Drug delivery system for administration of a water soluble,...

A - Human Necessities – 61 – K

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Details

A61K 47/20 (2006.01) A61K 9/14 (2006.01) A61P 35/00 (2006.01) A61K 31/136 (2006.01) A61K 31/337 (2006.01) A61K 31/704 (2006.01)

Patent

CA 2709268

A drug delivery system (DDS) for administration of a water soluble, cationic, and amphiphilic pharmaceutically active substance (API) which DDS comprises amorphous particles of <100 nm of a poorly water soluble complex of the API with a Na-salt of N-all-trans-retinoyl cysteic acid methyl ester and/or a Na-salt of N-13- cis-retinoyl cysteic acid methyl ester, which particles are entrapped in nanoparticles formed a Na-salt of N-all-trans- retinoyl cysteic acid methyl ester and/or a Na- salt of N-13--cis-retinoyl cysteic acid methyl ester, the w/w-ratio of Na-salt of N- alltrans-retinoyl cysteic acid methyl ester and/or a Na-salt of N-13-cis-retinoyl cysteic acid methyl ester to the complex is about 0.5:1 to about 20:1. A pharmaceutical composition comprising such a DDS. Methods for preparation of such a DDS and such a pharmaceutical composition. Use of such a DDS and pharmaceutical composition for treatment of cancer.

Cette invention concerne un système d'administration de médicament (DDS) destiné à l'administration d'une substance pharmaceutiquement active, amphiphile, cationique et hydrosoluble (API). Ce système d'administration de médicament (DDS) comprend des particules amorphes inférieures à 100 nm d'un complexe faiblement hydrosoluble constitué de l'API et d'un sel Na d'ester méthylique d'acide cystéique N-all-trans-retinoyl et/ou d'un sel Na d'ester méthylique d'acide cystéique N-13- cis-retinoyl, lesquelles particules sont piégées dans des nanoparticules formées d'un sel Na d'ester méthylique d'acide cystéique N-all-trans-retinoyl et/ou d'un sel Na d'ester méthylique d'acide cystéique N-13-cis-retinoyl, le rapport massique du sel Na d'ester méthylique d'acide cystéique N-all-trans-retinoyl et/ou d'un sel Na d'ester méthylique d'acide cystéique N-13-cis-retinoyl par rapport au complexe est d'environ 0.5:1 à environ 20:1. Cette invention concerne également une composition pharmaceutique comprenant un tel DDS, ainsi que des procédés permettant de préparer un tel DDS et une telle composition pharmaceutique. En outre, cette invention concerne l'utilisation d'un tel DDS ainsi que l'utilisation d'une telle composition pharmaceutique pour traiter le cancer.

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