Injectable depot composition and its' process of preparation

A - Human Necessities – 61 – K

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A61K 9/10 (2006.01) A61K 9/50 (2006.01) A61K 31/138 (2006.01) A61K 31/18 (2006.01) A61K 31/4196 (2006.01) A61K 47/34 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2665105

Novel injectable compositions are provided comprising an active agent which is tarnsulosin or letrozole or its pharmaceutically acceptable salts, derivatives, isomers, polymorphs, solvates, hydrates, analogues, enantiomers, tautomeric forms or mixtures thereof and one or more pharmaceutically acceptable excipient(s) wherein the compositions are preferably formulated as biodegradable microparticles or nanoparticles which can optionally be reconstituted with an aqueous, hydro-alcoholic or oily liquid vehicle prior to administration. The novel injectable compositions of the present invention preferably form a depot upon administration in vivo and are in the form of an in situ gelling composition or an implant composition which provides a prolonged release of tamsulosin or letrozole for extended periods of time. Also described are process for preparation of such novel compositions and method of using them.

Nouvelles compositions injectables comprenant comme principe actif de la tarnsulosine ou du létrozole ou bien des sels, dérivés, isomères, polymorphes, solvates, hydrates, analogues, énantiomères, formes tautomères ou mélanges de qualité pharmaceutique de ces substances ainsi qu'un ou plusieurs excipients de qualité pharmaceutique. Ces compositions, qui se présentent de préférence sous forme de microparticules ou de nanoparticules biodégradables, peuvent être éventuellement reconstituées avec un véhicule hydroalcoolique aqueux ou liquide huileux avant administration. Les compositions injectables de l'invention forment de préférence un dépôt lors de leur administration in vivo et se présentent in situ sous la forme d'une composition ou d'un implant gélifiant assurant la libération de tarnsulosine ou létrozole pendant un laps de temps prolongé. Sont également décrit un procédé de fabrication et une méthode d'utilisation de ces nouvelles compositions.

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