Polymorphs of crystalline...

C - Chemistry – Metallurgy – 07 – D

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C07D 453/02 (2006.01) A61K 31/435 (2006.01) A61P 1/08 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2372236

Two crystalline polymorphic forms of (2-Benzhydryl-1-azo-bicyclo[2.2.2]oct-3- yl)-(5-isopropyl-2-methoxybenzyl)-amine citrate monohydrate (the monohydrates) are Form A and Form B. The pharmaceutical composition containing at least one of these polymorphs has advantageous stability for formulation to treat acute emesis in patient receiving chemotherapy. The administration of this pharmaceutical composition is conventional oral by preferably tablet or capsule and intravenous. A method of making A and B Forms is also disclosed.

L'invention concerne deux formes polymorphiques cristallines de (2-Benzhydryl-1-azo-bicyclo[2.2.2]oct-3-yl)-(5-isopropyl-2-méthoxybenzyl)-amine citrate monohydrate (les monohydrates) désignées par Forme A et Forme B. La composition pharmaceutique, qui comprend au moins un de ces polymorphes, possède une stabilité avantageuse pour élaborer des traitements contre les vomissements aigus chez les patients sous chimiothérapie. L'administration de cette composition pharmaceutique se fait habituellement par voie orale, de préférence, par comprimé ou gélule et par voie intraveineuse. L'invention concerne également un procédé pour fabriquer Forme A et Forme B.

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