl palmitate, retinyl acetate, Vitamin A propionate), retinal and/or tretinoin (comprising all-trans retinoic acid and/or 13-cis-retinoic acid) or their mixture.More preferably retinoid is the retinoid except that tretinoin.Preferred retinoid has retinol, retinyl palmitate, retinyl acetate, Vitamin A propionate, retinal and their combination.More preferably Vitamin A propionate, consumption even more preferably about 0.1% to about 0.3%.
5. peptide
Compositions of the present invention can comprise the peptide of safe and effective amount, includes but not limited to dipeptides, tripeptides, tetrapeptide, pentapeptide and six peptides and their derivant.Described compositions preferably comprises by the about 1x10 of the weight of described compositions -6% is to about 20%, more preferably from about 1x10 -6% is to about 10%, even 1x10 more preferably from about -5% is about 5% peptide extremely.
Term used herein " peptide " is meant and comprises ten or still less amino acid whose peptide and their derivant, isomer, and with the coordination compound of other material such as metal ion (for example, copper, zinc, manganese, magnesium or the like).Peptide used herein not only refers to naturally occurring peptide but also refer to synthetic peptide.Also can be used for of the present invention is the naturally occurring and commercially available peptide combinations that contains.Preferred peptide is the lipophilic derivatives of dipeptides carnosine (Beta-alanine-histidine), tripeptides (glycine-histidine-lysine), pentapeptide (lysine-threonine-threonine-lysine-serine), peptide, and above-mentioned metal complex, as the copper complex of tripeptides (HIS-GLY-glycine) (being also referred to as Iamin).Preferred dipeptidase derivant is palmityl-lysine-threonine.The commercial composite that preferably comprises tripeptide derivative is Biopeptide CL , it comprises palmityl-glycine-histidine-lysine of 100ppm, and available from Sederma.The commercial composite that preferably comprises pentapeptide derivative is Matrixyl , palmityl-lysine-threonine-threonine-lysine-serine that it comprises 100ppm is purchased from Sederma.
6. plant sterol
Topical compositions of the present invention can comprise one or more plant sterols of safe and effective amount, and described plant sterol is selected from the group of being made up of following material: cupreol, campesterol, campesterol, Δ 5-avenasterol, lupeol, hitodesterol, stigmasterol, their derivant, analog and their combination.More preferably, described plant sterol is selected from the group of being made up of following material: cupreol, campesterol, campesterol, stigmasterol, their derivant (especially their ester) and their combination.More preferably, plant sterol is a stigmasterol.
Plant sterol derives from synthetic or natural, and can be used as pure chemical compound itself or the mixture (for example deriving from the extract of natural source) of chemical compound uses.Plant sterol is present in the not saponification part of plant oil ﹠ fat usually, and they obtain with the form of free sterol, acetyl derivatives, sterol ester, ethoxylation or glycosides derivatives.More preferably, plant sterol is a free sterol.Term used herein " plant sterol " comprises the isomer and the tautomer of above-mentioned substance, and can be commercially available from Aldrich Chemical Company, Sigma Chemical Company and Cognis.
In compositions of the present invention, the content of plant sterol is preferably about 0.0001% to about 25% by the weight of described compositions, and more preferably from about 0.001% to about 15%, even more preferably from about 0.01% to about 10%, also more preferably from about 0.1% to about 5%, even more preferably from about 0.2% to about 2%.
7. primoline
Can be used for primoline chemical compound among the present invention corresponding to having those of following chemical constitution:
Figure S2006800169259D00111
R wherein 1And R 2Comprise organic acid (as sulfonic acid etc.).
In compositions of the present invention, the content of primoline is preferably about 0.0001% to about 25% by the weight of described compositions, and more preferably from about 0.001% to about 10%, and more preferably from about 0.01% to about 5%, and even more preferably from about 0.02% to about 2.5%.
Topical compositions of the present invention can nonessentially comprise one or more primoline chemical compounds of safe and effective amount, its salt and its derivant.Primoline derivant used herein comprises all isomers and the tautomer of primoline chemical compound, includes but not limited to organic acid and mineral acid, for example sulfonic acid, carboxylic acid etc.Preferably, the primoline chemical compound comprises dihydroxy ethyl sulfonic acid primoline, and it is with trade name Elestab HP100 is commercially available from LaboratoiresSerobiologiques.
8. two alkanoyl hydroxyproline chemical compounds
Two alkanoyl hydroxyproline chemical compounds of the present invention are corresponding to having those of following chemical constitution:
R wherein 1Comprise H, X, C 1-C 20The straight or branched alkyl,
X comprises metal (Na, K, Li, Mg, Ca) or amine (DEA, TEA);
R 2Comprise C 1-C 20The straight or branched alkyl;
R 3Comprise C 1-C 20The straight or branched alkyl.
Topical compositions of the present invention can comprise one or more two alkanoyls hydroxyproline chemical compound and their salt and derivants of safe and effective amount.In compositions of the present invention, the content of two alkanoyl hydroxyproline chemical compounds is preferably about 0.01% to 10% by the weight of described compositions, and more preferably from about 0.1% to 5%, even more preferably from about 0.1% to 2%.
Suitable derivant includes but not limited to ester such as aliphatic ester, includes but not limited to three palmityl hydroxyprolines and two palmityl acetyl group hydroxyprolines.Especially available chemical compound is a dipalmitoyl hydroxyproline.Dipalmitoyl hydroxyproline used herein comprises all isomers and the tautomer of above-mentioned substance, and with trade name Sepilift DPHP From Seppic, Inc. is commercially available.The further argumentation of dipalmitoyl hydroxyproline can be announced WO 93/23028 referring to PCT.Dipalmitoyl hydroxyproline is preferably the triethanolamine salt of dipalmitoyl hydroxyproline.
9. salicylic acid compound
Topical compositions of the present invention can comprise the salicylic acid compound of safe and effective amount, its ester, its salt, or their combination.In compositions of the present invention, salicylic acid compound preferably comprises by the weight of described compositions about 0.0001% to about 25%, more preferably from about 0.001% to about 15%, even more preferably from about 0.01% to about 10%, also more preferably from about 0.1% to about 5%, even 0.2% to about 2% salicylic acid more preferably from about.
10.N-amic acid chemical compound
Topical compositions of the present invention can comprise one or more N-amic acid chemical compounds of safe and effective amount.Described aminoacid can be any aminoacid known in the art.N-acyl amino acid compound of the present invention meets the following formula structure:
Figure S2006800169259D00121
Wherein R can be the combination of hydrogen, alkyl (replace or unsubstituted, side chain or straight chain) or alkyl and aryl.Aminoacid known in the art may side chain tabulation be described among " Biochemistry " of the Stryer that announced by W.H.Freeman and Company in 1981.R 1Can be saturated or undersaturated, straight or branched, replacement or unsubstituted C 1To C 30Alkyl; Replace or unsubstituted aryl; Or their mixture.
N-amic acid chemical compound is preferably selected from N-acyl group phenylalanine, N-acyl group tyrosine, their isomer, their salt and their derivant.Aminoacid can be D or L isomer or their mixture.N-acyl group phenylalanine meets the following formula structure:
Figure S2006800169259D00131
R wherein 1Can be C 1To C 30Saturated or undersaturated, straight or branched, replacement or unsubstituted alkyl; Replace or unsubstituted aromatic group or their mixture.
N-acyl group tyrosine meets the following formula structure:
Figure S2006800169259D00132
R wherein 1Can be C 1To C 30Saturated or undersaturated, straight or branched, replacement or unsubstituted alkyl; Replace or unsubstituted aromatic group; Or their mixture.
What especially can be used as the cosmetic agent that makes local colour of skin unanimity (blast skin or reduce pigmentation) is N-endecatylene acyl-L-phenylalanine.This reagent belongs to generalized N-acyl group Phenylalamine derivatives classification, and its acyl group is a C11 monounsaturated fatty acid part, and aminoacid is the L-isomer of phenylalanine.N-endecatylene acyl-L-phenylalanine meets the following formula structure:
Figure S2006800169259D00141
N-endecatylene acyl group used herein-L-phenylalanine can trade name Sepiwhite Commercially available from SEPPIC.
In compositions of the present invention, the content of N-acylamino acid is preferably about 0.0001% to 25% by the weight of described compositions, and more preferably from about 0.001% to 10%, more preferably from about 0.01% to 5%, even more preferably from about 0.02% to 2.5%.
11. sunscreen actives
This theme invention compositions can not necessarily comprise the sunscreen actives agent." sunscreen actives " used herein comprises sunscreen and physical sunscreen frost.Suitable sunscreen actives can be organic or inorganic.
There is multiple conventional sunscreen actives to be applicable to this paper.People such as Sagarin disclose multiple suitable actives matter since 189 pages at the VIII chapter of " CosmeticsScience and Technology " (1972) to later part.Especially Shi Yi sunscreen is p-methoxycinnamic acid-2-Octyl Nitrite (commercially available with trade name PARSOL MCX), 4,4 '-tert-butyl group methoxy dibenzoyl methane (commercially available) with trade name PARSOL 1789,2-hydroxyl-4-methoxyl group benzophenone, the octyldimethyl para-amino benzoic acid, two times of acyl trioleates, 2,2-dihydroxy-4-methoxyl group benzophenone, 4-(two (hydroxypropyl)) benzocaine, 2-cyano group-3,3-diphenylacrylate-2-Octyl Nitrite, salicylic acid-2-Octyl Nitrite, para-amino benzoic acid glyceride, 3,3,5-trimethylcyclohexyl salicylate, artificial neroli oil, ESCAROL 507 or Aminobenzoate, ESCAROL 507-2-Octyl Nitrite, 2-Phenylbenzimidazole-5-sulfonic acid, 2-(to dimethylaminophenyl)-5-sulfonic acid benzoxazole acid, octocrylene, zinc oxide, titanium dioxide, and the mixture of these chemical compounds.
The organic sunscreen active substance that preferably can be used in the present composition is p-methoxycinnamic acid-2-Octyl Nitrite, PAROSOL 1789,2-hydroxyl-4-methoxy benzophenone, 2-Phenylbenzimidazole-5-sulfonic acid, octyldimethyl para-amino benzoic acid, octocrylene, zinc oxide, titanium dioxide and their mixture.Especially preferred sunscreen actives comprises 4,4 '-tert-butyl group methoxy dibenzoyl methane, p-methoxycinnamic acid-2-Octyl Nitrite, Phenylbenzimidazolesulfonic acid, octocrylene, zinc oxide and titanium dioxide and their mixture.
The content of sunscreen actives is preferably about 1% to about 20% by the weight of described compositions, and more preferably from about 2% to about 10%.Its accurate consumption will depend on selected sunscreen and required sun protection factor (SPF).
12. water soluble vitamins
The present composition can comprise one or more water soluble vitamins of safe and effective amount.The example of water soluble vitamins includes but not limited to water-soluble sexual type vitamin B (as vitamin B5 and vitamin B6 (as pyridoxin)), vitamin B derivant, vitamin C (ascorbic acid), vitamin C derivatives (as ascorbyl glucoside, magnesium ascorbyl phosphate, sodium ascorbyl phosphate and ascorbic palmitate), vitamin K, vitamin K derivant, their provitamin such as pantothenylol and their mixture.When containing element-vitamine compound in the present composition, said composition preferably comprises by the weight of described compositions about 0.0001% to about 50%, more preferably from about 0.001% to about 10%, also more preferably from about 0.01% to about 8%, and 0.1% to about 5% element-vitamine compound more preferably from about also.
13. fat soluble vitamin
Compositions of the present invention can comprise one or more fat soluble vitamins of safe and effective amount.The example of fat soluble vitamin includes but not limited to oil-soluble type vitamin D, vitamin D-derivatives, vitamin E (as vitamin e acetate), vitamin e derivative, their provitamin such as pantothenylol and their mixture.When comprising the fat soluble vitamin chemical compound in the compositions of the present invention, described compositions preferably comprises by the weight of described compositions about 0.0001% to about 50%, more preferably from about 0.001% to about 10%, also more preferably from about 0.01% to about 8%, 0.1% to about 5% fat soluble vitamin chemical compound more preferably from about also.
14. hesperetin
Compositions of the present invention can comprise the hesperetin of safe and effective amount.Hesperetin in the compositions is preferably its derivant glucityl hesperetin.Preferably, described compositions comprises by the weight of described compositions about 0.01% to about 10%, and more preferably from about 0.1% to about 5%, even 0.5% to about 3% hesperetin chemical compound more preferably from about.
Hesperetin and glucityl hesperetin are flavonoid.Because many stimulations as contact ultraviolet and stimulus object, and cause producing oxygen-derived free radicals in skin.Above-mentioned free radical also can be used as ordinary cells or anabolic by-product and produces.Oxygen-derived free radicals can stimulate pigment cell's (melanocyte) to increase the generation of melanocyte.Hesperetin and glucityl hesperetin have antioxidant properties, thereby can before oxygen-derived free radicals stimulates melanocyte they be removed.
The protein-tyrosine enzyme is that amino acid tyrosine is transformed into DOPA (Dihydroxyphenylalanine), further is transformed into other intermediate then and is aggregated to enzyme related in the dermal melanin process.Inhibition partially or completely to tryrosinase delays or has stoped the formation of melanocyte respectively, produces the brighter colour of skin (for example, having reduced the degree of depth of hyperpigmentation speckle).But hesperetin and glucityl hesperetin be restraint of tyrosinase also.
15. glycyrrhizic acid
Compositions of the present invention can comprise the glycyrrhizic acid of safe and effective amount and/or its salt.Preferably, described compositions comprises by the weight of described compositions about 0.01% to about 10%, and more preferably from about 0.05% to about 5%, even 0.1% to about 3% glycyrrhizic acid chemical compound more preferably from about.Glycyrrhizic acid is the component in the Radix Glycyrrhizae extract.
Glycyrrhizic acid is an antiinflammatory.Inflammatory mediators or cytokine can stimulate pigment cell's (melanocyte) to produce melanocyte.Therefore, inflammation situation such as ultraviolet injury, acne, ingrown hair, sting, scratch etc. will excite hyperpigmentation after the so-called inflammation.Though ultraviolet is the main inducer of all types cutaneous pigmentation, specifically, will promote the pigmentation of dark skin individuality (as Spaniard, Aisan) skin by the pigment of other inflammatory stimulus (acne etc.) generation.Will reduce pigmentation with the antiinflammatory inflammation-inhibiting.
It is believed that also glycyrrhizic acid is nitric oxide production scavenger.Nitric oxide (NO) is Pigmented stimulant.Use nitric oxide scavengers (reacting to stop it to stimulate chromatophorous material) will reduce pigmentation with nitric oxide.
Glycyrrhizic acid also is called as glycyrrhizin, glycyrrhizin or glycyrrhizin.
16. enoxolone
Compositions of the present invention can comprise the enoxolone of safe and effective amount and/or its salt.Preferably, described compositions comprises by the weight of described compositions about 0.01% to about 10%, and more preferably from about 0.05% to about 5%, even 0.1% to about 3% enoxolone chemical compound more preferably from about.Enoxolone is the component in the Radix Glycyrrhizae extract.
Enoxolone also is an antiinflammatory, is discussed in above in the glycyrrhizic acid part.Enoxolone structurally is different from glycyrrhizic acid, because enoxolone does not have the saccharide residue (glycoside) of connection.Enoxolone also is called as carbenoxolone, glycyrrhetinic acid or biosone.
17. carnosine
Compositions of the present invention can comprise the carnosine of safe and effective amount.Preferably, described compositions comprises by the weight of described compositions about 0.01% to about 20%, and more preferably from about 0.1% to about 15%, even 1% to about 10% carnosine chemical compound more preferably from about.
Carnosine is dipeptides and can be used as antioxidant.Described antioxidant mechanism is with above identical described in the hesperetin part.Carnosine is natural to be present in the human body.It is called as antidotal agent, because it is present in the life-span than in the long tissue with high-load, and is present in (as cataract) in the problematic tissue with low content.Comprise β-alanyl histamine, anserine, homocarnosine and Serpentis carnosine with the similar material of carnosine on the 26S Proteasome Structure and Function.
18. licochalcone A
Compositions of the present invention can comprise the extract of the Glycyrrhiza inflata Bat. of safe and effective amount, described Glycyrrhiza inflata Bat. comprises licochalcone A, its content counts about 0.01% to about 20% by the weight of described compositions, and preferred about 0.1% to about 15%, and more preferably from about 1% to about 10%.
A component in the Glycyrrhiza inflata Bat. aqueous extract is a licochalcone A, and it is a feature with the following formula structure:
Figure S2006800169259D00181
19. creatine and kreatinin
Compositions of the present invention can comprise creatine, creatine derivant, the kreatinin of safe and effective amount, or their combination.The content of creatine, creatine derivant or kreatinin counts about 0.01% to about 20% by the weight of described compositions, and preferred about 0.1% to about 15%, and more preferably from about 1% to about 10%.
The creatine derivant includes but not limited on phosphagen, sulphuric acid creatine, acetic acid creatine, ascorbic acid creatine and the carboxyl by the derivant of a sense or polyfunctional alcohol's esterification.Phosphagen is a kind of preferred creatine derivant and has following structure:
Figure S2006800169259D00182
Kreatinin is a feature with following structure:
20. Radix Agrimoniae extract
Compositions of the present invention can comprise the Radix Agrimoniae extract of safe and effective amount, and its content counts about 0.01% to about 20% by the weight of described compositions, and preferred about 0.1% to about 15%, and more preferably from about 1% to about 10%.
21. ergothioneine
Compositions of the present invention can comprise the ergothioneine of safe and effective amount.The content of ergothioneine counts about 0.01% to about 20% by the weight of described compositions, and more preferably from about 0.1% to about 15%, even more preferably from about 1% to about 10%.Preferred ergothioneine is Thiotaine , it is the commercial solution of chemicals ergothioneine, can be commercially available from Barnet Products.Ergothioneine shows to have antioxidant properties, and its mechanism as mentioned above.
22. Aden's perfume base malonic acid ethylhexyl
Compositions of the present invention can comprise Aden's perfume base malonic acid ethylhexyl of safe and effective amount.The content of Aden's perfume base malonic acid ethylhexyl counts about 0.01% to about 20% by the weight of described compositions, and more preferably from about 0.1% to about 15%, even more preferably from about 0.5% to about 10%.
Preferred Aden perfume base malonic acid ethylhexyl is Oxynex , its demonstration has antioxidant properties.It can be available from Rona/Merck.
23. sterol ester
Compositions of the present invention can comprise the sterol ester of safe and effective amount.The content of sterol ester counts about 0.01% to about 20% by the weight of described compositions, and more preferably from about 0.1% to about 15%, even more preferably from about 0.5% to about 10%.
When using sterol ester among the present invention, should so carry out the preparation of described compositions, so that the hydrolysis of ester not to take place.Therefore, the ideal pH scope that comprises the compositions of sterol ester is about 3 to about 8, preferred about 4 to about 7.
The sterol ester that can be used among the present invention comprises by the sterol of fatty acid or fatty acid mixt esterification or sterol mixture (specifically, being sitosterol, campesterol, stigmasterol, campesterol and other sterol).Described fatty acid (it can be a straight or branched, and is saturated or undersaturated) has 8 to 30 carbon atoms (preferred 16 to 22 carbon atoms).Sterol ester can be available from P﹠amp; GChemicals.
24. idebenone
Compositions of the present invention can comprise the idebenone of safe and effective amount.Preferably, described compositions comprises by the weight of described compositions about 0.001% to about 10%, and more preferably from about 0.005% to about 5%, even 0.01% to about 1% idebenone chemical compound more preferably from about.Alternatively, described compositions can comprise the idebenone chemical compound by the weight of described compositions about 0.1% to about 0.5%.
Herein, " idebenone " is meant following chemical compound, its ester and other derivant, salt, isomer, tautomer and their combination:
Figure S2006800169259D00201
A technical name of idebenone of the present invention is 6-(10-hydroxyl decyl)-2,3-dimethoxy-5-methyl isophthalic acid, 4-benzoquinone.
25. dehydroactic acid
Compositions of the present invention comprises the dehydroactic acid with following structure:
Figure S2006800169259D00202
Or their pharmaceutically useful salt, derivant or tautomer." pharmaceutically useful " used herein is meant that the mammiferous tissue that dehydroacetate salts is applicable to they will act on contacts, and do not have unsuitable toxicity, incompatibility, unstability, zest, atopic reaction etc.The technical name of dehydroactic acid is 3-acetyl group-6-methyl-2H-pyrans-2,4 (3H)-diketone, and can be commercially available from Lonza.
Officinal salt comprises alkali metal salt, as sodium salt and potassium salt; Alkali salt is as calcium salt and magnesium salt; Nontoxic heavy metallic salt; Ammonium salt; And trialkyl ammonium salts, as leptodactyline and triethyl ammonium salt.The sodium salt of dehydroactic acid, potassium salt and ammonium salt are preferred.It is highly preferred that can trade name Tristat SDHA available from the dehydro sodium acetate of Tri-K.The derivant of dehydroactic acid includes but not limited to any wherein CH 3Group is alone or in combination by amide, ester, amino, alkyl and the metathetical chemical compound of alcohol ester.The tautomer of dehydroactic acid be can easier mutual conversion the dehydroactic acid isomer, so their common balances exist.Therefore, the tautomer of dehydroactic acid can be described to have chemical formula C 8H 8O 4, and have said structure usually.
In one embodiment, compositions of the present invention can comprise by the weight of described compositions about 0.001% to about 25%, preferred about 0.01% to about 10%, more preferably from about 0.05% to about 5%, even more preferably from about 0.1% to about 1% dehydroactic acid or their pharmaceutically useful salt, derivant or tautomer.
The dermatological acceptable carrier
Topical compositions of the present invention also can comprise the dermatological acceptable carrier that is used for active substance.Phrase used herein " dermatological acceptable carrier " is meant that carrier is suitable for being locally applied to collenchyme, has good aesthetic properties, with active substance of the present invention and any other component compatibility, and does not cause any safety or toxicity problem.The carrier of safe and effective amount account for described compositions about 50% to about 99.99%, preferred about 60% to about 99.9%, more preferably from about 70% to about 98%, even more preferably from about 80% to about 95%.
Carrier can take various forms.For example, emulsion carriers can be used for the present invention.Described emulsion carriers includes but not limited to O/w emulsion, water-in-oil emulsion, water-covered siloxane emulsion, water-in-silicone emulsion, water-in-oil-in-water compositions and water-in-silicone bag fat liquor.
Preferred carrier comprises emulsion, as O/w emulsion and water-in-oil emulsion, and for example water-covered siloxane emulsion or water-in-silicone emulsion.Such just as understood as technical staff, given component will mainly be assigned in water or the oil phase, and this depends on the water solublity/allocability of this component in compositions.Especially preferred O/w emulsion.
Generally comprise aforesaid solution and lipoid or oil according to emulsion of the present invention.Lipoid and oil can derive from animal, plant or oil, and can natural or synthetic (promptly manually making).Preferred emulsions also comprises wetting agent, for example glycerol.By the weight of described compositions, emulsion preferably also comprises about 0.1% to about 10%, more preferably from about 0.2% to about 5% emulsifying agent.Emulsifying agent can be nonionic, anion or cationic.Examples of suitable emulsifiers is disclosed in " Detergentsand Emulsifiers " North America version the 317th of for example United States Patent (USP) 3,755,560, United States Patent (USP) 4,421,769 and McCutcheon in the 324th page (1986).
According to required product type, suitable emulsion can have the very wide viscosity of scope.Preferred exemplary low viscosity emulsion has about 5E-5m 2/ s (50 centistoke) or lower, more preferably from about 1E-5m 2/ s (10 centistoke) or lower, even 5E-6m more preferably from about 2/ s (5 centistoke) or lower viscosity.
Compositions of the present invention also can comprise the acceptable topical vehicle of other dermatological, and can comprise oral carrier.For example, another kind of topical vehicle can be the cleaning agent (for example, soap slab, shampoo, foamed cleanser, liquid cleaner, bath shampoo, cleaning towel etc.) that comprises surfactant.In above-mentioned carrier, surfactant can be anion, cation, amphion, nonionic or their mixture.Another kind of topical vehicle is coloured cosmetics (lip pomade, kermes, informer, mascara, foundation creams, refer to/the toenail wet goods).A kind of oral carrier is beverage, food, pill, capsule, powder, capsule sheet etc.
Optional component
The present composition can comprise other composition commonly used in the multiple given product type, and precondition is that they can change beneficial effect of the present invention acceptably.
In the time of in being incorporated into compositions, optional component should be applicable to human collenchyme and contact reasonably do not having unsuitable toxicity, incompatibility, unstability, atopic reaction or the like in the determination range." CTFA Cosmetic Ingredient Handbook " second edition (1992) has been described multiple non-limiting beauty treatment and the ingredient that is generally used for the skin nursing field, and they are applicable in the compositions of the present invention.Other example of these constituent classes comprises: grinding agent, absorbent, beauty treatment component such as aromatic, pigment, stain/coloring agent, quintessence oil, anti-caking agent, defoamer, binding agent, bio-additive, buffer agent, extender, chelating agen, chemical addition agent, coloring agent, the cosmetics astringent, the cosmetics insecticide, denaturant, the medicine astringent, external-use analgesic, film former or the film forming matter polymer (as eicosylene and vinylpyrrolidone copolymers) of aid composition film forming characteristics and affinity (as be used for), opacifier, the pH regulator agent, propellant, Reducing agent, sequestering agent and thickening agent.
Compositions of the present invention also can comprise synthetic cationic polymer polyquaternary ammonium salt-37 (methacryl ethyl-trimethyl salmiac homopolymer).Described polymer also can be used as powder or liquid dispersion is added in the described compositions.This polymer is can commercial name commercially available from Synthalen (3VSigma), Ultragel 300 (Cosmetic Rheologies Ltd), RheocareCTH (E) (Cosmetic Rheologies Ltd.), Salcare SC95 and SalcareSC96 (Ciba Specialty Chemicals).
Other optional component that can be used among the present invention comprises that the U.S. announces those that describe among the 2004-0175347A1, comprises the desquamation active substance, as salicylic acid and zwitterionic surfactant; Console agent and/or rehabilitation agent; Skin treatment agents; The skin sensitizer; Astringent etc. (as Oleum Caryophylli, menthol, Camphora, Eucalyptus oil, acetaminol, menthyl lactate, Radix Hamamelidis Mollis distillate); The anti-acne active substance is as resorcinol, sulfur, erythromycin, zinc, dehydroactic acid; Anti-wrinkle active substance/anti-atrophy active substance; Antioxidant/free radical scavenger is as tocopherol; Chelating agen is as furil-dioxime and derivant thereof; Flavonoid; Antiinflammatory; The scorching agent of anti-cellulite; Tanned active substance is as dihydroxy acetone; Skin lightening agent; Antimicrobial and antifungus active substance; Sunscreen actives; Conditioner is as glycerol, carbamide, vaseline, Olestra and their combination; Thickening agent is as carboxylic acid polyalcohol, cross-linked polyacrylate polymer, polyacrylamide polymers, polysaccharide, natural gum; Water soluble vitamins; And particulate material.Compositions of the present invention can comprise following one or more other active substance or compositions of safe and effective amount: fatty acid (especially polyunsaturated fatty acid); glycosamine; 1-oxygen-2-mercaptopyridine zinc (ZPT); mercaptan compound is (as the N-acetylcysteine; glutathion; the thioglycol acid esters); other vitamin is (as B1; B2; B5; B6; B12; C; D; E; F; K; P); beta-carotene; ubiquinone; idebenone; aminoacid; mineral is (as Zn; Mn; Mg; Cu; Fe and Se); hydroxy acid is (as 'alpha '-hydroxy acids; 2-ketoacid and beta-hydroxy acid); kojic acid; arbutin; mulberry extract; decorticating agent; dandruff agent etc.
Composition forms
The topical compositions of this theme invention includes but not limited to lotion, emulsion, mousse, serosity, spray, aerosol, foam, club, lip pencil thing, gel, cream and ointment, and described compositions can comprise the acceptable emollient of dermatological.Above-mentioned composition preferably comprises about 2% to about 50% emollient." emollient " used herein is meant and is used to the material that prevents or alleviate drying and be used to protect skin.Known have multiple suitable emollient, and can be used for herein.The 2nd edition the 1st volume of " Cosmetics, the Science and Technology " of Sagarin comprised many examples that are suitable for the material of making emollient in the 32nd to the 43rd page (1972).Preferred emollient is a glycerol.The consumption of glycerol is preferably about 0.001 to about 20% by the weight of described compositions, and more preferably from about 0.01 to about 15%, even more preferably from about 0.1 to about 10%.
The present composition that can be used for cleaning (" cleaning agent ") is with suitable carrier (for example, aforesaid carrier, and comprise dermatological acceptable surfactant by the weight of described compositions about 1% to about 90%) preparation.
The physical form of Cleasing compositions is unimportant.Described compositions can be configured to and for example wash one's hands and face soap slab, liquid, shampoo, bath gels, conditioner, hair oil, paste or mousse.The washing soap slab is preferred, because this is the cleaning agent form that is most commonly used to washed skin.Washing-off type Cleasing compositions such as shampoo need be suitable for active substance with capacity and be deposited on delivery system on skin and the scalp.Preferred delivery system relates to the undissolved complex of use.The more complete disclosure of above-mentioned delivery system can be referring to United States Patent (USP) 4,835,148.
The present composition also can be the cosmetics form.Suitable cosmetics form includes but not limited to foundation cream, lip pomade, kermes, mascara or the like.Above-mentioned cosmetics can comprise conventional composition, as oil, coloring agent, pigment, emollient, aromatic, wax, stabilizing agent etc.Be applicable to that the exemplary carrier of this paper and above-mentioned other composition for example are described in the United States Patent (USP) 6,060,547.
Compositions of the present invention can also be the formulation products form that shaves, and comprises example gel, foam, lotion and cream; And comprise aerosol and non-aerosol type.
Preparation of compositions
The present composition is usually by conventional method preparation, the method for preparing topical compositions as known in the art.The said method typical case relates to the state that composition is mixed to the comparison homogeneous in one or more steps, can need or not need conditions such as heating, cooling, use vacuum.The described compositions of preferred for preparation is so that active agent stability (physical stability, chemical stability, light stability) and/or send optimum.This optimization can comprise suitable pH value (as, less than 7), get rid of can be with active substance compound and thereby negative effect stability or substance for delivery (as despumation ferrum), use method (as suitable dispersant or dual compartment package) that the prevention complex generates, use suitable light stability method (as adding suntan lotion/sunscreen cream, using opaque packing) or the like.
Regulate the method for keratinous tissue conditions
Compositions of the present invention can be used for regulating numerous mammiferous keratinous tissue conditions.The adjusting of above-mentioned keratinous tissue conditions comprises preventative and therapeutic regulation.More particularly, above-mentioned control method relates to but is not limited to thicken collenchyme (promptly construct epidermal area and/or the skin corium and/or the hypodermic layer of skin, and under suitable situation, structure refers to/horny layer of toenail and hair shaft); By being used as blast skin or reducing Pigmented enamel and prevent, postpone and/or handle the uneven colour of skin; Prevention, postpone and/or handle the atrophy of mammal skin, softening and/or level and smooth mammiferous lip, hair and refer to/toenail; Prevention, delay and/or processing mammal skin pruritus; The appearance of prevention, delay and/or processing black eye and/or swollen eye; Prevention, delay and/or processing mammal colour of skin sallow; Prevention, delay and/or processing mammal skin sagging (being saccharification); Prevention and/or postpone that mammal skin is tanned, desquamation, decortication and/or increase renewal in the mammal skin; Reduce the pore size in the mammal skin; Regulate oiliness/glossy mammal skin outward appearance; Hyperpigmentation after prevention, delay and/or processing hyperpigmentation such as the inflammation; The appearance of spider shape blood vessel and/or erythema on prevention, delay and/or the processing mammal skin; Prevention, delay and/or processing mammal skin microgroove and wrinkle; Prevention, postpone and/or handle xerosis cutis (promptly coarse, peel, peel off); And the appearance that prevents, postpones and/or handle honeycomb inflammation in the mammal skin.The present composition also can be used for hair growth inhibition, reduce the shaving frequency, improve the shaving easiness, reduce the shaving frequency, make hair more soft and/or more very thin, make that hair is more unshowy, the hair regeneration that slows down long, reduce erythema and scytitis, make skin more smooth and/or more soft and improve the hair removing mode.The adjusting keratinous tissue conditions relates to the present composition to the safe and effective amount of collenchyme local application.The amount of composition of being used, the frequency of using and life cycle will change widely according to skin in the given compositions and/or hair-care active substance and/or other components contents and required regulating degree.
In a preferred embodiment, described compositions chronic administration is in skin." long-term local application " is meant the topical composition constantly for a long time in life the experimenter, the preferred time is at least about a week, more preferably at least about one month, even more preferably at least about three months, even more preferably at least about six months, and even more preferably at least about 1 year.Although beneficial effect still can obtain after the various maximum operating period (for example five, ten or 20 years), preferably use whole all the continuing for a long time in life of experimenter.In the time of above-mentioned continuity, the typical case according to every day rule approximately once use, yet frequency of administration can be weekly approximately to every day three times approximately or change in the scope more frequently.
The various consumptions of the present composition can be used to provide the beneficial effect of skin appearance and/or dermal sensation.With mg compositions/cm 2Skin meter, the amount that the each typical case of the present composition uses are about 0.1mg/cm 2To about 20mg/cm 2The amount of application that is particularly useful is about 0.5mg/cm 2To about 10mg/cm 2
Can by for example use skin distillate medicinal water, salubrious distillate medicinal water, milk distillate medicinal water, cream, gel, foam, ointment, paste, emulsion, spray, aerosol, conditioner, nourishing agent, cosmetics, lip pomade, foundation cream, refer to/nail polish, the compositions of aftershave lotion, ball rod or deodorant stick, powder, wet goods form implements the processing of keratinous tissue conditions.Described compositions is intended to be retained on skin or other collenchyme that some is aesthetic to reach, the beneficial effect (i.e. " leave " compositions) of in the prevention, in the treatment or others.After using compositions on the collenchyme (as skin), it is retained on the skin preferably at least about 15 minutes, more preferably at least about 30 minutes, even more preferably at least about 1 hour, even more preferably at least several hours, as about 12 hours at most.Can process facial, hair and/or refer to/any surperficial position of toenail (for example, face, lip, zone, eyelid, scalp, neck, trunk, arm, hands, lower limb, foot, fingernail, toenail, hair of scalp, eyelashes, eyebrow etc.) now.Described compositions can distribute maybe can integrate from bottle, wide mouthed bottle, pipe, folliculus, pouch, container, tottle, bottle, ampoule, capsule etc. and be included in delivery form such as the cleaning piece.Can carry out using of the present composition by using palm and/or finger.Also can wait and use as cotton balls, swab, liner, brush, eye dropper, powder puff, sponge, club, cleaning piece, foamed materials, nonwoven substrate, facial film, ball-type applicator, bar-shaped applicator, coating pen, spray applicator, aerosol apparatus, razor by means of device or instrument.Active substance can be included in two kinds of broken pouches between the substrate.
In another embodiment, topical compositions use can skin treatment such as cleaning, decortication or tanned after carry out.
Guaranteeing to make collenchyme and another method of the compositions Continuous Contact of minimum content at least is to be applicable to that by use for example the patch of face is used described chemical compound.Said method especially can be used for problematic skin area, and described skin area needs more intensive treatment (as facial crows-feet zone, place between the eyebrows stricture of vagina, zone, upper lip etc. now).Described patch can be occlusion, half occlusion or not occlusion, and can be viscosity or inviscid.Said composition can be comprised in the patch, or is applied on the skin before using patch.Described patch also can comprise additional active substance, as is used for the chemical initiator of exothermic reaction, as PCT application WO 9701313 and the United States Patent (USP) 5,821,250,5,981,547 and 5,972 of authorizing people such as Wu, those described in 957.Described patch also can comprise electric energy (as battery), for example to increase send (as the ionotherapy) of described compositions and activating agent.Patch applies retention time on collenchyme preferably at least about 5 minutes, more preferably at least about 15 minutes, and also more preferably at least about 30 minutes, even more preferably at least about 1 hour, even a kind of form of more preferably handling as night evening.
Also can use other device, with active compound combined use of the present invention.For example, ultrasonic, laser instrument, heater etc. can be used for strengthening the beneficial effect of skin and hair.
The another kind of method of enhanced activity material beneficial effect be to use have two kinds, three kinds or four kinds or more kinds of product and/or treatment step be (as decortication, use one or more active substance Local treatment of the present invention afterwards, alopecia, use one or more active substance Local treatment of the present invention afterwards, or the like) cover box or embodiment.Can be in short time period (for example in one hour), or in the long period section in a day (for example morning and night), or even longer time period in (for example weekly or carried out in every month step in the embodiment, and carry out other step in the embodiment with more regularly benchmark (for example every day)), use the various components in the embodiment.
It is packaging together that Orally administered composition and topical compositions can be used as the cover box.In another embodiment, described Orally administered composition and described topical compositions are not packaged in together as the cover box, but pass on (for example by advertisement, Product labelling) following information for the potential user of described embodiment: Orally administered composition and topical compositions can combine with one another to make and be used for regulating keratinous tissue conditions.
The present invention also provides the method for the personal care composition marketization that is used in prevention, postpones and/or handles the inhomogeneous colour of skin.Make a preferable methods of the above-mentioned composition marketization comprise the personal care composition that makes consumer can obtain to comprise skin and/or hair-care active substance, described active substance is selected from the group of being made up of following material: cetylpyridinium chloride, Dodecyl trimethyl ammonium chloride, TPC, the cetyl dimethyl benzyl ammonium chloride, chlorination 1-cetyl pyridinium, the dimethyl stearyl benzyl ammonium chloride, hexadecyltrimethylammonium chloride, cetyl trimethyl ammonium bromide, octadecyl trimethyl ammonium chloride, domiphen bromide, chlorination N-myristyl-4-ethylpyridine, dodecyl dimethyl (2-phenoxy group ethyl) ammonium bromide, benzyl dimethyl stearyl chlorination ammonium, quaternized 5-amino-1,3-two (2-ethylhexyl)-5-methyl hexahydropyrimidine, alkyl benzyl dimethyl ammonium chloride, iso-octyl phenoxy group ethoxyethyl group benzyl dimethyl ammonium chloride and methyl iso-octyl phenoxy group ethoxyethyl group benzyl dimethyl ammonium chloride; And pass on following information to consumer: the described personal care composition of local application can improve the skin color of consumer.Wherein the mode that conveys a message to consumer is nonrestrictive.Only as an example, can come realization information to pass on as TV, network and impurity advertisement by known advertisement skill.It can be the point of sale method that described information is passed on, and for example sticks on the information on shelf and/or the floor.And described information is passed on and can be taked to be arranged in the personal care composition packing and/or the mark pattern (literal, symbol, color, tone, figure etc.) on the packing.Described personal care composition can comprise annexing ingredient, comprise be described in the description of the present invention those and known to the skilled those.
The method of implementing business activity also is that the present invention is contemplated.A preferable methods comprises to consumer passes on following information: comprise first personal care composition of skin and/or hair-care active substance and do not comprise described skin and/or second personal care composition of hair-care active substance between the step of comparative result, described active substance is selected from the group of being made up of following material: cetylpyridinium chloride, Dodecyl trimethyl ammonium chloride, TPC, the cetyl dimethyl benzyl ammonium chloride, chlorination 1-cetyl pyridinium, the dimethyl stearyl benzyl ammonium chloride, hexadecyltrimethylammonium chloride, cetyl trimethyl ammonium bromide, octadecyl trimethyl ammonium chloride, domiphen bromide, chlorination N-myristyl-4-ethylpyridine, dodecyl dimethyl (2-phenoxy group ethyl) ammonium bromide, benzyl dimethyl stearyl chlorination ammonium, quaternized 5-amino-1,3-two (2-ethylhexyl)-5-methyl hexahydropyrimidine, alkyl benzyl dimethyl ammonium chloride, iso-octyl phenoxy group ethoxyethyl group benzyl dimethyl ammonium chloride and methyl iso-octyl phenoxy group ethoxyethyl group benzyl dimethyl ammonium chloride.Except the other factors relevant with regulating mammiferous keratinous tissue conditions, described comparative result also relates to the colour of skin, blast skin effects, skin whitening effect, pigmentation effect.
Embodiment
It below is the non-limiting example of the present composition.Providing of embodiment only is the purpose that illustrates for example, and should not be construed as is limitation of the present invention, because under the situation that does not deviate from the spirit and scope of the present invention, its many changes are possible, and this will be recognized by those of ordinary skill in the art.In an embodiment, except as otherwise noted, all concentration are all listed with percentage by weight, side by side except minor materials, as diluent, filler etc.Therefore, listed preparation comprises listed component and any trace substance relevant with this component.It is evident that concerning the those skilled in the art of this area the selected of these accessory constituents will be according to the physics of selected concrete composition with chemical characteristic and different, to make invention as herein described.
Content in the preparation (the component gram number in every 100g preparation)
Component A B C D E F
Disodiumedetate 0.100 0.100 0.100 0.100 0.100 0.100
Carnosine 5.000 0 0 0 0 0
The vanillin acetas 0 2.000 0 0 0 0
Tetrahydrocurcumin 0 0 0.500 0 0 0
Enoxolone 0 0 0 0.300 0 0
Thiotaine 0 0 0 0 5.000 0
Sinablanca 0 0 0 0 0 2.500
Cetylpyridinium chloride 0.200 0.200 0.200 0.200 0.200 0.200
Nicotiamide 5.000 5.000 5.000 5.000 5.000 5.000
Citric acid 0.015 0 0 0 0 0
2-Methylpentadecane 3.000 3.000 3.000 3.000 3.000 3.000
The isostearic acid isopropyl ester 1.330 1.330 1.330 1.330 1.330 1.330
N-Hamposyl L isopropyl ester 0 0 5.000 0 0 0
Poly-cottonseed acid sucrose ester 0.670 0.670 0.670 0.670 0.670 0.670
Poly methyl silsesquioxane 0.250 0.250 0.250 0.250 0.250 0.250
Cetearyl glucoside+16/octadecanol 0.200 0.200 0.200 0.200 0.200 0.200
Docosanol 0.400 0.400 0.400 0.400 0.400 0.400
Ethylparaben 0.200 0.200 0.200 0.200 0.200 0.200
Propyl p-hydroxybenzoate 0.100 0.100 0.100 0.100 0.100 0.100
Spermol 0.320 0.320 0.320 0.320 0.320 0.320
Stearyl alcohol 0.480 0.480 0.480 0.480 0.480 0.480
Tocopherol acetas 0.500 0.500 0.500 0.500 0.500 0.500
The PEG-100 stearate 0.100 0.100 0.100 0.100 0.100 0.100
Glycerol 7.000 7.000 7.000 7.000 7.000 7.000
Titanium dioxide 0.604 0.604 0.604 0.604 0.604 0.604
Polyacrylamide+C13-14 isoparaffin+laureth-7 3.000 2.000 2.000 2.000 2.000 2.000
Pantothenylol 1.000 1.000 1.000 1.000 1.000 1.000
Benzylalcohol 0.400 0.400 0.400 0.400 0.400 0.400
Polydimethylsiloxane+dimethiconol 2.000 2.000 2.000 2.000 2.000 2.000
Water (to 100g) To 100 To 100 To 100 To 100 To 100 To 100
Amount to 100 100 100 100 100 100
Content in the preparation (the component gram number in every 100g preparation)
Component G H I J K L
Disodiumedetate 0.100 0.100 0.100 0.100 0.100 0.100
The glucityl Hesperidin 1.000 0 0 0 0 0
Glycyrrhizic acid, ammonium salt 0 0.300 0 0 0 0
Cetylpyridinium chloride 0.200 0.200 0.200 0.200 0.200 0.200
Primoline 0 0 0.100 0 0 0
The N-n acetylglucosamine n 0 0 0 2.000 0 0
Oxynex 0 0 0 0 2.000 0
Yoshinox BHT 0 0 0 0 0 1.000
Nicotiamide 5.000 5.000 5.000 5.000 5.000 5.000
Polyquaternary ammonium salt 37 0 0 1.500 0 0 0
2-Methylpentadecane 3.000 3.000 3.000 3.000 3.000 3.000
The isostearic acid isopropyl ester 1.330 1.330 1.330 1.330 1.330 1.330
Poly-cottonseed acid sucrose ester 0.670 0.670 0.670 0.670 0.670 0.670
Poly methyl silsesquioxane 0.250 0.250 0.250 0.250 0.250 0.250
Cetearyl glucoside+16/octadecanol 0.200 0.200 0.200 0.200 0.200 0.200
Docosanol 0.400 0.400 0.400 0.400 0.400 0.400
Ethylparaben 0.200 0.200 0.200 0.200 0.200 0.200
Propyl p-hydroxybenzoate 0.100 0.100 0.100 0.100 0.100 0.100
Spermol 0.320 0.320 0.320 0.320 0.320 0.320
Stearyl alcohol 0.480 0.480 0.480 0.480 0.480 0.480
Tocopherol acetas 0.500 0.500 0.500 0.500 0.500 0.500
The PEG-100 stearate 0.100 0.100 0.100 0.100 0.100 0.100
Glycerol 7.000 7.000 7.000 7.000 7.000 7.000
Titanium dioxide 0.604 0.604 0.604 0.604 0.604 0.604
Polyacrylamide+C13-14 isoparaffin+laureth-7 2.000 2.000 0 2.000 2.000 2.000
Pantothenylol 1.000 1.000 1.000 1.000 1.000 1.000
Benzylalcohol 0.400 0.400 0.400 0.400 0.400 0.400
Polydimethylsiloxane+dimethiconol 2.000 2.000 2.000 2.000 2.000 2.000
Water (to 100g) To 100 To 100 To 100 To 100 To 100 To 100
Amount to 100 100 100 100 100 100
Component M N O P
Disodiumedetate 0.1 0.1 0.1 0.1
Nicotiamide 5.0 5.0 5.0 0
Cetylpyridinium chloride 0.2 0.2 0.2 0.2
The own oxygen phenylate of dihydroxy ethyl sulfonic acid 0 0 0 0.1
N-endecatylene acyl-L-phenylalanine 0.2 0 0 0
Dehydro sodium acetate 0.0 0.0 0.2 0.5
2-Methylpentadecane 3.0 3.0 3.0 3.0
The isostearic acid isopropyl ester 1.33 1.33 1.33 1.33
Poly-cottonseed acid sucrose ester 0.67 0.67 0.67 0.67
Poly methyl silsesquioxane 0.25 0.25 0.25 0.25
Cetearyl glucoside+16/octadecanol 0.2 0.2 0.2 0.2
Docosanol 0.4 0.4 0.4 0.4
Ethylparaben 0.2 0.2 0.2 0.2
Propyl p-hydroxybenzoate 0.1 0.1 0.1 0.1
Spermol 0.32 0.32 0.32 0.32
Stearyl alcohol 0.48 0.48 0.48 0.48
Tocopherol acetas 0.5 0.5 0.5 0.5
The PEG-100 stearate 0.1 0.1 0.1 0.1
Glycerol 7.0 7.0 7.0 7.0
Titanium dioxide 0.604 0.604 0.604 0.604
Polyacrylamide+C13-14 isoparaffin+laureth-7 2.0 2.0 2.0 2.0
Pantothenylol 1.0 1.0 1.0 1.0
Benzylalcohol 0.4 0.4 0.4 0.4
Polydimethylsiloxane+dimethiconol 2.0 2.0 2.0 2.0
Water (to 100g) To 100 To 100 To 100 To 100
Amount to 100 100 100 100
Although illustrated and described the present invention with specific embodiments, it will be apparent to those skilled in the art that many other variations and modifications may be made in the case of without departing from the spirit and scope of protection of the present invention.Therefore, in additional claims, comprise all such changes and modifications that belong in the scope of the invention consciously.
The relevant portion of all documents of quoting in background of invention, summary of the invention and the detailed Description Of The Invention is incorporated herein by reference.The quoting and may not be interpreted as of any document to its approval as prior art of the present invention.

Claims (10)

1. personal care composition, described compositions comprises:
A) skin and/or hair-care active substance, described active substance is selected from the group of being made up of following material: cetylpyridinium chloride, Dodecyl trimethyl ammonium chloride, TPC, the cetyl dimethyl benzyl ammonium chloride, chlorination 1-cetyl pyridinium, the dimethyl stearyl benzyl ammonium chloride, hexadecyltrimethylammonium chloride, cetyl trimethyl ammonium bromide, octadecyl trimethyl ammonium chloride, domiphen bromide, chlorination N-myristyl-4-ethylpyridine, dodecyl dimethyl (2-phenoxy group ethyl) ammonium bromide, benzyl dimethyl stearyl chlorination ammonium, quaternized 5-amino-1,3-two (2-ethylhexyl)-5-methyl hexahydropyrimidine, alkyl benzyl dimethyl ammonium chloride, iso-octyl phenoxy group ethoxyethyl group benzyl dimethyl ammonium chloride, methyl iso-octyl phenoxy group ethoxyethyl group benzyl dimethyl ammonium chloride, and/or their combination;
B) at least a additional skin and/or hair-care active substance, described active substance is selected from the group of being made up of following material: tetrahydrocurcumin, osamine, vitamin B 3Retinoid, hydroquinone, peptide, plant sterol, two alkanoyl hydroxyprolines, primoline, salicylic acid, n-acyl amino acid compound, sunscreen actives, water soluble vitamins, fat soluble vitamin, hesperetin, the Semen Brassicae Junceae extract, glycyrrhizic acid, enoxolone, carnosine, Yoshinox BHT (BHT) and butylated hydroxyanisol (BHA), ergothioneine, the vanillin or derivatives thereof, Aden's perfume base malonic acid ethylhexyl, melanonostatin, sterol ester, idebenone, dehydroactic acid, licochalcone A, creatine, kreatinin, the Radix Agrimoniae extract, yeast extract, beta glucan, alpha-glucans, their salt, their derivant, their precursor, and/or their combination; With
C) dermatological acceptable carrier.
2. personal care composition as claimed in claim 1, wherein said first skin and/or hair-care active substance are cetylpyridinium chloride.
3. personal care composition as claimed in claim 1 or 2, wherein said at least a additional skin and/or hair-care active substance comprise primoline.
4. as each described personal care composition in the claim 1 to 3, wherein said at least a additional skin and/or hair-care active substance also comprise vitamin B 3
5. as each described personal care composition in the claim 1 to 4, described compositions also comprises 0.001% to 10% annexing ingredient by weight, described annexing ingredient is selected from the group of being made up of following material: desquamation active substance, anti-acne active substance, wrinkle repairing activity material, antioxidant, free radical scavenger, chelating agen, flavonoid, antiinflammatory, the scorching agent of anti-cellulite, skin lightening agent, anti-microbial active matter, antifungus active substance, conditioner, thickening agent, water soluble vitamins, fat soluble vitamin, particulate matter, local anesthetic, and their combination.
6. as each described personal care composition in the claim 1 to 5, described compositions also comprises polyquaternary ammonium salt-37.
7. as each described personal care composition in the claim 1 to 6, wherein said at least a additional skin and/or hair-care active substance comprise nicotiamide, pantothenylol and vitamin e acetate.
8. as each described personal care composition in the claim 1 to 7, wherein said at least a additional skin and/or hair-care active substance comprise yeast extract and ascorbyl glucoside.
9. method of improving skin color, described method comprises the step of each described personal care composition in mammalian skin local application such as claim 1 to 8.
10. the method for blast skin and/or skin whitening, described method comprises the step of each described personal care composition in mammalian skin local application such as claim 1 to 8.
CNA2006800169259A 2005-05-17 2006-05-17 Regulation of mammalian keratinous tissue using personal care compositions comprising diethylhexyl syringylidene malonate Pending CN101175469A (en)

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