Zoniporide mesylate pharmaceutical compositions and...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/04 (2006.01) A61K 31/4709 (2006.01) A61P 9/00 (2006.01)

Patent

CA 2472342

A pharmaceutical composition comprising Zoniporide (N-(5-cyclopropyl-l- quinolin-5yl-lh-pyrazole-4-carbonyl)-guanidine) or its mesylate salt in the presence of an aqueous diluent in the ph range of 2 to 3.5.The composition is a sodium hydrogen exchange-1 (NHE-1)inhibitor for the prevention of,inter alia,perioperative myocardial ischemic injury in mammals.Moreover the application relates to a process for increasing the solubility of Zoniporide employing methanesulfonic acide

L'invention concerne une composition pharmaceutique comprenant du zoniporide (N-(5-cyclopropyl-l-quinolin-5yl-lh-pyrazole-4-carbonyl)-guanidine) ou son mésylate en présence d'un diluant aqueux, avec un pH compris entre 2 et 3,5. La composition constitue un inhibiteur d'échange-1 sodium/hydrogène (NHE-1) pour la prévention, inter alia, d'accident ischémique du myocarde périopératoire chez les mammifères. L'invention concerne, en outre, un procédé permettant d'augmenter la solubilité du zoniporide au moyen d'acide méthanesulfonique.

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