Gonadotropin releasing hormone antagonists

Details Gonadotropin releasing hormone antagonists Gonadotropin releasing hormone antagonists

A - Human Necessities

61

K

A61K 38/24 (2006.01) A61K 9/14 (2006.01) C07K 17/00 (2006.01)

Patent

CA 2574085

Antagonistic peptides of GnRH having improved water solubility are disclosed. These peptides are capable of suppressing serum testosterone levels in vivo to chemical castration levels of <=0.5 ng/ml. Stable, filter sterilizable, non- gelling solutions containing the GnRH antagonists at least at levels typically used in sustained release formulations also are disclosed, as is a method of increasing the solubility of GnRH antagonist in a polymer containing dispersed phase, which method comprises addition of an acid to the dispersed phase.

L'invention concerne des peptides antagonistes de la GnRH présentant une meilleure solubilité dans l'eau. Ces peptides peuvent rabaisser les niveaux de testostérone sérique in vivo jusqu'à des niveaux de castration chimique =0,5 ng/ml. L'invention concerne également des solutions stables et stérilisables, sans gélification, contenant les antagonistes de la GnRH au moins à des niveaux habituellement utilisés dans les formulations à libération prolongée, ainsi qu'une méthode d'augmentation de la solubilité d'un antagoniste de la GnRH dans une phase dispersée contenant un polymère, ladite méthode comprenant l'ajout d'un acide dans la phase dispersée.

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