Novel delivery of hydroxy carboxylic acids

A - Human Necessities – 61 – K

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Details

A61K 31/695 (2006.01) A61K 6/00 (2006.01) A61K 31/74 (2006.01) A61P 17/00 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2332114

The present invention provides greater than 99 % pure bis(triorganosilyl)hydroxycarboxylates of the general formulae: R3SiO-CHR1-COO- SiR3 and R3SiO-CHR1-R2COO-SiR3 wherein each R is independently a monovalent straight or branched chain alkyl or alkenyl group having from 1 to about 6 carbon atoms, or an aryl group, R1 may be hydrogen, a monovalent straight or branched chain alkyl group having from 1 to about 18 carbon atoms, or an aryl group, and R2 is a divalent straight or branched chain alkyl group having from 1 to about 18 carbon atoms, an aryl group, or a straight or branched chain alkaryl group having from 7 to about 18 carbon atoms; a process for producing the bis(trimethylsilyl)-hydroxycarboxylates comprising the trimethylsilylation with hexamethyldisilazane of the corresponding hydroxy carboxylic acids; cosmetic formulation comprising the greater than 99 % pure bis(trimethylsilyl)hydroxycarboxylates dissolved in aprotic media; and a method of delivering hydroxycarbxylic acids to the epidermis without apparent irritation or inflammation of the epidermis or stratum corneum.

La présente invention concerne des bis(triorganosilyl)hydroxycarboxylates purs à plus de 99 % des formules générales: R¿3?SiO-CHR?1¿-COO-SiR¿3? R¿3?SiO-CHR?1¿-R?2¿COO-SiR¿3? dans lesquelles chaque R représente indépendamment un groupe alkyle ou alcényle à chaîne droite ou ramifiée monovalent possédant 1 à 6 atomes de carbone environ, ou un groupe aryle; R?1¿ peut désigner un hydrogène, un groupe alkyle à chaîne droite ou ramifiée monovalent possédant 1 à 18 atomes de carbone environ, ou un groupe aryle; et R?2¿ désigne un groupe alkyle à chaîne droite ou ramifiée divalent possédant 1 à 18 atomes de carbone environ, un groupe aryle, ou un groupe alkaryle à chaîne droite ou ramifiée possédant 7 à 18 atomes de carbone environ. L'invention concerne également un procédé de production de bis(triméthylsilyl)-hydroxycarboxylates, le procédé consistant à soumettre les acides hydroxy carboxyliques correspondants à une triméthylsilylation avec hexaméthyldisilazane. L'invention concerne aussi une formulation cosmétique comprenant les bis(triméthylsilyl)hydroxycarboxylates purs à plus de 99 % dissous dans un milieu aprotique; et un procédé d'administration d'acides carboxyliques sur l'épiderme sans irritation ou inflammation apparente de l'épiderme ou de la couche cornée.

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