Pharmaceutical composition comprising ziprasidone, a process for preparing large crystals of ziprasidone hydrochloride monohydrate

摘要

Pharmaceutical composition comprising crystalline ziprasidone free base or crystalline ziprasidone hydrochloride particles having a mean particle size equal to or less than about micro meters and a pharmaceutically acceptable diluent or carrier. The composition is appropriate for treatment psychoses and schizophrenia. A process for preparing large crystals of ziprasidone hydrochloride monohydrate, according to which (1) ziprasidone free base is dissolved in a solvent comprising THF and water, in a volume ratio of about 22 - 35 unit volumes THF to about 1.5 - 8 volumes of water; (2) the solution resulting from step (1) is heated; (3) HCl is added to the solution resulting from step (2); and (4) the solution resulting from step (3) is cooled.