Injectable depot formulation comprising crystals of iloperidone

Details Injectable depot formulation comprising crystals of iloperidone Injectable depot formulation comprising crystals of iloperidone

C - Chemistry, Metallurgy

07

D

C07D 413/04 (2006.01) A61K 31/454 (2006.01) A61K 47/10 (2006.01) A61K 47/26 (2006.01) A61K 47/38 (2006.01)

Patent

CA 2492467

An injectable depot formulation comprising crystals having Structure (I) wherein R is (FII) and the X5o value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolite have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.

Cette invention concerne un préparation en dépôt injectable comprenant des cristaux de structure (I) dans laquelle R est (FII) et la valeur X¿5o? des cristaux se situe entre 1 et 200 microns. Les préparations en dépôt renferment des cristaux d'iloperidone ou de son métabolite présentent les avantages suivants: (i) la libération des cristaux dans le plasma peut être corrélée avec la taille des cristaux; (ii) l'absorption des cristaux dans le plasma peut être corrélée à la taille des cristaux; (iii) la taille particulaire des cristaux peut être déterminée au niveau de la fabrication et/ou du broyage; et (iv) les cristaux sont stables au stockage et stables aux méthodes de stérilisation telles que l'irradiation aux rayons gamma.

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