Polymeric delivery formulations of leuprolide with improved...

A - Human Necessities – 61 – K

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A61K 9/00 (2006.01) A61K 9/19 (2006.01) A61K 38/09 (2006.01) A61K 47/34 (2006.01) A61L 27/54 (2006.01) A61F 2/02 (2006.01) A61J 1/05 (2006.01)

Patent

CA 2436275

A flowable composition for use as a controlled release implant, comprising a biodegradable thermoplastic polyester that is at least substantially insoluble in aqueous medium or body fluid, a biocompatible polar aprotic solvent, miscible to dispersible in aqueous medium or body fluid and leuprolide acetate, an implantor a kit comprising such composition, a method for forming the flowable composition. The present invention is also directed to a biodegradable implant formed in situ, in a patient, to a method of forming a biodegradable implant in situ, in a living patient which includes injecting a flowable composition within the body of a patient and allowing the biocompatible polar aprotic solvent to dissipate to produce a solid biodegradable implant and a method of treating cancer in a patient by administering to the patient in need of such treatment an effective amount of a flowable composition of the present invention or a method of reducing LHRH levels in a patient.

L'invention concerne une composition fluide pouvant Útre utilis~e comme implant ~ lib~ration contrÙl~e. Cette composition fluide contient un polyester thermoplastique biod~gradable qui est au moins sensiblement insoluble dans un milieu aqueux ou un liquide organique. Cette composition fluide contient ~galement un solvant aprotique polaire biocompatible qui est miscible ~ dispersable dans un milieu aqueux ou un liquide organique. Cette composition fluide contient de l'ac~tate de leuprolide. Aussi, l'invention concerne une m~thode de pr~paration de la composition fluide, ainsi qu'un implant biod~gradable form~ <i>in situ</i>, chez un patient. La pr~paration de l'implant biod~gradable consiste ~ injecter une composition fluide dans le corps du patient et ~ permettre au solvant aprotique polaire biocompatible de se dissiper pour produire un implant biod~gradable solide. L'invention concerne en outre une m~thode de formation d'un implant biod~gradable <i>in situ</i>, chez un patient vivant. La m~thode consiste ~ injecter une composition fluide dans le corps du patient et ~ permettre au solvant aprotique polaire biocompatible de se dissiper pour produire un implant biod~gradable solide. Par ailleurs, l'invention concerne une m~thode de traitement du cancer chez un patient, consistant ~ lui administrer une dose efficace de la composition fluide. De plus, l'invention concerne une m~thode de r~duction des taux de LHRH chez un patient, consistant ~ lui administrer une dose efficace de ladite composition fluide. L'invention concerne ~galement un kit comprenant un premier r~cipient et un second r~cipient. Le premier r~cipient comprend une composition renfermant un polyester thermoplastique biod~gradable et un solvant aprotique polaire biocompatible. Le second r~cipient contient un ac~tate de leuprolide. Enfin, l'invention concerne un implant solide. Cet implant solide contient un polyester thermoplastique biocompatible et un ac~tate de leuprolide. L'implant solide pr~sente une matrice microporeuse g~latineuse ou solide, ayant l'aspect d'un noyau entour~ d'une peau. L'implant solide peut ~galement contenir un solvant organique biocompatible.

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