Biodegradable polyanhydrides derived from dimers of bile...

C - Chemistry – Metallurgy – 08 – G

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C08G 67/04 (2006.01) A61K 9/20 (2006.01) A61K 47/34 (2006.01)

Patent

CA 2202676

New biodegradable polyanhydrides are disclosed, which are prepared by homopolymerization of dimer of bile acid, especially lithocholic acid, or bycopolymerization with linear dicarboxylic acid, especially sebacic acid. These biodegradable polyanhydrides have degradation kinetics and a release rate that make them particularly useful for controlled drug release. More specifically, the degradation kinetics of such anhydrides and the release rate of molecules embedded therein make them useful as matrices for controlled drug release systems. The rates of degradation and release can be adjusted by the copolymer composition. The near zero-order kinetrics of release of the drug embedded in the matrices made of such anhydrides, make the same particularly useful since they can deliver an active ingredient at a constant rate for long period of time, avoiding the inauspicious saw-tooth pattern of conventional systemic administration.

Divulgation de nouveaux polyanhydrides biodégradables qui sont préparés par homopolymérisation de dimères de l'acide biliaire, en particulier de l'acide lithocholique, ou par copolymérisation d'acide dicarboxylique linéaire, en particulier de l'acide sébacique. Ces polyanhydrides biodégradables ont une cinétique de dégradation et un taux de libération qui les rendent particulièrement utiles pour la libération contrôlée des médicaments. Plus précisément, la cinétique de dégradation de tels anhydrides et le taux de libération des molécules qui y sont enchâssées les rendent utiles comme matrices pour les systèmes de libération contrôlée des médicaments. Les taux de dégradation et de libération peuvent être réglés par la composition de copolymères. La cinétique presque nulle de libération du médicament enchâssé dans les matrices fabriquées de tels anhydrides rend aussi ces derniers particulièrement utiles puisqu'ils peuvent libérer un principe actif à un taux constant pendant de longues périodes, évitant ainsi la courbe en dents de scie à éviter de l'administration systémique classique.

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