CN101182299A - Mydrial derivates,preparation method of mydrial derivates and cosmetics or skin medicinal composition - Google Patents

Abstract

The invention relates to a novel tyramine derivate and a method for preparing the compound. The invention also relates to a cosmetic or medical skin composition having the compound, as well as the application of the compound in the skin care field, in particular to the application in order to release the over-pigmentation.

Description

New tyrasamine derivative, its preparation method and makeup thereof or dermal drug composition

Technical field

The present invention relates to new tyrasamine derivative, its purposes contains the makeup or the pharmaceutical composition of described material, and the preparation method of these compounds, and skin care purposes are particularly in order to reduce the purposes of hyperpigmentation.

Background technology

At present, the natural pigmentation mechanism of skin has had clearly record: the melanocyte that is present in the basal layer of epidermis (stratum basale epidermidis) produces melanochrome, and it is synthetic in melanosome.Under uviolizing, melanic synthetic (melanocyte generation) increases.The physiological function of this brownization of skin can protect skin to avoid the uviolizing injury.

Various melanochrome generting machanism dysfunctions (result from outside infringement, hormonal imbalance or aging) cause the appearance, particularly freckle (spot) of foxiness and the formation of day hot spot or senile plaque.

The natural pigmentation that changes skin is Europe, Asia and America women's a common aspiration, though wherein the potential ultimate principle is also inequality.Some are U.S. with the white colour of skin, and the others attempts to weaken senile plaque, think that its expression is aging.The control cutaneous pigmentation is the theme of a sensitivity and has the target of considerable demand, this situation in the Asia, Europe is the same with America.

Three kinds of key enzymes generate relevant with melanocyte: the protein (TRP-1 and TRP-2) that tyrosine oxidase and tyrosine are relevant.These three kinds of enzymes all are arranged in the melanosome film.Wherein, tyrosine oxidase is a restriction enzyme in initial two steps that catalysis melanochrome generates: vicinal hydroxyl groups tyrosine forms levodopa (L-DOPA), and the oxidation latter forms the DOPA quinone then.And it is reported that TRP-1 and TRP-2 partly get involved the generation of melanocyte by stabilization tyrosine hydroxylase.

In addition, known melanogenic hormesis comprises that the cAMP level rises in the cell.CAMP can regulate the effect of protein kinase PKC-b, and in melanochrome was synthetic, it was conclusive that this kinases makes the effect of tyrosine oxidase phosphorylation.Based on this mechanism, can observe, in the melanocyte of cultivating, uviolizing increases PKC-b very significantly.

At last, in the metabolism of melanocyte, intracellular Ca2+ institute role also has definite record.

In order to change the pigmentation of skin, it is contemplated that degraded melanochrome, provide can with the interactional Melanogenesis inhibitor of aforementioned various targets, perhaps even suppress the distribution of melanochrome in cuticular cellulose.

But the most frequent selecteed target undoubtedly is a tyrosine hydroxylase, because of it forms a conditioning step during the course.

In the long duration, adopt quite effectively product to reach skin depigmentation and brightening, Resorcinol for example contains the phenolic compound of sulfo group or non-sulfo group and xitix.Yet these products have the very few effect of irreversible pigment unavoidably and cause inflammation.All these products all need be used in effect/security scope, thereby are not suitable for makeup.

At cosmetic field, by using various types of vitamin A derivatives, AHA, kojic acid and arbutin and address the above problem.

Exploitation Resorcinol, arbutin and kojic acid are that described catalytic activity is essential for the function of tyrosine oxidase because the active restraining effect of chelated copper ion pair tyrosinase catalysis is perhaps passed through in its tyrosine oxidase competitive inhibition.Yet these products are difficult to use, and may cause side effect.

Therefore, be a long felt need for the cosmetic product of innovation, its effective in vivo and nontoxicity.

Summary of the invention

We find some tyrasamine derivative unexpectedly, and generation has the inhibition potentiality more powerful than tyrasamine itself for melanocyte.It is described among the patent application FR-A-2 813 188.

The application theme that the present invention constituted is that we find and have proved that the tyrasamine derivative of general formula I reduces the melanochrome generation in a kind of effective and avirulent mode.The described tyrasamine derivative that constitutes the present patent application theme has bioavailability, solvability, activity, stability or toxicology characteristic preferably, also has value in these areas.

The present invention proposes to have the compound of following general formula I:

Wherein:

Radicals X is-NR ³R ⁴Or-N=CR ⁵R ⁶,

R ¹And R ²Each group can be identical or different, be hydrogen atom or halogen atom, perhaps alkyl, aryl, aralkyl, acyl group, alcohol or alkoxyl group,

R ³And R ⁴Each group can be identical or different, be hydrogen atom or alkyl, aryl, aralkyl, acyl group, alkylsulfonyl or glycosyl,

R ⁵And R ⁶Each group can be identical or different, be hydrogen atom or alkyl, aryl or aralkyl,

The compound of general formula I can exist by free form, perhaps exists with the salifiable form of the acceptable sour shape of makeup category.The present invention comprises free form and its salt of these compounds simultaneously.

The present invention does not comprise tyrasamine (general formula I, X=-NR ³R ⁴, R ¹=R ²=R ³=R ⁴=H), perhaps tyrasamine is by its OH or NH ₂On the group keyed jointing any straight or branched, saturated or unsaturated, can by hydroxylation or contain sulphur or not sulfur-bearing, by 1 to 24 formed derivative of the alkyl chain that carbon atom is formed.The present invention does not comprise synephrine (general formula I, X=-NR yet ³R ⁴, R ¹=OH, R ²=R ³=H, R ⁴=CH ₃).

The present invention also proposes makeup or dermal drug composition, and it is acceptable that described composition contains the makeup category, the vehicle of form, and the compound with general formula shown in the following formula I alone or in combination.But the present invention does not relate to the composition that contains tyrasamine or its following derivative, and described derivative is meant OH or the NH on the tyrasamine ₂On the group keyed jointing any straight or branched, the formed derivative of saturated or unsaturated alkyl chain, described alkyl chain can or contain sulphur or sulfur-bearing not by hydroxylation, is made up of 1 to 24 carbon atom.The present invention does not relate to the composition that contains synephrine yet.

In the present invention, term " the acceptable acid of makeup category " means any avirulent acid, comprises organic acid and mineral acid.This acid comprises acetate, para-amino benzoic acid, xitix, aspartic acid, Phenylsulfonic acid, phenylformic acid, the dimethylene Whitfield's ointment, Hydrogen bromide, spirit of salt, styracin, citraconic acid, citric acid, ethionic acid, FUMARIC ACID TECH GRADE, gluconic acid, L-glutamic acid, R-Glyceric acid, methylene-succinic acid, lactic acid, toxilic acid, oxysuccinic acid, amygdalic acid, methylsulfonic acid, mucic acid, nitric acid, Herba Oxalidis Corniculatae acid, palmitinic acid, pounce on acid, pantothenic acid, phosphoric acid, propionic acid, Whitfield's ointment, stearic acid, succsinic acid, thionamic acid, sulfuric acid, tartrate, tosic acid.Spirit of salt and acetate are particularly preferred.

In the present invention, term " alkyl " means any 1 to 20 carbon atom, straight or branched, replace or (particularly being replaced) and the saturated or undersaturated alkyl of non-replacement by alcohol, carboxylic acid or ammonia.Especially, alkyl can be a methyl.

In the present invention, term " aryl " means one or several aromatic nucleus, and 5 to 8 carbon atoms of each freedom constitute, and it can be the ring or the condensed ring of adjacency, and can be substituted not to have replacement yet.Especially, aryl can be a phenyl or naphthyl, substituting group be before defined halogen atom, alkoxyl group, alkyl defined previously or nitro.

In the present invention, term " aralkyl " means and any aryl defined previously of alkyl bonded defined previously.Especially, aralkyl is a phenmethyl.

In the present invention, term " alkoxyl group " means any-OR ⁷Group, wherein R ⁷Can be alkyl, aryl, aralkyl, acyl group, sulfo group or glycosyl defined previously.

In the present invention, term " acyl group " means any-C=OR ⁸Group, wherein R ⁸Can be alkyl, aryl, aralkyl or amino defined previously.Especially, acyl group can be ethanoyl (R ⁸=-CH ₃).

In the present invention, term " amino " means any-NR ⁹R ¹⁰Group, wherein R ⁹And R ¹⁰Can be identical or different, be separately before defined hydrogen atom or alkyl, aryl, aralkyl, acyl group, sulfo group or glycosyl.

In the present invention, term " sulfo group " means any-SO in the text ₂R ¹¹Group, wherein R ¹¹Can be alkyl, aryl, aralkyl, alkoxyl group or amino defined previously.Especially, sulfo group can be methylsulfonyl (R ¹¹=-CH ₃), trifyl (R ¹¹=-CF ₃) or tosyl group (R ¹¹=-Ph-CH ₃).

In the present invention, term " glycosyl " means any hexose, sugar or glucosides group.Especially, glycosyl can be glucose, pectinose, fructose, semi-lactosi, seminose, barley-sugar, lactose, sucrose or cellobiose base.

The described substituting group of general formula I can have asymmetric center and exist with the optical isomer form.The present invention includes various isolating optical isomers and any of these mixture of isomers.

The example of this compounds is: N-ethanoyl-tyrasamine, N-glycyl-tyrasamine/TFA; N-maleoyl-tyrasamine; N-glutaryl-tyrasamine; The soft ester acyl-tyrasamine of N-; The soft ester acyl-tyrasamine of O-/HBr; The N-tolylsulfonyl; N-tyrasamine-urea; N-benzoyl-tyrasamine; N-tosyl group-octopamine; N-Ben Yajiaji-tyrasamine; N, O-di-acetyl-octopamine; N-tosyl group-octopamine; N-methylsulfonyl-tyrasamine; N-g-hydroxyl-butyryl-tyrasamine; Two-oxo tyrasamine; N-oxalyl-tyrasamine; Tyrasamine-sulfuric ester; The N-ethyl, N-(N-dimethyl, 3-aminopropyl), N-tyrasamine base-guanidine; 2-2-sulfo group-N-benzoyl-tyrasamine; N-trifyl-tyrasamine; N-ethanoyl-octopamine; N-maleoyl-tyrasamine.

Under condition of the present invention, particularly advantageous compound is octopamine (structural formula I, X=-NR ³R ⁴, R ¹=OH, R ²=R ³=R ⁴=H), N-succinyl--tyrasamine (structural formula II), N-tosyl group tyrasamine (structural formula II I), N, N '-two tyrasamine urea (structural formula IV), (N, N or N, O) two tosyl group tyrasamines (structural formula V).

The present invention also comprises the preparation method of compound shown in the general formula I.Especially; the preparation method of these compounds is; alkali is being arranged or do not having in the presence of the alkali; with tyrasamine or octopamine or their a kind of salt and carbonyl or sulfonic derivatives reaction; the coupling reagent that described reaction can be used in peptide is synthetic (particularly; carbodiimide, acylimidazole, chloro-formic ester, BOP, CDI, DCC, EEDQ, HTBU

Acceptable material such as TBTU, WSC.HCl, for example, it can obtain from Novabiochem) exist or do not carry out under the existence condition.Especially, described carbonyl or sulfonic derivatives can be aldehyde, active or inactive ester, carboxylic acid or SULPHURYL CHLORIDE, acid anhydrides or isocyanic ester,

Tyrasamine and octopamine are commercially available as being used for the synthetic initial compounds, perhaps can be prepared with already known processes by commercially available starting raw material.

The compound of preferred construction formula I, II, III or IV is the compound that is made by tyrasamine salt by above-mentioned technology.

The compound of general formula I is used for makeup and dermal drug composition according to the present invention, its concentration range be 0.0001% (w/w) to 50% (w/w), but preferred 0.001 (w/w) be to 20% (w/w).

According to the present invention, preferred compositions comprises octopamine (structural formula I, X=-NR ³R ⁴, R ¹=OH, R ²=R ³=R ⁴=H), N-succinyl--tyrasamine (structural formula II), N-tosyl group tyrasamine (structural formula II I), N, N '-two tyrasamine urea (structural formula IV), (N, N or N, O) two tosyl group tyrasamines (structural formula V).

One preferred embodiment in, composition of the present invention also comprises at least a keratolytic and/or decorticating agent.The example of available keratolytic and/or decorticating agent comprise urea, Whitfield's ointment and its alkyl derivative, saturated and undersaturated monocarboxylic acid, saturated and α alkyd undersaturated dicarboxylic acid, tricarboxylic acid, monocarboxylic α alkyd and β alkyd, dicarboxylic acid and β alkyd, tricarboxylic α alkyd and β alkyd, ketone acid, polycarboxylic acid, monocarboxylic, the poly-hydroxy dicarboxylic acid, the tricarboxylic α ketone acid of poly-hydroxy of poly-hydroxy, β ketone acid.

Being exemplified as of these raw materials, 2-oxyacetic acid (oxyacetic acid); 2 hydroxy propanoic acid (lactic acid); 2-methyl-2 hydroxy propanoic acid (methyllactic acid); The 2-hydroxybutyric acid; The 2-hydroxypentanoic acid; The 2-hydroxycaproic acid; 2-hydroxyl enanthic acid; The 2-Hydroxyoctanoic acid; 2-hydroxyl n-nonanoic acid; The 2-hydroxydecanoic acid; 2-hydroxyl undecanoic acid; 2-hydroxy-dodecanoic acid (Alpha-hydroxy lauric acid); 2-hydroxyl tetradecane acid (Alpha-hydroxy myristic acid); 2-hydroxyl cetane acid (Alpha-hydroxy palmitinic acid); 2-hydroxyl octadecanoic acid (Alpha-hydroxy stearic acid); 2-hydroxyl arachic acid (alpha-hydroxy fatty acid); 2-phenyl-2-oxyacetic acid (amygdalic acid); 2,2-biphenyl-2-oxyacetic acid (benzilic acid); 3-phenyl-2 hydroxy propanoic acid (phenyl-lactic acid); 2-phenyl-2-methyl-2-oxyacetic acid (atrolactinic acid); 2-(4 '-hydroxyphenyl) the 2-oxyacetic acid; 2-(4 '-chloro-phenyl-)-the 2-oxyacetic acid; 2-(3 '-hydroxyl-4-4 '-aminomethyl phenyl) the 2-oxyacetic acid; 2-(4 '-hydroxyl-3 '-p-methoxy-phenyl) the 2-oxyacetic acid; 3 '-(2-hydroxyphenyl) 2 hydroxy propanoic acid; 3-(4 '-hydroxyphenyl) 2 hydroxy propanoic acid; And 2-(3 ', 4 ' dihydroxyphenyl), with the 2-oxyacetic acid, 5-n-decoyl Whitfield's ointment, 5-n-dodecanoyl Whitfield's ointment, 5-n-caprinoyl Whitfield's ointment, 5-n-octyl group Whitfield's ointment, 5-n-heptyl Whitfield's ointment, 4-n-heptyl Whitfield's ointment and 2-hydroxy-3-methyl phenylformic acid or its alkoxy derivative, for example 2-hydroxy 3-methoxybenzene formic acid.

Preferred keratolytic is selected from: oxyacetic acid, tartrate, Whitfield's ointment, citric acid, lactic acid, pyruvic acid, glyconic acid, glucuronic acid, oxysuccinic acid, amygdalic acid, oxalic acid, propanedioic acid, succsinic acid, acetate, phenol, Resorcinol, vitamin A acid, adapalene, trichoroacetic acid(TCA), 5 FU 5 fluorouracil, nonane diacid.Keratolytic also can be feasible cis or trans salt, ester, the racemic mixture of above-claimed cpd and/or its relevant dextrorotation or levorotatory form.This type of material can be individually or is worked in coordination with separately and use.

Other is suitable for can comprising the enzyme exfoliator at the keratolytic of this application, the Keratoline by name that it provides based on Sederma ^TMProteolytic enzyme.

In one embodiment, described composition contains and accounts for composition weight about 0.001% and be preferably about 0.1% to about keratolytic/decorticating agent of 5%, more preferably about 0.5% to about 2% to about 10%.

In preferred embodiment, composition of the present invention can also comprise skin Lightening/SYNTHETIC OPTICAL WHITNER.During application, described composition preferably contains and accounts for composition weight about 0.001% to about 10%, and more preferably from about 0.02% to about 5%, also preferred about 0.05% to about 2% skin lightener.The skin lightener that is suitable for comprises the prior art known substances, comprises kojic acid, Resorcinol, amino acid derivative, N-cholesterol oxygen base carbonyl-right-amino acid and N-ethoxy carbonyl-right-amino acid; The imino-phenol derivatives, the L-2-oxygen thiazolidine-4-carboxylic acid or third halfcystine with and salt or ester, arbutin, tranexamic acid, xitix and derivative thereof (for example ascorbic acid phosphoric acid esters enzyme or ascorbic acid phosphoric acid esters sodium, sweet candy of xitix and analogue (for example AA2G that can buy from Hayashibara)), and extract (mulberry extract for example, intacellin, Radix Scutellariae extract, the paper mulberry extract, oil soluble Radix Glycyrrhizae extract (for example can buy)) from Maeuzen, oil soluble Radix Glycyrrhizae extract (licorice, Flos Chrysanthemi extract (for example can buy)), m-tranexamic acid/ethyl xitix (for example can buy) from Shiseido from Kao, single adenosine phosphate disodium (APM that provides by Otsuka), ellagic acid (Lion), trans-resveratrol (Pola), ethyl xitix ether.Be suitable for skin lightener in this application and also comprise and be described in WO95/34280, PCT/US95/07432, co-pending.US08/390,152 and PCT/US 95/23780 in material.Useful especially is the Melaclear by name that provides with SEDERMA ^TM, Etioline ^TM, Melaslow ^TMAnd Lumiskin ^TMThe skin lightener use that combines, be described in FR 2 732 215 respectively, WO 98/05299, among WO 02/15871 and the PCT/FR03/02400.Other is suitable for can comprising at the skin lightener raw material of this application

(Cognis),

(Rona), Azeloglicina (Sinerga) and

(Seppic).Preferred skin lightener is the sweet candy of xitix.

I. additive

According to the present invention, described dermatology acceptable carrier can be water-based or water alcohol solution, water-in-oil emulsion, water external emulsion, micro emulsion, aqueous gel, anhydrous gel, serum or capsule dispersion.

Composition of the present invention can comprise various other supplementary components, and it can be active, functional, is generally used for makeup, personal care or part/transdermal drug product or others.Certainly, application-specific and formula for a product are depended in the selection of the interpolation of supplementary component and specific supplementary component.In addition, the boundary between " activity " composition and " nonactive " composition is artificial regulation, depends on application-specific and product type.In certain is used or in certain product, may " functional " composition in other application or product as the material of " activity " composition, vice versa.

Therefore, composition of the present invention can comprise one or more kind supplementary components, and it helps the purpose of composition.This type of supplementary component can comprise one or more materials, for example, but not as limiting sanitising agent, hair-care agent, skin-care agent, hairspray, antiscurf agent, hair growth promoting agent, flavouring agent, shading and/or sun screening compound, pigment, moistening agent, membrane-forming agent, hair pigment, makeup agent, washing agent, medicine, intensifier, emulsifying agent, wetting agent, negative catalyst, sanitas, reodorant, dermatology acceptable carrier and tensio-active agent.

In any embodiment of the present invention, useful therein activeconstituents can be classified according to its benefit that provides or according to the ultimate principle pattern of its effect.But, should be appreciated that also described useful therein activeconstituents can provide more than a kind of benefit or by the generation effect more than a kind of binding mode in some example.Therefore, the classification here is to make for convenience, does not mean that the application that described activeconstituents is limited to special applications or enumerates.

One preferred embodiment in, composition is to contact with people's collenchyme, described supplementary component should be suitable for collenchyme, also be, when integrating with composition, it is suitable for contacting people's collenchyme (hair, nail, skin, lip), and does not have over-drastic toxicity, uncompatibility, unstable, anaphylaxis and the analogue in the medical judgment test specification.

CTFA cosmetic composition handbook the tenth edition (makeup, toiletry and company limited of fragrance association by the Washington D.C. publish) (2004) has been described the various unconfined raw materials that can be added at this said composition.Other example of these constituent classes comprises, but be not limited only to: nursing agent, the skin anti-aging agent, the skin moisturizing agent, anti wrinkling agent, anti-atrophy agent, the skin smooth agent, antiseptic-germicide, anti-mycotic agent, antiparasitic, biocide, anti-inflammatory agent, the anti-agent of itching, external application narcotic, antiviral agent, keratolytic, free-radical scavengers, the anti-bleeding of sebum, the agent of anti-bits, the differentiation of adjusting skin, propagation or pigmentation agent and promotion infiltration, the preparation of decortication, discoloring agent or tinting material, anti-glycosylation agent, fastening agent, promote corium or epidermis to synthesize and/or prevent the preparation of its degeneration; Promote fibroblast and/or keratinocyte propagation or promote the preparation that keratinocyte breaks up; Muscle speeds to delay agent; Anti-pollutant and/or antifree radical agent; Slender dose, anti-liparitosis agent act on microcirculatory preparation; Act on the metabolic preparation of cellular energy, sanitising agent, hair conditioner, hairspray, hair tonic promotor, shading and/or sun screening compound, the makeup agent, washing agent, medicine, emulsifying agent, softener, sanitas, the deodorant activities composition, the makeup acceptable carrier, tensio-active agent, abrasive, absorption agent, the aesthetic feeling component, for example fragrant agent, freshen toner/tinting material, essential oil, the skin feel agent, the used for cosmetic astringent matter, anti-acne agents, the agent of resistive connection group, foam reducing composition, antioxidant, tackiness agent, biotic additives, enzyme, enzyme inhibitors, enzyme-containing formulation, coenzyme, plant milk extract, botanical derivative, the plant tissue extract, plant seed extract composition, vegetables oil, vegetable drug, the vegetable drug extract, ceramide, peptide, buffer reagent, swelling agent, sequestrant, the chemical derivative, tinting material, trichogen, the used for cosmetic biocide, denaturing agent, the medicine astringent matter, the external application pain killer, membrane-forming agent or pleurodiaphragmatic in terspace material, for example, the polymkeric substance that helps composition film forming characteristics and affinity, season derivative, increase the affinity agent, the emulsifying agent, pH regulator agent (for example trolamine), volatilizer, the agent of disappearing, sequestering agent, skin bleaching and brightening agent, the agent of brownization of skin, skin conditioning agent (for example, wetting agent comprises mixing type and dead front type (humidity-preserving type) wetting agent), skin smooth agent and/or analeptic and derivative, skin treatment agents, viscosifying agent, lipid viscosifying agent (for example stearic acid), with VITAMIN and derivative thereof, decorticating agent, moistening agent, solidifying agent, the lignanoids material, sanitas (for example Phenoxyethanol and benzoates), UV light absorber, cytotoxin, antitumor agent, the fat melting activeconstituents, clouding agent, viscosity modifier, dyestuff, non-volatile solvent, thinner, pearlescent additive, pore forming material, vaccine, water-soluble opalizer, antiperspirant, trichogen, aqua aromatica, be used to improve the fat-soluble opalizer material of drying or aging skin state, skin reforming agent (for example rare Xian extract), negative catalyst (C for example _12-15Phenylformic acid alkyl ester), vehicle, weighting agent, mineral substance, mycobacteria agent, anti-sensitizers agent, H ₁Or H ₂Antihistaminic agent, irritation agent, immunity system help and increase agent, immunity system inhibitor, insect driving agent, slipping agent, tinting material, hypopigmentation agent, sanitas, photostabilizer and their mixture.

Described supplementary component is selected from osamine; glycosamine; the D-glycosamine; the N-acetyl glucosamine; N-ethanoyl-D-glycosamine; mannosamine; niacinamide usp; sodium dehydroacetate; dehydroacetic acid (DHA) and its salt; plant sterol; salicylic acid compound; Urotropinum; two alkyloyl oxyproline compounds; soybean extraction and derivative; equol; isoflavones; flavonoid compound; Phytantriol; farnesol; Geraniol; peptide and its derivative; two-; three-; four-; five-; with six peptides and derivative thereof; Methionin-Threonine-Threonine-Methionin-Serine; hexadecanoyl-Methionin-Threonine-Threonine-Methionin-Serine; carnosine; N-acyl amino acid compound; retinoid; Vitamin A propionate; Vogan-Neu; retinyl palmitate; retinoic acid ester; retinene; vitamin A acid; water-soluble vitamins; ascorbate salt; vitamins C; xitix; the xitix glucosides; anti-bad blood acyl cetylate; magnesium ascorbyl phosphate; STAY-C 50; the salt of VITAMIN and derivative; pro-vitamin and its salt and derivative; STAY-C 50; the salt of VITAMIN and derivative; pro-vitamin and its salt and derivative; the ethyl panthenol; vitamins B; the vitamins B derivative; vitamins B ₁, vitamins B ₂, vitamins B ₆, vitamins B ₁₂, vitamin K, vitamin K derivative, vitamins B, vitamins B derivative, vitamins B ₁, vitamins B ₂, vitamins B ₆, vitamins B ₁₂Vitamin K, the vitamin K derivative, pantothenic acid and its derivative, general ethene ether, panthenol and its derivative, panthenol, the ethyl panthenol, vitamin H, amino acid and its salt and derivative, water-soluble amino acids, asparagine, L-Ala, indoles, L-glutamic acid, the water-insoluble VITAMIN, vitamin A, vitamin-E, vitamin F, vitamins D, single-, two-, with triterpenes, β-ionol, cypress camphor, with its derivative, water-insoluble amino acid, tyrosine, tryptamines, butylated hydroxytoluene, butylated hydroxyanisole, wallantoin, tocopheryl nicotinate, tocopherol, Renascin, soft ester acyl-glycine-Histidine-Methionin, plant sterol, hydroxy acid, oxyacetic acid, lactic acid, lactobionic acid, ketone acid, pyruvic acid, phytic acid, Ultrapole L, toluylene, laurate, trans-resveratrol, phytokinin, zeatin, dimethylaminoethanol, natural peptide, soybean peptide, sugar lime, manganese gluconate, Zinc Gluconate, particulate material, pigment raw material, the nature pigment, the pyridone thanomin, 3,4,4 '-trichlorocarbanilide, neko, Zinc Pyrithione, Resorcinol, kojic acid, xitix, magnesium ascorbyl phosphate, the ascorbigen glucosides, how hot pyrrole is, aloe, terpenol, wallantoin, bisabolene, Rizinsan K2 A2, R-Glyceric acid, sorbose alkyd, tetramethylolmethane acid, tetramethyleneimine ketone acid and its salt, Protosol, erythrulose, Glycerose, winestone aldehyde, Syzygium aromaticum stem oil, menthol, camphor, eucalyptus oil, oxymethoxyallylbenzene, the peppermint lactate, the witch hazel overhead product, Eicosene and nvp copolymer, carboxylamine iodo propyl group butyl ester, polysaccharide, corps acid, salicylate, glycyrrhetinic acid, carotinoid compounds, acyl sphingosine, and standard-acyl sphingosine, the lipid synthetics, acyl sphingosine and standard-acyl sphingosine, the lipid synthetics, oil is generally natural origin, as shea butter, Prunus amygdalus oil, Oenothera oil, Prunus amygdalus oil, plam oil, monoi oil, HEPES; Third halfcystine; O-decoyl-6-D-maltose; The disodium salt of methylglycine etheric acid, steroid, for example diosgenin and DHEA derivative; N-ethoxy carbonyl-4-para-aminophenol, Fructus Rubi extract; Plant hormone; The yeast saccharomyces cerevisiae extract; Algae Extract; Soya bean, lupine, Zea mays and/or Semen Pisi sativi extract; Alverine and its salt, particularly alverine Citrate trianion, Flower of Chinese Peashrub and horse-chestnut extract, this catalogue is not construed as limiting.

Effective especially when skin care and hair nursing activeconstituents and the combination of three/tetrapeptide mixture, further content can find in the trade literature of SEDERMA and in the website.All be incorporated herein by reference.

In any embodiment of the present invention, useful therein supplementary component can or act on basic reason pattern by its benefit that provides and be classified.But, should be appreciated that described useful therein activeconstituents can provide more than a kind of benefit or by the generation effect more than a kind of binding mode in some example.Therefore, the classification here is to make for convenience, does not mean that described activeconstituents is limited to specific application or the application of enumerating.

1. osamine (aminosugar)

Composition of the present invention can comprise osamine, and it has another name called aminosugar.Useful in the present invention osamine compound can be included in the PCT publication number be WO 02/076423 with the US patent No. 6,159,485 in description.

In one embodiment, described composition comprises and accounts for composition weight about 0.01% to about 15%, and more preferably from about 0.1% to about 10%, even 0.5% to about 5% described osamine composition more preferably from about.

Osamine can be synthetic or natural origin, can be used as the mixture of pure compound or compound and uses (for example, the extract of natural resource or synthetic materials mixture).For instance, glycosamine is typically found at many crustaceans biologies, also can be by fungic origin.When this used, " osamine " comprised that (for example, HCl salt) isomer and tautomer can be buied from Sigma Chemical company for itself or its salt.The example of useful osamine comprises glycosamine, N-acetyl glucosamine, mannosamine, N-acetylmannosamine, GalN, N-acetylgalactosamine, its isomer (for example, steric isomer) and its salt (for example, HCl salt).Preferred herein glycosamine, particularly D-glycosamine and N-acetyl glucosamine, particularly N-ethanoyl-D-glycosamine.

2. vitamin b 3 compound

Composition of the present invention can comprise vitamins B ₃Compound.Vitamins B ₃Compound is effective especially for regulating skin, is described in U.S. patent No.5, in 939,082.In one embodiment, described composition comprises and accounts for composition weight about 0.001% to about 50%, and more preferably from about 0.01% to about 20%, even more preferably from about 0.05% to about 10%, can also be more preferably from about 0.1% to about 7%, even 0.5% to about 5% described vitamins B more preferably from about ₃Compound.

" vitamins B as used herein ₃Compound " be compound shown in the following formula:

Wherein R is-CONH ₂(that is, niacinamide usp) ,-COOH (that is nicotinic acid) or-CH ₂OH (that is nicotinic alcohol); Its derivative; Salt with any above-mentioned substance.

Exemplary said vitamin B ₃The derivative of compound comprises nicotinate, comprises the nicotinate (for example, Vitamine E Nicotinate, myristyl nicotinate) of non-vasorelaxation, nicotinyl amino acids, the nicotinyl alcohol esters of carboxylic acid, nicotinic acid N-oxide compound and nicotinic acid amine n-oxide.

Suitable nicotinate comprises C ₁-C ₂₂Nicotinate, preferred C ₁-C ₁₆, more preferably C ₁-C ₆Alcohol.Non-vasorelaxation nicotinate comprises Vitamine E Nicotinate and Vasonicit; Vitamine E Nicotinate is preferred.

Other vitamins B ₃The derivative of compound is by replacing the niacinamide usp derivative that one or more amide group hydrogen atoms get, and the specific examples of this derivative comprises nicotinuric acid (C ₈H ₈N ₂O ₃) and nicotinyl hydroxamic acid (C ₆H ₆N ₂O ₂).Exemplary nicotinyl alcohol esters comprises carboxylic acid, Whitfield's ointment, acetate, oxyacetic acid, palmitinic acid nicotinyl alcohol esters and analogue.Other are at the vitamins B of this application ₃The limiting examples of compound is 2-chloro-nicotinamide, 6-aminonicotinamide, 6-methylnicotinamide, n-methyl-niacinamide, n, the n-Nikethamide, N-(methylol)-niacinamide, quinolinic acid imide, nicotinanilide, n-benzyl niacinamide, n-Ethylnicotinamide, Thylin, nicotine aldehyde, Yi Yansuan, methyl Yi Yansuan, Thionicotinamide, niaguitil (nialamide), 1-(3-pyridylmethyl) urea, 2-sulfydryl niacin, cholexamin and niaprazine.

Said vitamin B ₃Examples for compounds is to know in the prior art, and can buy from many sources commercial, for example, Sigma Chemical Company company (St. Louis, MO); ICNBiomedicals (Irvin, CA) and Aldrich Chemical company (Milwaukee, WI).

Can use one or more vitamins Bs in the present invention ₃Compound.Preferred vitamins B ₃Compound is niacinamide usp and Vitamine E Nicotinate.Niacinamide usp more preferably.

During application, the derivative of the salt of niacinamide usp, derivative and its salt is preferably renderd a service substantially identical with niacinamide usp material.

Vitamins B ₃Salt also be used for the present invention.Be applied to this vitamins B ₃The limiting examples of compound salt comprises the organic-or-inorganic salt, for example has the inorganic salt (for example, muriate, bromide, iodide, carbonate, preferred muriate) of anionic inorganic element, and organic carboxylic ester (comprise single-, two-and three-C ₁-C ₁₈Carboxylicesters, for example, acetic ester, salicylate, glycolate, lactate, malate, citrate, preferred monocarboxylic ester, for example acetic ester).These compounds and other vitamins B ₃The salt of compound can be by the ready-made preparation of those of skill in the art (" L-xitix and D-saccharosonic acid and nicotinic acid and acid amides reaction thereof " J. organic chemistry, Vol.14,22-26 (1949)).

The vitamins B that is comprised ₃Compound can be abundant pure raw material, or separates extract from natural origin (for example, plant) by proper physical and/or chemical process.It is pure that vitamin b 3 compound is preferably essence, more preferably refining pure.

3. dehydroacetic acid (DHA) (DHA)

Composition of the present invention can comprise the dehydroacetic acid (DHA) with following structure:

Perhaps its pharmacy acceptable salt, derivative or tautomer.The science name of dehydroacetic acid (DHA) is 3-ethanoyl-6-methyl-2H-pyrans-2,4 (3H)-diketone, can buy from Lonza.

Pharmacy acceptable salt comprises an alkali metal salt, for example sodium and sylvite; Alkaline earth salt, for example calcium and magnesium salts; Atoxic heavy metallic salt; Ammonium salt; And trialkyl ammonium salts, for example trimethyl ammonium and triethyl ammonium salt.Sodium, potassium and the ammonium salt of preferred dehydroacetic acid (DHA).More preferably sodium dehydroacetate, it can be bought from Tri-KTristat SDHA.The derivative of dehydroacetic acid (DHA) includes but are not limited to any CH ₃Group by acid amides, ester, amino, alkyl and alcohol ester individually or merge the compound that ground replaces.The tautomer of dehydroacetic acid (DHA) can be described as having chemical formula C ₈H ₈O ₄, have above-mentioned structure.

In one embodiment, composition of the present invention can comprise and accounts for composition weight 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% dehydroacetic acid (DHA) or its pharmacy acceptable salt, derivative or tautomer.

4. plant sterol

Composition of the present invention can comprise plant sterol.For example, one or more plant sterols can be selected from :-Sitosterol, campesterol, brassicasterol, D5-avennasterol, Lupeol, hitodesterol, Stigmasterol, they derivative, analogue, with and composition.More preferably, described plant sterol is selected from :-Sitosterol, campesterol, brassicasterol, Stigmasterol, their derivative, with and composition.More preferably, described plant sterol is a Stigmasterol.

Plant sterol can be synthetic or natural origin, can be used as the mixture (for example, natural resource extract) of refining pure compound or compound.What plant sterol was typically found at the plant oil ﹠ fat can not the saponification part, and available is free sterol, acetyl derivatives, sterol ester, oxyethyl group or joins sugar derivatives.More preferably, plant sterol is a free sterol." plant sterol " comprises its isomer and tautomer as used herein, can be from Aldrich Chemical company, and Sigma Chemical company and Cognis buy.

In one embodiment, composition of the present invention comprises and accounts for composition weight about 0.0001% to about 25%, and more preferably from about 0.001% to about 15%, even more preferably from about 0.01% to about 10%, more preferably from about 0.1% to about 5%, and even 0.2% to about 2% plant sterol more preferably from about.

5. salicylic acid compound

Composition of the present invention can comprise salicylic acid compound, its ester, salt, perhaps its combination.In one embodiment, composition salicylic acid compound of the present invention preferably comprises and accounts for composition weight about 0.0001% to about 25%, more preferably from about 0.001% to about 15%, more preferably from about 0.01% to about 10%, more preferably from about 0.1% to about 5%, and even and even more preferably from about 0.2 to about 2% Whitfield's ointment.

6. hexapradol

Composition of the present invention can comprise the hexapradol compound, its salt, and derivative.

In one embodiment, hexapradol accounts for described composition weight about 0.0001% to about 25%, 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%.

The hexapradol derivative of Shi Yonging comprises the isomer and the tautomer of any hexapradol compound herein, includes but not limited to organic acid and mineral acid, for example sulfonic acid, carboxylic acid or the like.Preferably, the hexapradol compound comprises hexapradol two isethionic acid esters, can be according to Eleastab

100 title is buied from LaboratoiresSerobiologiques.

7. two alkanoyl oxyproline compounds

Composition of the present invention can comprise one or more two alkanoyls oxyproline compounds and its salt and derivative.

In one embodiment, two alkanoyl oxyproline compounds preferably account for described composition weight about 0.01% to about 10%, and more preferably from about 0.1% to about 5%, and also more preferably from about 0.1% to about 2%.

Appropriate derivative is including, but not limited to ester, and for example fatty acid ester includes but not limited to three palmitoyl and two palm ethanoyl oxyprolines.Useful especially is two palmitoyl oxyprolines.When this used, two palmitoyl oxyprolines comprised its any isomer and tautomer, can be according to trade name Sepilift On market, buy from Seppic company.The further argumentation of two palmitoyl oxyprolines is published among the PCT publication number WO 93/23028.Preferably, two palmitoyl oxyprolines are triethanolamine salts of two palmitoyl oxyprolines.

8. flavonoid compound

Composition of the present invention can comprise flavonoid compound.Flavonoid compound mainly is disclosed in U.S. patent 5,686,082 and 5,686, in 367.When this uses, " flavones " non-replacement of expression or replacement flavones (i.e. list-replacement flavones, and/or two-replacement flavones, and/or three-replacement flavones).Being particularly suitable for flavonoid compound example of the present invention is one or more flavones, one or more flavanone, one or more isoflavones, one or more tonka bean camphors, one or more chromones, one or more dicoumarols, one or more chromanones, one or more chromanols, their isomer (for example, cis/trans isomer trans-isomer(ide)) and mixture.

Preferably flavones and isoflavones are applied to this, particularly daizeol (7,4 '-dihydroxy isoflavone), genistein (5,7,4 '-trihydroxy-isoflavone), equol (7,4 '-dihydroxyl isoflavan), 5,7-dihydroxyl-4 '-the methoxyl group isoflavones, this class mixture of soybean isoflavones (from the mixture of soybean extraction) and other plant origins is (for example, red clover) and their mixture.Also preferred flavanone, for example Hesperitin, Hesperidin and their mixture.

Flavonoid compound in this application can have been bought from many sources on market, for example, and IndofineChemical company, Steraloids company and Aldrich Chemical company.Suitable flavonoid compound is by name

, provide by SEDERMA, be described in WO 99/18927.

In one embodiment, described flavonoid compound accounts for described composition weight about 0.01% to about 20%, and more preferably from about 0.1% to about 10%, even more preferably from about 0.5% to about 5%.

9.N-acyl amino acid compound

Main component of the present invention can comprise one or more N-acyl amino acid compounds.Amino acid can be the known amino acid of any prior art.N-acyl amino acid compound of the present invention is corresponding with following chemical formula:

Wherein R can be a hydrogen, alkyl (replacing or non-replacement side chain or straight chain), the perhaps combination of alkyl and aromatic yl group.

Preferably, N-acyl amino acid compound is selected from: N-acyl group phenylalanine, N-acyl group tyrosine, their isomer, salt and derivative.Amino acid can be D or L isomer, perhaps their mixture.

In N-acyl group Phenylalamine derivatives classification widely, useful especially is can be according to trade name N-undecanoyl-L-phenylalanine of on market, having bought from Seppic.

In an embodiment of the invention, the N-acylamino acid preferably accounts for described composition weight about 0.0001% to about 25%, and more preferably from about 0.001% to about 10%, and more preferably from about 0.01% is about 5%, even more preferably from about 0.02% to about 2.5%.

10. retinoid

Described composition of the present invention can comprise retinoid, preferred security and significant quantity, safety when making composition be used to regulate keratinous tissue conditions and effectively, be preferred for regulating visible and/or palpable collenchyme ununiformity (for example, regulating the sign of skin aging).Described composition can comprise and accounts for composition weight about 0.001% to about 10%, and more preferably from about 0.005% to about 2%, and also more preferably from about 0.01% to about 1%, more preferably from about 0.01% to about 0.5%, retinoid.Its optimum concn that is used for composition depends on concrete selected retinoid, because their effectiveness can have sizable change.

When this used, " retinoid " comprised whole natural and/or synthetic retinoids or Vogan-Neu-have vitamin A biological activity in skin, and its geometrical isomer and steric isomer be similar compound so also.Retinoid is preferably from Vogan-Neu, retinol ester (for example, C ₂-C ₂₂The Vogan-Neu alkyl ester, comprise retinyl palmitate, retinoic acid ester, Vitamin A propionate), retinene and/or vitamin A acid (comprising complete-trans retinoic acid and/or 13-cis-vitamin A acid) or their mixture.More preferably retinoid is the retinoid except vitamin A acid.These compounds are that prior art is known, can buy in market from many sources, for example, Sigma Chemical company and Boerhinger Mannheim.Other retinoid that can be applicable to this is described in U.S. patent No.4,677,120, U.S. patent No 4,885,311, U.S. patent No 5,049,584, U.S. patent No 5,124,356 and reissue 34,075.Other suitable retinoid can comprise tocopherol-retinyl ester [Renascin of vitamin A acid (trans-or cis-), adapalene 6-[3-(1-adamantyl)-4-aminomethyl phenyl]-the 2-naphthoic acid }, and Tazarotene (ethyl 6-[2-(4,4-dimethyl sulphide chromanyl-6-y1)-and ethynyl] nicotinate).Preferably, retinoid comprises Vogan-Neu, retinyl palmitate, retinoic acid ester, Vitamin A propionate, retinene and their combination.Vitamin A propionate more preferably, most preferred quantities is about 0.1% to about 0.3%.

The retinoid that is comprised can be abundant pure raw material, or separates the extract that obtains from natural origin (for example, plant) by suitable physics and/or chemical process.Retinoid is preferably fully pure, more preferably refining pure.

11. optional peptide

Described composition of the present invention can comprise additional peptide.Suitable peptide can include, but are not limited to: two-, three-, four-, five-and six-peptide and their derivative.In one embodiment, described composition comprises and accounts for the about 1x10-7% of composition weight to about 20%, more preferably from about 1x10-6% to about 10%, also more preferably from about 1x10-5% arrives about 5% additional peptide.

When this used, " peptide " referred to contain ten kinds or less amino acid whose peptide and derivative thereof, isomer, and with other complex compounds of metal ion (for example, copper, zinc, manganese, magnesium and analogue) for example.When this used, peptide both can be that natural existence also can be the synthetic peptide.Can be applicable to the composition that contains peptide that to have bought on naturally occurring and the market also comprising of this.

Be suitable for dipeptides in this application including, but not limited to carnosine (Beta-alanine-Histidine), tyrosine-arginine, Xie Ansuan-tryptophane (WO 0164178), l-asparagine-phenylalanine, aspartic acid-phenylalanine.Be suitable for tripeptides in this application including, but not limited to arginine-Methionin-arginine (Peptide CK), HIS-GLY-glycine, glycine-Histidine-Methionin, glycine-glycine-Histidine, glycine-HIS-GLY, Methionin-phenylalanine-Methionin.Be suitable for the tetrapeptide of this application including, but not limited to, E peptide, arginine-Serine-arginine-Methionin, glycine-glutamine-proline(Pro)-arginine, penta suitable peptide is including, but not limited to Methionin-Threonine-Threonine-Methionin-Serine.Six suitable peptides are including, but not limited to Xie Ansuan-glycine-Xie Ansuan-L-Ala-proline(Pro)-glycine, and the material that is disclosed in Fr2854897 and Us 2004/0120918.

Other are suitable at the peptide of this application lipophilic derivatives including, but not limited to peptide, preferred soft ester acyl derivative and aforesaid metal complex (for example, the copper complex of HIS-GLY-glycine tripeptide).Preferred following dipeptidase derivant, the soft ester acyl-Beta-alanine of N--Histidine, N-ethanoyl-tyrosine-arginine-n-Hexadecane ester are (from the CALMOSENSINE of French sederma ^TM, WO 9807744, and US 6,372, and 717).The tripeptide derivative that preferably includes the soft ester acyl-glycine of N--Methionin-Histidine is (from the Pal-GKH of French SEDERMA; WO 0040611); as the copper derivative of lamin by the commercial HIS-GLY-glycine sold of Sigma; lipospondin (N-Elaidoyl-Methionin-phenylalanine-Methionin) and configuration thereof are replaced analogue; N-ethanoyl-arginine-Methionin-arginine-NH2 (Peptide CK+); N-Biot-glycine-Histidine-Methionin (N-Biot-GHK that SEDERMA provides, WO 0058347) and its derivative.Be suitable for tetrapeptide derivative in this application including, but not limited to the soft ester acyl-glycine of N--glutamine-proline(Pro)-arginine (French SEDERMA provides), pentapeptide derivative is including, but not limited to the soft ester acyl-Methionin of N--Threonine-Threonine-Methionin-Serine (MATRIXYL that French SEDERMA provides ^TM, WO 0015188 and US6,620,419), the soft ester acyl-tyrosine of N--glycine-glycine-phenylalanine-X, X is Met or leucine, perhaps their mixture.Suit at the hexapeptide derivatives of this application including, but not limited to the soft ester acyl-Xie Ansuan of N--glycine-Xie Ansuan-L-Ala-proline(Pro)-glycine and its derivative.

Preferred compositions comprises the Biopeptide-GL that commercially available tripeptides or SEDERMA provides ^TM, the Maxilip that SEDERMA provided ^TM(WO 0143701), the Biobustyl that SEDERMA provided ^TMThe preferred tetrapeptide of the composition that can buy on described market source comprises RIGIN ^TM(WO 0043417), EYELISS ^TM(WO 03068141), MATRIXYL ^TMRELOADED and contain 50 to 500ppm soft ester acyl-glycine-glutamine-proline(Pro)-arginic MATRIXYL 3000 ^TM, France (Us 2004/0132667) is provided by SEDERMA.

12. xitix and other VITAMIN

Composition of the present invention can comprise one or more VITAMIN, xitix class (for example, vitamins C, vitamin C derivatives, xitix, ascorbigen glucosides, anti-bad blood acyl cetylate, magnesium ascorbyl phosphate, STAY-C 50) for example.This biostearin can be including, but not limited to vitamins B, vitamins B derivative, vitamins B ₁To vitamins B ₁₂With their derivative, vitamin K, vitamin K derivative, vitamin H, vitamins D, vitamin D-derivatives, vitamin-E, vitamin e derivative and their pro-vitamin, for example panthenol and its mixture.The element-vitamine compound that is comprised can be abundant pure raw material, perhaps separates the extract that obtains from natural origin (for example, plant) by suitable physics and/or chemical process.In one embodiment, when element-vitamine compound is present in the described composition of the present invention, described composition comprises and accounts for composition weight about 0.0001 to about 50%, more preferably from about 0.001% to about 10%, be more preferably about 0.01% to about 8% and be more preferably about 0.1% to about 5% element-vitamine compound.

13. particulate material

Composition of the present invention can comprise one or more particulate materials.The unrestricted example that can be applicable to particulate material of the present invention comprise painted with uncoloured pigment, interfere pigment, inorganic powder, organic dust, composite powder, optical brightener particle and their composition.These particulates can be, for example, strip, spherical, extend shape or needle-like or irregularly shaped, top coat or not coating, perviousness or impermeability, charged or uncharged and, can powder type or the predispersion form add in the present composition.In one embodiment, be present in particulate material in the described composition and account for composition weight about 0.01% to about 20%, more preferably from about 0.05% to about 10%, is more preferably about 0.1% to about 5%.For the unspecial restriction of the pigment that uses in the described composition, tinting material or fill powder.

The particulate material that can be applied to this can include, but are not limited to: pearl white, silk Muscovitum, silica, mica, mica with barium sulfate or the processing of other raw materials, zeolite, kaolin, silica, boron nitride, lauroyl Methionin, nylon, polyethylene, talcum, vinylbenzene, polypropylene, polystyrene, ethene/acrylic ester rubber, aluminum oxide, silicone resin, barium sulfate, lime carbonate, cellulose acetate, tetrafluoroethylene, polymethylmethacrylate, starch, treated starch, starch octenyl succinate anhydride aluminium for example, silk, glass, with their mixture.Preferred organic dust/filler includes but not limited to, be selected from the polymer particles of methylsiloxane resin microsphere, for example, the product of the Tospearl 145A by name that sells by Toshiba silicone, poly (methyl methacrylate) micro-sphere, the product of the Micropearl M 100 by name that sells by Seppic for example, the spherical particle of crosslinked dimethione, special for example by the Trefil E 506C by name of Dow Corning Toray Silicone sale or the product of Trefil E 505C, polymeric amide spherical particle and specific nylon 12, the product of the special Orgasol 2002D Nat C05 by name that for example sells by Atochem, polystyrene microsphere, the product of the Dynospheres by name that sells by Dyno Particles for example, the ethylene acrylate copolymer of the FloBead EA 209 by name that sells by Kobo, tetrafluoroethylene, polypropylene, octene acyl succinic acid starch ester aluminium, the product of the Dry Flo by name that sells by National Starch for example, the polyethylene microballoon, the product of the Microthene FN 510-00 that sells by Equistar for example, silicone resin, the polymethyl siloxane silicon polymer, by the strip powder of L-lauroyl Methionin manufacturing, and their mixture.

What can also be applied to this is to disturb pigment.The example of modal interference pigment is to be superimposed with the thick TiO2 of about 50-300nm, Fe ₂O ₃, silica, stannic oxide and/or Cr ₂O ₃The mica of film.Applicable interference pigment can have been bought from various suppliers, for example, Rona (TimironTM and DichronaTM), Presperse (FlonacTM), Englehard (DuochromeTM), Kobo (SK-45-R and SK-45-G), BASF (Sicopearls) and Eckart (for example Prestige Silk Red).

Other is used for pigment of the present invention and mainly presents color by the visible light of selecting to absorb specific wavelength, comprises inorganic pigment, organic pigment and their combination.This class inorganic pigment comprises ferric oxide, high ferro ammonium ferrocyanide, manganese violet, ultramarine blue and chromic oxide.Organic pigment can comprise natural colorant and synthetic monomer and polymer tinting material.Example is phthalocyanine blue and marennin.Also available colour lake, elementary FD﹠amp; C or D﹠amp; C colour lake and their mixture.The also available solubilized of sealing or do not dissolve other tinting materials of dye well.Can be used for inorganic white of the present invention or uncoloured pigment, for example TiO ₂, ZnO, or ZrO ₂, can buy in many from the market sources.The example of suitable particulate material comprises can be from product (the TRONOX TiO of U.S.Cosmetics purchase ₂Series, SAT-T CR837, a rutile TiO ₂).

Pigment/powder of the present invention can increase retention of color and/or be convenient to preparation through surface treatment.The unrestricted example of the coating that is fit to comprises silicone resin, Yelkin TTS, amino acid, metallic soap, polyethylene and collagen.These surface treatment agents can be hydrophobicitys or hydrophilic, preferably use the hydrophobicity treatment agent.

14. sunscreen activity composition

Described composition of the present invention can randomly comprise the sunscreen activity composition.When this used, " sunscreen activity composition " comprised opalizer and physical sunscreen agent.The sunscreen activity composition that is fit to can be the organic or inorganic material.

The conventional organic or inorganic sunscreen activity composition of broad variety is suitable in this use.In one embodiment, described composition comprises and accounts for composition weight about 0.1% to about 20%, is more typically about 0.5% to about 10% sunscreen activity composition.Content depends on shading selection and required sunlight protection factor (SPF) accurately.

For the example of activated organic opalizer in ultraviolet ray-A and/or ultraviolet-B, below specialize its CTFA title:

-Para-Aminobenzoic derivative: para-amino benzoic acid, ethyl para-amino benzoic acid, ethyl dihydroxypropyl para-amino benzoic acid, because the para-amino benzoic acid of the ethylhexyl dimethyl para-amino benzoic acid of special " ESCALOL507 " by name that sells of ISP, glyceryl para-amino benzoic acid, " UVINULP25 " PEG-25 by name of selling by BASF

-salicyclic acid derivatives: two propyleneglycoles salicylates, the TEA salicylate of the Ethylhexyl salicylate of the Homosalate of " the EUSOLEX HMS " by name that sells by RONA/EM, " the NEO HELIOPAN OS " by name that sell by HAARMANN and REIMER, " DIPSAL " by name that sell by SCHER, sell by HAARMANN and REIMER, " NEO HELIOPAN TS " by name

-phenyl phenacyl ketone derivative: the trade mark of being sold by HOFFMANN LA ROCHE is PAROSOL 1789, the isopropyl diphenyl formyl radical methane of " PARSOL 1789 ",

-styrene derivatives: the trade mark that the trade mark of being sold by HOFFMANN LA ROCHE be the methoxy cinnamic acid (ethyl hexyl) ester, sec.-propyl Methoxycinnamate of " PARSOL MCX ", sold by HAARMANN and REIMER is isopentyl methoxyl group cinnamic ester, cinoxate, DEA methoxyl group cinnamic ester, methoxy cinnamic acid pair isopropyl esters, the thylhexoic acid glyceryl ester dimethoxy cinnamic ester of " NEO HELIOPAN E 1000 "

--diphenylacrylate: the trade mark of being sold by BASF is the Nifedipine difficult to understand of " UVINUL N 539 ", the trade mark of being sold by BASF is the Viosorb 910 of " UVINUL N 35 ",-benzophenone derivates: the trade mark of being sold by BASF is the benzophenone-1 of " UVINUL 400 ", the trade mark of being sold by BASF is the benzophenone-2 of " UVINUL D 50 ", the trade mark of being sold by BASF is the benzophenone-3 or the oxybenzone of " UVINUL M 40 ", the trade mark of being sold by BASF is the benzophenone-4 of " UVINUL MS 40 ", the trade mark of being sold by NORQUAY is the benzophenone-5 of " HELISORB 11 ", benzophenone-6, the trade mark of being sold by AMERICAN CYANAMID is the benzophenone-8 of " SPECTRA-SORB UV-24 ", the trade mark of being sold by BASF is the Benzophenone 9 of " UVINUL DS-49 ", benzophenone-12

-Ben Yajiaji camphanone derivative: 4-methylbenzene methylene radical camphanone, Ben Yajiaji camphanone sulfonic acid, camphanone zephiran metilsulfate, the terephthalylidene two of the benzylidene camphanone of 3-, " EUSOLEX 6300 " by name of selling by MERCK contract camphanone sulfonic acid, poly-formamide benzene methylene radical camphanone

-phenyl benzimidizole derivatives: the trade mark of being sold by MERCK is that the Phenylbenzimidazolesulfonic acid of " EUSOLEX 232 ", the trade mark of being sold by HAARMANN and REIMER are the benzoglyoxaline of " NEO HELIOPAN AP ",

-pyrrolotriazine derivatives: the trade mark of being sold by CIBA GEIGY is that the Anisotriazine of " TINOSORB S ", the trade mark of being sold by BASF are the diethylhexyl fourth aminotriazine ketone of " UVASORB HEB " for the ethylhexyl triazone of " UVINUL T 150 ", the trade mark of being sold by SIGMA 3V

-phenyl benzotriazole derivatives: by the drometrizole trisiloxanes that is called " SILATRIZOLE " of RHODIA CHIMIE sale,

-anthranilic acid derivative: the trade mark of being sold by HAARMANN and REIMER is the anthranilic acid menthyl ester of " NEO HELIOPANMA ",

-imidazolidine derivatives: ethylhexyl dimethoxy Ben Yajiaji dioxy imidazolylpropionic acid ester,

-Ben Yajiaji adipic acid ester derivative: the trade mark of being sold by HOFFMANN LA ROCHE is the polysiloxane with Ben Yajiaji adipic acid ester functional group of " PARSOL SLX " and their mixture.

-other: dihydroxycinnamic acid derivative (umbrella flower lactone, methyl umbrella flower lactone, methyl acetic acid-umbrella flower lactone); Trihydroxy--cinnamic acid derivative (Esculetin, methyl esculetin, Daphnetin and glucosides, Vitamin C2 and dephnin); Hydro carbons (diphenyl diethylene, toluylene); Dibenzalacetone and benzalacetophenone; Naphthalene sulphur ester (beta naphthal-3,6-disulfonic acid and beta naphthal-6, the sodium salt of 8-disulfonic acid); Two-carbonaphthoic acid and its salt; O-and p-hydroxy diphenyl disulfonate; Coumarin derivatives (7-hydroxyl, 7-methyl, 3-phenyl); Diazole (2-ethanoyl-3-bromo-indazole, phenyl benzoxazoles, methyl aphthoxazoles, various aryl benzothiazole); Quinine salt (hydrosulfate, vitriol, hydrochloride, oleate and tannate); Quinoline (8-8-cxine sulphate, 2-phenylquinoline); Uric acid and violuric acid; Tannic acid and its derivative (for example, Hexaethyl ether); (butyl carbotol) (6-propyl group piperonyl) ether; Resorcinol;

The organic uv screening agent is especially preferably from following compound: the Whitfield's ointment (ethyl hexyl) ester, butyl methoxydibenzoylmethise, the methoxy cinnamic acid (ethyl hexyl) ester, Ao Kelining, Phenylbenzimidazolesulfonic acid, the terephthalylidene two camphanone sulfo group that contracts, benzophenone-3, benzophenone-4, benzophenone-5,4-methylbenzene methylene radical camphanone, benzoglyoxaline, Ah rope's triazine, the ethylhexyl triazone, diethylhexyl fourth aminotriazine ketone, methylene his dialkylphosphine oxide-124 Triazole base tetramethyl butyl phenol, the drometrizole trisiloxanes, with their mixture.

Preferably be described in U.S. patent No.6 in addition, the described composition in 190,645, particularly the trade mark of being sold by Croda company is the opalizer of INCROQUAT-UV-283.

The inorganic screening agent that can be used for composition of the present invention is to apply or the nanometer pigment of coated metal oxide (main particulate mean sizes: usually between 5nm and 100nm not, between preferred 10nm and the 50nm), the example of nanometer pigment such as titanium dioxide (non-crystal crystalline rutile and/or octahedrite form), iron, zinc, zirconium or cerium dioxide and their mixture.In addition, be coating-forming agent alumina and/or aluminum stearate.This coating or the metal oxide nano pigment that do not have coating be at EP-A-0-518, special description arranged in 772 and EP-A-0-518,773.

When this uses, the content of inorganic sunscreen accounts for described composition weight about 0.1% to about 20%, preferred 0.5% to about 10%, and more preferably from about 1% to about 5%.

15. it is anti--the liparitosis agent

Composition of the present invention can also comprise anti-liparitosis agent.Suitable reagent can comprise, but be not limited to, Xanthine compounds (for example, caffeine, theophylline, Theobromine and aminophylline), in one embodiment, when anti--when the liparitosis compound is present in the described composition of the present invention, described composition comprises about 0.0001% to about 50%, more preferably from about 0.001% to about 10%, is more preferably from about 0.01% to about 8%, be more preferably about 0.1% to about 5% calculate by weight resist-the liparitosis compound.

Useful especially is to have Vexel by name ^TM(FR 2 654 619), Coaxel (FR 2 694 195), Cyclolipase ^TM(FR 2 733 149), Pleurimincyl ^TMAnd Lipocare ^TM(WO 98/43607) and Unislim ^TMThe composition of the anti-liparitosis of (FR 0306063)/slender dose, the said products is all provided by SEDERMA.

16. slender, toning or dehydration activity composition

Described composition can comprise one or more lysing adipose tissue agent, be selected from: Pimobendane (for example, xanthine derivative), α-2 retarding agent the compound that can block α-2 acceptor in fat cell surfaces, beta-adrenaline excitant and antagonist (for example alverine and its organic or inorganic salt, alverine Citrate trianion for example), suppress low-density lipoprotein and very low density lipoprotein receptor synthetic reagent, the inhibitor of fatty acid synthetase, acetyl-CoA carboxylase for example, or fatty acid synthetase or cerulenine, intensify the proteic compound of beta receptor and/or G, the glucose transport retarding agent, for example serutine or rutine, neuropeptide tyrosine (NPY) antagonist that can block npy receptor in fat cell surfaces, acceptable derivates on cAMP and its makeup, the adenylate cyclase enzyme activator, forskolin for example, the reagent of modified fatty acid transhipment, lysing adipose tissue peptide and lysing adipose tissue albumen, class peptide or proteinoid, for example derive from the peptide class of Rat parathyroid hormone 1-34, in patent documentation FR 2788058 and FR 2781231, special description is arranged.

The example of other available lysing adipose tissue agent comprises botanical and marine extracts.

In plant milk extract, more particularly can mention extracts of following plants: foreign ivy (HederaHelix), radix bupleuri (Bupleurum chinensis), arnica oil (Arnica Montana L), Rosmarinus officinalis (Rosmarinusofficinalis N), mary bush (Calendula officinalis), the circle red sage root (Salvia officinalis L), genseng (Panaxginseng), ginkgo, St.-John ' s-Wort (Hyperycum Perforatum), Flower of Chinese Peashrub, ruscus aculeatus (Ruscusaculeatus L), Europe silk tree (Filipendula ulmaria L), big-flowered Jarva tea (OrthosiphonStamincus Benth), algae (Fucus Vesiculosus), birch (Betula alba), green tea, laughable beans (ColaNipida), horse-chestnut, bamboo, Herba Centellae (Centella asiatica), Chinese photinia, black wrack, willow, the mouse fringe, the escin extract, Rhizoma Atractylodis extract, camomile extract, Armeniacea genus, AtractylodisPlaticodon, Sinnomenum, the Semen Pharbitidis, the plant milk extract of Root of Philippine Flemingia, the coleus extract, C.Forskohlii for example, C.blumei, C.esquirolii, C.scutellaroides, C.xanthantus and C.Barbatus, the root extract of coleus China pink for example, Ballote, Guioa, Davallia, Barringtonia, the mountain jute, antirobia, cecropia, argania, dioscoreae is Chinese yam or Mexican extract for example, the extract of-marine source: algae or plant plankton extract, for example palmate sea-tangle, diatom, marine alga sterol extract.Obviously all these extracts can mix use.

Composition according to the present invention can also comprise one or more additional activity compositions in addition, be selected from: act on microcirculatory reagent (vasculoprotectors or vasodilator), for example natural flavone compounds, ruscogenin, esculoside, escin, nicotinate, heperidine aminomethyl phenyl vinylbenzene ketone, Flower of Chinese Peashrub, lavender or rosemary ethereal oil, A Mi fennel extract; Anti--saccharifying agent, for example plant milk extract, particularly Fructus Rubi extract (Vacciniumangustifollium), vitamins C and its derivative, retionol and its derivative of Herba Centellae and Siegesbeckia extract, silicon, amadorine, ergothioneine and its derivative, hydroxystilbene and its derivative (for example trans-resveratrol), Cuculidae family.

17. butylated hydroxytoluene (BHT) and butylated hydroxyanisole (BHA)

Main component of the present invention can comprise dibutyl hydroxy toluene (BHT) (BHT) or butylated hydroxyanisole (BHA).

In one embodiment, dibutyl hydroxy toluene (BHT) and/or butylated hydroxyanisole account for composition weight about 0.0001% to about 20%, and more preferably from about 0.001% to about 10%, and also more preferably from about 0.01% to about 5% and be more preferably about 0.1% to about 0.5%.

18. local anesthetic

Composition of the present invention can also comprise the local anesthetic of safety and significant quantity, the example of local anesthetic comprises parathesin, lidocaine, bupivacaine, vovocan, cinchocaine, etidocaine, mepivacaine, dicaine, dyclonine, Hexylcaine, PROCAINE HCL, PHARMA GRADE, Cocaine, ketamine, pramoxine, phenol and their pharmacy acceptable salt.

19. decortication activeconstituents

Composition of the present invention can add the decortication activeconstituents.In one embodiment, described composition comprises and accounts for composition weight about 0.01% to about 10%, preferred about 0.1% to about 5%, more preferably from about 0.5% to about 2% decortication activeconstituents.

A kind of peeling system zwitterionics as used herein that is suitable for is described in U.S. patent No.5, in 652,228.Another kind is suitable for as used herein that peeling system comprises sulfhydryl compound and zwitterionics, is described in U.S. patent No.5, in 681,852.The zwitterionics of describing in these referenced patent can also be at this as decorticating agent, and cetyl betaine is particularly preferred.

20. it is anti--the acne activeconstituents

Composition of the present invention can comprise one or more anti--acne activeconstituentss.Available is anti--and the example of acne activeconstituents comprises Resorcinol, sulphur, erythromycin, Whitfield's ointment, benzoyl peroxide, dehydroacetic acid (DHA) and zinc.The further case description of suitable anti--acne activeconstituents is in U.S. patent No.5, in 607,980.The Ac.net by name that the useful especially SEDERMA of being (WO 03/028692 A2) provides ^TMThe composition of anti--acne composition.

In one embodiment, when anti--when the acne compound is present in the described composition of the present invention, described composition comprises and accounts for composition weight about 0.0001% to about 50%, more preferably from about 0.001% to about 10%, be more preferably about 0.01% to about 8%, be more preferably about 0.1% to about 5% resist-the acne compound.

21. it is anti--the wrinkle activeconstituents/anti--atrophy activeconstituents

Composition of the present invention can comprise one or more anti--wrinkle activeconstituentss or anti--atrophy activeconstituents.Exemplary be suitable for being used in that anti--wrinkle in the present composition/anti--the atrophy activeconstituents comprises the D and the L amino acid of sulfur-bearing, and derivative and salt, especially, for the N-acetyl derivative, preferred examples is N-ethanoyl-L-halfcystine; Mercaptan, for example ethane mercaptan, alcohol acid (as, β-the hydroxy acid of alpha-hydroxy acid of lactic acid and oxyacetic acid and so on or Whitfield's ointment and salicyclic acid derivatives and so on, for example decoyl derivative, lactobionic acid), ketone acid (for example, pyruvic acid), phytic acid, xitix (VITAMIN), toluylene, laurate, trans-resveratrol, phytokinin, zeatin, dimethylaminoethanol, (for example from the peptide of natural source, soybean peptides) and the salt of saccharic acid (for example, manganese gluconate, Zinc Gluconate), Thioctic Acid; Ultrapole L, exfoliating skin agent (for example phenol etc.), vitamins B ₃Compound and retinoid and other kind of vitamins B compound (for example, thiamines (vitamins B ₁), pantothenic acid (vitamins B ₅), riboflavin (vitamins B ₂), with and derivative and salt (for example, HCl salt or calcium salt).The Dermolectine by name that the useful especially SEDERMA of being provides ^TMAnd Sterocare ^TMThe composition (WO 99/18927) of anti-wrinkle agent.

In one embodiment, when anti--wrinkle/anti--when the atrophy compound is present in the described composition of the present invention, described composition comprises and accounts for composition weight about 0.0001% to about 50%, more preferably from about 0.001% to about 10%, be more preferably about 0.01% to about 8% and be more preferably anti--wrinkle/anti--atrophy compound of about 0.1% to about 5%.

22. it is anti--oxygenant/free-radical scavengers

Composition of the present invention can comprise anti--oxygenant/free-radical scavengers.In one embodiment, described composition comprises about 0.01% to about 10%, more preferably from about 0.1% to about 5% resist-oxygenant/free-radical scavengers.

Anti--oxygenant/free-radical scavengers can be xitix (vitamins C) and its salt, the ascorbigen ester of lipid acid, ascorbic acid derivates (for example, magnesium ascorbyl phosphate, STAY-C 50, the ascorbigen sorbic ester), tocopherol (vitamin-E), tocopherol sorbic acid ester, tocopherol acetate, other ester of tocopherol, butylation hydroxy-benzoic acid and its salt, superoxide, comprise hydrogen peroxide, perborate, the thiol acetic ester, persulphate, 6-hydroxyl-2,5,7,8-tetramethyl-benzo dihydropyrane-the 2-carboxylic acid (can be according to trade name On market, bought), gallic acid and its alkyl ester, Tenox PG particularly, uric acid and its salt and alkyl ester, amine (for example, N, N-diethyl oxyamine, amino-guanidine), nordihydroguaiaretic acid, Vitamin P complex, sulfhydryl compound (for example gsh), dihydroxy fumaric acid and its salt, lycine Magnesium Pidolate (lycine pidolate), arginine Magnesium Pidolate (argininepilolate), amino acid, Silymarin, Methionin, the 1-methionine(Met), proline(Pro), superoxide dismutase, Sorbic Acid and its salt, Thioctic Acid, Fructus Canrii Albi extract, tea extract, polyphenol, for example be derived from the proanthocyanidine of Cortex Pini, carotenoid, turmeric rope compound, for example tetrahydrochysene turmeric yellow, OCTA (L-2-oxo-4-Thiazolidinecarboxylacid acid), gsh, melanochrome, applicable rosemary extract and Pericarpium Vitis viniferae/seed extract.Preferred resisting-oxygenant/free-radical scavengers can be selected from the ester of tocopherol, more preferably tocopherol acetate and tocopherol sorbic acid ester (U.S. patent No.4,847,071).

23. wetting agent, moistening agent and amendment

Composition of the present invention can comprise the conditioning agent of safety and significant quantity, for example is selected from wetting agent, moistening agent and skin conditioning agent.This type of raw material of broad variety can be applied, and in one embodiment, it accounts for composition weight about 0.01% to about 20%, and more preferably from about 0.1% to about 10%, is more preferably about 0.5% to about 7%.These raw materials can comprise, be not limited to, guanidine, urea, oxyacetic acid, glycol hydrochlorate (for example glycolic acid ammonium and glycolic acid four alkane ammoniums), Whitfield's ointment, lactic acid, lactic acid salt (for example, DL-Lactic acid ammonium salt and lactic acid four alkane ammoniums), any various forms of aloe (for example, Aloe gel), polyhydroxy-alcohol, Sorbitol Powder for example, mannitol, Xylitol, butantetraol, glycerol, hexanetriol, trihydroxybutane, propylene glycol, butyleneglycol, hexylene glycol or the like, polyoxyethylene glycol, sugar (for example, chinaberry disaccharide), starch, sugar and starch derivative (for example, alkoxylate glucose, fructose, glycosamine), unsulphated glycolsaminoglycan, the lactic amide monoethanolamine, the ethanamide monoethanolamine, panthenol, wallantoin, oil and their mixture.What can also be applied to this is propenoxylated glycerol, is described in U.S. patent No.4, in 976,953.

That can also use is the C of various sugar ₁-C ₃₀Monoesters and polyester and related raw material.These esters stem from sugar or polyvalent alcohol root and one or more carboxylate radicals.

Preferably, amendment is selected from urea, guanidine, sucrose polyester, panthenol, panthenol, wallantoin, glycerol and their composition.

Wetting agent can be selected from: the unionized polymer of polyvalent alcohol, water soluble alkoxylated and their mixture.The polyvalent alcohol that can be applied to this comprises aforesaid polyhydroxy-alcohol and glycerine, hexylene glycol oxyethyl group glucose, 1,2-hexylene glycol, dipropylene glycol, trehalose, two glycerol, maltose alcohol, maltose, glucose, fructose, Sodium chondroitin sulfate A, hyaluronate sodium, adenylic acid sodium, Sodium.alpha.-hydroxypropionate, pyrrolidone carbonic ether, glycosamine, cyclodextrin and their mixture.The water miscible alkoxylate unionized polymer that can be applied to this comprises polyoxyethylene glycol and polypropylene glycol, and its molecular weight is at most about 1000, and for example its CTFA name is called PEG-200, PEG-400, PEG-600, PEG-1000 and their mixture.

24. active oxygen formation inhibitor

Composition of the present invention can also comprise the active oxygen formation inhibitor, be selected from quercetin, rutin, taxifolin, kaempferol, 3,5,7,3 ', 4 ', 5 '-quercetagetin, turmeric rope, trans-resveratrol methylarecaidin, versulin, wogonin, digicitrine, tectorigenin and their mixture.

These active oxygen formation inhibitor content can account for composition weight about 0.001% to about 5, and more preferably from about 0.01% to about 3%.

25. sequestrant

Composition of the present invention can also comprise inner complex or sequestrant.When this uses, " inner complex or sequestrant " expression can be removed the active ingredient agent of metal ion by forming complex compound, metal ion can not be participated in or the formation of Catalytic Oxygen free radical. in one embodiment, composition of the present invention adds sequestrant, preferred its accounts for composition weight about 0.00001% to about 10%, and more preferably from about 0.001% to about 5%.The exemplary sequestrant that can be applied to this is disclosed in U.S. patent No.5, and 487,884, among WO 91/16035 and the WO91/16034.The example of sequestrant comprises N-hydroxy-succinamide, ethylenediamine tetraacetic acid (EDTA), nitrilotriacetic acid, Deferoxamine, hydroxamic acid and their salt, phytic acid, myo-Inositol hexaphosphate, glyconic acid and its salt, shifts ferritin (Transferrine), lactoferrin; Lian Kangxian dioxime and their derivative.

26. anti-inflammatory agent

Anti-inflammatory agent can add composition of the present invention.In one embodiment, the level that adds anti-inflammatory agent is to account for composition weight about 0.01% to about 10%, preferred about 0.5% to about 5%.The anti-inflammatory agent that is used for the anti-inflammatory dosage application-specific of described composition accurately is because this type of reagent is renderd a service the variation range broad.

The steroid anti-inflammatory agent can comprise, is not limited to reflunomide, for example hydrocortisone.In addition, non-steroidal anti-inflammatory agent can be used at this.The compound of various these categories is known to those skilled in the art.The concrete non-steroidal anti-inflammatory agent that can be applied to composition of the present invention includes, but are not limited to woluoke kind, for example piroxicam, salicylate, for example acetylsalicylic acid; Acetogenin, for example felbinac, fragrant that ester class, for example etofenamate, Flufenamic Acid, vialidon, meclofenamic acid; Propanoic derivatives, for example Ibuprofen BP/EP, Naproxen Base, pyrazoles and their mixture.Also can use the mixture of these non-steroidal anti-inflammatory agents, and acceptable salt and ester on the dermatology of these anti-inflammatory agenies.

At last, use alleged " natural " anti-inflammatory agent in the inventive method.This reagent can obtain as extract from natural resource (for example, plant, fungi, microbial product) by proper physical and/or chemical separation method, perhaps can be synthetic.For example, gama wax, Hydagen B are (for example, the α Hydagen B), aloe, plant sterol, (for example, plant sterol), Manjistha (is derived from the Rubia plant, the extract of madder particularly) and Guggal (be derived from the bdellium plant, the extract of myrrh particularly), Soudan coffee extract, camomile, red clover extract, piper methysticum extract (Kava Kava, SEDERMA provide (FR 2 771 002 and WO 99/25369)), Bacopa monieri extract (Bacocalmine ^TM, SEDERMA provides, and WO 99/40897) and the gorgonian extract, these materials can use.The anti-inflammatory agent that can be applied to this comprises wallantoin and Radix Glycyrrhizae compound family (genus/class of liquorice root), comprises carbenoxalone, Potenlini and their derivative (for example, salt and ester).The salt of suitable above-claimed cpd comprises metal and ammonium salt.Suitable ester comprises C ₂-C ₂₄Saturated or the preferred C of unsaturated ester of acid ₁₀-C ₂₄, more preferably C ₁₆-C ₂₄Above-mentioned specific examples comprises oil-soluble Radix Glycyrrhizae extract, Potenlini and carbenoxalone itself, monoammonium glycyrrhizinate, dipotassium glycyrrhizinate, Rizinsan K2 A2,1-β-carbenoxalone, stearyl Radix Glycyrrhizae acid esters and 3-octadecane oxygen base-glycyrrhetinic acid and 3-amber acyloxy-β-disodium glycyrrhizinate.Stearyl Radix Glycyrrhizae acid esters is preferred.The anti-inflammatory agent that adds comprises diosgenol, Saponin/TSM, sapogenin, lignan, triterpenes saponosides compound and glucoside unit (genines).

27. brownization activeconstituents

Composition of the present invention can comprise brownization activeconstituents.In one embodiment, described composition comprises and accounts for composition weight about 0.1% to about 20%, and more preferably from about 2% to about 7%, even more preferably from about 3% to about 6% brownization activeconstituents.Preferred brownization activeconstituents is a Protosol, has another name called dehydroacetic acid (DHA) or 1,3-dihydroxyl-2-acetone.The Tyr-ol by name that the useful especially SEDERMA of being provides ^TMThe composition of brownization agent, be described in Fr 2702766 and WO 03/017966 respectively.

28. antimicrobial, antibiotic and anti-mycotic activity composition

Composition of the present invention can comprise one or more anti--fungies or anti--microbic activity composition.Can add the antimicrobial of safety and significant quantity or anti-mycotic activity composition in the composition of the present invention.In one embodiment, described composition comprises and accounts for composition weight about 0.001% to about 10%, preferred about 0.01% to about 5%, and 0.05% to about 2% antimicrobial or anti-mycotic activity composition more preferably from about.

Suitable anti--microorganism active composition comprises coal tar, sulphur, the whitfield ointment, castellani coating, aluminum chloride, Viola crystallina, octopirox (piroxicam ketoamine), 3,4,4 '-trichlorocarbanilide (trichlosan), neko, Ciclopirox Olamine, undecylenic acid and its metal-salt, potassium permanganate, selenium sulfide, Sulfothiorine, propylene glycol, neroli bigarade oil, Carmol, grisovin, 8-8-hydroxyquinoline ciloquinol, sulfo-dibazol, thiocarbamate, haloprogin, polyene, pyridone ketone, morpholine, moringine, allylamine (for example Terbinafine), tea tree oil, clove leaf oil, coriandrum, rusha grass, barberry sulphur, hundred li red, Oleum Cinnamomi, phenylacrolein, citronellic acid, hinokitol, the sulfonation shale oil, Sensiva SC-50, Elestab HP-100, nonane diacid, lyticase, iodine propiolic alcohol butyl mephenesin Carbamate (IPBC), the Isothiazalinones compounds, for example octyl group isothiazolinone and pyrroles and their composition.Preferred biocide comprises itraconazole, KETOKONAZOL, selenium sulfide and coal tar.In one embodiment, one or more anti--fungies or anti--microbic activity composition combine with the antiscurf activeconstituents that is selected from the 2-Mercaptopyridine-N-oxide polyvalent metal salt.

A. pyrroles

Anti--microorganism pyrroles comprises imidazoles, for example benzoglyoxaline, benzothiazole, bifonazole, Nitric acid butoconazole, diazole butanone, clotrimazole, Croconazole, Eberconazole, chlorobenzene first chlorine imidazoles, elubiol, fenticonazole, fluconazole, flutrimazole, Travogyn, KETOKONAZOL, lanoconazole, Vagimid, miconazole, neticonazole, omoconazole, Oxiconazole Nitrate, Sertaconazole, sulconazole nitrate, tioconazole, thiazole and triazole, for example R-42470 and itraconazole and their mixture.When being present in described composition, antimicrobial pyrroles's active component content accounts for composition weight about 0.01 to about 5%, preferred about 0.1% to about 3%, and more preferably from about 0.3% to about 2%.Preferred especially KETOKONAZOL and diazole butanone.

B. selenium sulfide

The present invention is anti--microorganism anti--dandruff agent selenium sulfide is a particulate, its effective concentration scope is to account for composition weight about 0.1% to about %, preferred about 0.3% arrive about 2.5%, more preferably from about 0.5% to about 1.5%.

C. sulphur

Sulphur also can be used as anti--microorganism/anti--dandruff agent in of the present invention resisting-microbial composite.Typically, the sulfur particle of effective concentration accounts for composition weight about 1% to about 4%, preferred about 2% to about 4%.

D. additional resisting-the microorganism active composition

Additional resisting of the present invention-microorganism active composition can comprise one or more keratolytics, for example Whitfield's ointment, melaleuca (tea tree) extract and gac.The present composition can also comprise Stockholm tar and sulphur composition, Whitfield's ointment and pyrithione Zn composition, octopirox and climbasole composition and Whitfield's ointment and octopirox composition and their mixture.

The activeconstituents preferred embodiment that can be applied to this comprises: benzoyl peroxide, the 3-hydroxy-benzoic acid, oxyacetic acid, lactic acid, the 4-hydroxy-benzoic acid, the 2-hydroxybutyric acid, the 2-hydroxypentanoic acid, the 2-hydroxycaproic acid, phytic acid, Thioctic Acid, nonane diacid, arachidonic acid, benzoyl peroxide, tsiklomitsin, Ibuprofen BP/EP, Naproxen Base, hydrocortisone, Paracetamol, Resorcinol, Phenoxyethanol, phenoxypropanol, the phenoxy group Virahol, 2,4,4 '-three chloro-2 '-dihydroxy diphenyl ether, 3,4,4 '-trichlorocarbanilide, octopirox, cyclopirox, Xylotox, clotrimazole, miconazole, KETOKONAZOL, neomycinsulphate and their mixture.

The OSMOCIDE by name that the useful especially SEDERMA of being provides ^TMThe composition of composition range (WO97/05856).

29. thickening material (comprising thickening material and jelling agent)

Composition of the present invention can comprise one or more thickening materials.In one embodiment, thickening material accounts for composition weight about 0.05% to about 10%, preferred about 0.1% to about 5%, and more preferably from about 0.25% to about 4%.Do not limit the thickening material of classification to comprise following material:

A. carboxylic acid polyalcohol

These polymkeric substance are cross-linking compounds, comprise one or more and derive from vinylformic acid, substitutional crylic acid, and the monomer of the salt of described vinylformic acid and substitutional crylic acid and ester, wherein linking agent comprises two or more carbon-to-carbon double bonds, stems from polyvalent alcohol.Can be used for polymkeric substance of the present invention and be described in U.S. patent No.5 more fully, 087,445, U.S. patent No.4,509,949, U.S. patent No.2 is in 798,053 and the international components of cosmetics dictionary of CTFA the tenth edition, in 2004.

The commercially available carboxylic acid polyalcohol example that can be applied to this comprises carbomer, and it is the allyl ether or the crosslinked homopolymer of tetramethylolmethane of vinylformic acid and sucrose.Carbomer can be used

Series (for example, is provided by B.F.Goodrich

954).Shi Yi carboxylic acid polymer reagent comprises in addition

10 (B.F.Godrich) and C10-30 alkyl acrylate and the acrylic acid multipolymer of one or more monomers, methacrylic acid or their a kind of short chain (that is C, _1-4Alcohol) ester, wherein linking agent is the allyl ether or the tetramethylolmethane of sucrose.Known these multipolymers are acrylate/C ₁₀-C ₃₀Alkyl acrylate cross-linked polymer,

1342,

1382, Pemulen TR-1 and Pemulen TR 2 can buy from B.F.Goodrich on market.In other words, the example that can be applied to this carboxylic acid polymer thickening material is selected from carbomer, acrylate/C ₁₀-C ₃₀Alkyl acrylate crosslinked polymer and their mixture.

B. cross-linked polyacrylate polymer

Composition of the present invention can randomly comprise the cross-linked polyacrylate polymer as thickening material or jelling agent, comprises positively charged ion and non-ionized polymkeric substance, and is cationic normally preferred.Useful crosslinked unionized polyacrylate polymers and cross-linked cationic polyacrylate polymers are described in U.S. patent 5,100,660, U.S. patent No.4,849,484, U.S. patent No.4,835,206, U.S. patent No.4,628,078,4,599,379 and EP 228,868 in.

C. polyacrylamide polymers

Composition of the present invention can randomly comprise polyacrylamide polymers, and especially, the unionized polyacrylamide polymers comprises replacement side chain or unbranched polymkeric substance.Preferably non-ionized polymer among these polyacrylamide polymers is given in polyacrylamide and isoparaffin and laureth-7 that CTFA indicates, can buy from Seppic company according to trade name Sepigel 305.

Other polyacrylamide polymers that can be applied to this comprises the many-block copolymer of acrylamide and substituted acrylamide and vinylformic acid and substitutional crylic acid.The example of these many-block copolymers comprises HypanSR150H, SS500V, and SS500W, SSSA100H is provided by Lipo Chemicals company.

Described composition can also comprise thickening and multiviscosisty gel, and its exemplary type is provided by UnitedGuardian, and is by name

These gels have humidification, multiviscosisty, stability, and the usable concentration scope is between 1 to 99%, and is best between 5 to 15%.

D. polysaccharide

The polysaccharide of broad variety can be applied to this." polysaccharide " refers to comprise the jelling agent of repetition sugar (that is carbohydrate) unit main chain.The unrestricted example of polysaccharide jelling agent comprises cellulose, carboxymethyl hydroxyethyl cellulose, cellulose acetate propionate carbonyl acid ester, Natvosol, hydroxyethyl ethylcellulose, hydroxypropylcellulose, Vltra tears, methyl hydroxyethylcellulose, Microcrystalline Cellulose, Ushercell and their mixture.What can also be applied to this is alkyl-replacement cellulose.In alkyl hydroxy alkyl cellulose ether, the preferred indicated raw material hexadecyl of CTFA Natvosol, it is the ether of hexadecanol and Natvosol.This source commodity title is

CS Plus is provided by Aqualon company.

Other available polysaccharide comprises the sclerosis dextran, and its glucose unit that contains per three (1-3) connection has the straight chain of the glucose of one (1-6) connection, and commercially available example is the Clearogel that Michel MercierProducts Inc. provides ^TMCS 11.

E. colloid

Other thickening material and jelling agent that can be applied to this mainly comprises raw material from natural source.The unrestricted example of these jelling agent colloids comprises gum arabic, agar, algin, Lalgine, the alginic acid ammonium, amylopectin, alginate calcium, calcium carrageenan, carnitine, carrageenin, dextrin, gelatin, gum gellan, guar gum, guar hydroxypropyltrimonium chloride, hectorite, unsulphated glycolsaminoglycan, hydrated silica, the hydroxypropyl chitosan, hydroxypropylguar gum, kuteera gum, bulk kelp glue, Viscogum BE, natto gum, potassium alginate, carrageenin potassium, Protanal Ester SD-LB, hardenite glue, carboxymethyl dextran sodium, carrageenin sodium, tragacanth gum, xanthan gum, with their mixture.

30. hidroschesis activeconstituents

Composition of the present invention can also add the hidroschesis activeconstituents.Suitable hidroschesis activeconstituents comprises the inorganic and organic salt of metallic salt astringent matter, particularly aluminium, zirconium and zinc, and their mixture.Particularly preferably be the raw material or the salt that contain aluminium and/or zirconium, for example aluminum halide, chlorine oxyaluminum, hydroxyhalides, zirconyl oxyhalides, zirconyl hydroxyhalide and their mixture.In one embodiment, when the hidroschesis activeconstituents is present in the described composition of the present invention, described composition comprises and accounts for composition weight about 0.01% to about 50%, and more preferably from about 0.1% to about 40%, is more preferably from about 1% to about 30% hidroschesis compound.

31. detergent surfactants

Composition of the present invention can comprise detergent surfactants, and content is about 1% to about 90%, more preferably from about 5% to about 10%.The detergent surfactants component that is comprised can make described composition have clean-up performance.The detergent surfactants component can comprise the cleansing surfactants of negatively charged ion cleansing surfactants, zwitter-ion or both sexes electric charge or their composition successively.The suitable negatively charged ion cleansing surfactants component that is applied in the described composition comprises the well-known cleansing that is used in hair nursing or other personal care.In the time of in being included in composition, the anion surfactant component concentrations can preferably can enough provide the scope of cleaning and lathering property, is generally about 5% to about 50%, preferred about 8% to about 30%, more preferably from about % is to about 25%, and also more preferably from about 12% to about 22%.

Preferably being suitable for using the anion surfactant in described composition is alkyl and alkyl ether sulphate.Other suitable negatively charged ion cleansing surfactants is an organism, the fatty acid amide sodium of the water-soluble salt of sulfuric acid reaction product, alkanoyloxy isethionic acid ester, methyl tauride or sylvite, olefin sulfonate, β-alkoxyalkyl sulphonate.

The negatively charged ion cleansing surfactants that is preferred for described composition comprises myrceane ammonium sulfate; AESA; myrceane sulfuric acid triethylamine; fatty alcohol-polyoxyethylene ether sulfuric acid triethylamine; trolamine sulfuric acid ten diester; fatty alcohol-polyoxyethylene ether sulfuric acid trolamine; myrceane sulfuric acid monoethanolamine; fatty alcohol-polyoxyethylene ether sulfuric acid monoethanolamine; myrceane sulfuric acid diethanolamine; fatty alcohol-polyoxyethylene ether sulfuric acid diethanolamine; monoglyceride sulfuric acid Laurus nobilis resin acid; sodium lauryl sulphate; polyoxyethylenated alcohol sodium sulfate; the myrceane vitriolate of tartar; the fatty alcohol-polyoxyethylene ether vitriolate of tartar; sodium lauryl sarcosinate; sodium lauroyl sareosine; the lauryl sarkosine; cocounut oil fatty acyl group sarkosine; cocounut oil fatty acyl group ammonium sulfate; lauroyl ammonium sulfate; cocounut oil fatty acyl group sodium sulfate; lauroyl sodium sulfate; cocounut oil fatty acyl group vitriolate of tartar; the myrceane vitriolate of tartar; trolamine sulfuric acid ten diester; trolamine sulfuric acid ten diester; cocounut oil fatty acyl group sulfuric acid monoethanolamine; myrceane sulfuric acid monoethanolamine; the tridecyl benzene sulfonic acid sodium salt; Sodium dodecylbenzene sulfonate; cocounut oil fatty acyl group sodium isethionate and their composition.

Suitable be applied to described composition contain positive and negative charge or zwitterionic cleansing surfactants comprises the well-known product that is used for hair nursing or other personal cleanliness nursing.This cleansing surfactants concentration range preferably about 0.5% of positive and negative charge that contains is to about 20%, preferred about 1% to about 10%.The suitable zwitter-ion or the unrestricted case description of amphoterics are in U.S. patent Nos.5,104,646; 5,106,609.

The ampholytic detergent tensio-active agent comprises fatty primary secondary amine and fat tertiary amine.

Composition of the present invention can further comprise the additional surfactants of using with above-mentioned negatively charged ion cleansing surfactants combination of components.Suitable option list surface-active agent comprises non-ionized and cats product.Any known this type of tensio-active agent that is used for hair or personal care product all can use, as long as described optional additional surfactants chemistry and physically with the main component of described composition contradiction not, or exceedingly do not weaken product performance, aesthetic feeling or stability.The concentration of optional additional surfactants can be changed according to other component and other requirements of the prior art that exist in the described tensio-active agent of cleaning or lathering property, selection, product concentration, the described composition in the described composition.

Other is suitable for being used in unrestricted case description anionic, zwitterionic, that contain positive and negative charge or optional additional surfactant in the described composition in emulsifying agent and the washing agent of McCutcheon, in 1989 annuals, publish by M.C. publishing company, with U.S. patent Nos.3,929,678,2,658,072; 2,438,091; In 2,528,378.

32. cationic, anionic and amphiphilic polymers

Composition of the present invention can comprise polymkeric substance, its can be homopolymer, multipolymer, terpolymer, or the like.For for the purpose of the convenient description of polymkeric substance, the monomeric unit that is present in the polymkeric substance can be called monomer, and they can be by monomer derived.Described monomer can be an ionic (for example, anionic, cationic, amphoteric, zwitterionic) or non-ionic.

When described composition comprised cationic polymers, its representational concentration range was about 0.05% to about 3%, and preferred about 0.075% to about 2.0%, more preferably from about 0.1% to about 1.0.

A. cationic polymers

The cationic polymers that is suitable for the present composition comprises the part that contains cationic nitrogen, for example quaternary ammonium or cationic protonated amino part.Any anionic counter-ion all can be united use with cationic polymers, as long as described polymkeric substance can keep in the condensed phase of water-soluble, described composition or described composition, and described counterion should be at physics and chemically do not contradict with the main component of described composition, perhaps is unlikely to undue weakening product performance, stability or aesthetic feeling.The unrestricted example of this counterion comprises halogenide (for example, muriate, fluorochemical, bromide, iodide), vitriol and Methylsulfate.The unrestricted case description of described polymkeric substance is in CTFA.

The unrestricted example of suitable cationic polymers comprises the vinyl monomer multipolymer, it has cationic protonated amines or quaternary ammonium functional group, with water miscible spacer monomer, for example acrylamide, Methacrylamide, alkyl and dialkyl group acrylamide, alkyl and dialkyl methyl acrylamide, alkyl acrylate, alkyl methacrylate, vinyl caprolactone or vinyl pyrrolidone.

The example of cationic monomer comprises the monomer that derives from acrylic or methacrylic acid, the epihalohydrin product of quaternized trialkylamine, the alkyl of described trialkylamine has 1 to 5 carbon atom, for example (methyl) propenyloxy group propyl group TMA (TriMethylAmine) muriate and (methyl) propenyloxy group propyl group TMA (TriMethylAmine) bromide; Derive from the methacrylic acid sulfonamide derivatives or the Methacrylamide sulfonamide derivatives of methacrylic acid or Methacrylamide and have C ₁-C ₆The dialkyl group alkanolamine of alkyl, for example dimethyl aminoethyl (methyl) acrylate, diethyllaminoethyl (methyl) acrylate, dimethylaminopropyl (methyl) acrylate or dimethylaminopropyl (methyl) acrylamide.

The protonated amino of positively charged ion and the quaternary ammonium monomer that are suitable in the cationic polymers of described composition comprise, vinyl compound with following material replacement: dialkyl aminoalkyl acrylate, the dialkyl aminoalkyl methacrylic ester, the alkyl monosubstituted amino alkyl acrylate, the alkyl monosubstituted amino alkylmethacrylate, trialkyl methacrylic acid alkoxyl group ammonium salt, trialkyl vinylformic acid alcoxyl base ammonium salt, the hexadiene quaternary ammonium salt, with have the ring-type cationic and contain the ethene quaternary ammonium monomer of azo-cycle, pyridinium salt for example, imidazole salts, with quaternized pyrrolidone, for example, alkyl vinyl imidazole salts, alkylvinylpyridines salt, alkyl vinyl pyrrolidone salt.

Other cationic polymers that is suitable for described composition comprises l-vinyl-2-pyrrolidone and the 1-vinyl-the 3-methylimidazole salt (for example, hydrochloride) multipolymer is (referring to makeup, toiletry and fragrance association industrial standards, " CTFA ", Onamer M 6); The multipolymer of l-vinyl-2-pyrrolidone and dimethylaminoethyl methacrylate (referring to CTFA industrial standards Onamer M 1); The polymkeric substance of cation hexadiene quaternary ammonium comprises, for example, and the multipolymer of dimethyldiallylammonium hydrochloride homopolymer, acrylamide and dimethyldiallylammonium hydrochloride (respectively referring to CTFA industry, polyquaternary amine 6 and polyquaternary amine 7); The vinylformic acid ampholyte copolymer comprises that the multipolymer of vinylformic acid and dimethyldiallylammonium hydrochloride is (referring to the CTFA industrial standards, polyquaternary amine 22), the terpolymer (referring to CTFA industrial standards polyquaternary amine 47) of the terpolymer of vinylformic acid and dimethyldiallylammonium hydrochloride and acrylamide (referring to CTFA industrial standards polyquaternary amine 39) and vinylformic acid and methylpropenyl oxypropyl trimethyl hydrochloride and methacrylate.The preferred cation substituted monomer is dialkyl aminoalkyl acrylamide, the dialkyl aminoalkyl Methacrylamide that positively charged ion replaces.With their composition.Unrestricted example is polymethyl base aminopropyl three ammonium salt hydrochlorates, can buy from Rhone-Poulenc according to trade(brand)name Polycare 133.

Other cationic polymers that is suitable for described composition comprises polysaccharide polymer, for example cationic derivatived cellulose and cationic starch derivative.

The preferred cation cellulose polymer compound is the salt of Natvosol and the reaction of trimethyl ammonium substituted epoxide, referring to industrial standards (CTFA), polyquaternary amine 10, it can (Edison, N.J. USA) have bought from Amerchol company, Polymer LR, JR and KG series polymer by name.Other suitable cationic cellulose type comprises the epoxide reactive polymer quaternary ammonium salt that Natvosol and lauryl dimethyl ammonium replace, referring to industrial standards (CTFA), polyquaternary amine 24.These raw materials can obtain from Amerchol company, and trade name is Polymer LM-200.

Other suitable cationic polymers comprises positively charged ion guar gum derivative, guar gum Hydroxyproyl Trimethyl ammonium salt hydrochlorate for example, its specific examples comprise the N-Hance series that Jaguar series that Rhone-Poulenc company provides and Aqualon Division of Hercules company provide.Other suitable cationic polymers comprises the ether of cellulose that contains four nitrogen, and some case descriptions are in U.S. patent No.3, in 962,418.Other suitable cationic polymers comprises the multipolymer of etherified cellulose, and guar gum and starch, some case descriptions is in U.S. patent No.3, in 958,581.When this uses cationic polymers, this cationoid polymerisation dissolves in described composition, perhaps also dissolves in by the complex coacervation in cationic polymers and the negatively charged ion of mentioning before this, amphoteric and/or the formed composition of zwitterionic cleansing surfactants component mutually.The complex coacervate of cationic polymers can also be formed in the described composition with other electrically charged raw material.

B. anionic polymer

The example of anionic polymer is the multipolymer of vinyl acetate and Ba Dousuan, and the multipolymer of vinyl acetate, Ba Dousuan and α-these three kinds of materials of side chain saturated fatty monocarboxylic acid vinyl acetate, described α-side chain saturated fatty monocarboxylic acid vinyl acetate for example is a vinyl neodecanoate; With the multipolymer of vinyl methylether and maleic anhydride, comprise the acrylic copolymer and the terpolymer of acrylic or methacrylic acid.The example of anionic monomer comprises unsaturated carboxylic acid monomer, for example vinylformic acid, methacrylic acid, toxilic acid, toxilic acid half ester, methylene-succinic acid, fumaric acid and Ba Dousuan; The half ester of unsaturated multi-anhydride, for example acrylate and/or the methacrylic ester of succinyl oxide, phthalic anhydride etc. and hydroxyl, hydroxy ethyl methacrylate for example, hydroxyethyl methylacrylate, hydroxypropyl acrylate etc.; Has sulfonic monomer, for example styrene sulfonic acid, thio-ethyl acrylate and methacrylic ester or the like; With monomer with phosphate, for example acid phosphorus oxygen ethyl propylene acid esters and methacrylic ester, 3-chloro-2-acid phosphorus oxygen propyl group acrylate and methacrylic ester or the like.

C. ampholytic monomer

The example of ampholytic monomer comprises the bisexual ion purification derivative of aforementioned sulfonamide derivatives, i.e. the sulfonamide derivatives of (methyl) vinylformic acid or (methyl) acrylamide, for example dimethyl aminoethyl (methyl) acrylate; Dimethylaminopropyl (methyl) acrylamide, it is by halogenated aliphatic acid salt, as the amino methyl propylate of Monochloro Acetic Acid potassium, monobromo Sodium Propionate, Monochloro Acetic Acid, triethanolamine salt of monochloroacetic acid or the like; The sulfonamide derivatives of (methyl) vinylformic acid or (methyl) acrylamide as mentioned above, forms with the modification of third sultone.

33. non-ionized polymkeric substance

Described composition can comprise non-ionic polymers.For example, have molecular weight and surpass about 1000 polyglycol.Preferred polyethylene glycol polymer comprises that PEG-2M (has another name called Polyox

N-10 can obtain from UnionCarbide, i.e. PEG-2,000); PEG-5M (has another name called Polyox

N-35 and Polyox

N-80 can obtain from Union Carbide, i.e. PEG-5,000 and Polyethylene Glycol300,000); (a has another name called Polyox to PEG-7M

N-750 can obtain from Union Carbide); PEG-9M (has another name called Polyox

N-3333 can obtain from Union Carbide); And PEG-14M (has another name called Polyox

N-3000 can obtain from Union Carbide).

The example of non-ionic monomer is C ₁-C ₂₄The acrylate or methacrylate ester of alcohol, described alcohol for example is methyl alcohol, ethanol, the 1-propyl alcohol, the 2-propyl alcohol, the 1-butanols, 2-methyl isophthalic acid-propyl alcohol, the 1-amylalcohol, the 2-amylalcohol, the 3-amylalcohol, 2-methyl-1-butene alcohol, 1-methyl isophthalic acid-butanols, 3-methyl isophthalic acid-butanols, 1-methyl-1-pentene alcohol, 2-methyl-1-pentene alcohol, 3-methyl-1-pentene alcohol, uncle-butanols, hexalin, 2-ethyl-1-butanols, the 3-enanthol, phenylcarbinol, sec-n-octyl alcohol, 6-methyl isophthalic acid-enanthol, 2-ethyl-1-hexanol, 3,5-dimethyl-1-hexanol, 3,5,5-trimethylammonium-1-hexanol, the 1-decanone, the 1-dodecanol, the 1-hexadecanol, the 1-octadecanol, be vinylbenzene, chloro-styrene, vinyl ester, vinyl acetate for example, vinylchlorid, vinylidene chloride, vinyl cyanide, alpha-methyl styrene, tert-butyl vinylbenzene, divinyl, cyclohexadiene, ethene, propylene, Vinyl toluene, alkoxyalkyl (methyl) acrylate, methoxy ethyl (methyl) acrylate, butoxyethyl group (methyl) acrylate, allyl acrylate, allyl methacrylate(AMA), the cyclohexyl acrylate, and methacrylic ester, oleyl acrylate and methacrylic ester, benzyl acrylate and methacrylic ester, tetrahydrofurfuryl acrylate and methacrylic ester, ethylene glycol bis-acrylate and-methacrylic ester, 1,3 butylene glycol is two-acrylate and-methacrylic ester, diacetone acrylamide, isobornyl (methyl) acrylate, the n-butyl methacrylate, methylacrylic acid isobutyl fat, 2-ethylhexyl methacrylic ester, methyl methacrylate, the tert-butyl acrylate, the tert-butyl methacrylic ester, with their mixture.

34. hair conditioner

Amendment comprises any material that is used to improve the collenchyme special status.For example, hair treatment composition, suitable amendment comprise that one or more help that light, softness, cardability, static resistance, control are wet, damage, easily processing, body and oily preparation.The amendment useful to composition of the present invention can comprise water-insoluble, water dispersible, non--volatile liquid, forms the emulsifying aq particulate.The amendment that is suitable for described composition comprise have the silicone resin characteristic usually amendment (for example, silicone oil, positively charged ion silicone resin, silicone gum, high refractive index silicone resin and silicone resin), organic conditioning oil (for example, hydrocarbon ils, polyolefine and fatty ester) or their composition, or in aqueous tenside matrix, form the amendment of liquid, dispersed particle in addition.

When described composition comprised amendment, its concentration in described composition was advisable so that required conditioning effect enough to be provided, and this those of ordinary skill for this field is conspicuous.Described concentration can be according to the type of the mean particle size of amendment, conditioning performance demand, amendment particulate, other component and concentration, and other similar factors and being changed.

A. silicone resin

The silicone resin amendment of the preferred indissoluble of amendment of composition of the present invention.Described silicone resin amendment particulate can comprise volatile silicone, non-volatility silicone resin or their composition.The amendment of preferred non-volatility silicone resin.If there is volatile silicone, it also uses solvent or carrier, silicone gum and the resin of commercially available various non-volatile silicone material components usually.Silicone resin amendment particulate can comprise the silicone oil amendment, can also comprise other composition, for example improves the silicone resin of silicone oil sedimentation effect or raising hair gloss degree.

The concentration range of typical silicone resin amendment is about 0.01% to about 10%, preferred about 0.1% to about 8%, and more preferably from about 0.1% to about 5%, more preferably from about 0.2% to about 3%.The unrestricted example of suitable silicone resin amendment and the optional suspension agent that is used for silicone resin are described in U.S. reissue patent No.34, and 584, U.S. patent No.5 is in 104,646 and U.S. patent No.5,106,609.

The silicone resin background material comprises the part of discussing silicone oil, colloid and resin, and the silicone resin manufacturing is found in Polymer Science and Engineering encyclopedia, vol.15,2d ed, pp 204-308, John Wiley ﹠amp; Sons, Inc. (1989).

B. silicone oil

Silicon liquid comprises silicone oil, is the flowing agent silicone material, and when 25 ℃ were measured, its viscosity was lower than 1,000, and 000csk, preferably about 5csk be to about 1,000,000csk, more preferably from about 100csk arrive about 600,000csk.The silicone oil that is suitable for the present composition comprises poly-alkylsiloxane, poly-aryl siloxanes, polyoxyethylene alkyl aryl radical siloxane, polyether siloxane copolymer and their mixture.Other indissoluble, non-volatile silicone oil with hair nursing performance also can use.

C. amino and cationic silicone resin

The cationic silicone oil that is suitable for being used in the present composition includes, but are not limited to be called as the polymer of " trimethyl silyl ammonia dimethyl silicone oil ".

Other silicone resin cationic polymers that can be used for the present composition can be UCARE siliconeALE

, can obtain from Union Carbide.

D. silicone gum

What other was suitable for using in composition of the present invention is insoluble silicon rubber.These colloids are silicone materials, and when measuring down for 25 ℃, it has more than or equal to 1,000, the viscosity of 000csk.Silicon rubber is described in U.S. patent No.4,152,416; Noll and Walter, Chemistry and Technologyof Silicones, New York:Academic Press (1968); In the silicone rubber products data sheet SE of General Electric 30, SE 33, SE 54 and SE 76.The concrete unrestricted example that is used for the silicon rubber of the present composition comprises dimethione, (dimethione) (ethylene methacrylic radical siloxane) multipolymer, poly-(dimethyl siloxane) (diphenyl siloxane) (ethylene methacrylic radical siloxane) multipolymer and their mixture.

E. high refractive index silicone resin

Other non-volatile indissoluble silicone oil amendment that is suitable for being used in the present composition is the material that is called as " high refractive index silicone resin ", and it is about 1.46 that its specific refractory power is at least, preferably at least about 1.48, more preferably at least about 1.52, more preferably at least about 1.55.It is about 1.70 that the specific refractory power of polyorganosiloxane fluid is usually less than, and typically is lower than about 1.60.Herein, polysiloxane " liquid " comprises oil and colloid.

When the high refractive index silicone resin is used for composition of the present invention, it is preferred in the solution, use with dispersion agent, for example silicone resin or tensio-active agent, by its dispersed surface tension that reduces of abundant raising, thereby raising is through the glossiness (after the drying) of the hair of described compositions-treated.

The silicone oil that is suitable for being used in the present composition is disclosed in U.S. patent .No.2, and 826,551, U.S. patent .No.3,964,500, U.S. patent .No.4,364,837, English Patent .No.849,433 and Silicon Compounds, Petrarch Systems is among the Inc. (1984).

F. silicone resin

Silicone resin can add in the silicone resin amendment of the present composition.These resins are high crosslinking polymerization siloxanes systems.Described crosslinked be during making silicone resin, by trifunctional and silicane of four functional groups and simple function group or bifunctional, or both silane combinations of having concurrently and producing.

35. organic conditioning oil

Composition of the present invention also can comprise organic conditioning oil.In one embodiment, about 0.05% to about 20%, preferred about 0.08% to about 1.5%, and more preferably from about at least a organic conditioning oil of 0.1% to about 1% is added in the amendment, its can be independent or also can with other amendment for example silicone resin (described here) combine.

A. hydrocarbon ils

The organic conditioning oil that is suitable for being used as in the composition of the present invention amendment comprises, but be not limited to, have the hydrocarbon ils at least about 10 carbon atoms, for example cyclic hydrocarbon, straight chain aliphatic hydrocarbon (saturated or unsaturated) and branched chain aliphatic hydrocarbons about are saturated or unsaturated), comprise their polymkeric substance and mixture.The straight chain hydrocarbon ils preferably comes from about C12 to about C19.The side chain hydrocarbon ils comprises hydrocarbon polymer, typically contains to surpass 19 carbon atoms.

The concrete unrestricted example of these hydrocarbon ils comprises: paraffin oil, mineral oil, saturated and undersaturated dodecane, saturated and undersaturated tridecane, saturated and the undersaturated tetradecane, saturated and undersaturated pentadecane, saturated and undersaturated n-Hexadecane, polybutene, poly decene, with their mixture, the branched chain isomer of these compounds, and more the hydrocarbon of long-chain also can use, and the example comprises multiple-limb, saturated or unsaturated alkane, for example full methyl-replacement isomer, for example, full methyl-replacement the isomer of n-Hexadecane and eicosane, for example 2,2,4,4,6,6,8,8-dimethyl-10-methyl undecane and 2,2,4,4,6,6-dimethyl-8-methylnonane can obtain from permethyl company, hydrocarbon polymer, for example polybutene and poly decene.Preferred hydrocarbon polymer is a polybutene, for example the multipolymer of iso-butylene and butylene.These types are the L-14 polybutene that AmocoChemical company provides at commercially available material.

B. polyolefine

The organic conditioning oil that is used for the present composition can also comprise liquid polyolefin, more preferably liquid poly-alpha-olefin, more preferably hydrogenant liquid poly-alpha-olefin.Polyolefine passes through C as used herein ₄To about C ₁₄The alkene monomer polymerization and prepare preferably about C ₆To about C ₁₂

The unrestricted example that preferably is used to prepare the alkene monomer of polyolefin liquid comprises ethene, propylene, 1-butylene, 1-amylene, 1-hexene to 1-hexadecene, 1-octene, 1-decene, 1-laurylene, 1-tetradecylene, branched chain isomer, for example 4-methyl-1-pentene and their mixture.The refinery's raw material or the effluent that comprise alkene also are suitable for preparing described polyolefin liquid.

C. fatty ester

Other organic conditioning oil that suits to be used as amendment in composition of the present invention includes, but are not limited to, and has the fatty ester of at least 10 carbon atoms.These fatty esters comprise having the ester that derives from lipid acid or alcohol (for example monoesters, polyol ester and two-, tri-carboxylic acids ester) hydrocarbyl chain.The described hydrocarbyl group of fatty ester can other compatible functional group of covalency keyed jointing, for example acid amides and alkoxyl group root (for example, oxyethyl group or ehter bond, or the like).

Preferred fatty ester specific examples includes, but are not limited to: Unimac 5680 isopropyl ester, lauric acid hexyl ester, lauric acid dissident's ester, palmitinic acid dissident ester, Wickenol 111, decyl oleate, Isodecyl oleate, cetyl stearic, stearic acid ester in the last of the ten Heavenly stems, Unimac 5680 isopropyl ester, hexanodioic acid dihexyl ester in the last of the ten Heavenly stems, Lauryl lactate, Tetradecyl lactate, cetyl lactate, stearic acid oil alkene ester, oleic oil alkene ester, TETRADECONIC ACID oil alkene ester, acetic acid lauryl, propionic acid n-Hexadecane ester and hexanodioic acid oil alkene ester.

Other fatty ester that is suitable for being used in the present composition is the monocarboxylate of general formula R ' COOR, and wherein R ' and R are alkyl or alkenyl, and the total number of carbon atoms among R ' and the R is 10 at least, preferably at least 22.

Other fatty ester that is suitable for being used in the present composition be carboxylic acid two-, three-alkyl and alkenyl ester, for example C ₄To C ₈The ester of dicarboxylic acid (C for example ₁To C ₂₂Ester, preferred C ₁To C ₆Succsinic acid, pentanedioic acid and hexanodioic acid).Concrete carboxylic acid two-, the unrestricted example of three-alkyl and alkenyl ester comprises stearic iso-16 alkyl esters, the two isopropyl esters of hexanodioic acid, citric acid three-octadecane ester.

Other fatty ester that is suitable for being used in the present composition is called as polyol ester.This polyol ester comprises the alkylene glycol ester, glycol monomethyl for example, two-fatty acid ester, diglycol monotertiary-, two-fatty acid ester, polyethyleneglycol-, two-fatty acid ester, the propylene glycol list-, two-fatty acid ester, the polypropylene glycol monooleate, polypropylene glycol 2000 monostearates, the oxyethyl group propylene glycolmonostearate, the glyceryl list-, two-fatty acid ester, polyglycerol gathers-fatty acid ester, the oxyethyl group glyceryl monostearate, 1,3-butyleneglycol monostearate, the 1,3 butylene glycol SUNSOFT Q-182S, the polyoxyethylene polyhydric alcohol fatty acid ester, sorbitan-fatty acid ester, with the polyoxyethylene sorbitan-fatty acid ester.

Other fatty ester that is suitable for being used in the present composition is a glyceryl ester, includes but not limited to, single-, two and Three-glycerol ester, preferred two-, Three-glycerol ester, more preferably triglyceride level.Application in described composition is described in this, preferred glycerol of glyceryl ester and long-chain carboxylic acid's list-, two-and three-ester, for example C ₁₀To C ₂₂Carboxylic acid.This type of material can obtain from plant and animal fat and oil, for example Viscotrol C, Thistle oil, oleum gossypii seminis, Semen Maydis oil, sweet oil, haddock liver oil, Prunus amygdalus oil, Lipoval A, plam oil, sesame oil, lanolin and soya-bean oil.Synthetic oil includes, but are not limited to, triolein and glycerine three hard ester acid dilaurates.

Other fatty ester that is suitable for being used in the present composition is water-insoluble synthetic fat ester.

The concrete unrestricted example of the suitable synthetic fat ester that is used for the present composition comprises: P-43 (C ₈-C ₁₀Trimethylolpropane triester), MCP-684 (3,3-di-alcohol-1, four esters of 5-pentanediol), MCP 121 (C ₈-G ₁₀Di adipate), all can obtain from Mobil Chemical company.

36. antiscurf activeconstituents

Composition of the present invention also can comprise the antiscurf agent.The unrestricted example of suitable antiscurf particulate comprises: pyrimidine thioketone salt, pyrroles, selenium sulfide, sulfur particle and their mixture.Preferred pyrimidine thioketone salt, particularly 1-hydroxyl-2-pyrimidine thioketone salt.Typical pyrimidine thioketone antiscurf particulate loading scope for account for described composition weight about 0.1% arrive to about 4%, preferred about 0.1% about 3%, more preferably from about 0.3% to about 2%.Preferred pyrimidine thioketone salt is formed by following heavy metal element, for example zinc, tin, cadmium, magnesium, aluminium and zirconium, preferably zinc, the more preferably zinc salt of 1-hydroxyl-2-pyrimidine thioketone (being called as " pyrimidine thioketone zinc " or " ZPT ").The agent of pyrimidine thioketone antiscurf is described in, for example, and U.S. patent .2,809,971; U.S. patent .No.3,236,733; U.S. patent .No.3,753,196; U.S. patent .No.3,761,418; U.S. patent .No.4,345,080; U.S. patent .No.4,323,683; U.S. patent .No.4,379,753; With U.S. patent .No.4, in 470,982.

37. wetting agent

Composition of the present invention can comprise wetting agent.Wetting agent can be selected from polyvalent alcohol, water soluble alkoxylated non-ionic polymers and their mixture.When using wetting agent, preferred content is about 0.1% to about 20%, more preferably from about 0.5% to about 5%.

Can comprise glycerine, Sorbitol Powder, propylene glycol, butyleneglycol, hexylene glycol, oxyethyl group glucose, 1 at the polyvalent alcohol of this application, 2-hexylene glycol, hexanetriol, dipropylene glycol, butantetraol, trehalose, two glycerol, Xylitol, maltose alcohol, maltose, glucose, fructose, Sodium chondroitin sulfate A, hyaluronate sodium, adenosine phosphate sodium, Sodium.alpha.-hydroxypropionate, carbonic acid pyrrolidone, glycosamine, cyclodextrin and their mixture.

The water soluble alkoxylated non-ionic polymers that can be applied to this comprises polyoxyethylene glycol and polypropylene glycol, and its molecular weight is at most about 1000, for example has the material of CTFA title PEG-200, PEG-400, PEG-600, PEG-1000 and their mixture.

38. suspension agent

Composition of the present invention can further comprise suspension agent, with its concentration the water-insoluble material is present in the described composition with discrete form and is advisable.Described concentration range is preferably about 0.1% to about 10%, and more preferably from about 0.3% to about 5.0%.The suspension agent that can be applied to this comprises anionic polymer and non-ionic polymers.Can be in this application be vinyl polymer, for example the CTFA name is called the crosslinked acrylic acid polymer of Carbomer, derivatived cellulose and modified-cellulose polymkeric substance, methylcellulose gum for example, ethyl cellulose, nitrocellulose, Xylo-Mucine, crystalline cellulose, cellulose powder, polyvinylpyrrolidone, polyvinyl alcohol, guar gum, hydroxypropylguar gum, Sudan Gum-arabic, Polygalactan, tragon, pectin, agar, smoke tree (Cydonia oblonga Cydonia oblonga Mill) of closing the eyes, starch (rice, Zea mays, potato, wheat), algae colloid (Algae Extract), the microniological proudcts polymkeric substance, dextran for example, the succsinic acid dextran, pulleran, starch-based polymer, carboxymethyl starch for example, the methyl hydroxypropylated starch, the Lalgine based polyalcohol, sodium alginate for example, propylene glycol alginate, acrylic ester polymer, sodium polyacrylate for example, poly-ethyl propylene acid esters, polyacrylamide, polymine, with inorganic water-soluble material, for example wilkinite, neusilin, LAPONITE, hectonite, and anhydrous silicic acid.Aforesaid activeconstituents such as thickening material also can be used as suspension agent.

The commercially available viscosity modifier that can be applied to this comprises carbomer, trade name is a carboxyvinyl polymer 934, carboxyvinyl polymer 940, carboxyvinyl polymer 950, carboxyvinyl polymer 980, with carboxyvinyl polymer 981, it all can obtain from B.F.Goodrich company, the trade name of acrylate/steareth-20 alkylmethacrylate polymer is ACRYSOL 22, it can obtain from Rohm and Hass, trade name is the nonoxynyl Natvosol of AMERCELL POLYMERHM-1500, it can obtain from Amerchol, trade name is the methylcellulose gum of BENECEL, trade name is the natrosol of NATROSOL, trade name is the hydroxy propyl cellulose of KLUCEL, trade name provides by Hercules for the hexadecyl Natvosol of POLYSURF 67, and trade name is CARBOWAX PEGs, POLYOX WASRs, provide by Amerchol with oxyethane and/or the propylene oxide based polyalcohol of UCON.

Other optional suspension agent comprises the xln suspension agent, and it is categorized as acyl derivative, long-chain amine oxide compound, long acyl derivative and their mixture.Suspension agent is described in U.S. patent No.4, in 741,855.Preferred suspension agent comprises the glycol ester of lipid acid, the triacontanol amine compound of lipid acid, the long-chain ester (for example, stearyl stearate, cetyl palmitate or the like) of longer chain fatty acid; The long-chain ester of long chain alkanol amine (for example, distearyl acid diethanolamine stearylamide, stearic acid Monoethanolamine MEA BASF stearylamide); And glyceryl ester (for example, distearin, trihydroxy-stearin, methyl behenate), its coml example is that Rheox company provides

Other suitable suspension agent comprises the primary amine with fatty alkyl root, described fatty alkyl root 16 carbon atoms of having an appointment at least, the example comprises palm acid amide or Stearyl Amine, with have two secondary amine that respectively have at least about the fatty alkyl root of 12 carbon atoms, the example comprises two palmitic amides or two (hydrogenated fat) amine.Other suitable suspension agent also comprises two (hydrogenated fat) phthalandione amine and crosslinked maleic anhydride-vinyl methylether multipolymer.

39. terpenol

Composition of the present invention can comprise the composition of terpenol or terpenol.When this used, " terpenol " referred to that two or more have the 5-carbon isoprene unit [CH of terminal hydroxyl ₂=C (CH ₃)-CH=CH ₂] the synthetic organic compound.Preferably, described composition can comprise and accounts for composition weight about 0.001% to about 50%, preferred about 0.01% to about 20%, more preferably from about 0.1% to about 15%, also more preferably from about 0.1% to about 10, be more preferably about 0.5% to about 5% and be more preferably about 1% to about 5% terpenol.

Can comprise isomer, Geraniol, the Geraniol derivative of farnesol, farnesol derivative, farnesol, isomer, Phytantriol, Phytantriol derivative, the isomer of Phytantriol and their mixture of Geraniol at the example of the terpenol of this application.The terpenol that preferably can be applicable to this is a farnesol.

A. farnesol and its derivative

Farnesol is a natural occuring article matter, it has been generally acknowledged that it is precursor and/or intermediate in the process of biosynthesizing squalene and sterol, particularly cholesterol.Farnesol also participates in protein modification and adjusting (for example, proteic method Buddhist nunization), has nuclear receptor that farnesol is produced and replys.

Chemically, farnesol is [2E, 6E]-3,7,11-trimethylammonium-2,6, and 10-12 carbon triolefin-1-alcohol, when this used, " farnesol " comprised its isomer and tautomer.Farnesol can have been bought on market, for example, and the product of farnesol (isomer mixture, Dragoco provides) by name and trans-trans-farnesol (Sigma chemical company).Suitable farnesol derivative is a method of acetic acid Buddhist nun ester, can buy from Aldrich chemical company.

B. Geraniol and its derivative

Geraniol is a common name, and its chemical name is 3,7-dimethyl-2,6-octadiene-1-alcohol.When this used, " Geraniol " comprised its isomer and tautomer.Geraniol can have been bought from AldrichChemical company.Suitable Geraniol derivative comprises meraneine, Geraniol geraniol ester, geranyl pyrophosphate and pyrophosphate salt geranyl geraniol ester, and it all can have been bought from Sigma chemical company.For example, Geraniol can be used as regulation agent, wound treatment agent, the anti-liparitosis agent of hyperpigmentation after arachnoid pipe/erythema regulation agent, black eye/edema eye regulation agent, sallow colour of skin regulation agent, sagging regulation agent, the anti-agent of itching, skin stiffeners, pore reduction agent, oil/light reduction agent, the inflammation and comprises wrinkle and the skin texture of fine rule is regulated.

C. Phytantriol and its derivative

Phytantriol is a common name, and its chemistry is called 3,7,11,15-tetramethyl-n-Hexadecane-1,2,3 ,-triol.Phytantriol can have been bought from BASF on market.For example, Phytantriol can be used as regulation agent, wound treatment agent, the anti-liparitosis agent of hyperpigmentation after arachnoid pipe/erythema regulation agent, black eye/edema eye regulation agent, sallow colour of skin regulation agent, sagging regulation agent, the anti-agent of itching, skin stiffeners, pore reduction agent, oil/light reduction agent, the inflammation and comprises wrinkle and the skin texture of fine rule is regulated.

40. enzyme, enzyme inhibitors and zymoexciter (coenzyme)

Composition of the present invention can comprise one or more enzymes, enzyme inhibitors or the zymoexciter (coenzyme) of safety and significant quantity.The example of enzyme is lipase, proteolytic enzyme, catalase, superoxide-dismutase, amylase, glucuronidase, peroxidase, particularly Selenoperoxidase or lactoperoxidase, ceramidase, Unidasa.All these enzymes can obtain by the biotechnical processes that extracts or ferment.The example of enzyme inhibitors comprises trypsin inhibitor, Bowmann Birk inhibitor, chymotrypsin inhibitor, contains or do not contain the botanical extract of following material: the Xanthaurine of tannic acid, flavonoid compound, inhibitory enzyme activity.Zymin can find by trade(brand)name, and for example, the name that SEDERMA provides is called the product of VENUCEANE, France (WO 02/066668).Zymoexciter and coenzyme comprise coenzyme A, Coenzyme Q10 99.0 (ubiquinone), glycyrrhizidine, barberry sulphur, chrysin.

II. carrier

Composition of the present invention can comprise oral or the dermatology acceptable carrier, or injectable liquids, and this depends on needed product form.

A. dermatology acceptable carrier

The main component that is used for the present composition can also comprise the dermatology acceptable carrier.In one embodiment, the concentration level that carrier exists is, accounts for composition weight about 50% to about 99.99%, preferred about 60% to about 99.9%, and more preferably from about 70% to about 98%, even more preferably from about 80% to about 95%.

Described carrier can be the form of broad variety.Unrestricted example comprises simple solution (water or butyrous), emulsion and solid-state (gel, lipstick).The example emulsion carrier can include, but are not limited to oil-in-water, water-in-oil, silicone resin Bao Shui, water-in-oil-in-water, silicone oil bag water emulsion bag oil.

According to required product form, preferred carrier can comprise for example emulsion of water external emulsion (for example, silicone resin is scattered in the water) and water-in-oil emulsion.Those skilled in the art will be understood that given component both can be dispensed into water, also can be dispensed into oil phase, and this depends on the water dissolvable/dispersibility of component described in the composition.In one embodiment, water external emulsion is particularly preferred.

Can comprise water and lipid or oil according to emulsion of the present invention.Lipid and oil can also can be natural or synthetic (being synthetical) from animal, plant or oil.Described emulsion can also comprise wetting agent, for example glycerine.Emulsion can further comprise and accounts for composition weight about 0.1% to about 10%, more preferably from about 0.2% to about 5% emulsifying agent.Emulsifying agent can be non-ionic, anionic cationic.Examples of suitable emulsifiers is disclosed in, for example, U.S. patent 3,755,560, in the U.S. patent 4,421,769 and the Detergents and emulsifiers of McCutcheon, north-american version, 317 to 324 pages (1986).Suitable emulsion can have the viscosity of various scopes, and this depends on required product form.

Composition of the present invention can be the form (under ambient conditions) of pourable liquid.Therefore described composition can comprise aqueous carrier, and its typical contents level is about 20% to about 95%, preferred about 60% to about 85%.Water and ORGANIC SOLVENT MIXTURES that aqueous carrier can comprise water or can mix mutually, but the moisture and bottom line of preferred package or do not have the organic solvent of obvious concentration is unless its trace ingredients as other basal component or optional components is integrated with in the described composition separately.

Described emulsion also can comprise foam reducing composition, and foam minimizes when making it be applied to collenchyme.Foam reducing composition comprises the material that high molecular weight silicone and other are commonly used in this technical field.

Below preferred silicone resin Bao Shui and water external emulsion carrier are described in detail ground more.

1. silicone oil bag water emulsion

Silicone oil bag water emulsion has successive silicone resin phase and dispersive water.

A. continuous silicone resin phase

Preferred silicone oil bag water emulsion carrier comprises and accounts for composition weight about 1% to about 60%, preferred about 5% to about 40% among the present invention, more preferably from about 10% to about 20% continuous silicone resin phase.Described continuous silicone resin exists as external phase, and it comprises or surround the discontinuous water of the following stated.

Described continuous silicone resin comprises polysiloxane oil mutually.Preferred silicone oil bag water emulsion system can make activeconstituents of the present invention have oxidative stability through preparation.The continuous silicone resin of described these emulsions preferably comprises about 50% and the organopolysiloxane of about 99.9 weight percents oil and the non-silicone oil that is less than about 50% weight percent mutually.In an optimization embodiment, described continuous silicone resin comprises it mutually and accounts for its weight at least about 50%, preferred about 60% to about 99.9%, more preferably from about 70% to about 99.9%, even 80% to about 99.9% polysiloxane oil more preferably from about, and the non-silicone oil that contains described continuous silicone resin phase weight about 50% at the most, preferably be lower than about 40%, more preferably less than about 30%, even more preferably less than about 10%, even more preferably less than about 2%.

The organopolysiloxane that is used for described composition can be the mixture of volatility, non-volatile or volatility and non-volatile silicone resin.The term that uses in this article " nonvolatile substances " refers to be the silicone resin of liquid under the ambient conditions that its burning-point (under the normal atmosphere) is greater than about 100 ℃.Term used herein " volatile matter " refers to all other silicone oil.Suitable organopolysiloxane can be selected from the silicone resin of broad variety, and these silicone resin have the volatility and the viscosity of large span scope.Suitable organopolysiloxane oil comprises poly-alkylsiloxane, the poly-alkylsiloxane of ring-type and polyoxyethylene alkyl aryl radical siloxane.

The poly-alkylsiloxane that is applied to described composition comprises that 25 ℃ of following viscosity are the about 0.5 poly-alkylsiloxane to about 1,000,000 centistoke.Commercially available poly-alkylsiloxane comprises dimethione, has another name called dimethicone, and the example comprises to be sold by General Electric Corporation

The Dow that series and DowCorning company sell

200 series.The specific examples of suitable dimethione comprises Dow

200 liquid, the example of suitable alkyl-substituted dimethyl polysiloxane comprises hexadecyl dimethicone and dodecyl dimethicone.

The poly-alkylsiloxane of ring-type that is suitable for being used in described composition comprises commercially available cyclosiloxane, for example Dow

244 liquid, Dow

344 liquid, Dow

245 liquid and Dow

345 liquid.

Available is a trimethylsiloxy group silicate material for example in addition.Commercially available trimethylsiloxy group silicate is the mixture D ow with dimethicone

593 liquid.

Dimethyl silscone also is suitable for being used in described composition, commercially available dimethyl silscone normally with the mixture of dimethicone or cyclomethicone (Dow for example

1401,1402 and 1403 liquid).

The polyoxyethylene alkyl aryl radical siloxane also is suitable for being used in described composition.25 ℃ of following viscosity are that about 15 PSIs to about 65 centistokes are useful especially.

Preferred is the organopolysiloxane that is selected from following material as used herein: dimethicone, cyclosiloxane, trimethylsiloxy group silicate, dimethyl silscone, polyoxyethylene alkyl aryl radical siloxane and their mixture that alkyl replaces are poly-alkylsiloxane and cyclosiloxane in this application more preferably.Dimethicone preferably in the poly-alkylsiloxane.

As mentioned above, the continuous silicone resin can comprise one or more non-silicone oil mutually.Suitable non-silicone oil has about 25 ℃ or lower fusing point under a normal atmosphere.Being suitable for the example of the non-silicone oil that uses in mutually at the continuous silicone resin, is the topical personal care product of the water-in-oil emulsion form known in the chemical field, for example, and mineral oil, vegetables oil, synthetic oil, semi-synthetic wet goods etc.

B. disperse water

Topical composition of the present invention comprises about 30% to about 90%, and more preferably from about 50% to about 85%, is more preferably about 70% to about 80% dispersion water.In the emulsion technology, term " disperse phase " is well known to those skilled in the art, and the phase that its expression exists with particulate or droplet is suspended in the external phase and is held by it.Phase or discontinuous phase in disperse phase has another name called.Described dispersion water is the little water particulate or the droplet of dispersion, is suspended in the aforesaid continuous silicone resin to be held by it.

Water can be a water, or water and one or more combinations water-soluble or the water dispersible component.The example of described component comprise thickening material, acid, alkali, salt, chelating reagent, colloid, the water-soluble or pure and mild polyvalent alcohol of water dispersible, buffer reagent, sanitas, opalizer, tinting material, or the like.

Topical composition of the present invention typically comprises and accounts for described composition weight about 25% to about 90%, preferred about 40 to about 80%, more preferably from about 60% to about 80% by the water of dispersion aqueous phase.

C. be used to disperse the emulsifying agent of water

Silicone oil bag water emulsion optimum system choosing of the present invention comprises emulsifying agent.One preferred embodiment in, described composition comprises the emulsifying agent that accounts for composition weight about 0.1% to about 10%, more preferably from about 0.5% to about 7.5%, is more preferably about 1% to about 5%.Described emulsifying agent helps water to disperse in mutually and suspend at described continuous silicone resin.

The emulsifying agent of broad variety can be applied to this, to form preferred silicone oil bag water emulsion system.Known or traditional emulsifying agent can be applicable to described composition, as long as selected emulsifying agent is chemistry and physically do not contradict with the component of the present composition, and has required dispersing characteristic.Examples of suitable emulsifiers comprises the silicone resin emulsifying agent, no silicon or siliceous emulsifying agent and their mixture, and it is the topical personal care product that is used for well known to those skilled in the art.Preferred these emulsifying agents have and are about 14 or lower HLB value, more preferably from about 2 arrive approximately 14, are more preferably about 4 to about 14.The HLB value can be used with other emulsifier combination at these extraneous emulsifying agents, to reach favourable average HLB value, it is fallen in these scopes.

The silicone resin emulsifying agent is preferred.The silicone resin emulsifying agent of broad variety can be used at this.These silicone resin emulsifying agents organically are revised as organopolysiloxane usually, and as the silicone surface promoting agent, this also is well known to those skilled in the art.Available silicone resin emulsifying agent comprises the dimethicone polyol copolymer.These materials are modified polydimethylsiloxanes, and it has polyether lateral chain, for example the mixing of polyoxyethylene, polyoxytrimethylene chain and these chains and the polyether chain that comprises the root that derives from ethylene oxide and propylene oxide.Other example comprises the dimethicone polyol copolymer that alkyl is modified, and also, comprises C ₂-C ₃₀Modify the compound of side chain.Other useful dimethicone polyol copolymer comprises, has the material that various cationic, anionic, amphoteric and zwitter-ion are modified root.

Can comprise as the dimethicone polyol copolymer of emulsifying agent and the unrestricted example of other silicone surface promoting agents at this, dimethione copolyether with polyethylene oxide side-chain has the dimethione copolyether of polyoxytrimethylene side chain, dimethione copolyether with blended polyoxyethylene and polyoxytrimethylene side chain, dimethione copolyether with poly-(ethene) (propylene) oxide compound side chain of blended, dimethione copolyether with organo-metallic trimethyl-glycine side chain, dimethione copolyether with carbonyl acid ester side chain, dimethione copolyether with quaternary ammonium side chain; And further modify comprise C ₂-C ₃₀The multipolymer the preceding of straight chain, side chain or cyclic alkyl root.The example at commercially available dimethicone polyol copolymer that can be applied to this is sold by Dow Corning company, Dow by name 190,193, Q2-5220,2501Wax, 2-5324 liquid, and 3225C (a kind of raw material in back is as selling with the mixture of cyclomethicone).Hexadecyl dimethicone polyol copolymer can have been bought on market, itself and polyglyceryl-4 isostearate (with) mixture of lauric acid hexyl ester, commodity are by name

WE-09 (Goldschmidt provides).Hexadecyl dimethicone polyol copolymer also is commercially available, itself and lauric acid hexyl ester (with) polyglyceryl-3 oleic acid ester (with) mixture of hexadecyl dimethicone, trade name is WS-08 (Goldschmidt provides).The unrestricted example of other dimethicone also comprises lauryl dimethicone polyol copolymer, dimethicone polyol copolymer acetic ester, dimethicone polyol copolymer adipic acid ester, dimethicone copolymerization amine, dimethicone polyol copolymer behenate, dimethicone polyol copolymer butyl ether, dimethicone polyol copolymer hydroxy stearic acid ester, dimethicone polyol copolymer isostearate, dimethicone polyol copolymer laurate, dimethicone polyol copolymer methyl ether, dimethicone polyol copolymer phosphoric acid ester, with dimethicone polyol copolymer stearate.

Can be described at the dimethicone polyol copolymer emulsifying agent of this application, for example, U.S. patent 4,960764 is among the European patent No.EP 330,369.

The adaptable emulsifying agent that does not contain silicone resin is various nonionics and anionic emulsifier, for example sugar ester and polyester, alkoxylate sugar ester and polyester, C ₁-C ₃₀The C of Fatty Alcohol(C12-C14 and C12-C18) ₁-C ₃₀Fatty acid ester, C ₁-C ₃₀The C of Fatty Alcohol(C12-C14 and C12-C18) ₁-C ₃₀The alkoxy derivative of fatty acid ester, C ₁-C ₃₀The C of the alkoxylated ether of Fatty Alcohol(C12-C14 and C12-C18), the polyglycerol ester of lipid acid, polyvalent alcohol ₁-C ₃₀The C of ester, polyvalent alcohol ₁-C ₃₀Ether, alkyl phosphate, polyethylene glycol fatty family ether phosphate, fatty acid amide, acyl lactylates, soap and their mixture.Other examples of suitable emulsifiers is described in the document, for example, McCutcheon ' s, Detergents and Emulsifiers, north-american version (1986) is published by Allured publishing company; U.S. patent No.5,011,681; U.S. patent No.4,421,769; With U.S. patent No.3,755,560.

These not the limiting examples of siliceous emulsifying agent comprise: polyoxyethylene glycol 20 mono laurate sorbitan esters (polysorbas20), polyoxyethylene glycol 5 soyasterols, stearyl alcohol polyethers-20, ceteareth-20, PPG-2 methyl glucose ether SUNSOFT Q-182S, hexadecanol polyethers-10, tween 80, hexadecanyl phosphate, potassium cetyl phosphate, the diethanolamine hexadecanyl phosphate, polysorbate60, stearin, the PEG-100 stearate, polyoxyethylene 20 sorbitan trioleates (polysorbate 85), the mono laurate sorbitan ester, polyoxyethylene 4 bay ether sodium stearate, poly-glyceryl-4 isostearate, lauric acid hexyl ester, stearyl alcohol polyethers-20, ceteareth-20, PPG-2 methyl glucose ether SUNSOFT Q-182S, hexadecanol polyethers-10, the diethanolamine hexadecanyl phosphate, stearate glycerine, the PEG-100 stearate, with their mixture.

D. silicone elastomer

Composition of the present invention also comprises the silicone elastomer component that accounts for composition weight about 0.1% about 30%.Preferably, described composition comprises and accounts for composition weight about 1% to about 30%, more preferably from about 2% to about 20% silicone elastomer component.

Being suitable for silicone elastomer as used herein, can be emulsification or non-emulsive crosslinked siloxane elastomer, or their mixture.There is not concrete restriction in constituent polyorganosiloxane composition for curable type, and described composition can serve as the elastomeric starting raw material of crosslinked organopolysiloxane.Example in this respect is addition reaction-curing constituent polyorganosiloxane composition, and described composition carries out addition reaction by two organopolysiloxane that contain SiH-with the organopolysiloxane with silicon keyed jointing vinyl and solidifies under platinum catalysis; Condensation-curing constituent polyorganosiloxane composition, described composition can be in the presence of organo-tin compounds, and the dehydrogenation reaction between two organopolysiloxane by having terminal hydroxyl and two organopolysiloxane that contain SiH-is solidified; And condensation-curing constituent polyorganosiloxane composition, described composition solidifies in the presence of organo-tin compound or titanic acid ester.

Addition reaction-curing constituent polyorganosiloxane composition is preferred, because of it has solidification rate and outstanding curing uniformity rapidly.Particularly preferred addition reaction-curing constituent polyorganosiloxane composition prepares certainly: the organopolysiloxane that a) has at least 2 subordinate's alkenyls in each molecule; B) in each molecule, has the organopolysiloxane of at least 2 silicon keyed jointing hydrogen atoms; And c) platinum class catalyzer.

Composition of the present invention can comprise the crosslinked organopolysiloxane elastomerics of emulsive, the crosslinked organopolysiloxane elastomerics of non-emulsive, or their mixture.Being defined as at this term " non-emulsive " does not have the unitary crosslinked organopolysiloxane elastomerics of polyoxyalkylene.Term " emulsive " expression has the unitary crosslinked organopolysiloxane elastomerics of at least a polyoxyalkylene (for example, polyoxyethylene or polyoxypropylene).Preferred emulsifying elastomer comprises by divinyl compound particularly having the siloxane polymer of at least two free ethylene bases, the polyoxyalkylene modified elasticity body that forms with Si-H key reaction on the polysiloxane backbone.Preferably, described elastomerics is a dimethyl polysiloxane, and its crosslinked Si-H key that is positioned on the spherical MQ resin of molecule is crosslinked.The crosslinked organopolysiloxane elastomerics of emulsive can be selected from U.S. patent Nos.5 especially, the cross-linked polymer of describing in 412,004,5,837,793 and 5,811,487.In addition, the emulsive elastomerics by dimethicone polyol copolymer crosslinked polymer (with) dimethicone forms, its commodity are called KSG-21, can obtain from Shin Etsu.

Advantageously, non-emulsive elastomerics is dimethicone/vinyl-dimethyl polysiloxane crosslinked polymer.This dimethicone/vinyl-dimethyl polysiloxane crosslinked polymer is provided by many suppliers, comprise Dow Corning (DC 9040 and DC 9041), General Electric (SFE 839), Shin Etsu (KSG-15,16,18[dimethicone/phenyl vinyl dimethicone crosslinked polymer]) and Grant Industries (GRANSIL (TM) line of elastomers).Can be used for crosslinked organopolysiloxane elastomerics of the present invention and its manufacturing process and be further described in U.S. patent No.4,970,252, U.S. patent No.5 is in 760,116 and U.S. patent No.5,654,362.

Preferred commercially available as used herein elastomerics is the 9040 silicone elastomer mixtures of Dow Corning, the KSG-21 of Shin Etsu and their mixture.

E. the carrier that is used for silicone elastomer

Topical composition of the present invention can comprise the appropriate carrier that is used for above-mentioned crosslinked organopolysiloxane elastomeric component that accounts for composition weight about 1% to about 80%, when combining with crosslinked organopolysiloxane elastomer fine particle of the present invention, described carrier suspends and the expansion elastomer fine particle, forms reticulation or matrix elastic, similar gels.Being used for cross-linked siloxane elastomer is liquid under ambient conditions, and preferably it has low viscosity, to improve the extensibility on skin.

The concentration of the described carrier in the make-up composition of the present invention is mainly along with the type and the amount of carrier, and used crosslinked siloxane elastomer and changing.The concentration of preferred vector is for accounting for composition weight about 5 to about 50%, and more preferably from about 5% to about 40%.

Be used for cross-linked siloxane elastomer and comprise that one or more are suitable for being locally applied to the liquid vehicle of human skin.These liquid vehicles can be organically, contain silicone resin or fluorine-containing, volatile or nonvolatile, polar or nonpolar, as long as arrive under about 250 ℃ of temperature at about 28 ℃, preferred about 28 ℃ to about 100 ℃, under preferred about 28 ℃ to about 78 ℃, described liquid vehicle can form the liquid or the liquid dispersion of solution or other homogeneous with selected crosslinked siloxane elastomer with selected silicone elastomer concentration.The material that refers to all non-" non-volatilities " that define before this at this used term " volatile ".When this used, phrase " relative polarity " expression had more polarity according to solubility parameter than another kind of material; That is, solubility parameter is high more, and described liquid has multipolarity more.Term " nonpolar " ordinary representation solubility parameter is lower than about 6.5 (cal/cm ³＞) 05 material.

F. nonpolar, ethereal oil

Described composition of the present invention can comprise nonpolar, ethereal oil.Nonpolar ethereal oil helps to make composition of the present invention to have desirable aesthetic feeling performance.Accordingly, described nonpolar ethereal oil is preferably used with suitable high level.For being silicone oil, hydrocarbon and their mixture in the useful especially nonpolar ethereal oil of the present invention.This nonpolar ethereal oil is disclosed in, for example, by the Cosmetics that Balsamand Sagarin is compiled, Science, and Technology volume 1,27-104 is in 1972.The example of preferred nonpolar volatile hydrocarbon comprises poly-decane, for example Permethyl 99A. and isodecane are (for example, full methyl that can obtain from Presperse company-99A) and C7-C8 are to the isoparaffin of C12-C15 (for example, can from the Isopar series of Exxon Chemicals acquisition).25 ℃ of following viscosity generally are lower than the straight chain volatile silicone of about 5 centistokes, and 25 ℃ of following viscosity are lower than the ring-type silicone resin of 10 centistokes.The example of particularly preferred volatile silicone oils comprises the cyclosiloxane that changes viscosity, for example, and Dow Corning 200, Dow Corning 244, Dow Corning 245, Dow Corning 344, with Dow Corning 345, (can obtain .) from Dow Corning company; SF-1204 and SF-1202Silicone silicon liquid (can obtain) from G.E.Silicones, GE7207 and 7158 (can obtain) from General Electric company; And SWS-03314 (can obtain) from SWSSilicones company.

G. relative polarity, nonvolatile oil

Described composition of the present invention can comprise the nonvolatile oil of relative polarity.Compare with above-mentioned nonpolar volatile oil, described fixed oil is " relative polarity ".Therefore, non-volatile associating-carrier has more polarity (promptly having high solubility parameter) than at least a described nonpolar ethereal oil.May be used for relative polarity nonvolatile oil of the present invention and be disclosed in, for example, by the Cosmetics that Balsam and Sagarin is compiled, Science, and Technology, Vol.1,27-104,1972; U.S. patent Nos.4 is in 202,879 and 4,816,261.Can be used for the preferred following silicone oil of relative polarity nonvolatile oil of the present invention: hydrocarbon ils, lipid acid, one and dicarboxylic acid and one and the mixture of the polyoxytrimethylene ether of ester, polyoxyethylene, polyoxytrimethylene, polyoxyethylene and the Fatty Alcohol(C12-C14 and C12-C18) of polyvalent alcohol and their mixture.

H. nonpolar, nonvolatile oil

Except that the liquid of the above, be used for cross-linked siloxane elastomer and can randomly comprise non-volatile non-polar oil.Typical non-volatile nonpolar softener is disclosed in, for example, by the Cosmetics that Balsam andSagarin is compiled, Science, and Technology, Vol.1,27-104,1972; U.S. patent Nos.4 is in 202,879 and 4,816,261.Can be used for nonvolatile oil of the present invention is the non-volatile polysiloxane of purified, paraffin hydrocarbon ils and their mixture.

2. water external emulsion

Other preferred topical carrier comprises water external emulsion, and it has successive water and the hydrophobic water insoluble mutually (" oil phase ") that is scattered in wherein.Described " oil phase " can comprise oil, silicone resin or their mixture and partly include, but are not limited to above-mentioned oil and silicone resin at water external emulsion.Whether the feature of milk sap is that the difference of oil-in-water or water bag silicone resin is whether oil phase mainly is made up of oil or silicone resin.The water of these milk sap mainly is made up of water, but can also comprise various other compositions, the water-phase component in for example above listed those water-in-oil emulsions.Preferred water external emulsion comprises and accounts for composition weight about 25% to about 98%, preferred about 65% to about 95%, more preferably from about 70% to about 90 water.

Except that continuous water and dispersive oil or silicone resin mutually, these oil-in-water compositions also comprise the emulsifying agent of stablizing described milk sap.The emulsifying agent that can be applied to this is to know in the prior art, comprises non-ionic, anionic, cationic and amphoteric emulsifier.The unrestricted example that can be used for the emulsifying agent of water external emulsion of the present invention is given in McCutcheon ' s, Detergents and Emulsifiers, north-american version (1986), U.S. patent .No.5,011,681; U.S. patent No..4,421,769; And U.S. patent No.3 is in 755,560.Suitable oil-in-water emulsion carrier case description is in U.S. patent No.5, in 073,371 and U.S. patent No.5,073,372.Particularly preferred water external emulsion comprises structurising agent, hydrophilic tensio-active agent and water, below is described in detail.

A. structurising agent

Preferred water external emulsion comprises structurising agent, and it participates in forming the gel with liquid crystal structure network structure.Bound by theory can not thought that structurising agent helps the rheological characteristics of described composition, and improve the stability of described composition.Structurising agent also can have the function of emulsifying agent or tensio-active agent.The preferred present composition comprises and accounts for composition weight about 0.5% to about 20%, and more preferably from about 1% to about 10, also 1% to about 5% structurising agent more preferably from about.

Preferred structurising agent of the present invention comprises stearic acid, palmitinic acid, stearyl alcohol, hexadecanol, behenyl alcohol, have average about 1 polyglycol ether to the stearyl alcohol of about 21 ethylene oxide unit(s)s, have average about 1 arrives the polyglycol ether of hexadecanol of about 5 ethylene oxide unit(s)s and their mixture.Preferred structurising agent of the present invention is selected from stearyl alcohol, hexadecanol, behenyl alcohol, have the polyglycol ether (stearyl alcohol polyethers-2) of the stearyl alcohol of average about 2 ethylene oxide unit(s)s, the polyglycol ether (stearyl alcohol polyethers-21) with stearyl alcohol of average about 21 ethylene oxide unit(s)s, the polyglycol ether of hexadecanol with average about 2 ethylene oxide unit(s)s and their mixture.Even preferred structurising agent is selected from stearic acid, palmitinic acid, stearyl alcohol, hexadecanol, behenyl alcohol, stearyl alcohol polyethers-2, stearyl alcohol polyethers-21 and their mixture.

B. hydrophilic tensio-active agent

Preferred water external emulsion comprises about 0.05% to about 10%, preferred about 1% to about 6%, 1% to about 3% at least a hydrophilic surfactant active more preferably from about, and it can be aqueous phase dispersing hydrophobic thing (pressing the weight percentage of described topical carrier).Described tensio-active agent must have enough wetting abilities that is scattered in the water at least.

Preferred hydrophilic surfactant active is selected from nonionic surface active agent. and among nonionic surface active agent, what can be applied to this is extensively to be defined as long-chain alcohol, for example C _8-30Alcohol, with the condensation product of sugar or starch polymer, just, glycoside. these compounds can represent that wherein S is sugared root, for example glucose, fructose, seminose and semi-lactosi with chemical formula (S) n-O-R; N is from about 1 to about 1000 integer, and R is C _8-30Alkyl.In the example of long-chain alcohol, its alkyl can be deutero-, comprises decyl alcohol, hexadecanol, stearyl alcohol, lauryl alcohol, tetradecanol, oleyl alcohol or the like.The example of preferred these tensio-active agents comprises that wherein S is the glucose root, and R is C _8-20Alkyl and n are from about 1 to about 9 integers.The example of commercially available these tensio-active agents comprises decyl poly glucoside (can obtain APG 325 by name from Henkel) and lauryl poly glucoside (can obtain APG 600CS by name and 625CS from Henkel).

Other useful nonionic surface active agent comprises the condensation product (being oxidation of fatty acids alkene ester) of oxyalkylene and lipid acid, the condensation product of oxyalkylene and 2 moles of fatty acids (being oxidation of fatty acids alkene diester), the condensation product of oxyalkylene and Fatty Alcohol(C12-C14 and C12-C18) (being the oxyalkylene ether of Fatty Alcohol(C12-C14 and C12-C18)), the condensation product of oxyalkylene and lipid acid and Fatty Alcohol(C12-C14 and C12-C18) [promptly wherein polyoxyalkylene part at an one end and a fatty acid esterification, its other end and a Fatty Alcohol(C12-C14 and C12-C18) etherificate (promptly being connected) by ehter bond].The unrestricted example of these oxyalkylene deutero-nonionic surface active agent comprises hexadecanol polyethers-6, hexadecanol polyethers-10, hexadecanol polyethers-12, ceteareth-6, ceteareth-10, ceteareth-12, stearyl alcohol polyethers-6, stearyl alcohol polyethers-10, stearyl alcohol polyethers-12, stearyl alcohol polyethers-21, the PEG-6 stearate, the PEG-100 stearate, the PEG-12 stearate, PEG-20 glyceryl stearate, PEG-80 glyceryl tallow acid esters, PEG-10 glyceryl stearate, PEG-30 glyceryl coconut palm acid esters, PEG-80 glyceryl coconut palm acid esters, PEG-200 glyceryl tallow acid esters, the PEG-8 dilaurate, the PEG-10 SUNSOFT Q-182S, with their mixture.

Other can also with nonionic surface active agent comprise polyhydroxy fatty acid amide surfactant, the particularly preferred tensio-active agent that is equivalent to said structure is a coconut palm alkyl N-methyl glucoside acid amides.The method that manufacturing comprises polyhydroxy fatty acid amide is disclosed in, U.S. patent No.2 for example, 965,576; U.S. patent No.2,703,798, and U.S. patent No.1 is in 985,424.

Among nonionic surface active agent, preferably it is selected from stearyl alcohol polyethers-21, ceteareth-20, ceteareth-12, sucrose coconut palm acid esters, stearyl alcohol polyethers-100, PEG-100 stearate and their mixture.

Other is suitable for nonionic surface active agent C sugar ester and polyester, alkoxylate sugar ester and polyester, C as used herein ₁-C ₃₀The C of Fatty Alcohol(C12-C14 and C12-C18) ₁-C ₃₀Fatty acid ester, C ₁-C ₃₀The C of Fatty Alcohol(C12-C14 and C12-C18) ₁-C ₃₀The alkoxy derivative of fatty acid ester, C ₁-C ₃₀The alkoxylated ether of Fatty Alcohol(C12-C14 and C12-C18), C ₁-C ₃₀The polyglycerol ester of lipid acid, the C of polyvalent alcohol ₁-C ₃₀The C of ester, polyvalent alcohol ₁-C ₃₀Ether, alkyl phosphate, polyoxyalkylene fatty ether phosphoric acid ester, fatty acid amide, acyl lactylates and their mixture.The unrestricted example of these emulsifying agents comprises: polyoxyethylene glycol 20 mono laurate sorbitan esters (polysorbas20), polyoxyethylene glycol 5 soyasterols, stearyl alcohol polyethers-20, ceteareth-20, PPG-2 methyl glucose ether SUNSOFT Q-182S, hexadecanol polyethers-10, tween 80, hexadecanyl phosphate, potassium cetyl phosphate, the diethanolamine hexadecanyl phosphate, polysorbate60, the glyceryl stearate, polyoxyethylene 20 sorbitan trioleates (polysorbate 85), the mono laurate sorbitan ester, polyoxyethylene 4 lauryl ether sodium stearate, poly-glyceryl-4 isostearate, lauric acid hexyl ester, PPG-2 methyl glucose ether SUNSOFT Q-182S, the PEG-100 stearate, with their mixture.

The nonionic surface active agent that can be applied to this in addition is based on the fatty acid ester blends of sorbitanic or Sorbitol Powder fatty acid ester and sucrose fatty acid ester mixture, the preferred separately C of described lipid acid ₈-C ₂₄, more preferably C ₁₀-C ₂₀Preferred fatty acid ester emulsifier is the C of sorbitanic or Sorbitol Powder ₁₆-C ₂₀Fatty acid ester and sucrose C ₁₀-C ₁₆The mixture, particularly sorbitan stearate of fatty acid ester and the mixture of sucrose coconut palm acid esters.It can obtain from ICI (ICI), and commodity are called Arlatone 2121.

Other suitable tensio-active agent that can be applied to this comprises various cationic, anionic, zwitterionic and amphotericses, and for example prior art is known and at the following material that more expounds adequately.The hydrophilic surfactant active that can be applied to this can comprise single surfactant, or the combination of any suitable tensio-active agent.The accurate selection of tensio-active agent (or combinations-of surfactants) depends on the pH value of described composition, and the component that exists in addition.

What can also be applied to this is cats product, dialkyl quats compound particularly, and the example is described in U.S. patent 5,151,209; U.S. patent 5,151, and 210; U.S. patent 5,120, and 532; U.S. patent 4,387, and 090; U.S. patent 3,155, and 591; U.S. patent 3,929, and 678; U.S. patent 3,959, and 461; McCutcheon ' s, Detergents ﹠amp; Emulsifiers, (north-american version 1979) M.C.Publishing Co.; And Schwartz, et al., Surface Active Agents, Their Chemistryand Technology, New York:Interscience Publishers, 1949.

The unrestricted example of these cationic emulsifiers comprises stearic acid aminopropyl PG-dichloride ammonium phosphoric acid ester, mountain Yu acid aminopropyl PG dichloride ammonium, stearic acid aminopropyl second two ammonium esilates, stearic acid aminopropyl dimethyl (acetic acid myristin) ammonium chloride, stearic acid aminopropyl dimethyl hexadecyl ammonium tosylate ester, stearic acid aminopropyl dimethyl ammonium chloride, stearic acid aminopropyl diformazan DL-Lactic acid ammonium salt and their mixture.Particularly preferably be mountain Yu acid aminopropyl PG dichloride ammonium.

The unrestricted example of quaternary cationics is selected from the cetyl chloride ammonium, the hexadecyl brometo de amonio, lauryl chlorination ammonium, lauryl bromination ammonium, stearyl chlorination ammonium, the stearyl brometo de amonio, the hexadecyl dimethyl ammonium chloride, hexadecyl diformazan brometo de amonio, the lauryl dimethyl ammonium chloride, lauryl diformazan brometo de amonio, the stearyl dimethyl ammonium chloride, stearyl dimethyl brometo de amonio, palmityl trimethyl ammonium chloride, the 16 basic trimethylammonium bromides of washing, lauryl trimethyl ammonium chloride, the lauryl trimethylammonium bromide, stearyl trimethyl ammonium chloride, the stearyl trimethylammonium bromide, the lauryl dimethyl ammonium chloride, stearyl dimethyl hexadecyl two tallow base dimethyl ammonium chlorides, dicetyl ammonium chloride, the dicetyl brometo de amonio, connection dodecyl chlorination ammonium, connection dodecyl bromination ammonium, the connection octadecyl ammonium chloride, connection octadecyl bromination ammonium, the dicetyl ammonio methacrylate, dicetyl methyl brometo de amonio, connection dodecyl methyl ammonium chloride, connection dodecyl methyl brometo de amonio, connection octadecyl methyl ammonium chloride, connection octadecyl methyl brometo de amonio, with their mixture.Other quaternary ammonium salt comprises C ₁₂To C ₃₀Alkyl carbon chain stems from the material of tallow fatty acid or coconut fatty acid.Term " tallow base (tallow) " refers to derive from the alkyl of tallow fatty acid (being generally hydrogenated tallow acid), and it generally is C ₁₆To C ₁₈The mixture of the alkyl chain of scope.Term " coconut palm base (coconut) " refers to derive from the alkyl of coconut fatty acid, and it generally is C ₁₂To C ₁₄The mixture of the alkyl chain of scope.The example of quaternary ammonium salt derives from these tallow bases and coconut palm Ji Yuan, comprises two tallow base dimethyl ammonium chlorides, two tallow base dimethylammonium methyl-sulfates, two (hydrogenated-tallow group) dimethyl ammonium chloride, two (hydrogenated-tallow group) dimethyl acetic acid ammonium, two tallow base dipropyl ammonium phosphate, two tallow base dimethyl ammonium nitrate, two (coconut palm alkyl) dimethyl ammonium chloride, tallow ammonium chloride, coconut palm ammonium chloride and their mixture.Example with quaternary ammonium compound of alkyl and ester bond is two tallow base oxethyl dimethyl ammonium chlorides.

Preferred cats product is selected from mountain Yu acid aminopropyl PG dichloride ammonium, connection dodecyl dimethyl ammonium chloride, connection octadecyl dimethyl ammonium chloride, connection tetradecyl dimethyl ammonium chloride, the dicetyl dimethyl ammonium chloride, connection octadecyl dimethyl ammonium chloride, stearic acid aminopropyl PG-dichloride ammonium phosphoric acid ester, stearic acid aminopropyl ethyl diamino ethyl sulfonic acid, stearic acid aminopropyl dimethyl (acetic acid myristyl ester) ammonium chloride, stearic acid aminopropyl dimethyl spermaceti ammonium tosylate ester, stearic acid aminopropyl dimethyl ammonium chloride, stearic acid aminopropyl dimethyl DL-Lactic acid ammonium salt, with their mixture.

The cats product that is more preferably is selected from mountain Yu acid aminopropyl PG dichloride ammonium, connection dodecyl dimethyl ammonium chloride, connection octadecyl dimethyl ammonium chloride, connection tetradecyl dimethyl ammonium chloride, dicetyl dimethyl ammonium chloride and their mixture.

The combination of preferred cationic surfactants and structurising agent, be mountain Yu acid aminopropyl PG dichloride ammonium and/or behenyl alcohol, the preferred optimizing of its ratio remains and improves physics and chemical stability, particularly when this combination comprises ionic and/or high polar solvent.

Can also use various anion surfactants at this.The unrestricted example of anion surfactant comprises the alkyloyl isethionic acid ester, and alkyl and alkyl oxide sulphonate, and it is lipid acid and hydroxyethylsulfonic acid esterification and neutral reaction product, just, typically has chemical formula RCO-OCH ₂CH ₂SO ₃The alkyloyl isethionate of M, wherein R is about 10 alkyl or alkenyls to about 30 carbon atoms, M is a water-soluble cationic, for example ammonium, sodium, potassium and trolamine.For example, described lipid acid is from cocounut oil or palmitic derivative.The unrestricted example of these isethionates comprises the alkyloyl isethionate that is selected from following material, and cocounut oil acyl isethionate, concrete example are as cocounut oil acyl sodium isethionate, bay sodium isethionate, stearyl sodium isethionate and their mixture.Also that suitable application is the amids of fatty acid ester, methyl taurides.Other similar anion surfactant is described in U.S. patent Nos2,486,921; In 2,486,922 and 2,396,278.

Alkyl and alkylether sulfonate generally have chemical formula ROSO separately ₃M and RO (C ₂H ₄O) _xSO ₃M, wherein R is about 10 to the alkyl or the alkenyls of about 30 carbon atoms, and x is about 1 to about 10, and M is water miscible positively charged ion, for example ammonium, alkanolamine, for example trolamine, monovalent metal, for example sodium and potassium and multivalent metal cation, for example magnesium and calcium.Preferably, in alkyl and the sulfated alkyl ether, R has about 8 to about 18 carbon atoms, and more preferably from about 10 to about 16 carbon atoms, even more preferably from about 12 arrive about 14 carbon atoms.Described this sulfated alkyl ether is generally as ethylene oxide with have about 8 and prepare to the condensation product of the monohydroxy-alcohol of about 24 carbon atoms.Alcohol can be synthetic or stem from for example fat of Oleum Cocois, plam oil, Tallow, beef.It is preferred deriving from Oleum Cocois or palmitic lauryl alcohol and straight chain alcohol.The reaction of this alcohol and ethylene oxide, the mol ratio of described ethylene oxide is between about 0 and about 10, preferred about 2 to about 5, and more preferably from about 3, the mixture of the molecular species of gained has, and for example average each mol of alcohol has 3 mole ethylene oxides, by sulphating and neutralization.

The suitable classification of other anion surfactant is organic water soluble salt, has the sulfuric acid reaction product of following general formula:

R ¹--SO ₃--M

R wherein ¹Be selected from straight or branched, and have about 8, preferred about 10 representative examples of saturated aliphatic hydrocarbyl groups to about 16 carbon atoms to about 24 carbon atoms; M is above-described positively charged ion.And the classification of other anionic synthetic surfactant comprises succinamate, has about 12 ethylenic sulfonate and b-alkoxyalkyl sulfonate to about 24 carbon atoms.The example of these materials is sodium lauryl sulphate and myrceane ammonium sulfate.Other anion surfactant that is suitable for being used in described composition is a succinate, and the example comprises the N-disodium octadecyl sulfosuccinate; Lauryl sulfo-succinic acid disodium; Lauryl sulfo-succinic acid two ammoniums; N-(1,2-oxalic acid ethyl)-N-octadecyl sulfo-succinic acid four sodium; The diamyl ester of sodium sulfosuccinate; The own diester of sodium sulfosuccinate; Hot diester with sodium sulfosuccinate.Other suitable anion surfactant comprises having about 10 ethylenic sulfonates to about 24 carbon atoms.Except that containing real olefin sulfonate and a part of hydroxyl sulfonated alkane, also may comprise a small amount of other material in the olefin sulfonate, for example, because during sulfonation reaction, the alkenyl stilbene-4,4'-bis-(1-azo-3, 4-dihydroxy-benzene)-2,2'-disulfonate that forms in view of factor such as the impurity that brings in reaction conditions, reactant ratio, initiator alkene character and olefin feedstock and the side reaction.The unrestricted case description of this sulfonated mixture is in U.S. patent 3,332,880.

The anion surfactant that is suitable for being used in another classification of described composition is β-alkoxyalkyl sulfonate.These tensio-active agents meet following chemical formula:

R wherein ¹Be to have about 6 straight chained alkyls, R to about 20 carbon atoms ²Be to have about 1 low alkyl group to about 3 carbon atoms, preferred 1 carbon atom, M is a water-soluble cationic described above.Other anionic materials that can be applied to this is fatty acid metal salt (is an alkali metal salt, for example, sodium or sylvite), and it has about 8 usually to about 24 carbon atoms, and preferred about 10 to about 20 carbon atoms.The lipid acid that is used to make described fatty acid metal salt can obtain from natural source, for example, for example, the glyceride of plant or animal derived (for example, plam oil, Oleum Cocois, soya-bean oil, Viscotrol C, tallow, lard or the like).Described lipid acid can also be synthetic.Fatty acid metal salt is described in greater detail in U.S. patent No.4, in 557,853.

Doubly charged and zwitterionics also can be used at this.The example that can be used for the doubly charged and zwitterionics of the present composition is the material that is described to secondary aliphatic amine and tertiary amines derived thing of broad variety, its aliphatic radical can be a straight or branched, and one of them aliphatics substituting group comprises about 8 to about 22 carbon atoms (preferred C ₈-C ₁₈), a substituting group comprises the water solubilizing group of an anionic property, for example carboxyl, sulfonate radical, sulfate radical, phosphate radical or phosphonate radical.Example is the inferior glycinate of alkyl, and imino-alkanoate and amino-alkane hydrochlorate, and its chemical formula is RN[CH ₂) mCO ₂M] ₂And RNH (CH ₂) _mCO ₂M, wherein m is 1 to 4, R is C ₈-C ₂₂Alkyl or alkenyl, M is H, basic metal, alkaline-earth metal, ammonium or alkanol ammonium.Amphoterics preferred for the present invention comprises cocounut oil acyl both sexes guanidine-acetic acid salt, cocounut oil acyl both sexes base diacetin, lauroyl both sexes guanidine-acetic acid salt, lauroyl both sexes base diacetin and their mixture.Comprise imidazoles and ammonium derivative in addition.The specific examples of suitable amphoterics comprises 3-sodium dodecyl aminopropionitrile, 3-dodecyl amino propane sulfonic acid sodium, N-alkyl taurine, the product by the preparation of n-Laurylamine and sodium isethionate for example, this reaction is by U.S. patent 2,658, and 072 illustrates; N-senior alkyl aspartic acid, for example according to U.S. patent 2,438, shown in 091 and the preparation product; Product with commodity " Miranol " by name is described in the U.S. patent 2,528,378.Other available both sexes charged surface promoting agent comprises phosphoric acid salt, for example coamidopropyl PG dichloride ammonium phosphoric acid salt (available on the market, Monaquat PTC by name obtains from Mona company).

The zwitterionics that is suitable for being used in described composition is that prior art is known, comprise those tensio-active agents that are described to aliphatic quaternary ammonium derivative, phosphorus and sulfonium compound widely, aliphatic radical wherein can be a straight or branched, one of them aliphatics substituting group comprises about 8 to about 18 carbon atoms, a substituting group comprises anionic group, for example carboxyl, sulfonic group, sulfate radical, phosphate radical or phosphate radical.Zwitterionic is preferred, for example betaine compound.The example of betaine compound comprises the senior alkyl trimethyl-glycine, coconut palm base dimethyl carboxymethyl betaine for example, the lauryl dimethyl carboxymethyl betaine, lauryl dimethyl α carboxylic acid ethyl trimethyl-glycine, the hexadecyldimethyl benzyl ammonium carboxymethyl betaine, the hexadecyldimethyl benzyl ammonium trimethyl-glycine (can obtain from Lonza company, 16SP by name), lauryl two-(2-hydroxyethyl) carboxymethyl betaine, stearyl two-(2-hydroxypropyl) carboxymethyl betaine, oleyl dimethyl γ carboxyl CAB, lauryl two-(2-hydroxypropyl) α carboxy ethyl trimethyl-glycine, coconut palm base dimethyl sulfopropyl betaine, the stearyl dimethyl sulfopropyl betaine, lauryl dimethyl thio-ethyl trimethyl-glycine, lauryl two-(2-hydroxyethyl) sulfopropyl betaine, with amino β amine and amino sulfo group β amine (wherein RCONH (CH2) 3 bases are connected in the nitrogen-atoms of trimethyl-glycine), the oleyl trimethyl-glycine (can obtain from Henkel, amphoteric Velvetex OLB 50 by name), with cocoa base aminopropyl trimethyl-glycine (can obtain Velvetex BK 35 by name and BA 35) from Henkel.

Other available is doubly charged to comprise sultaine and hydroxyl sulfo betaine with zwitterionics, for example cocoa base propyl hydroxy sultaine (can obtain from Rhone Poulenc, be called Mirataine CBS), and relevant chemical formula is RCON (CH ₃) CH ₂CH ₂CO ₂The alkyloyl sarcosinate of M, wherein R is about 10 to the alkyl or the alkenyls of about 20 carbon atoms, M is water miscible positively charged ion, for example ammonium, sodium, potassium and three alkanolamines (for example, trolamine), its preferred examples is a sodium lauroyl sareosine.

C. water softener

Preferred water external emulsion comprises and accounts for described topical carrier weight about 25% to about 98%, preferred about 65% to about 95%, more preferably from about 70% to about 90% water.

Hydrophobicly be scattered in continuous aqueous phase mutually.Described hydrophobic water-insoluble or the being partly dissolved property material that can comprise mutually, known those materials of prior art for example, include but not limited to described here about the silicone resin in the water bag silicone resin, and other above-described oil and lipid about milk sap.

Topical composition of the present invention includes, but are not limited to washing lotion and creme, and it can comprise the acceptable softener of dermatology.This composition preferably comprises about 1% to about 50% softener.When this used, " softener " referred to be used for prevention or removes the exsiccant material, also comprises the material that is used for skin care.The known various suitable softener of prior art can use at this.Sagarin, Cosmetics, Science andTechnology, second edition, volume 1,32-43 page or leaf (1972) comprise many suitable examples of materials as softener.Preferred softener is a glycerine.The glycerine preferable amount is about 0.001 to about 30%, and more preferably from about 0.01 to about 20%, is more preferably about 0.1 to about 10%, for example, and 5%.

Generally comprise solution carrier system and one or more softeners according to washing lotion of the present invention and creme.Washing lotion and creme generally comprise about 1% to about 50%, preferred about 1% to about 20% softener; About 50 to about 90%, preferred about 60% to about 80% water; As the compound of theme of the present invention and the interpolation skin care active composition (or various active composition) of above-mentioned quantity.Creme is general thick in washing lotion, because of it contains higher levels of softener or higher levels of thickening material.

Ointment of the present invention can comprise the simple carrier based on animal or plant oil or semi-solid hydro carbons (oily); Can absorb water and form the suction ointment matrix of milk sap; Or water miscible carrier, for example, water miscible solution carrier.Ointment can further comprise thickening material, for example is described in Sagarin, Cosmetics, Scienceand Technology, second edition, volume 1, the thickening material of 72-73 page or leaf (1972), and/or softener.For example, ointment can comprise about 2% to about 10% softener; About 0.1% to about 2% thickening material; With skin care active composition (or various active composition) as the interpolation of the compound of object of the present invention and amount described above.

The composition of the present invention that is used to clean (" sanitising agent ") can be with suitable carrier preparation, for example, as described above, preferably comprises about 1% to about 90%, more preferably from about 5% to about 10% dermatology acceptable surfactant.Described tensio-active agent correspondingly is selected from anionic, non-ionic, zwitterionic, doubly charged and amphoterics, also has these surfactant mixtures.This tensio-active agent is that the de-sludging those skilled in the art are known.Reasonably the unrestricted example of tensio-active agent comprises different ceteareth-20, methyl cocounut oil fatty acyl group tallow fatty acid sodium, methyl oleoyl tallow fatty acid sodium and sodium lauryl sulphate.See U.S. patent No.4,800,197, it can be used as exemplary table surface-active agent as used herein.The various interpolation surfacants that can be applied to this are described in McCutcheon ' sDetergents and Emulsifiers, and north-american version (1986) is published by Allured Publishing company.Described cleaning compositions can randomly comprise, and on technology-establishment level, other routine is used for the material of cleaning compositions.

When this used, term " substrate " referred to liquid, semiliquid, semisolid or solid skin cosmetic, includes, but are not limited to washing lotion, creme, gel, lotion, muffin or the like.Usually, substrate is to use on large-area skin, for example on the face, and so that specific outward appearance to be provided.Substrate generally is used for providing adherent base to colored cosmetic, for example kermes, rouge, powder or the like, it helps to hide skin blemishes, gives skin with slick outward appearance.Substrate of the present invention comprises the dermatology acceptable carrier, also can comprise conventional composition, for example oil, tinting material,, softener, flavouring agent, wax, stablizer or the like.Be suitable for exemplary as used herein carrier and other composition and be described in, for example, among PCT application WO 96/33689 and the U.K. patent GB 2274585.

B. oral acceptable carrier

Composition of the present invention can also comprise the oral carrier accepted if be ingested.Any prior art is known or other is suitable orally absorbs carrier or carrier format all can use.The unrestricted example of oral personal care composition can include, but are not limited to tablet, pill, capsule, potus, beverage, syrup, granule, pulvis, VITAMIN, supplement, health bar, contain agent, masticatory and drops.

C. injection liquid

If composition of the present invention is used for injection, can also comprises and be applicable to intracutaneous or hypodermic liquid.Known or other the suitable acceptable liquid of any prior art all can use.

III. preparation of compositions

The described composition that can be used for the inventive method is usually by ordinary method preparation, for example known partial and oral composition of prior art and the manufacture method of composition for injection.These methods generally comprise with described composition one the step or more mix in the multistep, reach relatively stable uniform state, can use in the process or not application of heat, cooling, vacuum-treat or the like.

The physical form of composition according to the present invention is not important: creme, washing lotion, ointment, emulsion, gel, milk sap, dispersion, solution, suspension, sanitising agent, substrate, anhydrous formulation (club, particularly lipstick, health massage oil and bath oil), shower and bath gels, shampoo and scalp treatment liquid, the frost of nursing skin or hair or conditioning liquid, sun screen, sunscreen or sunscreen, artificial sun-screening agent, artificial sunscreen or artificial sunscreen, blow frost or foam recklessly, after shave lotion, mascara or nail varnish, lipstick, skin " essential oil ", serum, jointing material or absorbing material, transdermal patch, powder, skin lotion, milky lotion, skin cream, the spray and the finish that are used for health and shower, the foundation cream color base, brilliantine, colloid, briquet or solids suspension, eyebrow pencil, but spray preparations, can brush preparation or the like.These compositions can also be used for applying color or protect lip to split as the form of lipstick on lip, or are used for the makeup product of eye or the product of face's colouring and foundation cream color base.

It is also conceivable that the composition that uses foam or aerosol form, comprise the pressure propellent.

Make-up composition can also be applied to ability to speak, for example toothpaste.In this case, described composition can comprise adjuvant and the additive that is generally used for the oral cavity use, particularly, tensio-active agent, thickening material, moistening agent, rumbling compound, for example silica, various active substance, for example fluorochemical, particularly Sodium Fluoride and, may contain sweetening agent, for example soluble saccharin.

Composition according to the present invention can be following form, solution, dispersion, milk sap, lotion or powder.They can be discrete or be pre-mixed in vehicle, for example big-, little-or nanocapsule, big-, little-or nanometer ball, liposome, oleosome or chylomicron, big-, little-or nanoparticle, big-, little-or nanosponges, big-, little-or nanometer milk sap.They also can be adsorbed in organic polymer powder, mica, bentonite, or on other inorganic or organic support.

They also can be adsorbed on organic polymer powder, mica, bentonite or other inorganic support.

Compound as object of the present invention, with and makeup and dermal drug composition, can under any form, use alone or in combination, perhaps be incorporated into, perhaps be incorporated in or be adsorbed in big-, little-and nanoparticle in, or big-, little-and nanocapsule in, be used to handle fabric, natural or synthetic fiber, wool and any that be used for daytime or night and contacted clothes of skin or underwear, for example tights, shirt, scarf or clothing, with via this type of skin/its makeup effect of fabric contact performance, discharge and be able to the persistence part.

IV. be used to handle the method for keratinous tissue conditions

The invention still further relates at least a compound of Formula I except tyrasamine and its derivative that defines below, perhaps the compound of Formulae II, III, IV, V and being used for reduces the application at makeup or dermal drug composition of octopamine that melanochrome generates, and definition, that will get rid of here derivative is meant the OH or the NH of tyrasamine ₂On the group keyed jointing any straight or branched, saturated or unsaturated, can hydroxylated or sulfur-bearing or sulfur-bearing, that do not form by 1 to 24 alkyl chain that carbon atom is formed derivative and synephrine (general formula I, X=-NR ³R ⁴, R ¹=OH, R ²=R ³=H, R ⁴=CH ₃).According to the present invention, described compound is for using separately or uniting use.One preferred embodiment in, the compound of Formula I, II, III, IV or the IV that is obtained by method described above is applied in makeup or the dermal drug composition, is used to reduce melanochrome and generates.

The invention still further relates to these compounds in makeup that reduce the melanochrome generation or the purposes in the dermal drug composition, the lightization colour of skin particularly, the desalination senile plaque, evenly the colour of skin or any pigmentation relevant with melanochrome of lightization comprise these effects of hair.

The invention still further relates to the purposes of these compounds, be used for reducing the melanochrome generation at makeup or dermal drug composition in concentration described above.

The present invention also covers these compounds, and the purposes that contains the makeup or the dermal drug composition of described compound individually or jointly, be used to prepare makeup or the dermal drug that reduces the melanochrome generation, its objective is the minimizing pigmentation, particularly, comprise hair for the light colour of skin, desalination senile plaque, the even colour of skin or any pigmentation relevant of lightization with melanochrome.

The invention still further relates to the purposes that compound and octopamine with Formula I, II, III, IV or V are used for makeup or dermal drug composition individually or jointly, be used to prepare and suppress melanocyte and generate or be used for its painted under natural or artificial uviolizing of the medical product, particularly lightization skin of skin care and minimizing.

Description of drawings

Fig. 1 represents it is the restraining effect that melanochrome external among the embodiment 10 generates

Embodiment

V. embodiment

Below provide embodiment, as realizing non-limiting example of the present invention.

Synthesizing of embodiment 1:N-succinyl--tyrasamine (Compound I I)

At room temperature, to the tyrasamine hydrochlorinate tyrasamine (1.00g that is dissolved in 20mlTHF; 5.76 mmole) solution adds 1 normal salt of wormwood (K ₂CO ₃) (0.80g; 5.76 mmole) and 1.04 normal succinyl oxide (0.60g; 5.99 mmole).Through stirring a night, add water (10ml) described mixture is hydrolyzed under the room temperature, add 4g Amberlite resin IR120 (R-SO ₃H) wash and stir 15 minutes (pH=0-1).After-filtration and washing, the cold THF that boils off.0.92g (3.88 mmoles; 67.3%) N-succinyl--tyrasamine is separated out as white crystal.

C ₁₂H ₁₅NO ₄

MM＝237.257gmol ^-1

Fusing point: 135-136 ℃

CHN: calculated value: 60.75%C; 6.35%H; 5.90%N

Measured value: 61.33%C; 6.05%H; 5.86%N

Infrared spectra: 3313; 3055; 2930; 1694; 1643; 1542; 1517; 1426; 1238;

1208cm ^-1

Synthesizing of embodiment 2:N-tosyl group-tyrasamine (compound III)

At room temperature, add 1 normal salt of wormwood (K in the tyrasamine hydrochloride solution in being dissolved in 4ml THF ₂CO ₃) (0.16g; 1.16 mmole) and 1.10 normal toluene sulfonyl chloride (0.12g; 1.27 mmole).At room temperature stir, add water (4ml) mixture is hydrolyzed, add 4g Amberlite resin IR 120 (R-SO through a night ₃H) wash and stir 1 hour.After-filtration and washing with water, the cold then solvent THF that boils off leaches solid.0.19g (0.65 mmole; 56.00%) N-tosyl group-tyrasamine is separated out as white crystal.

C ₁₅H ₁₇NSO ₃

MM＝291.37gmol ^-1

Fusing point: 169-172 ℃

CHN: calculated value: 61.83%C; 5.88%H; 4.81%N

Measured value: 61.94%C; 5.83%H; 4.78%N

Infrared spectra: 3335; 3220; 1613; 1598; 1515; 1435; 1312; 1229; 1149; 1063; 913; 833; 812cm ^-1

Embodiment 3:N, N's '-two-tyrasamine-urea (compound IV) is synthetic

At room temperature, to the tyrasamine hydrochloride (0.20g of solution in 4ml THF; 1.15 mmole) solution adds 1 normal salt of wormwood (K ₂CO ₃) (0.16g; 1.16 mmole) and 0.54 normal carbonyl-diimidazole (0.10g; 0.62 mmole).At room temperature stirred, add water (4ml) and THF (4ml) mixture is hydrolyzed, and add 4g Amberlite resin IR 120 (R-SO through two days ₃H) wash and stir 15 minutes.After-filtration and use the 4ml water washing then with 4ml THF, the cold solvent that boils off leaches solid subsequently.0.09g (0.27 mmole; 43.20%) N, N '-two-tyrasamine-urea is separated out as white crystal.

C ₁₇H ₂₀N ₂O ₃

MM＝300.3605gmol ^-1

Fusing point: 95-98 ℃

Mass spectroscopy: (m/z)=301.2[M+H] ⁺

CHN: calculated value: 67.98%C; 6.71%H; 9.33%N

Measured value: 67.66%C; 6.73%H; 9.36%N

Infra?Red：3336；3104；2930；1605；1515；1445；1240；1169；1050；822cm ^-1

Embodiment 4: day cream G/100g

Volpo?S20 2.4

Volpo?S2 2.6

Prostearyl?15 8.0

Beeswax 0.5

Stearic oxygen base dimethicone 3.0

Propylene glycol 3.0

Carbomer 0.25

NaOH?30％ 0.25

Octopamine 0.1

Water and sanitas qs 100g

This creme is used for lightization and humidification skin of face.

Embodiment 5: the emulsion of moistening and brightization body

Crillet?3 2.5

Novol 0.9

Fluilan 2.5

Carbopol?940 0.3

Beeswax 2.0

NaOH?30％ 0.1

Glycerine 5.0

N-tosyl group-tyrasamine (III) 0.01

Water and sanitas qs 100g

Embodiment 6: the lightization gel G/100g

Carbomer 0.3

Propylene glycol 2.0

Glycerine 1.0

White vaseline 1.5

Cylomethicone 6.0

Crodacol?C90 0.5

Lubrajel?MS 10.0

Trolamine 0.3

N-succinyl--tyrasamine (II) 0.02

Water, sanitas and flavouring agent qs 100g

Embodiment 7: whitening cream G/100g

Cromul?EM?1207 2.4

Volpo?S2 2.6

Prostearyl?15 8.0

Beeswax 0.5

Stearic oxygen base dimethicone 3.0

Propylene glycol 3.0

Carbopol?941 0.25

Trolamine 0.25

N, N '-two-tyrasamine-urea (IV) 0.007

Water, sanitas and flavouring agent qs 100g

Embodiment 8: the milk sap of whitening G/100g

Deionized water qs100

Carbopol?Ultrez?10 0.40

Glycerine 5.00

Potassium sorbate 0.10

Phenova 0.80

Crodamol?OP 4.00

Crodacol?CS90 0.50

Crodamol?ML 0.30

Crillet?1 1.00

DC?345 2.00

Pemulen?TR2 0.20

NaOH?30％ 0.60

Acetate 0.05

Two-tosyl group-tyrasamine (V) 0.20

Flavouring agent qs

Embodiment 9: lightization hand frost G/100g

Part A

Deionized water qsp 100

Ultrez 10 (carbomer) 0.15

Part B

Sanitas 0.80

Glycerine 10.00

Portion C

Crodacol C90 (hexadecanol) 3.00

Crill?3 3.00

Crillet?3 2.50

DC200 (dimethicone) 2.00

Shea butter (Butyrospermum parkii) 2.00

Crodamol?GTCC 6.00

Part D

Potassium sorbate 0.10

Part E

Deionized water 2.00

Sodium hydroxide 30% 0.15

Part F

N-succinyl-tyrasamine (II) 0.01

Part G

Kojic acid 0.05

Section H

Whitfield's ointment 0.05

Part I

Flavouring agent 0.10

In water, disperse Ultrez 10, place 20 minutes (part A).B is mixed into part A with part.

Heating (A+B) is to 75 ℃ in water-bath.Hot spots is poured part (A+B) into for C to 75 ℃.Then, pour part D into, mix.Add part E at about 50 ℃, add F then and go into (A+B+C+D).G to 60 ℃ of hot spots also adds in (A+B+C+D+E+F).Insert the section H that is heated to 60 ℃, add part I then.

Embodiment 10: suppress melanochrome synthetic (external)

The effect that test products generates for melanochrome on the stable cell line of cultivating.

The melanocyte of cell strain B16 is used for research.Cell strain B16 routine is used to test the melanochrome level and changes.

Described cell was cultivated in test products 48 hours, and control cells single culture in substratum.

Through 48 hours, make cell through after lysis is dissolved in sodium hydroxide, measure the total melanochrome (phaeomelanin and eumelanin) in the described cell.This analyzes and is colorimetric analysis.

The melanochrome level that described test products is produced under various concentration is compared with the melanochrome level that control cells is produced.Data are with the protein content normalizing of sample.

Among the figure one, shown the variation of the melanochrome generation that is exposed to kojic acid 48 hours (positive control) on the one hand, and shown that on the other hand the melanochrome synthetic that is exposed to multiple tyrasamine derivative changes.Can observe, be exposed to described product after 48 hours, the restraining effect that melanochrome generates depends on test concentrations.Described restraining effect changes in-5 to-70% scopes.This proves that all compounds all have the melanogenic activity of the inhibition that receives much attention, and it is better than the activity of tyrasamine itself, particularly under lower concentration (≤0.8 mmole/liter).

These derive from new compound and its make-up composition of tyrasamine, and the embodiment of their purposes is not restrictive.

Described makeup or dermal drug composition can also be used to prepare pharmaceutical prod, are used for skin care, particularly make skin Lighteningization and skin be exposed to natural or artificial uviolizing following time and reduce that it is painted.In addition, described compound and composition as theme of the present invention can be used for making cloth, fabric and the clothing with makeup effect, especially for light skin or hair.

New tyrasamine derivative (1/4)

N-ethanoyl-tyrasamine

N-glycyl-tyrasamine

N-maleoyl-tyrasamine

N-glutaryl-tyrasamine

The soft ester acyl-tyrasamine of N-

The soft ester acyl-tyrasamine of O-/HBr

The N-tosyl group, N '-tyrasamine-urea

New tyrasamine derivative (2/4)

N, N '-two-tyrasamine-urea

N-benzoyl-tyrasamine

N-tosyl group-tyrasamine

N-Ben Yajiaji-tyrasamine

N, O-di-acetyl-octopamine

N-tosyl group-octopamine

N-methylsulfonyl-tyrasamine

New tyrasamine derivative (3/4)

N-2-(4-hydroxyphenyl)-ethyl-glycine

N-g-hydroxyl-butyryl-tyrasamine

Two-oxo tyrasamine

N-oxalyl-tyrasamine

Tyrasamine-sulfonate

The N-ethyl, N-(N-dimethyl, 3-aminopropyl), N-tyrasamine base-guanidine

2-sulfo group-N-benzoyl-tyrasamine

New tyrasamine derivative (4/4)

N-trifyl-tyrasamine

N-ethanoyl-octopamine

Two-tosyl group-tyrasamine (N, N or N, O)

N-benzoyl-tyrasamine

N, O-di-acetyl-octopamine

N-succinyl--tyrasamine

Claims (22)

1. the compound that has general formula I:

Wherein:

Radicals X is-NR ³R ⁴Or-N=CR ⁵R ⁶,

R ¹And R ²Each group can be identical or different, be hydrogen atom or halogen atom, perhaps alkyl, aryl, aralkyl, acyl group, alcohol or alkoxyl group,

R ³And R ⁴Each group can be identical or different, be hydrogen atom or alkyl, aryl, aralkyl, acyl group, alkylsulfonyl or glycosyl,

R ⁵And R ⁶Each group can be identical or different, be hydrogen atom or alkyl, aryl or aralkyl,

And its makeup category of this compound of Formula I is acceptable, with the optically pure isomer of acid formation or the salt of isomer mixture form,

In the compound defined above, what need eliminating is: tyrasamine (general formula I, X=-NR ³R ⁴, R ¹=R ²=R ³=R ⁴=H) with by its OH or NH ₂On the group keyed jointing any straight or branched, saturated or unsaturated, can by hydroxylation contain sulphur or not sulfur-bearing, by 1 to 24 formed derivative of the alkyl chain that carbon atom is formed, and synephrine (general formula I, X=-NR ³R ⁴, R ¹=OH, R ²=R ³=H, R ⁴=CH ₃).

2. compound as claimed in claim 1, wherein said compound is N-succinyl--tyrasamine, has following structural formula II:

Or their any salt.

3. compound as claimed in claim 1, wherein said compound are N-tosyl group tyrasamines, have following structural formula:

Or their any salt.

4. compound as claimed in claim 1, wherein said compound is N, N '-two tyrasamine urea has following structural formula IV:

Perhaps their any salt.

5. compound as claimed in claim 1, wherein said compound are two tosyl group tyrasamines, have following structural formula V:

Perhaps their any salt.

6. the preparation method of compound shown in structural formula I, II, III, IV or V; it is characterized in that; described method comprises the coupled reaction of tyrasamine or its salt; it is having alkali or is not having in the presence of the alkali; with carbonyl or sulfonyl-derivatives, the coupling reagent that uses in peptide is synthetic exists or does not react under the existence condition.

7. the preparation method of compound shown in structural formula I, II, III, IV or V; it is characterized in that; described method comprises the coupled reaction step of octopamine or its salt; it is having alkali or is not having in the presence of the alkali and coupling reagent existence that carbonyl or sulfonyl-derivatives use in peptide is synthetic or do not react under the existence condition.

8. as claim 6 or 7 described preparation methods, wherein said carbonyl or sulfonyl-derivatives are aldehyde, active or nonactive ester, carboxylic acid or SULPHURYL CHLORIDE, acid anhydrides or isocyanate.

9. compound shown in structural formula I, II, III, IV or V is characterized in that, described compound is made by tyrasamine salt by claim 7,8 method.

10. makeup or dermal drug composition, by makeup category vehicle acceptable, independent or merging form with have following compound in structural formula I and form:

Wherein:

Radicals X is-NR ³R ⁴Or-N=CR ⁵R ⁶,

R ¹And R ²Each group can be identical or different, be hydrogen atom or halogen atom, perhaps alkyl, aryl, aralkyl, acyl group, alcohol or alkoxyl group,

R ³And R ⁴Each group can be identical or different, be hydrogen atom or alkyl, aryl, aralkyl, acyl group, alkylsulfonyl or glycosyl,

R ⁵And R ⁶Each group can be identical or different, be hydrogen atom or alkyl, aryl or aralkyl,

And its makeup category of compound in structural formula I is acceptable, with the optically pure isomer of acid formation or the salt of isomer mixture form,

In the compound defined above, what need eliminating is: tyrasamine (general formula I, X=-NR ³R ⁴, R ¹=R ²=R ³=R ⁴=H) pass through its OH or NH with tyrasamine ₂On the group keyed jointing any straight or branched, saturated or unsaturated, can by hydroxylation contain sulphur or not sulfur-bearing, by 1 to 24 formed derivative of the alkyl chain that carbon atom is formed, and synephrine (general formula I, X=-NR ³R ⁴, R ¹=OH, R ²=R ³=H, R ⁴=CH ₃).

11. composition as claimed in claim 12, wherein said compound concentrations be 0.0001 (w/w) to 50% (w/w), be preferably 0.001 (w/w) to 20% (w/w).

12. as claim 10 or 11 described compositions, wherein said compound is (structural formula I, the X=-NR of the octopamine shown in the structural formula I ³R ⁴, R ¹=OH, R ²=R ³=R ⁴=H), and or N-succinyl--tyrasamine, or have the N-tosyl group tyrasamine of following structural formula II I, or have the N of following structural formula IV with following structural formula II, N '-two tyrasamine urea, or have two tosyl group tyrasamines of following structural formula V,

Or their any salt.

13. each the described composition as claim 10 to 12 is characterized in that described composition comprises at least a keratolytic and/or decorticating agent.

14. composition as claimed in claim 13, it comprises and accounts for composition weight 0.001% to 10%, and is preferred 0.1% to 5%, more preferably 0.5% to 2% described keratolytic and/or decorticating agent.

15. each the described composition as claim 10 to 14 is characterized in that described group comprises at least a skin lightener.

16. composition as claimed in claim 15, it comprises and accounts for composition weight 0.001% to 10%, and is preferred 0.02% to 5%, more preferably 0.05% to 2% described skin lightener.

17. each described composition as claim 10 to 16, it also comprises at least a supplementary component, be selected from: analeptic, the skin anti-aging agent, the skin moisturizing agent, anti-wrinkle agent, anti-atrophy agent, the skin smooth agent, antiseptic-germicide, anti-mycotic agent, antiparasitic, biocide, anti-inflammatory agent, the anti-agent of itching, external application narcotic, antiviral agent, keratolytic, free-radical scavengers, the anti-bleeding of sebum, the agent of anti-bits, the differentiation of adjusting skin, propagation or pigmentation agent and promotion infiltration, the preparation of decortication, discoloring agent or tinting material, anti-glycosylation agent, fastening agent, promote corium or epidermis to synthesize and/or prevent the preparation of its degeneration; Promote fibroblast and/or keratinocyte propagation or promote the preparation that keratinocyte breaks up; Muscle speeds to delay agent; Anti-pollutant and/or antifree radical agent; Slender dose, anti-liparitosis agent act on microcirculatory preparation; Act on the metabolic preparation of cellular energy, sanitising agent, hair conditioner, the agent of hair random sample, hair tonic promotor, shading and/or sun screening compound, the makeup agent, washing agent, medicine, emulsifying agent, softener, sanitas, the deodorant activities composition, the makeup acceptable carrier, tensio-active agent, abrasive, absorption agent, the aesthetic feeling component, for example fragrant agent, freshen toner/tinting material, essential oil, the skin feel agent, the used for cosmetic astringent matter, anti-acne agents, the agent of resistive connection group, foam reducing composition, antioxidant, tackiness agent, biotic additives, enzyme, enzyme inhibitors, enzyme-containing formulation, coenzyme, plant milk extract, botanical derivative, the plant tissue extract, plant seed extract composition, vegetables oil, vegetable drug, the vegetable drug extract, ceramide, peptide, buffer reagent, swelling agent, sequestrant, the chemical derivative, tinting material, trichogen, the used for cosmetic biocide, denaturing agent, the medicine astringent matter, the external application pain killer, membrane-forming agent or pleurodiaphragmatic in terspace material, for example, the polymkeric substance that helps composition film forming characteristics and affinity, season derivative, increase the affinity agent, the emulsifying agent, the pH regulator agent, volatilizer, the agent of disappearing, sequestering agent, skin bleaching and brightening agent, the agent of brownization of skin, skin conditioning agent (for example, wetting agent, comprise and mix type and dead front type wetting agent), skin smooth agent and/or analeptic and derivative, skin treatment agents, viscosifying agent, with VITAMIN and derivative thereof, decorticating agent, moistening agent, solidifying agent, the lignanoids material, sanitas, UV light absorber, cytotoxin, antitumor agent, the fat melting activeconstituents, clouding agent, viscosity modifier, dyestuff, non-volatile solvent, thinner, pearlescent additive, pore forming material, vaccine and their mixture.

18. as any described composition in the claim 10 to 17, the wherein said component of selecting is selected from: osamine, glycosamine, D-glycosamine, N-acetyl glucosamine, N-ethanoyl-D-glycosamine, mannosamine, N-acetylmannosamine, GalN, N-acetylgalactosamine, vitamins B ₃With its derivative; niacinamide usp; sodium dehydroacetate; dehydroacetic acid (DHA) and its salt; plant sterol; salicylic acid compound; Hexamine; two alkanoyl oxyproline compounds; soybean extraction and derivative; equol; isoflavones; flavonoid compound; Phytantriol; farnesol; Geraniol; peptide and their derivative; two-; three-; four-; five-; with six peptides and their derivative; Methionin-Threonine-Threonine-Methionin-Serine; soft ester acyl-Methionin-Threonine-Threonine-Methionin-Serine; carnosine; N-acyl amino acid compound; retinoid; Vitamin A propionate; Vogan-Neu; retinyl palmitate; retinoic acid ester; retinene; vitamin A acid; water-soluble vitamins; ascorbate salt; vitamins C; xitix; the ascorbigen glucosides; anti-bad blood acyl cetylate; magnesium ascorbyl phosphate; STAY-C 50; the salt of VITAMIN and its derivative; pro-vitamin and their salt and derivative; the ethyl panthenol; vitamins B; the vitamins B derivative; vitamins B ₁, vitamins B ₂, vitamins B ₆, vitamins B ₁₂VITAMIN, the vitamin K derivative, pantothenic acid and its derivative, general ethene ether, panthenol and its derivative, panthenol, vitamin H, amino acid and their salt and derivative, water-soluble amino acids, asparagine, L-Ala, indoles, L-glutamic acid, the water-insoluble VITAMIN, vitamin A, vitamin-E, vitamin F, vitamins D, one-, two-, and triterpenes, β-ionol, cypress camphor, with their derivative, water-insoluble amino acid, tyrosine, tryptamines, butylated hydroxytoluene, butylated hydroxyanisole, wallantoin, the tocopherol nicotinate, tocopherol, Renascin, soft ester acyl-glycine-Histidine-Methionin, plant sterol, hydroxy acid, oxyacetic acid, lactic acid, lactobionic acid, ketone acid, pyruvic acid, phytic acid, Ultrapole L, toluylene, laurate, trans-resveratrol, phytokinin, zeatin, dimethylaminoethanol, native peptides, soybean peptides, the salt of saccharic acid, manganese gluconate, Zinc Gluconate, particulate material, dye material, natural pigment, the pyridone thanomin, 3,4,4 '-trichlorocarbanilide, neko, Zinc Pyrithione, Resorcinol, kojic acid, xitix, magnesium ascorbyl phosphate, the ascorbigen glucosides, how hot pyrrole is, aloe, terpenol, wallantoin, Hydagen B, Rizinsan K2 A2, R-Glyceric acid, sorbose alkyd, tetramethylolmethane acid, tetramethyleneimine ketone acid and its salt, Protosol, erythrulose, Glycerose, winestone aldehyde, Syzygium aromaticum stem oil, menthol, camphanone, eucalyptus oil, oxymethoxyallylbenzene, the peppermint lactate, the witch hazel overhead product, Eicosene and nvp copolymer, butyl carboxylamine iodo propyl ester, polysaccharide, indispensable fatty acid, salicylate, glycyrrhetinic acid, carotinoid compounds, acyl sphingosine and standard-acyl sphingosine, lipid complex, be generally the oil of natural origin, for example shea butter, Prunus amygdalus oil, Oenothera oil, Prunus oil, plam oil, monoi oil, HEPES; L-2-oxygen thia azoles alkane-4-carboxylic acid; O-decoyl-6-D-maltose; Methylglycine oxalic acid, steroid, for example derivative of diosgenin and DHEA; N-ethoxy carbonyl-4-para-aminophenol, Fructus Rubi extract; Plant hormone; Yeast extract; Algae Extract; Soybean, lupine, Zea mays and/or Semen Pisi sativi extract; Alverine and its salt, particularly alverine Citrate trianion, Flower of Chinese Peashrub extract and horse-chestnut extract and their mixture.

19. as before any described composition of claim, wherein said compound is with solution, dispersion, milk sap, lotion or form of powder are used separately or are used as the premixture in the vehicle, described vehicle is the high score ascus for example, micro-capsule, or nanocapsule, the high score bulbec, microballoon or nanometer ball, liposome, oleosome or chylomicron, polymeric particles, particulate, or nano particle, or polymer sponge, scintilla sponge or nanosponges, or be adsorbed in the powder of organic polymer, talcum powder, bentonite, or on other inorganic support.

20. as each described makeup or dermal drug composition in the claim 10 to 19, wherein said composition has following form, frost, washing lotion, ointment, breast, gel, milk sap, dispersion, solution, suspension, sanitising agent, foundation cream, anhydrous preparation (club, particularly lipstick, health massage oil and bath oil), shower and bath gels, shampoo and scalp treatment conditioning liquid, the frost of nursing skin or hair or conditioning liquid, sun screen, sunscreen or sunscreen, artificial sun-screening agent, artificial sunscreen or artificial sunscreen, blow frost or foam recklessly, after shave lotion, mascara or nail varnish, lipstick, skin " essential oil ", serum, jointing material or absorbing material, transdermal patch, powder, skin lotion, milky lotion, skin cream, the spray and the finish that are used for health and shower, the foundation cream color base, brilliantine, colloid, briquet or solids suspension, eyebrow pencil, but spray preparations, can brush preparation.

21. be used to reduce the purposes that melanochrome generates as any described makeup or dermal drug composition in the claim 10 to 20, especially for the light colour of skin, desalination senile plaque, homogenizing pigmenting of skin or any pigmentation that comprises hair relevant of lightization with melanochrome.

22. the purposes of claim 1 or 5 or 9 described compounds or octopamine, it separately or merge and be used for described makeup of one of claim 10 to 21 or dermal drug composition, the pharmaceutical prod that is used to be prepared as following purpose and designs: skin care, reduce melanochrome and generate, particularly skin Lighteningization and reducing is exposed to painted under natural or the artificial uviolizing.

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