Polymorphs of crystalline azo-bicyclo 2,2,2,oct-3-yl amine...

C - Chemistry – Metallurgy – 07 – D

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C07D 453/02 (2006.01) A61K 31/435 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2375265

Two crystalline polymorphic forms of (2-Benzhydryl-1-azo-bicyclo[2,2,2]Octyl-3- yl)-(5-iso-propyl-2-methoxybenzyl)amine dihydrochloride dihydrate are Form I and Form II. The pharmaceutical composition containing at least one of these polymorphs has advantageous stability for formulation to treat emesis in patients receiving chemotherapy. The administration of this pharmaceutical composition is conventional oral by preferably tablet or capsule or intravenous. A method of making Forms I and II is also disclosed.

Selon l'invention, deux formes polymorphes cristallines du dihydrate de dihydrochlorure de (2-Benzhydryl-1-azo-bicyclo[2.2.2]Octyl-3-yl)-(5-iso-propyl-2-méthoxybenzyl)amine représentent la forme I et la forme II. La composition pharmaceutique contenant au moins un de ces polymorphes possède une stabilité favorable aux préparations destinées à traiter les vomissements chez les patients recevant une chimiothérapie. L'administration de cette composition pharmaceutique se fait habituellement par voie orale, de préférence par comprimés ou gélules, ou par voie intraveineuse. L'invention concerne également une méthode de préparation des formes I et II.

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