CN1933801A - Use of (2-hydroxyphenyl) alcohols, and cosmetic or therapeutic formulations containing said compounds - Google Patents

Use of (2-hydroxyphenyl) alcohols, and cosmetic or therapeutic formulations containing said compounds Download PDF

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Publication number
CN1933801A
CN1933801A CNA2005800088011A CN200580008801A CN1933801A CN 1933801 A CN1933801 A CN 1933801A CN A2005800088011 A CNA2005800088011 A CN A2005800088011A CN 200580008801 A CN200580008801 A CN 200580008801A CN 1933801 A CN1933801 A CN 1933801A
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acid
unbranched
replacement
side chain
alkyl
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加布里埃莱·菲尔哈伯
卡林·雅各布斯
海因茨-于尔根·伯特伦
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Haarmann and Reimer GmbH
Symrise AG
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/347Phenols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • A61Q5/08Preparations for bleaching the hair

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  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Cosmetics (AREA)

Abstract

The invention relates to the use of compounds from the group of (2-hydroxyphenyl) alcohols and the derivatives thereof for bleaching skin and/or hair as well as cosmetic or therapeutic formulations containing said compounds from the group of (2-hydroxyphenyl) alcohols. According to a first embodiment of the invention, a compound of formula (I), wherein n = 1-10, R<1> represents a substituent from the group comprising H, branched or straight C1-C14 alkyl or alkenyl, substituted or unsubstituted arylalkyl, cyclohexyl, cyclopentyl, substituted or unsubstituted phenyl, substituted or unsubstituted monosaccharide, SO3, (CH2)1-10OH, COR, SiRR'R'', SR, PO3RR', or formula (Ia), R, R', R'' independently representing H, C1-C14 alkyl, C1-C14 alkenyl, C1-C14 alkynyl, cyclohexyl, cyclopentyl, substituted or unsubstituted phenyl, or a heterocyclic ring, and R<2> represents an enzymatically cleavable substituent or a substituent selected independently of R<1 >from the group comprising H, branched or straight C1-C14 alkyl or alkenyl, cyclohexyl, cyclopentyl, substituted or unsubstituted phenyl, is used for bleaching skin and/or hair.

Description

The purposes of (2-hydroxyphenyl) alcohol and cosmetics that contain this chemical compound or treatment preparation
The present invention relates to (2-hydroxyphenyl) pure compounds of group and derivant thereof and be used to make thin out purposes of skin and/or chroma of hair and cosmetics or the treatment preparation that contains described chemical compound.
Make the thin out effective ingredient of skin colour intervene melanin metabolism or melanin catabolism with arbitrary form.Melanin normally brown forms in the dermal melanin cell to black, is transferred to keratinocyte, and gives skin or hair color.In mammal, the ArAA that the eumelanin of pitchy-black is mainly replaced by hydroxyl for example L-tyrosine and L-DOPA forms, and yellow to red is had a liking for the chrome black pigment and formed (Cosmetics ﹠amp by sulfur-containing molecules in addition; Toiletries 1996,111 (5), 43-51).Originate in L-tyrosine, form L-3 by cupric key enzyme tryrosinase, 4-dihydroxyphenylalanine (L-DOPA), and change into dopachrome (dopachrome) once more by tryrosinase.By the catalytic step of a series of various enzymes, the oxidized formation melanin of dopachrome.
Use skin whitener that multiple reason is arranged: if for a certain reason, form melanic melanocyte uneven distribution in the application on human skin, mottle will occur, this mottle is more shallow or dark than surrounding skin field color.For overcoming this problem, skin and hair brightening agent are sold, and it helps this mottle of balance to small part.In addition, many people have the needs of its natural low and deep colour of skin of brilliant white or prevention chromogenesis.This just needs as safe as a house and effective skin and hair brightening agent.Many skins and hair brightening agent more or less contain strong tyrosinase inhibitor.Yet this only is to make a skin and a thin out possibility approach of chroma of hair.
In addition, the ultra-violet absorption material also is used to prevent the increase that formed by the skin pigment that ultraviolet light causes.Yet this is pure physics inducement effect, must be distinguished the biological agent that melanocyte forms with skin whitener, and it also can detect when lacking ultraviolet light.And UV absorbent can not make skin really bleach, and only is the increase that the skin pigment that suppresses to be caused by ultraviolet light forms.
Particularly, use for example arbutin, vitamin C, ascorbic acid derivates ascorbic palmitate, kojic acid and kojic acid derivative Palmic acid kojic acid diester for example for example of hydroquinone, hydroquinone derivatives in the preparation in the cosmetics that make the thin out commercial practices of skin and chroma of hair or treatment.
Hydroquinone is a kind of the most frequently used skin and hair brightening agent.Yet this chemical compound has cytotoxin effect and chafe to melanocyte.For example, no longer ratify this preparation in Europe, Japan and South Africa for this reason be used for cosmetics.In addition, hydroquinone is very easy to oxidation and very unstable in cosmetic formulations.
Arbutin is a hydroquinone glucoside, its in position hydrolysis form hydroquinone, therefore equally with hydroquinone aspect toxicology queried.
Vitamin C and ascorbic acid derivates only have inadequate effect to skin.And they directly do not work as tyrosinase inhibitor, but reduce biosynthetic coloured intermediate product stage of melanin.
Kojic acid (5-hydroxyl-2-methylol-pyrokomane) is a tyrosinase inhibitor, and it is by the catalytic action of the copper atom inhibitory enzyme in the chelatase; It is used in commercial skin and the hair brightening agent, but it has the probability of height sensitization and causes contact allergy.
Salicin is as preventing wrinkle, aging, xerosis cutis and coarse activating agent and as prevention of inflammation with promote the protective agent of wound healing to be widely used in cosmetics.
In JP 2002275060 A2, salicylic acid and the saligenin derivant effective ingredient as the chafe brown stain has been described.
Funayama et al. (Seibutsu Kogaku Kaishi (1997), 75 (5), 333-337) detected of the inhibition of various polyphenol glucosides, comprised 2-hydroxybenzylalcohol-α-D-glucoside (α-salicin) the melanin generation of B16 mouse black-in tumor cell.Yet, do not find the inhibitory action that this last chemical compound generates melanin in the B16 cell.
The objective of the invention is to remedy the deficiencies in the prior art, the highly effective skin brightening agent of the celelular mechanism of restraint of tyrosinase preferably or other chromogenesis particularly is provided.
According to a first aspect of the invention, by use have chemical formula (I) be used for make skin and/or the thin out chemical compound of chroma of hair reach specific purpose,
Figure A20058000880100061
Wherein:
n=1-10,
R 1Be selected from and comprise H, side chain or unbranched C 1-C 14Alkyl, side chain or unbranched C 2-C 14Thiazolinyl, side chain or unbranched C 2-C 14Alkynyl, replacement or unsubstituted aryl alkyl, cyclohexyl, cyclopenta, replacement or unsubstituted phenyl, replacement or unsubstituted monosaccharide, SO 3H, SO 3Na, (CH 2) 1-10OH, COR, SiRR ' R ", PO 3HNa, PO 3Na 2With Set,
Wherein R, R ', R " separate being selected from comprise H, C 1-C 14Alkyl, C 2-C 14Thiazolinyl, C 2-C 14Alkynyl, cyclohexyl, cyclopenta, replacement or unsubstituted phenyl and heterocyclic set and
R 2Be enzymatic cutting substituent group or be selected from and comprise H, side chain or unbranched C 1-C 14Alkyl, side chain or unbranched C 2-C 14Thiazolinyl, side chain or unbranched C 2-C 14The set of alkynyl, cyclohexyl, cyclopenta, replacement and unsubstituted phenyl or replacement or unsubstituted aryl alkyl.
Chemical compound with chemical formula (I) comprises their stereoisomer and any mixture of tautomer and these isomers.Chemical compound with chemical formula (I) also comprises all the relevant salt, particularly alkali metal and the salt of alkaline-earth metal.
Find in our research that surprisingly the chemical compound with chemical formula (I) used according to the invention suppresses the chromogenesis of melanocyte especially effectively.Particularly, many more effective than kojic acid basically according to having in (2-hydroxyphenyl) of the present invention alcohol.Therefore with they as cosmetics (comprising dermatological) with and treatment be very suitable with the effective ingredient in skin and the hair brightening agent.
Can be used for making in the thin out chemical compound set of skin and chroma of hair preferred such chemical compound, wherein R according to the present invention with chemical formula (I) 2Be to be selected to comprise SO 3H, SO 3Na, (CH 2) 1-10OH, COR, PO 3HNa and PO 3Na 2The enzymatic cutting substituent group of set, wherein separate being selected from of R, R ' comprises H, C 1-C 14Alkyl, C 2-C 14Thiazolinyl, C 2-C 14Alkynyl, cyclohexyl, cyclopenta, replacement or unsubstituted phenyl and heterocyclic set, perhaps R 2Be enzymatic cutting, replacement or unsubstituted monosaccharide, be selected from the set that comprises glucose, mannose or galactose.
The monosaccharide of final name is preferably the pyranose form.Substituted monosaccharide specifically comprises 6 '-O-acetyl pyranose, 6 '-O-benzoyl pyranose, 2 '-O-acetyl pyranose and 2 '-O-benzoyl pyranose.
In addition, in chemical compound set with chemical formula (I)---particularly the enzymatic in above-mentioned form cuts substituent R 2Existence under---preferred such chemical compound, wherein:
n=1-4,
R 1Be selected from and comprise H, side chain or unbranched C 1-C 14Alkyl, side chain or unbranched C 2-C 14Thiazolinyl, side chain or unbranched C 2-C 14Alkynyl, replacement or unsubstituted aryl alkyl, replacement or unsubstituted phenyl, replacement or unsubstituted monosaccharide, (CH 2) 1-10OH, COR, SR, PO 3RR ' and
Figure A20058000880100081
Set,
Wherein separate being selected from of R, R ' comprises H and C 1-C 14The set of alkyl.
The chemical compound that below has chemical formula (I) also is preferred, wherein
n=1-4,
R 1Be selected from and comprise H, side chain or unbranched C 1-C 14Alkyl, side chain or unbranched C 2-C 14Thiazolinyl, side chain or unbranched C 2-C 14Alkynyl, replacement or unsubstituted aryl alkyl, replacement or unsubstituted phenyl, replacement or unsubstituted monosaccharide, (CH 2) 1-10OH, COR, SR, PO 3RR ' and Set, wherein separate being selected from of R, R ' comprises H and C 1-C 14The set of alkyl and
R 2Be selected from and comprise H, side chain or unbranched C 1-C 14Alkyl, side chain or unbranched C 2-C 14Thiazolinyl, side chain or unbranched C 2-C 14The set of alkynyl, replacement or unsubstituted phenyl.
Scheme or except above-mentioned preferred compound as an alternative, in can being used for making the thin out chemical compound set of skin and chroma of hair according to the present invention with chemical formula (I), the preferred wherein chemical compound of n=2-10, particularly n=2-4.
Particularly make skin and/or thin out saligenin (2-hydroxy-benzyl alcohol), the Forlan glycosides (fragilin of chroma of hair by use, 6 '-O-acetyl salicin), populoside (6 '-O-benzoyl salicin), quaking aspen glycosides (tremuloidin, 2 '-the benzoyl salicin), salicortin (salicortin), 2-O-acetyl salicortin or Tremulacin (tremulacin, 2-O-benzoyl salicortin) reach specific purpose.In the invention is intended to, particularly preferably be salicin ((methylol)-phenyl-β-D-glycopyranoside) most.
Second aspect of the present invention relates to cosmetics or treatment preparation, particularly topical cosmetic preparation, and it contains has one or more of amount of the thin out effect of color and luster to have the chemical compound of chemical formula (I) to skin and/or hair.More than the narration selected all about substituent group also be applicable to this aspect naturally.
According to cosmetics of the present invention or treatment preparation by known produced in conventional processes itself, make be integrated in according to one or more (2-hydroxyphenyl) alcohol used in the present invention have that tradition is formed and also be can be used for treating except making the thin out effect of skin and chroma of hair, maintenance and cleaning skin or hair and as in the cosmetics or dermatological formulation of modifying the cosmetic product in the property cosmetics.
Therefore the invention still further relates to (particularly) topical cosmetic or treatment preparation, particularly skin and the hair brightening agent of cosmetics (comprising dermatological) usefulness, except other different traditional constituent, it also comprises (2-hydroxyphenyl) alcohol according to effective dose used in the present invention.According to preparation of the present invention, based on the total formulation weight amount, preferably contain (2-hydroxyphenyl) alcohol that 0.01 weight %-30 weight % the present invention uses, more preferably 0.01-20 weight %, but preferred especially 0.01 weight %-5 weight %, and can take following form: " Water-In-Oil ", " oil-in-water ", " W/O/W ", " Water-In-Oil bag oil " emulsion, the PIT emulsion, the Pickering emulsion, the low oil content emulsion, microemulsion, gel, solution, for example oil, alcohol or silicone oil, rod, soap, aerosol, the make up dipping solution of tissue paper of spray or foams or be used to.It also is favourable using (2-hydroxyphenyl) alcohol with capsule form, for example with the form of gelatin, waxy substance, liposome or cellulose capsule.The auxiliary agent that comprises in other traditional cosmetics and the amount of additive based on the total formulation weight amount, can be 5-99 weight %, preferred 10-80 weight %.Can also contain based on the total formulation weight amount the paramount water that reaches 99.99 weight %, preferred 5-80 weight % in the preparation.
Do not mention decolourization or their application in skin and hair brightening agent of chemical compound in the prior art with chemical formula (I).
(2-hydroxyphenyl) alcohol that has chemical formula (I) according to the present invention can extract that for example glycosidase or lipase produce from 2-hydroxybenzylalcohol enzymatic from for example bark of willow (purple osier or Salix daphinoides) with by chromatography or two-phase extraction method purification or by hydrolytic enzyme.
According to cosmetics of the present invention or treatment (particularly local) preparation, particularly skin and hair brightening agent, can contain cosmetic additive and additive, for example tradition is used for the material of series preparation down, sunscreen for example, antiseptic, bactericide, antifungal, antiviral, coolant, anthelmintic (DEET for example, IR 3225, Dragorepel), plant extract, antiinflammatory, promote the material (for example chitin or chitosan and derivant thereof) of wound healing, film forming matter (for example polyvinylpyrrolidone or chitosan or derivatives thereof), traditional antioxidants, vitamin (for example vitamin C and derivant, tocopherol and derivant, vitamin A and derivant), 2-hydroxy carboxylic acid (citric acid for example, malic acid, L-, D-or dl-lactic acid), dye agent (for example Juglans regia L. extract or dihydroxy acetone), skin care agent (cholesterol for example, ceramide, intend ceramide)/softening, the skin moistening and/or the material of preserving moisture (for example glycerol or carbamide), fat, oil, satisfied fatty acid, single unsaturated or polyunsaturated fatty acid, alpha-hydroxy acid, polyhydrony fatty acid or derivatives thereof (linoleic acid for example, alpha-linolenic acid, gamma-Linolenic acid or arachidonic acid and natural or synthetic ester thereof), wax or other traditional used for cosmetic or dermatosis are for example pure with the preparation composition, polyhydric alcohol, polymer, foam stabiliser, electrolyte, organic solvent, silicone derivative or chelating agen (for example ethylenediaminetetraacetic acid and derivant), dandruff removing agent (Ke Ningbasuo for example, ketoconazole, Piroctone Olamine, pyrrole sulfur zinc), hair care product, spice, the control foaming material, dyestuff, pigment with pigmentation, thickening agent, the surface active substance, emulsifying agent, plant part and plant extract (Arnica montana for example, Aloe, palpus shape lichens (beardlichen), Caulis Hederae Sinensis, stinging nettle, Radix Ginseng, Flos Impatientis, Chamomile, Flos Tagetis Erectae, Herba Rosmarini Officinalis, Salvia japonica Thunb., Herba Equiseti Hiemalis or Herba thymi vulgaris), animal extracts is royal jelly for example, propolis, protein, protolysate, yeast extract, Flos lupuli (Flos Humuli Lupuli) and Semen Tritici aestivi extract, peptide or thymic extract.
Rely on the characteristic of specific products, those skilled in the art are by simple trial-and-error method, are easy to the auxiliary agent that used for cosmetic under definite every kind of situation or dermatosis use and the amount of additive and spice.
In the above-mentioned example, with the amount that makes the thin out effective ingredient of skin and chroma of hair in the preparation (one or more chemical compounds), based on the total formulation weight amount, can be 0.01-30 weight % according to used for cosmetic of the present invention and dermatosis, preferred 0.01-20 weight %, preferred especially 0.01-5 weight %.
Also can preferably contain other effective ingredient according to preparation of the present invention, it is thin out by chemistry or natural mode chafe and chromotrichia or color and luster.By this way, can obtain faster, based on the effect of cooperative effect.Particularly preferably be tryrosinase substrate or substrate analogue such as L-tyrosine at this; L-DOPA or L-dihydroxyphenylalanine; tyrosinase activity or expression stimulus object are such as theophylline; caffeine; the proopiomelanocortin peptide is such as thyroliberin (ACTH); α-melanotropin (α-MSH); the material of its peptide analogues and other and melanin cortin receptors bind; purine; pyrimidine; folic acid; phenylalanine derivative is phenylalanine endecatylene amide for example; DG; aliphatic series or cyclic diols; psoralen; prostaglandin and analog thereof; adenylate cyclase activating agent and activate chemical compound that melanosome shifts to horn cell such as serine protease or PAR-2 receptor stimulating agent; chrysanthemum species plant or plant part extract; Juglans regia L. extract; Erythrulose and dihydroxy acetone.
Yet, also can contain for example NeoHeliopans  of ultraviolet light,long wave and/or UV-B medium in addition according to preparation of the present invention, the total amount of medium wherein, based on the total formulation weight amount, can be 0.1-30 weight %, preferred especially 0.2-10 weight %, especially 0.5-5 weight % wherein obtain for example skin and hair photoprotection agent.
Suitable light stabilizer for example organic uv absorbers class comprises 4-amino benzoic Acid and derivant, salicyclic acid derivatives, benzophenone derivates, dibenzoylmethane derivative, the diphenylacrylate ester, 3-imidazol-4 yl acrylic acid and ester thereof, benzofuran derivatives, phthalic acid benzal ester derivant, polymerization UV absorbent (containing one or more organosilicon radicals), cinnamic acid derivative, camphor derivatives, triphenylamine-s-pyrrolotriazine derivatives, 2-hydroxy-phenyl benzotriazole derivant, Phenylbenzimidazolesulfonic acid derivant and salt thereof, Antisolaire, benzotriazole derivatives, indole derivatives.
Below for being not restricted to this certainly by the UV absorbent list that the invention is intended to use.
The 4-amino benzoic Acid, the 4-benzocaine, 4-dimethylaminobenzoic acid-2-Octyl Nitrite, the 4-glyceryl aminobenzoate, the high  ester of salicylic acid, salicylic acid-2-Octyl Nitrite, triethanolamine salicylate, 4-isopropyl benzyl salicylate, Antisolaire, the diisopropyl ethyl cinnamate, p-methoxycinnamic acid-2-Octyl Nitrite, the diisopropyl methyl cinnamate, iso-amyl p-methoxycinnamate, the p-methoxycinnamic acid diethanolamine salt, the p-methoxycinnamic acid isopropyl ester, 2-ethylhexyl-2-cyanogen-3,3-diphenylacrylate ester, ethyl-2-cyanogen-3,3 '-the diphenylacrylate ester, 2-Phenylbenzimidazole-5-sulfonic acid and salt thereof, 3-(4 '-trimethylammonium) benzylidene-camphane-2-ketone methylsulfuric acid ester, terephthalylidene two camphane sulfonic acid and salt, 4-normal-butyl-4 '-the methoxy dibenzoyl methane, β-imidazoles-4 (5)-acrylic acid (urocanic acid), 2-hydroxyl-4-methoxy benzophenone, 2-hydroxyl-4-methoxy benzophenone-5-sulfonic acid, dihydroxy-4-methoxy benzophenone, 2, the 4-dihydroxy benaophenonel, tetrahydroxybenzophenone, 2,2 '-dihydroxy-4,4 '-the dimethoxy benzophenone, Octabenzone, 2-hydroxyl-4-methoxyl group-4 '-the methyldiphenyl ketone, 3-(4 '-sulfo group) benzylidene-camphane-2-ketone and salt thereof, 3-(4 '-the methylbenzene methylene) Camphora, 3-benzylidene Camphora, 3,3 '-(1,4-phenylene two methines)-two-(7,7-dimethyl-2-oxo-bicyclo--[2.2.1] heptane-1-pyrovinic acid and salt thereof, 4-isopropyl diphenyl formyl methane, 2,4,6-triphen amido-(right-carbonyl-2 '-ethylhexyl-1 '-oxygen)-1,3, the 5-triazine, phenylene-1,4-pair-(2-benzimidazole)-3,3 '-5,5 '-tetrasulfonic acid and salt thereof, especially its corresponding sodium, potassium or triethanolamine salt, disodium salt particularly, 2,2 '-(1, the 4-phenylene)-two-(1 hydrogen-benzimidazole-4, the 6-disulfonic acid), single sodium salt, N-[(2 and 4)-[2-(oxo spinach-3-subunit) methyl] acrylamide polymer benzyl), phenol, 2-(2H-benzotriazole-2-yl)-4-methyl-6-(2-methyl-3-(1,3,3,3-tetramethyl-1-(trimethyl silyl) oxygen) propyl group siloxanes)), 4,4 '-[(6-[4-(1, the 1-dimethyl) amino carbonyl) phenylamino]-1,3,5-triazine-2,4-two bases) diimino] two-(benzoic acid-2-Octyl Nitrite), 2,2 '-di-2-ethylhexylphosphine oxide-(6-(2H-benzotriazole-2-yl)-4-1,1,3, the 3-tetramethyl butyl) phenol), 2,4-pair-[4-(2-ethyl hexyl oxy)-2-hydroxyphenyl]-1,3, the 5-triazine, benzylidene malonic acid polysiloxanes, glyceryl thylhexoic acid dimethoxy-cinnamic acid, disodium-2,2 '-dihydroxy-4,4 '-dimethoxy-5,5 '-the disulfo benzophenone, the dipropylene glycol Salicylate, hydroxyl methoxy benzophenone sodium sulfonate, 4,4 ', 4-(1,3,5-triazine-2,4,6-three basic three imino groups)-three-benzoic acid three (2-Octyl Nitrite), 2,4-pair-[(4-(2-ethyl hexyl oxy)-2-hydroxyl } phenyl]-6-(4-anisyl)-1,3, the 5-triazine, 2,4-pair-[{ (4-(3-sulfonate group)-2-hydroxyl propoxyl group)-2-hydroxyl } phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine sodium salt, 2,4-pair-[{ (3-(2-propoxyl group)-2-hydroxyl propoxyl group)-2-hydroxyl } phenyl]-6-(4-methoxyphenyl)-1,3,5-triazines, 2,4-pair-[{ 4-(2-ethyl hexyl oxy)-2-hydroxyl } phenyl]-6-[4-(2-methoxy ethyl carbonyl) phenylamino]-1,3, the 5-triazine, 2,4-pair-[{ 4-(3-(2-propoxyl group)-2-hydroxyl propoxyl group)-2-hydroxyl } phenyl]-6-[4-(2-second carboxyl) phenylamino]-1,3, the 5-triazine, 2,4-pair-[{ 4-(2-ethyl hexyl oxy)-2-hydroxyl } phenyl]-6-(1-methylpyrrole-2-yl)-1,3, the 5-triazine, 2,4-pair-[{ 4-three-(trimethyl silica monosilane propoxyl group)-2-hydroxyl } phenyl]-6-(4-anisyl)-1,3,5-triazines, 2,4-pair-[4-(2 " metacryloxy)-the 2-hydroxyl } phenyl]-6-(4-anisyl)-1; 3,5-triazine; 2,4-pair-[4-(1 '; 1 '; 1 ', 3 ', 5 '; 5 ', 5 '-seven methyl silica-2 " the methyl propoxyl group)-the 2-hydroxyl } phenyl]-6-(4-anisyl)-1,3,5-triazines; 2-(4-diethylamino-2-oxybenzene formyl) hexyl-benzoate.
In addition, can use microgranular ultraviolet filter agent or inorganic pigment, it can randomly be hydrophobic, such as titanium oxide (TiO 2), zinc oxide (ZnO), iron oxides (Fe 2O 3), Zirconium oxide (ZrO 2), Si oxide (SiO 2), Mn oxide (for example MnO), aluminum oxide (Al 2O 3), cerium oxide (Ce for example 2O 3) and/or its mixture.
Also can contain (extra) antioxidant or antiseptic according to preparation of the present invention.All antioxidants suitable or that be usually used in cosmetics and/or dermatosis application can be used as antioxidant or antiseptic.
Antioxidant in the invention is intended to is all materials that can reduce free base unit weight in the cell or tissue.Antioxidant advantageously is selected from the set that comprises following material: aminoacid (glycine for example; histidine; tyrosine; tryptophan) and derivant; imidazoles (for example urocanic acid) and derivant thereof; peptide is D for example; the L-carnosine; the D-carnosine; L-carnosine and derivant thereof (for example anserine); carotenoid; carotene (alpha-carotene for example; beta-carotene; lycopene) and derivant; thioctic acid and derivant thereof (for example dihydrolipoic acid); aurothioglucose; propylthiouracil and other mercaptan (thioredoxin for example; glutathion; cysteine; cystine; cystamine and glycosyl; the N-acetyl group; methyl; ethyl; propyl group; amyl group; butyl and dodecyl; palmityl; oil base; γ-Ya oil base; cholesteryl; glyceryl and oligomerization glyceride thereof) and salt; dilauryl thiodipropionate; distearyl thiodipropionate; thio-2 acid and its derivant (ester; ether; peptide; lipid; nucleotide; nucleoside and salt) and sulfoxide amines (buthionine sulfoximine for example; homocysteine sulfoxide amine; fourth methyllanthionine sulfone; penta-; oneself-; heptan methyllanthionine sulfoxide amine) very little dosage (for example pmol-μ mol/kg) tolerating; it also can be (metal) chelating agen (alpha-hydroxy fatty acid for example; Palmic acid; phytic acid, lactoferrin); 'alpha '-hydroxy acids (citric acid for example; lactic acid; malic acid); humic acid; bile acid; bile extract; tannin; bilirubin; biliverdin; EDTA; EGTA and its derivant; unsaturated fatty acid and its derivant (gamma-Linolenic acid for example; linoleic acid; oleic acid); folic acid and derivant thereof; ubiquinone and pantothenylol and derivant thereof; vitamin C and derivant (ascorbic palmitate for example; the phosphoric acid Magnesium ascorbate; the acetic acid acid ascorbyl ester); tocopherol and derivant (for example vitamin e acetate); the coniferyl benzoate of vitamin A and derivant (vitamin A palmitate) and benzoic acid resin; rutinic acid and derivant thereof; ferulic acid and derivant thereof; caffeic acid and derivant thereof; sinapic acid and derivant thereof; Curcuminoids and derivant thereof; biostearin; ursolic acid; levulic acid; butylated hydroxytolyene; butyl oxybenzene methyl ether; nordihydroguaiaretic acid; trihydroxybutyrophenone; uric acid and derivant thereof; mannose and derivant thereof; zinc and derivant thereof (ZnO for example; ZnSO 4), selenium and derivant (for example SLM), stilbene and derivant thereof (stilbene oxide for example, trans-stilbene oxide) and the derivant of these effective ingredient of being quoted (salt, ester, ether, sugar, nucleotide, nucleoside, peptide and lipid), it is according to being fit to according to the present invention.Natural extract is for example from green tea, algae, Semen Vitis viniferae, Fructus Hordei Germinatus, Fructus Phyllanthi, Herba Rosmarini Officinalis; Flavone compound and glycosylation precursor thereof, quercetin, Phenoxybenzamine.
Same suitable is coenzyme, for example the derivant of coenzyme Q10, plastoquinone, menaquinone, pantothenylol 1-10, ubiquinone 1-10 or these materials.
The amount of antioxidant in the preparation of the present invention (one or more chemical compounds) based on the total formulation weight amount, is preferably 0.01-20 weight %, preferred especially 0.05-10 weight %, especially 0.2-5 weight %.
If vitamin E and/or its derivant are used as antioxidant, based on the total formulation weight amount, it selects favourable concentration is 0.001-10 weight %.
If vitamin A or vitamin A derivative or carotene or derivatives thereof are used as antioxidant, based on the total formulation weight amount, advantageously selecting its concentration is 0.001-10 weight %.
It also is favourable using counter-stimulus in preparation according to the present invention.With regard to counter-stimulus, can be all effective content of anti inflammation or alleviate the effective ingredient that reddens and itch that these compositions are to be fit to or to be generally used for cosmetics and/or dermopathic application.Preferably all can reduce the material of cytokine, interleukin, prostaglandin and/or leukotriene amount in cell and the tissue.
Cortical steroid steroid anti-inflammatory substance, for example hydrocortisone, dexamethasone, dexamethasone phosphate, methyl prednisolone or cortisone, it is favourable being used as effective content of anti inflammation or alleviating the effective ingredient that reddens and itch, and can enlarge its list by adding other steroid antiinflammatory.Also can use the on-steroidal antiinflammatory.At this specifiable embodiment is for example piroxicam or tenoxicam of former times health class; Salicylate is such as aspirin, salsalate, solprin or fendosal; Acetogenin is such as diclofenac sodium, fenclofenac, indomethacin, sulindac, Tolmetin or clindanac; Pacify fragrant sodium (fenamate) for example mefenamic acid, meclofenamic acid, flufenamic acid or niflumic acid; Propanoic derivatives is for example phenylbutazone, hydroxyphenyl butazone, febrazone or azapropazone (azapropazone) of ibuprofen, naproxen, benzene  Lip river sweet smell or pyrazoles for example.As selection, can use natural anti-inflammatory substance or alleviate the material that reddens and itch.Can use plant extract, particularly high-efficiency plant extracts partly and isolating high-purity active substance from plant extract.Especially preferably from extract, fraction and the active substance of Chamomile, Aloe, bdellium, Rubia, purple coneflower, willow, willow herb, Herba bromi japonici, black tea and green tea, Semen Ginkgo, coffee, Fructus Piperis, Ribes nigrum L., Fructus Lycopersici esculenti, Rhizoma et radix valerianae, apricot and pure material such as wherein bisabolol, cosmosiin, boswellic acid, phytosterol, glycyrrhizic acid, glabridin or licochalcone A.
According to the amount of counter-stimulus in the preparation of the present invention (one or more chemical compounds), based on the total formulation weight amount, preferred 0.01-20 weight %, preferred especially 0.03-10 weight %, especially 0.05-5 weight %.
Also can contain the regulator of preserving moisture according to preparation of the present invention (particularly topical cosmetic preparation).For example Xia Mian material can be used as the regulator of preserving moisture (wetting agent): sodium lactate; carbamide; alcohols; sorbitol; glycerol; propylene glycol; collagen; elastin laminin or hyaluronic acid; the diacyl adipic acid; vaseline; the osmotic pressure regulatory factor; urocanic acid; lecithin; pantothenylol; phytantriol; lycopene; Sargassum extract; ceramide; cholesterol; the glycolipid class; chitosan; chondroitin sulfate (hondroitin sulfate); polyamino acid and saccharide; lanoline; the lanoline esters; aminoacid; 'alpha '-hydroxy acids (citric acid for example; lactic acid; malic acid) and derivant; saccharide (for example inositol); alpha-hydroxy fatty acid; phytosterol; the triterpene olefin(e) acid is belulinic acid Betulinic acid or ursolic acid for example; Sargassum extract.
Advantageously be selected from the set that comprises following material mutually according to the lipid in the preparation of the present invention (particularly topical cosmetic preparation): mineral oil (advantageously paraffin oil), mineral wax, Hydrocarbon (advantageously squalane or Squalene), synthetic or semisynthetic triglyceride oils (for example capric acid or sad triglyceride), natural oils (Apricot kernel oil for example, American Avocado Tree oil, cotton seed oil, borage seed oil, Ji oil, Oleum Arachidis hypogaeae semen, γ-Mi paddy phenol, Fructus Rosae seed oil, cannabis oil, hazelnut oil, blackcurrant seed oil, Oleum Cocois, the Fructus Pruni pseudocerasi kernel oil, trout oil, oleum lini, Semen Maydis oil, macadamia oil, almond oil, Radix Oenotherae erythrosepalae oil, ermine oil, olive oil, Petiolus Trachycarpi oil, hickory oil, Semen Persicae oil, pistachio nut oil, Oleum Brassicae campestris, Testa oryzae oil, Oleum Ricini, safflower oil, Oleum sesami, soybean oil, sunflower oil, tea tree oil, Oleum Vitis viniferae or wheat germ oil or the like), natural ester oil (for example Jojoba oil), synthetic ester oil (preferred saturated and/or unsaturated esters, have the saturated and/or unsaturated of 3-30 carbon atom, straight chain and/or branched alkyl carboxylic acid, straight chain and/or side chain alcohols and saturated and/or unsaturated aromatic carboxylic acid esters with 3-30 carbon atom, have the straight chain and/or the side chain alcohols of 3-30 carbon atom, particularly be selected from the set that comprises following material: isopropyl myristic acid ester, Emerest 2310, isopropyl cetylate, the isopropyl oleate, the normal-butyl stearate, the n-hexyl laurate, positive decyl laurate, the iso-octyl stearate, different nonyl stearate, the different pelargonate of different nonyl, 2-ethylhexyl cetylate, 2-ethylhexyl laurate, 2-ethylhexyl ethylhexoate, 16 stearic acid-2-ethylhexanoate, 2-stearic acid hexyldecanol ester, 2-octyl group decanol cetylate, the oil base oleate, the oil base eruciate, the erucic acid ester, synthetic or the natural mixing of savoy eruciate and this esters), fat, wax and other natural with synthetic fat-body, the aliphatic alcohol ester of preferred low carbon number alcohol (isopropyl alcohol aliphatic alcohol ester for example, propylene glycol aliphatic alcohol ester or glycerin fatty alcohol ester) or low carbon number alkanoic acid or fatty acid ester fatty alcohol, alkyl benzoate (dodecyl for example, the n-tridecane base, n-tetradecane base and Pentadecane yl benzoic acid ester admixture) and ring-type or straight chain silicone oil (dimethyl polysiloxane for example, the diethyl polysiloxanes, diphenyl polysiloxanes and mixed type thereof).
According to the water of preparation of the present invention (particularly topical cosmetic preparation) can be favourable arbitrarily contain low carbon number alcohol, glycol or polyalcohols, and ether, preferred alcohol, isopropyl alcohol, propylene glycol, glycerol, ethylene glycol, ethylene glycol one ethyl or monobutyl ether, Glycol Monomethyl ether, one ethyl or monobutyl ether, diethylene glycol monomethyl or monoethyl ether and analog, it also can be low carbon number alcohol, ethanol for example, isopropyl alcohol, 1, the 2-propylene glycol, glycerol, it also can be α-or β-hydroxy acid, preferred lactic acid, citric acid or salicylic acid, it also can be emulsifying agent, it can advantageously be selected from ionic, non-ionic, polymeric, contain phosphatic and amphion emulsifying agent group, one or more thickening agents particularly, it can advantageously be selected from the set that comprises following material: silicon dioxide, aluminium silicate, bentonite for example, the polysaccharide or derivatives thereof, hyaluronic acid for example, guar gum, HANSHENGJIAO, hydroxypropyl emthylcellulose or psicose derivant, especially advantageously be selected from the set that comprises polyacrylate, preferably from the polyacrylate of so-called Ka Baibo (carbopol) set, in each case for independent form or be combining form or the set that is selected from polyurethane.
According to containing coolant in the preparation of the present invention (particularly topical cosmetic preparation) is favourable.Specifiable coolant example is: 1-menthol, menthone glycerol acetal, menthyl lactate, replacement menthyl-3-hydroxy acid amino-compound (for example menthyl-3-hydroxy acid-N-ethamine), 2-isopropyl-N-2,3-trimethyl butyramide, substituted cyclohexane hydroxy acid amide, 3- Oxy-1,2-propylene glycol, 2-ethoxy carbonic acid menthyl ester, 2-hydroxypropyl carbonic acid menthyl ester, acetylaminoacetic acid menthyl ester, hydroxyl carboxylic acid menthyl ester (for example menthyl-3-hydroxyl butyl ester), a succinic acid menthyl ester, 2-sulfydryl ring decanone, menthyl-2-pyridine-5-esters of keto-carboxylic acid.
It also is favourable containing antibiotic effective ingredient according to preparation of the present invention (particularly topical cosmetic preparation).Specifiable embodiment is:
Aryl-or aryloxy group-replacement, unbranched or monoalkyl-and many alkyl-side chains saturated or single-to five undersaturated (maximum five two keys or triple bond also can be blended alkene/alkine compounds) aliphatic alcohol, fatty aldehyde and fatty acid, it has C 2-C 40Chain length.
Aryl-or aryloxy group-replacement, unbranched or monoalkyl-and many alkyl-side chains saturated or single-to five undersaturated (maximum five two keys or triple bond also can be blended alkene/alkine compounds) alkyl diol, dialdehyde and dicarboxylic acids, it has C 2-C 40Chain length, preferred especially C 4-C 12Chain length.
Aryl-or aryloxy group-replacement, unbranched or monoalkyl-and many alkyl-side chains saturated or single-(single-and oligomerization glycerol monoalkyl ether to five undersaturated (maximum five two keys or triple bond also can be blended alkene/alkine compounds) aliphatic alcohol (single-and oligomerization glycerol monoalkyl ether), fatty acid (single-and oligomerization glycerol mono alkyl ester), alkyl diol; Two (single-/the oligomerization glyceryl) the alkyl diether) and dicarboxylic acids (single-and oligomerization glycerol mono alkyl ester; Two (single-/oligomerization glyceryl) alkyl diether) list-and oligomerization glyceride (maximum 4 per glycerol units), it has C 2-C 40Chain length.
Has C 2-C 40Unbranched or the monoalkyl of chain length-and many alkyl-side chains saturated or single-to five undersaturated (maximum five two keys or triple bond also can be blended alkene/alkine compounds), also can choose the carboxylic acid of aryl or aryloxy group-replacement wantonly and have C 2-C 40Unbranched or the monoalkyl of chain length-and many alkyl-side chains saturated or single-to five undersaturated (maximum five two keys or triple bonds, also can be blended alkene/alkine compounds), also can choose aryl-or the fatty acid ester that monohydroxy-the hexahydroxy aliphatic alcohol is formed of aryloxy group-replacement wantonly.
Plant and tallow fatty acid segment, contain unbranched or monoalkyl-and many alkyl-side chains saturated or single-to five undersaturated (maximum five two keys or triple bond also can be blended alkene/alkine compounds) aliphatic alcohol, fatty aldehyde and fatty acid, it has C 2-C 40Chain length (for example coconut fatty acid, palm kernel fatty acid, lanoceric acid).
Lanoline, lanolin alcohol and lanoceric acid list-and oligomerization glyceride (glycerol wool grease acid esters for example, neocerite), glycyrrhetinic acid and derivant (for example glycyrrhetinic acid stearate), natural and synthetic cardenolide (digitoxin for example, dogoxin, Digitoxin, gitoxygenin, strophanthin and strophanthidin), natural and synthetic bufadienolide (Scillaren A for example, the scillarenin gamabufotalin), sapogenin and triterpene saponin (amyrin for example, caryophyllin, digitonin, gitogenin (gitogenin), tigogenin (tigogenin) and diosgenin), the steroid alkaloid of plant and animal origin (tomatidine (tomatidin) for example, Solanin, solanidine, holarrhine, bufotoxin and same bufotoxin).
Single-and poly-halo nitrile, dintrile, three nitriles or four nitriles.
Has C 2-C 24The list of chain length-and oligomerization hydroxy fatty acid (for example lactic acid, 2-hydroxy-palmitic acid), and oligomer and/or polymer and the plant and the animal material that contain these.
Acyclic terpene: terpene hydrocarbon (for example ocimene, myrcene), terpenol (for example geraniol, linalool, citronellol), terpene aldehyde and ketone (for example citral, pseudoionone, β-ionone); Monocyclic terpene: terpene hydrocarbon (for example terpinene, terpinolene, limonene), terpenol (for example terpinol, thymol, menthol), terpenone (for example pulegone, carvone); Bicyclic terpene: terpene hydrocarbon (for example carane, pinane, camphane), terpenol (for example Borneolum Syntheticum, isoborneol), terpenone (for example Camphora); Sesquiterpene: acyclic sesquiterpene alkene (for example farnesol, nerolidol), monocyclic sesquiterpene alkene (for example bisabolol), dicyclo sesquiterpene (for example cadinene, selinene, vetivazulene, the ancient azulene (guajazulene) that holds), tricyclic sesquiterpene alkene (for example santalene), two terpenes (for example phytol), tricyclic diterpene alkene (for example rosin acid), triterpene (Squalene class material; Squalene for example), tetraterpene.
Ethoxylation, propoxylation or blended ethoxylated/propoxylated used for cosmetic aliphatic alcohol, fatty acid and fatty acid ester, it has C 2-C 40Chain length has 1-150E/O and/or P/O unit.
Antimicrobial peptide and protein with amino acid no 4-200, for example peptide, germ-resistant/permeability-increasing protein [BPI], cation microbial polypeptide [CAP], the lysozyme of skin antimicrobial peptide (SAP), tongue antimicrobial peptide (LAP), people's beta-alexin (particularly h-BD1 and h-BD2), lactoferrin and hydrolyzate thereof and therefrom acquisition.
Most suitable carbohydrate or " carbohydrate derivates ", it also can be included in the term " carbohydrate " for concise and to the point expression, and they are to contain sugar and replace sugar or the chemical compound of glycosyl group.Particularly sugar also comprise deoxidation and dideoxy form, N-acetylgalactosamine-, N-acetyl-glucosamine-and aluminosilicate-substitutive derivative and sugar ester and sugar ether.Preferably:
A) monosaccharide particularly comprises pentose and hexose,
B) disaccharide particularly comprises sucrose, maltose, lactobiose,
C) oligosaccharide, particularly comprise trisaccharide and tetrose and
D) polysaccharide, particularly comprise starch, glycogen, cellulose, dextran, tunicin, inulin, chitin, particularly chitosan, chitin hydrolyzate, alginic acid and alginate, plant gum, body mucosa, pectin, mannan, galactan, xylan, arabinan, polysaccharide, chondroitin sulfate, heparin, hyaluronic acid and glycosaminoglycans, hemicellulose, substituted cellulose and substituted starch, particularly hydroxyalkyl-substituted polysaccharide in each case.
Amylose, amylopectin, HANSHENGJIAO, α-, β-and γ-dextrin be specially suitable.Polysaccharide can be by for example 4-1,000,000 monosaccharide, especially 10-100, and 000 monosaccharide is formed.Selected chain length should be guaranteed that effective ingredient dissolves in maybe and can be integrated in the particular formulations under every kind of situation.
Sphingolipid is sphingol for example; N-one alkyl sphingol; N, N-dialkyl group sphingol; The sphingosine-1-phosphate ester; Sphingol-1-sulfuric ester; Psychosine (sphingol-β-D-galactopyranose); Phosphorylcholine sheath ammonia glycosides; Molten sulfatide (lysosulfatide) (sheath ammonia galactose sulfuric ester; Molten E.C. 3.1.6.8); Lecithin; Sphingomyelins; Sphingol.
Also can use so-called " natural " antibiotic effective ingredient, its major part is a quintessence oil.Typical oil with antibacterial action is aniseed oil for example, Fructus Citri Limoniae oil, tangerine oil, oil of rosemary, wintergreen oil, cloves oil, thyme oil, Oleum lavandula angustifolia, hop oil, citronella oil, little wheat oil, lemonweed (Herba Cymbopogonis Citrari) oil, cedarwood oil, Oleum Cinnamomi, Oleum Pelargonii Graveolentis, sandalwood oil, violet oil, Eucalyptus oil, Oleum menthae, Resin benzoin oil, basil oil, fennel oil, menthol oil and Ocmea origanum, canada yellow-root (Hydastis carradensis), Berberidaceae oil, Ratanhiae or turmeric oil.
The important substance with anti-microbial effect that can find in quintessence oil is anethole, catechol, camphene, carvacrol, acetaminol, eucalyptus oil element, ferulic acid, farnesol, hinokitol, tropolone, limonene, menthol, cresotic acid, thymol, terpineol, verbenone, berberine, curcumin, caryophyllene oxide, nerol (nerolodol), geraniol for example.
Cited effective system or effective ingredient mixture and the active ingredient composition that contains these effective ingredient also can use.
The amount of effective ingredient in the preparation, based on the gross weight of preparation, preferred 0.01-20 weight %, preferred especially 0.05-10 weight %.
Can comprise deodorizer according to preparation of the present invention (particularly cosmetics comprise dermatological formulation), promptly have the effective ingredient of deodorization and anti-hidropoiesis.For example comprise, the fragrance ingredient that the abnormal smells from the patient cover material is for example common, antiperspirant based on aluminum, zirconium or zinc salt, odour absorbents for example discloses the rock stratum silicate of describing among the patent specification DE-P 40 09 347, for example, particularly Montmorillonitum, kaolinite, nontronite, saponite, Strese Hofmann's hectorite., bentonite, terre verte and castor oil acid zinc salt.Also comprise deodorizer, sterilization or bacteriostatic deodorization material, hexachlorophene for example, 2,4,4 '-three chloro-2 '-hydroxyl diphenyl ether (Irgasan), 1,6-two-(4-chlorobenzene biguanide) hexane (chlohexidine), 3,4,4 '-trichlorine diphenylurea, and at disclosed patent specification DE-37 40 186, DE-39 38 140, DE-42 04 321, DE-42 29 707, DE-42 29 737, DE-42 37 081, DE-43 09 372, the potent agent of describing among the DE-43 24 219 and contain for example for example Grillocin  (combinations of zinc ricinoleate and various additives) or triethyl citrate of quaternary ammonium salt and odour absorbents of active cation material randomly makes up with ion exchange resin.
The amount of deodorant and/or hidroschesis effective ingredient in the preparation, based on the gross weight of preparation, preferred 0.01-20 weight %, preferred especially 0.05-10 weight %.
Also can comprise antiseptic according to preparation of the present invention.On the other hand, all antioxidants that be fit to or that be generally used for cosmetics and/or dermatosis application can be used as antiseptic.
Traditional preservatives (for example, formaldehyde, glutaraldehyde, parabens (methyl for example, ethyl, propyl group and butyl p-Hydroxybenzoate), the dibromo dicyanobutane, imidazolidinyl urea (" Germall "), isothiazolone (" Kathon "), the methyl chloride Thiazolidine, methylthiazol alkane, organic acid (benzoic acid for example, sorbic acid, salicylic acid) and salt and ester, propanoic acid and formic acid and salt thereof, ethylene glycol (propylene glycol for example, 1,2-dihydroxy alkanes), based on the antiseptic adminicle of plant and flavonoid (deflazacort (lantadin A) for example, caryophyllene, Hesperidin, Barosmin, phellandrene, pigenin, Quercetin, hypericin, aucubin, diosgenin, plumbagin, corlilagin or the like) and glycosylated derivative (for example glycosyl rutin).
According to preparation of the present invention, particularly dermatological formulation, can also advantageously comprise dyestuff and/or colored pigment, if particularly use it for the modification cosmetic field.Dyestuff and colored pigment can be selected from the EU catalogue that Germanization is made up corresponding positive catalogue in the product regulations or cosmetics coloring agent.In most of the cases, they are consistent with the dyestuff that approval is used for food.Favourable colored pigment is titanium dioxide, Muscovitum, ferrum oxide (Fe for example for example 2O 3, Fe 3O 4, FeO (OH)) and/or stannum oxide.Favourable dyestuff is fuchsin, Berlin blue, chrome oxide green, ultramarine and/or manganese violet for example.
If dermatological formulation according to the present invention is used to facial zone, can be easily from following set, select one or more materials as dyestuff: 2,4-dihydroxy diphenyl diimide, 1-(2 '-chloro-4 '-nitro-1 '-benzeneazo)-2 hydroxy naphthalene, red (Ceres red) lights up, 2-(4-sulfo group-1-naphthyl nitrogen) Neville acid, 2-hydroxyl-1,2 '-azonaphthalene-1 '-sulfonic acid calcium salt, 1-(2-sulfo group-4-methyl isophthalic acid-benzeneazo)-2-naphthyl carboxylic acid calcium salt and barium salt, 1-(2-sulfo group-1-naphthalene nitrogen)-beta naphthal-3-carboxylic acid calcium salt, 1-(4-sulfonic acid-1-benzeneazo)-beta naphthal-6-sulfonic acid aluminum salt, 1-(4-sulfo group-1-naphthalene nitrogen)-beta naphthal-3,6-disulfonic acid aluminum salt, 1-(4-sulfo group-1-naphthalene nitrogen)-beta naphthal-6, the 8-disulfonic acid, 4-(4-sulfo group-1-benzeneazo)-1-(4-sulfo group phenyl)-5-hydroxypyrazoles-3-ALUMINUM CARBOXYLIC salt, 4,5-dibromofluorescein aluminum salt and zirconates, 2,4,5,7-eosin aluminum salt and zirconates, 3 ', 4 ', 5 ', 6 '-tetrachloro-2,4,5,7-eosin and aluminum salt thereof, 2,4,5,7-tetraiodofluorescein aluminum salt, quinophthalone disulfonic acid aluminum salt, indigo disulfonic acid aluminum salt, red ferric oxide and Black Rouge (CIN:77491 (red) and 77499 (deceiving)), hydrated ferric oxide (CIN:77492), diphosphonic acid manganese ammonium and titanium dioxide.
The oil-soluble natural dye also is favourable, for example red pepper extract, beta-carotene and alkermes.
In the intent of the present invention, the pearlescent pigment that dermatological formulation contains also is favourable.Below listed pearlescent pigment type be particularly preferred:
1. natural peral colour lustre pigments, for example
-" Margarita elite " (guanine/hypoxanthine mixed crystal that obtains from fish scale) and
-" Concha Margaritifera " (concha Anodonta seu Cristaria that pulverizes)
2. monocrystalline pearlescent pigment bismuth oxychloride (BiOCl) for example
3. stratiform substrate pigment (layered substrate pigments): Muscovitum/oxidized metal for example
The main component of pearlescent pigment is for example formed by the Oleum Ricini dispersion of powdered pigment or bismuth oxychloride and/or titanium dioxide and bismuth oxychloride and/or the titanium dioxide on the Muscovitum.The colour lustre pigments advantageous particularly of for example in CIN 77163, listing.
Cited pearlescent pigment list has more than naturally and is limited to this.Known favourable pearlescent pigment of the present invention can obtain by many modes in itself.For example, the substrate except Muscovitum can be by other oxidized metal coating, for example Silicon stone or the like.For example, use TiO by what Merck sold 2And Fe 2O 3The SiO of coating 2Granule (" Ronaspheres ") is favourable, and the optics that is particularly suitable for the microgroove line reduces.
For example not using fully, the such substrate of Muscovitum also is favourable.It is particularly preferred not using the ferrum pearlescent pigment of Muscovitum manufacturing.For example, such pigment can obtain from BASF, trade name Sicopearl Copper 1000.
Can be from the commodity that Flora Tech obtains Metasomes Standard/Glitter by name, the special effect pigments with different colours (yellow, red, green, blueness) also is particularly advantageous.Here, light-emitting particles is mixed with various auxiliary agents and dyestuff (for example using color index (CI) number is 19140,77007,77289,77491 dyestuff).
But dyestuff and pigment individualism and mixing exist and coating each other, and wherein different color effects can obtain by changing coating layer thickness usually.What the total amount of dyestuff and coloring pigment was favourable selects in following scope: in each case all based on the gross weight of cosmetic formulations, for example, 0.1 weight %-30 weight %, preferred 0.5-15 weight %, particularly 1.0-10 weight %.
Cited effective system mixture also can use.
According to the effective ingredient amount in the preparation of the present invention, based on the total formulation weight amount, preferred 0.01-20 weight %, preferred especially 0.05-10 weight %.
For use, according to topical formulations of the present invention, particularly make the thin out preparation of skin and chroma of hair, be applied to skin and/or hair by the traditional approach that is applicable to cosmetics with abundant amount.
Other preferred embodiment of the present invention is found in following examples and claims:
Embodiment 1: " oil-in-water " emulsion
Part Material name (manufacturer) Chemical name Content is in wt%
A B C D Arlatone 983 S (ICI) Brij 76 (ICI) Cutina MD (Cognis) Baysilone oil M10 (GE Bayer) Eutanol G (Cognis) paraffin oil 65 cp (Henry Lamotte) distilled water Phenopip (Nipa Laboratorien) Trilon BD (BASF) 1,2-propylene glycol glycerol 99% salicin distilled water Carbopol 2050 (B.F. Goodrich) sodium hydrate aqueous solution, 10% aromatic oil PEG-5 tristerin stearyl polyoxyethylene (10) ether tristerin dimethyl silicone polymer octyl dodecanol mineral profit phenoxetol (with) nipagin (with) aethyl parabenum (with) Butyl Chemosept (with) nipasol (with) p-hydroxybenzoic acid isobutyl ester disodium ethylene diamine tetraacetate propane diols glycerol liquor carbomer NaOH spices (aromatic substance) 1.2 1.2 3.5 0.8 3.0 8.0 49.6 0.5 0.1 2.0 3.0 0.2 25.0 0.4 1.2 0.3
A is partially mixed and be heated to 80 ℃.B is partially mixed and be heated to 90 ℃ and it is joined in the A part stir simultaneously.To the C part, Carbopol carefully is scattered in the water also with sodium hydroxide solution (pH 6.9) neutralization.Then C is partly joined in the mixture of 60 ℃ A and B part.D is partly joined among A, the B and C mixture partly of room temperature.
Embodiment 2: " Water-In-Oil " emulsion with the protection of UVA/B broad band
Part Material name (manufacturer) Chemical name Content is in wt%
A B C Dehymuls PGPH (Cognis) Monomuls 90-O 18 (Cognis) Permulgin 2550 (Koster Keunen Holland) Myritol 318 (Cognis) Witconol TN (Witco) Cetiol SN (Cognis) Copherol 1250 (Cognis) Solbrol P (Bayer) Neo Heliopan AV (Symrise) Neo Heliopan E 1000 (Symrise) Neo Heliopan MBC (Symrise) Neo Heliopan Neutral zinc oxide (Symrise) distilled water of OS (Symrise) octyl triazone Trilon BD(BASF) phenyl phenol Solbrol M (Bayer) glycerol 99% Neo Heliopan AP (Symrise), 15% sodium salt 5-benzoyl-4-hydroxyl-2-methoxy benzenesulfonic acid salicin aromatic oil bisabolol Dimerization hydroxy stearic acid polyglycereol, (2) ester oil acid glyceride Cera Flava three, (caprylic/capric) glyceride C 12-C 15The different n-nonanoic acid 16 of alkyl benzoate and octadecane ester tocopherol acetate nipasol ethylhexyl methoxy cinnamate Neo Heliopan E1000 4 methyl benzylidene camphor ethylhexyl salicylate Uvinul T 150 Zinc oxide water disodium ethylene diamine tetraacetate nipagin Neo Heliopan AP 5-benzoyl-4-hydroxyl-2-methoxy benzenesulfonic acid spices bisabolol 3.0 1.0 1.0 6.0 6.0 5.0 1.0 0.1 4.0 4.0 2.0 3.0 1.0 7.0 39.5 0.1 0.7 0.2 4.0 10.0 0.5 0.5 0.3 0.1
To the A part, all substances except that zinc oxide are heated to 85 ℃, zinc oxide carefully is scattered in the mixture.B part composition is mixed together, is heated to 85 ℃, it is joined in the A part stir simultaneously.C partly joined in A and the partially mixed thing of B with the dispersion instrument mixture is homogenized then.
Embodiment 3: " oil-in-water " emulsion with the protection of UVA/B broad band
Part Material name (manufacturer) Chemical name Content is in wt%
A B C Arlacel 165 (ICI) Emulgin B2 (Cognis) Lanette O (Cognis) Myritol 318 (Cognis) Cetiol SN (Cognis) Abil 100 (Goldschmidt) Bentone Gel MIO (Rheox) Cutina CBS (Cognis) Neo Heliopan 303 (Symrise) Neo Heliopan BB (Symrise) Neo Heliopan MA (Symrise) N, N-dimethyl-PABA-2-ethylhexyl superfine titanic oxide distilled water Trilon BD(BASF) Veegum ultra (Vanderbilt) Natrosol 250 HHR (Aqualon) glycerol Phenopip (Nipa Laboratorien) salicin aromatic oil The reactant of tristerin and polyethylene glycol (100) stearate cetearyl alcohol alcohol ether-200 six and the 18 different n-nonanoic acids 16 of alcohol three (caprylic/capric) glyceride and octadecane ester dimethyl silicone polymer mineral oil and dihydro tallow alkyl dimethyl ammonium chloride and hectorite and propylene carbonate tristerin and hexadecanol and 18 pure and mild hexadecyl palmitates and cocounut oil glyceride octocrylene ESCALOL 567 menthyl anthranilate titanium dioxide disodium ethylene diamine tetraacetate sulfuric acid magnalium CMC glycerine phenoxetol (with) nipagin (with) aethyl parabenum (with) Butyl Chemosept (with) nipasol (with) the p-hydroxybenzoic acid isobutyl ester 3.0 1.0 1.15 5.0 4.0 1.0 3.0 2.0 7.0 1.0 3.0 3.0 5.0 53.85 0.1 1.0 0.3 3.0 0.3 2.0 0.3
To the A part, all substances except that titanium dioxide are mixed together and are heated to 85 ℃; Titanium dioxide carefully is scattered in the mixture.To the B part, will be mixed together except that all substances Veegum and the Natrosol, be heated to 90 ℃, be scattered in Veegum and Natrosol in the mixture and mixture joined in the A part and stir simultaneously.C is partly added in the mixture of A and B part and with the dispersion instrument mixture is homogenized then.
Embodiment 4: " oil-in-water " emulsion with the protection of UVA/B broad band
Part Material name (manufacturer) Chemical name Content is in wt%
A B C D Emulsiphos(Symrise) Cutina MD (Cognis) Lanette 16 (Cognis) neutral oil (Symrise) Cetiol SN (Cognis) Copherol 1250 (Cognis) Solbrol P (Bayer) Abil 100 (Goldschmidt) Trilon BD (BASF) Neo Heliopan HMS(Symrise) Neo Heliopan 357 (Symrise) distilled water 1,3 butylene glycol Sobrol M (Bayer) phenyl phenol Carbopol ETD 2050 (B.F. Goodrich) Keltrol T (Calgon) Neo Heliopan AP (Symrise) kojic acid salicin sodium hydrate aqueous solution, 10% aromatic oil bisabolol The high  ester of the different n-nonanoic acid hexadecane of phosphoric acid hexadecanol ester hydrogenation palm oil glyceride tristerin hexadecanol three (caprylic/capric) glyceride ester tocopherol acetate nipasol dimethyl silicone polymer disodium ethylene diamine tetraacetate salicylic acid butyl methoxydibenzoylmethise nipagin carbomer xanthan gum Neo Heliopan AP kojic acid NaOH aromatic oil bisabolol 1.50 2.0 1.2 5.0 5.0 0.5 0.1 0.3 0.1 5.0 2.0 47.1 3.0 0.2 0.7 0.2 0.2 22 0.5 0.2 2.8 0.3 0.1
A partly is heated to 85 ℃.Carbopol and Keltrol cooling is scattered in the residual components, with mixture heated to 85 ℃ and join in the A part.Immediately C is partly joined in the mixture of 80 ℃ A and B part and it was homogenized 5 minutes with the dispersion instrument.At room temperature add the D part at last and mixture is homogenized with the dispersion instrument.
Embodiment 5: " oil-in-water " emulsion with the protection of UVA/B broad band
Part Material name (manufacturer) Chemical name Content is in wt%
A B C Hostacerin DGMS (Clariant) Lanette 16 (Cognis) Prisorine 3505 (UniQema) Tegosoft TN (Goldschmidt) Copherol 1250 (Cognis) neutral oil (Symrise) Solbrol P (Bayer) SF 1214 (Bayer) Corapan TQ (Symrise) Neo Heliopan HMS(Symrise) Neo Helippan 357(Symrise) Keltrol T (Kelco) distilled water Lanette E (Cognis) 99% glycerol phenyl phenol (Symrise) Edeta BD (BASF) Neo Heliopan Hydro (with neutral 15% aqueous solution of NaOH) is Neo Heliopan (Symrise) AP (with neutral 10% aqueous solution of NaOH) is salicin Solbrol M (Symrise) (Bayer) Symrise aromatic oil (Symrise) 10%NaOH aqueous solution Polyglycereol-2-stearate hexadecanol isostearic acid C 12-C 15Alkyl benzoate tocopherol acetate three (caprylic/capric) glyceride nipasol cyclopentasiloxane; Dimethyl silicone polymer 1, the high  ester of 6-naphthalenedicarboxylic acid ethylhexyl salicylic acid butyl methoxydibenzoylmethise xanthan gum water cetearyl sodium sulphate glycerine phenoxetol disodium ethylene diamine tetraacetate Phenylbenzimidazolesulfonic acid Neo Heliopan AP nipagin aromatic oil NaOH 3.0 2.0 0.5 2.0 0.5 5.0 0.1 1.0 3.0 9.5 0.6 0.2 49.25 0.75 4.0 0.7 0.1 6.7 10.0 0.2 0.2 0.5 0.2
A partly is heated to 80 ℃.Behind the dissolving all the components,, add Keltrol and also stirred the mixture 5 minutes mixture heated to 85 ℃.Stirring with the dispersion instrument then homogenized mixture in 10 minutes.With mixture heated to 85 ℃, add the B part, stirring the mixture at 80 ℃ homogenized it at 60 ℃ in 10 minutes then.At room temperature add the C part at last and mixture is homogenized with the dispersion instrument.
Embodiment 6: the nothing oil daylight spraying with the protection of UVA/B broad band
Part Material name (manufacturer) Chemical name Content is in wt%
A B Distilled water 99% glycerol Neo Heliopan Hydro (with neutral 15% aqueous solution of NaOH) is Neo Heliopan (Symrise) AP, (with neutral 10% aqueous solution of NaOH), (Symrise) salicin D-panthenol, (BASF) Keltrol T (Kelco) Euxyl K 100 (Schülke & Mayr) Dow Corning 193 (Dow Corning) Aloe extract (Symrise) chamomile extract (Symrise) Radix Hamamelidis Mollis extract (Symrise) ethanol (96%) Glycerine Phenylbenzimidazolesulfonic acid Neo Heliopan AP panthenol xanthan gum phenmethylol; Methylchloroisothiazandnone, methylisothiazolinone dimethicone copolyol ethanol 22.2 4.5 33.3 22.0 0.2 0.5 0.2 0.1 1.0 1.0 1.0 1.0 13.0
All the components except that Keltrol in the A part is mixed together.Add Keltrol and stir simultaneously, continue stirring and homogenize until mixture.Add B part and stirring until homogenizing.
Embodiment 7: the skin whitening face cream with UVB/UVA protection
Part Material name (manufacturer) The INCI title %(w/w)
A B C D Demineralization water Hydrolite, (Symrise) Carbopol ETD 2001, (Noveon) salicin Keltrol T, (Kelco) Neo Heliopan Hydro (with 15% aqueous solution of NaOH neutralization) 10% sodium hydrate aqueous solution Neo Heliopan  AV (Symrise) Neo Heliopan  E 1000 (Symrise) Neo Heliopan  MBC (Symrise) Neo Heliopan  357 (Symrise) α-bisabolol Baysilone Oil PK 20 (GE Bayer) Tegosoft TN (Degussa) Unimer U-151 (Induchem) Copherol 1250 (Cognis) Edeta BD (BASF) ethanol (96 volume %) sex change Symrise aromatic oil phenoxetol (Symrise) Solbrol M (Bayer) Solbrol P (Bayer) Water pentanediol carbomer xanthan gum Phenylbenzimidazolesulfonic acid NaOH ethylhexyl methoxy cinnamate Neo Heliopan E1000 4 methyl benzylidene camphor butyl methoxydibenzoylmethise bisabolol phenyl gathers trimethicone C12-C 15Alkyl benzoate PVP/ hexadecene copolymer tocopherol acetate disodium ethylene diamine tetraacetate diethyl phthalate modification alcohol spices (aromatic substance) phenoxetol nipagin nipasol 51.70 4.30 0.50 1.0 0.30 10.00 2.20 5.00 5.00 2.00 1.50 0.10 5.00 4.00 0.50 0.50 0.10 5.00 0.30 0.70 0.20 0.10
All raw materials except that Keltrol and Carbopol in the A part are mixed together.Careful Keltrol and the Carbopol while vigorous stirring of adding.All raw materials of B part are mixed together and join stirring simultaneously in the A part.All raw materials of C part are fully mixed and heat 357 dissolvings gradually until Neo Heliopan .In A/B part, add the C part then and stir until evenly.To the D part, Solbrol P and M are dissolved in other raw material, then it is slowly joined in the A/B/C part.Stirring up to product evenly and homogenize.The pH value of end-product should be 7.2-7.5.
Produce 15% Neo Heliopan  Hydro solution:
82.85% demineralization water,
02.15% 99% sodium hydroxide,
15.00% Neo Heliopan  Hydro PN 103089
2/3rds sodium hydroxide are soluble in water, add Neo Heliopan  Hydro then and stir simultaneously.Adding remaining sodium hydroxide gets limpid until solution becomes.The pH value of final Neo Heliopan  Hydro solution should be 7.5-8.0.Recommend the extra antiseptic that adds to extend storage period.
Embodiment 8: the skin whitening aerosol foam with UVB/UVA protection
Part Material name (manufacturer) The INCI title %(w/w)
A B C D Emulsiphos (Symrise) Cutina MD (Cognis) Lanette 16 (Cognis) Texapon N 70 (Cognis) neutral oil (Symrise) Tegosoft TN (Degussa) Copherol 1250 (Cognis) Solbrol P (Bayer) Edeta BD (BASF) Neo Heliopan  AV (Symrise) Neo Heliopan  MBC (Symrise) Neo Heliopan  357 (Symrise) demineralization water salicin 99% glycerine Solbrol M (Bayer) phenoxetol (Symrise) Carbopol ETD 2050 (Noveon) 10% sodium hydrate aqueous solution Neo HeliopanHydro (with neutral 15% aqueous solution of NaOH) is Symrise aromatic oil α-bisabolol (Symrise) (Symrise) Phosphoric acid hexadecanol ester hydrogenation Petiolus Trachycarpi oil glyceride tristerin hexadecanol laureth-, (1-4) sodium sulfate three, (caprylic/capric) glyceride C 12-C 15Alkyl benzoate tocopherol acetate nipasol disodium ethylene diamine tetraacetate ethylhexyl methoxy cinnamate 4 methyl benzylidene camphor butyl methoxydibenzoylmethise water glycerine nipagin phenoxetol carbomer NaOH Phenylbenzimidazolesulfonic acid aromatic substance (spices) bisabolol 1.50 2.00 0.50 0.10 2.00 2.00 0.50 0.10 0.10 6.00 4.00 1.50 58.30 0.50 3.00 0.20 0.70 0.10 2.90 13.30 0.40 0.10
A partly is heated to 85 ℃.To the B part, Carbopol is dispersed in the water, add B all other raw materials of part then and be heated to 85 ℃.Adding the B part in the A part stirs simultaneously.In the A/B part, directly add the C part and allow its cooling.In A/B/C part, add the D part and be incorporated in the aerosol container.The pH value of end-product should be about 7.5.
Embodiment 9: skin whitening non-aerosol foam
Part Material name (manufacturer) The INCI title %(w/w)
A B C D Demineralization water 99% glycerine Hydrolite5 (Symrise) D-pantothenyl aleohol (BASF) salicin Lara Care A-200 (Rahn) Texapon N 70 (Cognis) Baysilone Oil M 10 (Bayer) Edeta BD Copherol 1250 (Cognis) Neo Heliopan  MBC (Symrise) Neo Heliopan  AV (Symrise) Neo Heliopan  E 1000 (Symrise) the Neo Heliopan  natural α-bisabolols of 357 (Symrise) (Symrise) Symrise aromatic oil Pemulen TR 2 (Novion) Cetiol OE (Cognis) phenoxetols (Symrise) Solbrol M (Bayer) Solbrol P (Bayer) 10% sodium hydrate aqueous solution Sodium sulphate dimethyl silicone polymer disodium ethylene diamine tetraacetate tocopherol acetate 4 methyl benzylidene camphor ethylhexyl methoxy cinnamate Neo Heliopan E1000 butyl methoxydibenzoylmethise bisabolol aromatic substance (spices) acrylate/C10-30 alkyl acrylate crosslinked polymer two caprylyl ether phenoxetol nipagin nipasol NaOH of water glycerine 1,2 pentanediol panthenol galactolipin araban laureth-(1-4) 70.50 4.00 5.00 0.50 0.20 0.25 0.50 1.00 0.10 0.50 3.00 2.00 6.00 1.50 0.10 0.20 0.25 3.00 0.70 0.20 0.10 0.60
With all material dissolutions of A part in water.To the B part, Neo Heliopan  MBC and NeoHeliopan  357 are dissolved in heating simultaneously among Neo Heliopan  AV and the E 1000.At room temperature, to wherein adding all other compositions of B part.Homodisperse Pemulen is vigorous stirring simultaneously.In the A part, add B part and mix homogeneously.To the C part, dissolving Solbrol M and P are heated to about 50 ℃ and join in the A/B part simultaneously in phenyl phenol.D partly joined to stir simultaneously in the A/B/C part make it even.The pH value of end-product should be about 7.0.
Embodiment 10: have the shampoo that makes the skin whitening characteristic
Part Material name (manufacturer) The INCI title %(w/w)
A B C D CrinipanAD(Symrise) Dragocide Liquid(Symrise) Texapon NSO BZ(Cognis) Dehyton K Softigen 767 Neo Heliopan Hydro (15% aqueous solution neutralised with NaOH) is the natural α bisabolol of Arlypon F witch hazel distillate (Symrise) (Symrise) Symrise aromatic oil D-pantothenyl aleohol demineralization water salicin polymer JR 400 solubilizer (Symrise) Neo Heliopan 357 (Symrise) (Symrise) The Ke Ningbasuo phenoxetol, (with) nipagin, (with) aethyl parabenum, (with) Butyl Chemosept, (with) nipasol, (with) p-hydroxybenzoic acid isobutyl ester laureth-, (1-4) sodium sulphate Cocoamidopropyl betaine PEG-6 caprylic/capric glyceride Phenylbenzimidazolesulfonic acid lauryl alcohol-2 witch hazel distillate bisabolol aromatic substance, (spices) panthenol water Polyquaternium-10 Cremophor RH40; Tridecyl polyoxyethylene (9) ether; Propane diols, the water butyl methoxydibenzoylmethise 0.50 0.70 27.00 12.00 2.50 3.38 2.00 1.00 0.10 0.50 0.40 47.82 0.2 0.40 3.0 0.5
Crinipan  AD is added stirring simultaneously in the Dragocide liquid, dissolve fully up to Crinipan  AD.With B part all the components and A partially mixed stir simultaneously until A/B partially mixed evenly.Xiang Shuizhong adds polymer (C part) and stirs simultaneously until dissolving fully.Join then in the A/B part.To the D part, dissolved oil composition in solubilizing agent joins in the A/B/C part and stirs simultaneously.The pH value of final anti-dandruff shampoo should be about 7.5.
Embodiment 11: the skin whitening hair regulator that the UVB/UVA protection is arranged
Part Material name (manufacturer) The INCI title %(w/w)
A B C Lanette O (Cognis) Eumulgin B 2 (Cognis) Neo Heliopan 357 Neo Heliopan  E 1000 (Symrise) demineralization water Crotein Q (Croda) Dehyquart SP salicin citric acid Symrise aromatic oil Phenonip (Clariant) Cetostearyl alcohol cetearyl alcohol alcohol ether-20 butyl methoxydibenzoylmethise Neo Heliopan E1000 water hydrolytic collagen Hydroxyproyl Trimethyl quaternary ammonium salt C16-18 alkyl three (polyoxyethylene groups) ammonium phosphate citric acid aromatic substance (spices) phenoxetol (with) nipagin (with) aethyl parabenum (with) Butyl Chemosept (with) nipasol (with) the p-hydroxybenzoic acid isobutyl ester 2.50 0.70 0.50 2.00 91.57 1.00 0.50 0.20 0.13 0.40 0.50
A partly is heated to 70 ℃.The B part material of dissolving except that aromatic oil in water is heated to 90 ℃ and also this solution added stirring simultaneously in the A part.Slowly stir down emulsion is cooled to 40 ℃, add aromatic oil and stir simultaneously.Preserve after 24 hours, add Phenopip and stir simultaneously.The pH value of end-product should be about 3.5.
Embodiment 12: skin whitening moisturiser O/W
Part Material name (manufacturer) Chemical name Content is in wt%
A B C PCL liquid (Symrise) Dragophos S (Symrise) Isodragol (Symrise) Dracorin GMS (Symrise) Lanette 18 (Care Chemicals) Dow Corning 200 Fluid (Dow Corning) water Hydrolite-5 (Symrise) salicin magnesium ascorbyl phosphate Dragocid Liquid (Symrise) 10% citric acid solution aromatic oil The cetearyl ethylhexoate, isopropyl myristate dihydroxy cetyl sodium phosphate glycerol three different pelargonate tristerin stearyl alcohol polydimethylsiloxane water pentanediol magnesium ascorbyl phosphate nipagins, phenyl phenol, aethyl parabenum, Butyl Chemosept, propyl parabene, p-hydroxybenzoic acid isobutyl ester citric acid aromatic substance 3.0 2.0 7.0 2.0 4.5 2.0 71.0 3.0 1.0 3.0 0.8 0.35 0.35
Swelling Carbopol in water.Heat respectively A mutually with B to 80 ℃.With B be added to A mutually in, just make its emulsifying then.With the cold stirring of blade mixer.When descending, temperature reduces mixing speed.The raw material that in the time of 40 ℃, adds the C phase.
Embodiment 13: skin whitening facial cream O/W
Part Material name (manufacturer) Chemical name Content is in wt%
A B Dracorin 100 s.e.P (Symrise) Dracorin GMS (Symrise) E level paraffin oil 5 (Parafluid) Lanette 16 (Care Chemicals) isopropyl myristate (Symrise) Abil 350 (Goldschmidt) water propane diols-1,2 99 P GC (Dow Benelux) salicin Neo-Dragocid powders (Symrise) 10% sodium hydroxide solution aromatic oil Tristerin; PEG-100 stearate tristerin atoleine hexadecanol isopropyl myristate dimethyl silicone polymer water propane diols nipagin; Sorbic acid; Dehydroacetic acid, nipasol NaOH aromatic substance 8.0 3.0 4.0 2.0 8.0 0.3 67.85 5.0 0.5 0.8 0.25 0.30
The preparation explanation:
Heat A respectively mutually and extremely about 80 ℃ mutually of B.In the Ultra-Turrax agitator, B is added to A mutually in and emulsifying.With the cold stirring paste of blade mixer, when descending, temperature reduces mixing speed from 250rpm.In the time of about 40 ℃, add the C phase.
Test 1 (decolourization)
With the B16V mouse black-in tumor cell with 5 * 10 3The concentration of cells/well intersperses among in the 96 hole microtitration plates.In the RPMI culture medium, at 37 ℃, 5%CO 2Condition under cultivate after 24 hours, nourish with 10% hyclone, add the detection material of variable concentrations and 0.3mM tyrosine and 10nM α-MSH (α-melanocyte stimulates hormone) and further cultivation 96 hours.The IC of the maximum working concentration of used detection material and cytotoxin check 200.1 times of value of value is consistent.Same, with 0.01mM, 0.1mM and 1mM kojic acid cultured cell in contrast.After cultivating, add SDS and NaOH (final concentration is respectively: 1mM and 1M) in culture medium, measure the trap (A) at 400nm place after 3 hours.
The suppression ratio of yyyy chromogenesis in the presence of test compound or kojic acid calculates with the equation below available:
The suppression ratio of chromogenesis (%)=100-[A Test compound/ A Contrast* 100]
Calculate the IC of each test compound by the chromogenesis suppression ratio (%) of a series of dilution test chemical compounds 50Value.This is the repressed test compound concentration of 50% chromogenesis.
Table 3
Test substances IC 50(μM)
Kojic acid 452.3
2-(methylol)-phenyl-β-D-pyranglucoside (salicin) 164.3
2-(methylol) benzyl alcohol (saligenin) 210.9
2-hydroxy 3-methoxybenzene methanol Non-activity
This data show salicin and saligenin have strong about 3 times decolourization than kojic acid to the B16V melanoma cells.Methoxyl group other on 3 of phenyl ring substitutes the active forfeiture that causes fading.

Claims (9)

1. the purposes that has the chemical compound of chemical formula (I) is used for making skin and/or chroma of hair thin out,
Wherein:
n=1-10,
R 1Be selected from and comprise H, side chain or unbranched C 1-C 14Alkyl, side chain or unbranched C 2-C 14Thiazolinyl, side chain or unbranched C 2-C 14Alkynyl, replacement or unsubstituted aryl alkyl, cyclohexyl, cyclopenta, replacement or unsubstituted phenyl, replacement or unsubstituted monosaccharide, SO 3H, SO 3Na, (CH 2) 1-10OH, COR, SiRR ' R ", PO 3HNa, PO 3Na 2With
Figure A2005800088010002C2
Set,
Wherein R, R ', R " separate being selected from comprise H, C 1-C 14Alkyl, C 2-C 14Thiazolinyl, C 2-C 14Alkynyl, cyclohexyl, cyclopenta, replacement or unsubstituted phenyl and heterocyclic set and
R 2Be enzymatic cutting substituent group or be selected from and comprise H, side chain or unbranched C 1-C 14Alkyl, side chain or unbranched C 2-C 14Thiazolinyl, side chain or unbranched C 2-C 14The set of alkynyl, cyclohexyl, cyclopenta, replacement and unsubstituted phenyl or replacement or unsubstituted aryl alkyl.
2. according to the purposes of claim 1, wherein for chemical compound with chemical formula (I):
R 2Be selected from and comprise SO 3H, SO 3Na, (CH 2) 1-10OH, COR, PO 3HNa and PO 3Na 2The set of enzymatic cutting substituent group, wherein separate being selected from of R, R ' comprises H, C 1-C 14Alkyl, C 2-C 14Thiazolinyl, C 2-C 14Alkynyl, cyclohexyl, cyclopenta, replacement or unsubstituted phenyl and heterocyclic set.
3. according to the purposes of claim 1, wherein in chemical formula (I):
R 2Be selected from set enzymatic cutting, replacement or unsubstituted monosaccharide, described set comprises glucose, mannose or galactose.
4. according to each purposes of aforementioned claim, wherein in chemical formula (I):
n=1-4,
R 1Be selected from and comprise H, side chain or unbranched C 1-C 14Alkyl, side chain or unbranched C 2-C 14Thiazolinyl, side chain or unbranched C 2-C 14Alkynyl, replacement or unsubstituted aryl alkyl, replacement or unsubstituted phenyl, replacement or unsubstituted monosaccharide, (CH 2) 1-10OH, COR, SR, PO 3RR ' and
Figure A2005800088010003C1
Set, wherein separate being selected from of R, R ' comprises H and C 1-C 14The set of alkyl.
5. according to the purposes of claim 1, wherein in chemical formula (I):
n=1-4,
R 1Be selected from and comprise H, side chain or unbranched C 1-C 14Alkyl, side chain or unbranched C 2-C 14Thiazolinyl, side chain or unbranched C 2-C 14Alkynyl, replacement or unsubstituted aryl alkyl, replacement or unsubstituted phenyl, replacement or unsubstituted monosaccharide, (CH 2) 1-10OH, COR, SR, PO 3RR ' and Set, wherein separate being selected from of R, R ' comprises H and C 1-C 14The set of alkyl and
R 2Be selected from and comprise H, side chain or unbranched C 1-C 14Alkyl, side chain or unbranched C 2-C 14Thiazolinyl, side chain or unbranched C 2-C 14The set of alkynyl and replacement or unsubstituted phenyl.
6. saligenin, Forlan glycosides, populoside, quaking aspen glycosides, salicortin, 2-O-acetyl salicortin or Tremulacin are used to make skin and/or the thin out purposes of chroma of hair.
7. salicin is used to make skin and/or the thin out purposes of chroma of hair.
8. cosmetics or treatment preparation contain the chemical compound that skin and/or hair is had the chemical formula (I) of the amount of the thin out effect of color and luster, are used for making skin and/or chroma of hair thin out,
Wherein: n=1-10,
R 1Be selected from and comprise H, side chain or unbranched C 1-C 14Alkyl, side chain or unbranched C 2-C 14Thiazolinyl, side chain or unbranched C 2-C 14Alkynyl, replacement or unsubstituted aryl alkyl, cyclohexyl, cyclopenta, replacement or unsubstituted phenyl, replacement or unsubstituted monosaccharide, SO 3H, SO 3Na, (CH 2) 1-10OH, COR, SiRR ' R ", PO 3HNa, PO 3Na 2With
Figure A2005800088010004C1
Set,
Wherein R, R ', R " separate being selected from comprise H, C 1-C 14Alkyl, C 2-C 14Thiazolinyl, C 2-C 14Alkynyl, cyclohexyl, cyclopenta, replacement or unsubstituted phenyl and heterocyclic set and
R 2Be enzymatic cutting substituent group or be selected from and comprise H, side chain or unbranched C 1-C 14Alkyl, side chain or unbranched C 2-C 14Thiazolinyl, side chain or unbranched C 2-C 14The set of alkynyl, cyclohexyl, cyclopenta, replacement and unsubstituted phenyl or replacement or unsubstituted aryl alkyl.
9. cosmetics or treatment preparation contain saligenin, salicin, Forlan glycosides, populoside, quaking aspen glycosides, salicortin, 2-O-acetyl salicortin or Tremulacin that skin and/or hair are had the amount of the thin out effect of color and luster.
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