The present invention relates to the use of specific organic UV filters for preventing tanning of the human skin and to their use in cosmetic formulations.
The topical application of UV-filters in order to prevent or reduce sunburn, premature aging and pathologic alterations of the skin has become well established for Caucasians where sensitive skin types are abundant and social cultural habits propagate body exposure and a well tanned skin complexion.
But also Non-Caucasians are prone to UV-sensitive pigmentation disorders such as vitiligo or melasma. Such disturbances can manifest much more in a colored complexion and may even reach the level of disfigurement. This is one of the reasons why the beauty ideal of many colored persons and especially those of Asian origin traditionally avoid skin exposure to the sun and show only light pigmentation.
Since dressing habits and outdoor-activities are changing towards more sun exposure, daily cosmetics containing sun protection factors are becoming increasingly popular. Nonetheless, to our knowledge only few clinical reports focus on UV-induced skin damage in Non-Caucasians and most of them concentrate on the impact of UV-light rather than on the efficacy of prevention.
Particularly in Asian countries, there is therefore a great interest in light protection filters or mixtures of light protection filters which preserve the color of the skin following solar irradiation and, moreover, are able to impart a lighter appearance to the skin.
The object of the present invention is therefore to find organic UV filters, which prevent tanning of the skin and at the same time, in combination with pigment-regulators are able to lighten the skin.
Surprisingly, we have now found that specific benzophenone organic UV filters can achieve this object.
The present invention therefore provides for the use of (a) UV filters selected from the compounds of formula
R1 and R2, independently from each other are hydrogen; C1-C20alkyl; C2 -C10alkenyl; C3-C10cycloalkyl; C3-C10cycloalkenyl; or R1 and R2 together with the nitrogen atom to which they are bonded can form a 5- or 6-membered ring;
R3 and R4, independently from each other are C1-C20alkyl; C2-C10alkenyl; C3-C10-cycloalkyl; C3-Clocycloalkenyl; C1-C12alkoxy; C1-C20alkoxycarbonyl; C1-C12alkylamino; C1-C12dialkylamino; C6-C10aryl; C6-C10heteroaryl, optionally substituted, substituents which confer solubility in water, chosen from the group consisting of a nitrile group, carboxylate, sulfonate or ammonium radicals;
X is hydrogen; COOR5; CONR6R7;
R6 and R7, independently from each other are hydrogen; C1-C20alkyl; C2-C10alkenyl; C3-Clocycloalkyl; C3-C10cycloalkenyl; or (Y—O)o-Z-aryl;
Y is —(CH2)2—; —(CH2)3; —(CH2)4—; —CH(CH3)—CH2—;
Z is —CH2—CH3; —CH2—CH2—CH3; —CH2—CH2—CH2—CH3; —CH(CH3)—CH3;
m is a number from 0 to 3;
n is a number from 0 to 4; and
o is a number from 1 to 20;
as organic UV filters for preventing tanning human skin.
Alkyl radicals R1 to R7 which may be mentioned are branched or unbranched C1-C20alkyl chains, preferably methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, n-pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, 2,2-dimethylpropyl, 1-ethylpropyl, n-hexyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, 1,1-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, 3,3-dimethylbutyl, 1-ethylbutyl, 2-ethylbutyl, 1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, 1-ethyl-1-methylpropyl, 1-ethyl-2-methylpropyl, n-heptyl, n-octyl, 2-ethylhexyl, n-nonyl, n-decyl, n-undecyl, n-dodecyl, n-tridecyl, n-tetradecyl, n-pentadecyl, n-hexadecyl, n-heptadecyl, n-octadecyl, n-nonadecyl or n-eicosyl.
Alkenyl radicals R1 to R7 which may be mentioned are branched or unbranched C2-C10alkenyl chains, preferably vinyl, propenyl, isopropenyl, 1-butenyl, 2-butenyl, 1-pentenyl, 2-pentenyl, 2-methyl-1-butenyl, 2-methyl-2-butenyl, 3-methyl-1-butenyl, 1-hexenyl, 2-hexenyl, 1-heptenyl, 2-heptenyl, 1-octenyl or 2-octenyl.
Cycloalkyl radicals which may be mentioned for R1 to R7 are preferably branched or unbranched C3-C10-cycloalkyl chains such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, 1-methylcyclopropyl, 1-ethylcyclopropyl, 1-propylcyclopropyl, 1-butylcyclopropyl, 1-pentylcyclopropyl, 1-methyl-1-butylcyclopropyl, 1,2-dimethylcyclopropyl, 1-methyl-2-ethylcyclopropyl, cyclooctyl, cyclononyl or cyclodecyl.
Cycloalkenyl radicals which may be mentioned for R1 to R7 are preferably branched or unbranched C3-C10cycloalkenyl chains with one or more double bonds such as cyclopropenyl, cyclobutenyl, cyclopentenyl, cyclopentadienyl, cyclohexenyl, 1,3-cyclohexadienyl, 1,4-cyclohexadienyl, cycloheptenyl, cycloheptatrienyl, cyclooctenyl, 1,5-cyclooctadienyl, cyclooctatetraenyl, cyclononenyl or cyclodecenyl.
The cycloalkenyl and cycloalkyl radicals may be unsubstituted or substituted by one or more, e.g. 1 to 3, radicals such as halogen, e.g. fluorine, chlorine or bromine, cyano, nitro, amino, C1-C4-alkylamino, C1-C4-dialkylamino, hydroxyl, C1-C4-alkyl, C1-C4-alkoxy or other radicals, or contain 1 to 3 heteroatoms such as sulfur, nitrogen, whose free valences can be saturated by hydrogen or C1-C4-alkyl, or oxygen in the ring.
Suitable alkoxy radicals for R3 and R4 are those having 1 to 12 carbon atoms, preferably having 1 to 8 carbon atoms.
Examples which may be mentioned are: methoxy, ethoxy, isopropoxy, n-propoxy, 1-methylpropoxy, n-butoxy, n-pentyloxy, 2-methylpropoxy, 3-methylbutoxy, 1,1-dimethylpropoxy, 2,2dimethylpropoxy, hexyloxy, 1-methyl-1-ethylpropoxy, heptyloxy, octyloxy or 2-ethylhexyloxy.
Examples of alkoxycarbonyl radicals for R3 and R4 are esters containing the abovementioned alkoxy radicals or radicals derived from higher alcohols, e.g. having up to 20 carbon atoms, such as iso-C15 alcohol.
Suitable mono- or dialkylamino radicals for R3 and R4 are those containing alkyl radicals having 1 to 12 carbon atoms, such as methyl, n-propyl, n-butyl, 2-methylpropyl, 1,1-dimethylpropyl, hexyl, heptyl, 2-ethylhexyl, isopropyl, 1-methylpropyl, n-pentyl, 3-methylbutyl, 2,2-dimethylpropyl, 1-methyl-1-ethylpropyl and octyl.
Aryl means aromatic rings or ring systems having 6 to 18 carbon atoms in the ring system, for example phenyl or naphthyl, each of which may be unsubstituted or substituted by one or more radicals such as halogen, e.g. fluorine, chlorine or bromine, cyano, nitro, amino, C1-C4-alkylamino, C1-C4-dialkylamino, hydroxyl, C1-C4-alkyl, C1-C4-alkoxy or other radicals. Unsubstituted or substituted phenyl, methoxyphenyl and naphthyl are preferred.
Heteroaryl radicals are advantageously simple or fused aromatic ring systems having one or more heteroaromatic 3- to 7-membered rings. Heteroatoms which may be present in the ring or ring system are one or more nitrogen, sulfur and/or oxygen atoms. Hydrophilic radicals, i.e. those making it possible for the compounds of the formula (1) to dissolve in water. R3 and R4 are, for example, the nitrile group and carboxyl and sulfoxy radicals and, in particular, their salts with any physiologically tolerated cations, such as the alkali metal salts or such as the trialkylammonium salts, such as tri(hydroxyalkyl)ammonium salts or the 2-methyl-1-propanol-2-ammonium salts. Also suitable are ammonium radicals, especially alkylammonium radicals, with any physiologically tolerated anions.
The substituents R1 and R2 may, together with the nitrogen atom to which they are bonded, form a 5- or 6-membered ring, for example a pyrrolidine or piperidine ring.
The amino group can be in the ortho, meta or para position relative to the carbonyl group. The para position is preferred.
Preferably compounds of formula
are used, wherein R1 and R2 independently from each other are hydrogen, C1-C12alkyl; or R1 and R.2 together with the nitrogen atom to which they are bonded form a 5- or 6-membered ring; and
R5 is hydrogen, C1-C12alkyl, C3-C6cycloalkyl.
Preferably compounds of formula (1) are used, wherein R1 and R2, independently from each other are C1-C5alkyl; and
R5 is C1-C12alkyl; and more preferably compounds of formula (1) or (2), wherein
R1 and R2, independently from each other are C1-C5alkyl; and
R5 is C1-C12alkyl.
Compounds of formula (1) or (2), wherein R1 and R2 have the same meaning, are of most preferred interest.
Most preferably the compound of formula
is used.
The compounds of formula (1) are suitable as active ingredients in cosmetic preparations. The compounds can preferably be used in dissolved form.
The cosmetic formulations or pharmaceutical compositions according to the present invention may additionally contain one or more than one further UV filter (b).
The additional UV filters (b) are selected from p-aminobenzoic acid derivatives, salicylic acid derivatives, benzophenone derivatives different from those of formula (1), dibenzoylmethane derivatives, diphenylacrylates, 3-imidazol4-ylacrylic acid and esters; benzofuran derivatives, polymeric UV absorbers, cinnamic acid derivatives, camphor derivatives, hydroxyphenyltriazine compounds, benzotriazole compounds, trianilino-s-triazine derivatives, 2-phenylbenzimidazole-5-sulfonic acid and salts thereof, menthyl o-aminobenzoates, physical coated or non-coated sunscreens, perfluoroalcohol phosphate, aminohydroxy-benzophenone derivatives and phenyl-benzimidazole derivatives.
Preferably, the following UV filter combinations are of special interest:
(a1) at least one UV-filter of formula (1) and
(a2) at least one aminobenzophenone derivative
(b1) at least one UV-filter of formula (1), preferably the compound of formula (3); and
(b2) benzoic acid,4,4′-[[6-[[4-[[(1,1 -dimethylethyl)amino]carbonyl]phenyl]amino]1,3,5-triazine-2,4-diyl]diimino]bis-,bis(2-ethylhexyl)ester; diethyihexyl butamido triazone (Uvasorb HEB);
(c1) at least one UV filter of formula (1); and
(c2) at least one benzotriazole derivative of formula
wherein
T2 is C1-C10alkyl or phenyl-substituted C1-C4alkyl;
(d1) at least one UV-filter of formula (1); and
(d2) at least hydroxyphenyltriazine compound
Most preferred are UV-filter combinations (D1) comprising
(d3) the compound of formula (3); and
(d4) the compound of formula
(f1) at least one UV-filter of formula (1); and
(f2) at least one dibenzoylmethane derivative
Most preferred are UV-filter combinations (F1) comprising
(f3) the compound of formula (3); and
(f4) 1-[4-(1,1-dimethylethyl)phenyl]-3-(4-methoxyphenyl)propane-1,3-dione (Avobenzone);
(g1) at least one UV-filter of formula (1), preferably the compound of formula (3); and
(g2) disodium phenyl dibenzimidazole tetrasulfonate (Heliopan AP).
(h1) at least one symmetrical triazine derivatives of formula (1); and
(h2) benzoxazole-substituted triazines of formula
R1, R2 and R3 independently from each other are branched or unbranched C1-C12alkyl.
Furthermore, UV filter combination (H2) comprising
(h5) the compound of formula (3); and
(h6) at least one of the compound of formula (h21), wherein
(h61) R1 and R2 are tert.amyl; and R3 is tert.butyl; or wherein
(h62) R1 and R2 are tert.butyl and R3 is tert.octyl; or wherein
(h63) R1 and R2 are tert.butyl; and R3 is 2-ethylhexyl; or wherein
(h64) R1 and R2 are tert.amyl; and R3 is 2-ethylhexyl; are of preferred interest.
(i1) at least one UV-filter of formula (1), preferably the compound of formula (3); and
(i2) 2-(2H-benzotriazol-2-yl)-4-methyl-6-[2-methyl-3-[1,3,3,3-tetramethyl-1-[(trimethyl-silyl)oxy]disiloxanyl]propyl]-; (CAS-No. 155633-54-8; Drometrizole Trisiloxane; Mexoryl XL);
(k1) at least one UV-filter of formula (1), preferably the compound of formula (3); and
(k2) siloxanes and silicones, di-Me, 1-[[4-[3-ethoxy-2-(ethoxycarbonyl)-3-oxo-1-propenyl]phenoxy]methyl]ethenyl Me, 3-[4-[3-ethoxy-2-(ethoxycarbonyl)-3-oxo-1-propenyl]-phenoxy]-1-propenyl Me, Me hydrogen (Dimethicodiethylbenzalmalonate; CAS-No. 207574-74-1);
(l1) at least one UV-filter of formula (1), preferably the compound of formula (3); and
(l2) (+/−)-1,7,7-trimethyl-3-[(4-methylphenyl)methylene]bicyclo[2.2.1]heptan-2-one; p-methyl benzylidene camphor;
(m1)at least one UV-filter of formula (1), preferably the compound of formula (3); and
(m2) 1-(2-oxoborn-3-ylidene)toluene4-sulphonic acid and its salts (Mexoryl SL);
(n1) at least one UV-filter of formula (1), preferably the compound of formula (3); and
(n2) methyl N,N,N-trimethyl-4-[(4,7,7-trimethyl-3-oxobicyclo[2,2,1]hept-2-ylidene)methyl]-anilinium sulphate (Mexoryl SO);
(o1) at least one UV-filter of formula (1), preferably the compound of formula (3); and
(o2) 2-ethylhexyl 2-cyano,3,3-diphenylacrylate (Octocrylene);
(p1) at least one UV-filter of formula (1), preferably the micronized compound of formula (3); and
(p2) 2-ethylhexyl 4-methoxycinnamate (octyl methoxy cinnamate);
(q1) at least one UV-filter of formula (1), preferably the compound of formula (3); and
(q2) benzoic acid, 4,4′,4″-(1,3,5-triazine-2,4,6-triyltriimino)tris-,tris(2-ethylhexyl)ester; 2,4,6-Trianilino-(p-carbo-2′-ethylhexyl-1′-oxi)-1,3,5-triazine (Ethylhexyl Triazone);
(r1) at least one UV-filter of formula (1), preferably the compound of formula (3); and
(r2) 2-phenyl-1H-benzimidazole-5-sulphonic acid (Phenylbenzimidazol sulfonic Acid);
Cosmetic compositions comprising a UV filter according to component (a) and optionally of component (b) are useful anti-tanning agents.
Cosmetic or pharmaceutical preparations contain from 0.05-40% by weight, based on the total weight of the composition, of a UV filter according to component (a) and optionally of component (b).
Preference is given to the use of mixing ratios of the UV absorber of formula (1) (component (a)) and optionally further UV filters (component (b)) (as for example described in Table 1-3) from 1:99 to 99:1, preferably from 1:95 to 95:1 and most preferably from 10:90 to 90:10, based on weight. Of special interest are mixing ratios of from 20:80 to 80:20, preferably from 40:60 to 60:40 and most preferably approximately 50:50. Such mixtures can be used, inter alia, to improve the solubility or to increase UV absorption.
The UV filters of component (b) according to the present invention can be used either in the dissolved state (soluble organic filters, solubilized organic filters) or in the micronised state (nanoscalar organic filters, particulate organic filters, UV-absorber pigments).
Any known process suitable for the preparation of microparticles can be used for the preparation of the micronised UV absorbers, like wet-milling, wet-kneading, spray-drying from a suitable solvent, by the expansion according to the RESS process (Rapid Expansion of Supercritical Solutions) of supercritical fluids (e.g. CO2) in which the UV filter or filters is/are dissolved, or the expansion of fluid carbon dioxide together with a solution of one or more UV filters in a suitable organic solvent; or by reprecipitation from suitable solvents, including supercritical fluids (GASR process=Gas Anti-Solvent Recrystallisation/PCA process=Precipitation with Compressed Anti-solvents).
The micronised UV absorbers so obtained usually have an average particle size from 0.02 to 2, preferably from 0.03 to 1.5, and more especially from 0.05 to 1.0 micrometer.
The UV absorbers according to the present invention can also be used as dry substrates in powder form.
The UV absorbers according to the present invention can also be used in specific carriers for cosmetics, for example in solid lipid nanoparticles (SLN) or in inert sol-gel microcapsules wherein the UV absorbers are encapsulated (Pharmazie, 2001 (56), p. 783-786). Lipid nanoparticles (CLN,=Crystalline Lipid Nanoparticles) as described in Internat. J. Pharmaceutics, 2002, 242, P. 373-375 can be used as active carrier for UV filter according to the invention.
The cosmetic composition used according to the present invention may additionally contain one or more than one further UV filter.
The UV filters according to component (a) and (b) can be prepared for their use in cosmetic preparations by physically mixing the UV filter(s) with the adjuvant using customary methods, for example by simply stirring together the individual components, especially by making use of the dissolution properties of already known cosmetic UV fitlers, like octyl methoxy cinnamate, salicylic acid isooctyl ester, etc. The UV filter can be used, for example, without further treatment, or in the micronised state, or in the form of a powder.
As component (c) cosmetic and/or pharmaceutical active substances can be used.
Examples of active ingredients which can be used and which may be mentioned are:
As component (d) pigment regulators, preferably skin whitening agents, may additionally be used.
Useful representatives for component (d) are the following classes of substances:
1. γ-pyron derivates according to formula
wherein R is hydrogen (=kojic acid; 5-hydroxy-2-hydroxymethyl-4H-pyran-4-on); or the radical of formula
2. Hydrochinon, also as glycosides and hydrochinon derivatives as glycosides, like 4-hydroxyphenyl-D-glucopyranoside (=α-, or β-Arbutin) of formula
(β-Arbutin); 4-methoxyphenethylmethylether-D-glucopyranoside; 1,5,9,13-tetramethyl-4,8,12-tetradecatrienyl (9CI); 5,9,13-pentadecatriene-2-ol, 6,10,14-trimethyl-(9CI); 1,5,9,1 3-tetramethyltetradecyl-D-glucopyranoside.
3. Resorcin derivatives like glabridin (1,3-benzenediol, 4-[(3R)-3,4-dihydro-8,8-dimethyl-2H,8H-benzo[1,2-b:3,4-b′]dipyran-3-yl]-) or 4-butylresorcinol (=rucinol); 2,4-di-hydroxybenzophenones and isomeric benzophenones;
4. Glycines, L-α-glutamyl-L-cysteinyl- (=glutathion); cetylcystein; oligopeptides;
5. Alkyldicarboxclic acids, like azelain acid (nonandicarboxylic acid) and its mono- and diester;
6. 1,2-dihydroxyphenyl derivatives, like 4-(3,4-dihydroxyphenyl)butan-2-ol; 4-hydroxy-3-methoxybenzylacetone (=gingerone); 4H-1-benzopyran-4-one, 2-(3,4-dihydroxy-phenyl)-3,5,7-trihydroxy-(=quercitin), of formula
7. Urea, (2,5-dioxo-4-imidazolidinyl)- (=allantoin) of formula
8. Furanones, like 3-Hydroxy4,5-dimethyl-2(5H)-furanone; 3-Hydroxy-4-methyl-5-ethyl-2(5H)-furanone;
9. Phenylacetaldehydes;
10. Benzaldehydes; like 4-hydroxybenzaldehyd and 3-methylbenzaldehyd;
11. 4-methoxycinnamaldehyde;
12. Isomeric Decene acid (C10H18O2);
13. Ascorbic acid and derivatives thereof, like 6-aycylascorbic acid-2-glucoside; sulfate, stearate or phosphate of ascorbic acid;
14. Salicylic acid derivatives like 6-[(8Z)-8-pentadecenyl]-salicylic acid; (anacardinacid-monoen) and 6-[(8Z, 11Z)-8, 11, 14-pentadecatrienyl] salicylic acid (anacardinacid-triene);
15. phenolic compounds like 3-[8(Z)-pentadecenyl]phenol or curuminphenolic compounds like curcumin or hydroxydiphenylether compounds like Triclosan or Diclosan;
16. Benzo[b]pyranderivative like [1]benzopyrano[5,4,3-cde][1]benzopyran-5, 10-dion, 2,3,7,8-tetrahydroxy- (7CI, 8CI, 9CI) (=Ellagic acid); 2′-hydroxy-2,4,4,7,4′-pentamethylflavan; 2′-Flavanol, 2,4,4,4′,7-pentamethyl-, acetate; 2-(3,4-dihydro-2,4,4,7-tetramethyl-2H-1-benzopyran-2-yl)-5-methylphenyl und (8β-giglycopyranosyl-7-hydroxy-5-methyl-2-(2-oxopropyl)-4H-1-benzopyran-4-on (Aloesin), of formula
17. Bornyl- and cinnamate-derivatives, like 2-propenoic acid, 3-(4-hydroxyphenyl)-,1,7,7-trimethylbicyclo[2.2.1]hept-2-yl ester, endo-; 2-propenoic acid, 3-(4-methoxyphenyl)-, 1,7,7-trimethylbicyclo[2.2.1]hept-2-yl ester, endo-; 2-propenoic acid, 3-(4-hydroxyphenyl)-, 1-methyl-3-(2,2,6-trimethylcyclohexyl)propyl ester; 2-propenoic acid, 3-phenyl-, 1 -methyl-3-(2,2,6-trimethylcyclohexyl)propyl ester; 2-propenoic acid, 3-[4-(β-D-glucopyranosyloxy)phenyl]-, (1R,2S,4R)-1,7,7-trimethylbicyclo[2.2.1]hept-2-yl ester.
18. Azulenes and derivatives thereof like Guajazulen or Vetivazulen and Guaiol;
19. Cell messenger substances like cytokines; prostaglandines and peptide growth factors;
20. α-Hydroxy-carboxylic acids like α-hydroxypropionic acid, citric- and aconite acid
21. Compounds of formula
22. Compounds of formula
Preferably, the pigment regulator (d) is selected from kojic acid, arbutin, quercitin, aloesin, azelain acid, guaiol, and ellac acid.
The cosmetic or pharmaceutical preparations used for the present invention can be prepared by physically mixing components (a)-(d) with the adjuvant using customary methods, for example by simply stirring together the individual components, especially by making use of the dissolution properties of already known cosmetic UV absorbers, like octyl methoxy cinnamate, salicylic acid isooctyl ester, etc.
The cosmetic or pharmaceutical preparations may be, for example, creams, gels, lotions, alcoholic and aqueous/alcoholic solutions, emulsions, wax/fat compositions, stick preparations, powders or ointments. In addition to the above mentioned UV filters, the cosmetic or pharmaceutical preparations may contain further adjuvants.
As water- and oil-containing emulsions (e.g. W/O, O/W, O/W/O and W/O/W emulsions or microemulsions) the preparations contain, for example, from 0.1 to 30% by weight, preferably from 0.1 to 15% by weight and especially from 0.5 to 10% by weight, based on the total weight of the composition, of one or more UV absorbers, from 1 to 60% by weight, especially from 5 to 50% by weight and preferably from 10 to 35% by weight, based on the total weight of the composition, of at least one oil component, from 0 to 30% by weight, especially from 1 to 30% by weight und preferably from 4 to 20% by weight, based on the total weight of the composition, of at least one emulsifier, from 10 to 90% by weight, especially from 30 to 90% by weight, based on the total weight of the composition, of water, and from 0 to 88.9% by weight, especially from 1 to 50% by weight, of further cosmetically acceptable adjuvants.
The cosmetic or pharmaceutical compositions are useful agents for tanning prevention, skin wrinkling, anti-skinlifting and, together with pigment regulators (=component (d)), as skin lightening agents.
The cosmetic or pharmaceutical compositions/preparations according to the invention may also contain one or one more additional compounds like-fatty alcohols, esters of fatty acids, natural or synthetic triglycerides including glyceryl esters and derivatives, pearlescent waxes, hydrocarbon oils. silicones or siloxanes (organosubstituted polysiloxanes), fluorinated or perfluorinated oils, emulsifiers, super-fatting agents, surfactants, consistency regulators/thickeners and rheology modifiers, polymers. deodorising active ingredients, anti-dandruff agents, hvdrotropic agents, preservatives, antimicrobials, perfume oils, colourants, insect repellents or polymeric beads or hollow spheres as SPF enhancers
Cosmetic or Pharmaceutical Preparations
Cosmetic or pharmaceutical formulations are contained in a wide variety of cosmetic preparations, like skin-care preparations, cosmetic personal care preparations, light-protective preparations, skin-tanning preparations, depigmenting preparations, insect-repellents or preparations for cleansing and caring for blemished skin,
Presentation Forms
The final formulations listed may exist in a wide variety of presentation forms, for example:
Of special importance as cosmetic preparations for the skin are light-protective preparations, such as sun milks, lotions, creams, oils, sunblocks or tropicals, pretanning preparations or after-sun preparations, also skin-tanning preparations, for example self-tanning creams. Of particular interest are sun protection creams, sun protection lotions, sun protection milk and sun protection preparations in the form of a spray.
The examples below serve to illustrate the invention without limiting it thereto. The cosmetic active substances are primarily given with their INCI name (INCI=Intemational Nomenclature of Cosmetic Ingredients).
Materials and Methods
1. Skin Color Measurement:
Skin color was measured in the L*a*b* colour by means of a Minolta CM-508i®) Chromameter).
2. Biophysical Skin Parameters
Skin moisture was assessed with a Corneometer® and skin elasticity and tension by a Cutometer®) (both from Courage & Khazaga, Kön, Germany).
Skin smoothness and skin wrinkles were measured by contact-free profilometry, Leica, Quantimet 6® (Leica Heidelberg, Germany).
3. Testpanel
a. Asian Volunteers
10 Volunteers of originating from S-E-Asia and with a skinlightness L* between 65.4 and 40.8 were recruited following COLIPA-Guidelines.
b. Indian Volunteers
10 Volunteers of Indian origin with a skinlightness L* between 41.1. and 33.6 were recruited following COLIPA-Guidelines.
c. White Caucasian Volunteers
10 Volunteers of European origin with a skin lightness L* between 68.8 and 56.2 were recruited following COLIPA-Guidelines.
4. Volunteers and Measurements
The influence of extensive sun exposure on skin pigmentation and the protective effects of day care cosmetics were directly measured on the back of volunteers:
40 and 20 minutes prior to irradiation volunteers treated on the back with 2 mg/cm2 of cream formulation.
Then tey were irradiated with simulated solar light for 12 weeks, 3-times a week with a dose≦1 MED (Minimal erythema dose; MED adjusted monthly).
The skin of the volunteers was assessed prior to the test and monthly prior to cream application and irradiation.
Tanning Prevention
The influence of extensive sun exposure on skin pigmentation and the protective effects of a day cream containing
Aqua (up to 100%);
was directly measured on the back of Asian volunteers.
The skin of the volunteers was assessed prior to the test and monthly prior to cream application and irradiation for skin color by a Minolta Colorimeter 508i.
As documented, skin tanning could be markedly prevented by the day cream
Prevention of Skin Wrinkling by UV-A Absorbing Day Cream
Skin smoothness and skin wrinkles were assessed on the back of 10 Indian volunteers prior to the test and monthly prior to cream application and irradiation by a contact-free profilometry, Leica, Quantimet 600® (Leica Heidelberg, Germany).
Manufacturing Instruction:
Part A by is prepared by incorporating all ingredients, then stirred under moderate speed and heated to 75° C. Part B s prepared and heated to 75° C. At this temperature part B is poured into part A under progressive stirring speed. Then the mixture is homogenized (30sec., 15000 rpm ). At a temperature<55° C. the ingredients of part C are incorporated. The mixture is cooled down under moderate stirring, then the pH is checked and adjusted with triethanolamine.
Retention of Moisturing Activity of Day Cream Thanks to UV-Absorber Measured on 12 Caucasian Volunteers
Skin moisture was assessed with a Corneometer® prior to the test and monthly prior to irradiation.
As can besen from the results of Table 3, the moisturing activity is significantly enhenced with the UV absorber containing cream as sued in the present invetion.
Number | Date | Country | Kind |
---|---|---|---|
04101375.6 | Apr 2004 | EP | regional |
Filing Document | Filing Date | Country | Kind | 371c Date |
---|---|---|---|---|
PCT/EP05/51325 | 3/23/2005 | WO | 9/20/2006 |