Polymorphs of a crystalline azabicyclo (2,2,2) octan-3-amine...

Details Polymorphs of a crystalline azabicyclo (2,2,2) octan-3-amine... Polymorphs of a crystalline azabicyclo (2,2,2) octan-3-amine...

C - Chemistry, Metallurgy

07

D

C07D 453/02 (2006.01) A61K 31/439 (2006.01) A61P 1/08 (2006.01)

Patent

CA 2372238

A single crystalline polymorphic form (2S, 3S)-N-(2-methoxy-5-t-butylphenyl)methyl-2-diphenylmethyl-1-azabicyclo [2,2,2] octan-3-amine citrate monohydrate and its pharmaceutical composition. The pharmaceutical composition of the polymorphic form of the citrate monohydrate has advantageous stability for formulation to treat emesis. The administration of this pharmaceutical composition is immediate release, oral dosage form preferably by tablet or capsule or intravenous.

L'invention concerne une forme polymorphe cristalline unique (2S, 3S)-N-(méthoxy-5-t-butylphénylméthyl-2-diphénylméthyl-1-azobicyclo (2,2,2) octan-3-amine citrate(monohydrate de citrate) et sa composition pharmaceutique. Ladite composition est de forme polymorphe, si le monohydrate de citrate présente une stabilité avantageuse sur le plan de sa préparation destinée à traiter l'émèse. L'administration de cette composition pharmaceutique est à libération immédiate, et s'effectue par dosage buccal, sous forme de comprimé ou de gélules, ou par voie intraveineuse.

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