Ziprasidone formulations
AssigneePfizer Inc.
InventorsDaniel R. Arenson, Frank Robert Busch, Angela G. Hausberger, Bijan Rasadi
Life of this patent
Estimating the term…
Abstract
Compositions comprising crystalline ziprasidone free base or crystalline ziprasidone hydrochloride particles having a mean particle size less than 85 .mu.m, and a pharmaceutically acceptable carrier, are substantially bioequivalent and can be used to treat psychoses such as schizophrenia.
Claims34
A composition comprising crystalline ziprasidone free base or crystalline ziprasidone hydrochloride particles having a mean particle size equal to or less than about 85 .mu.m and a pharmaceutically acceptable diluent or carrier.
A composition comprising crystalline ziprasidone free base or crystalline ziprasidone hydrochloride particles having a mean particle size equal to or less than about 85 .mu.m, as measured by Malvern light scattering, and a pharmaceutically acceptable carrier, said composition exhibiting a mean AUC and/or C.sub.max which is at least 80% of the mean AUC exhibited by a composition equivalent thereto but differing only in that it has a crystalline ziprasidone hydrochloride mean particle size of 20 .mu.m.
A composition as defined in clam 17, which comprises crystalline ziprasidone hydrochloride monohydrate.
A process of preparing large crystals of ziprasidone hydrochloride monohydrate, comprising the steps of:
- 1) dissolving ziprasidone free base in a solvent comprising THF and water, in a volume ratio of about 22-35 unit volumes of THF to about 1.5-8 volumes of water;
- 2) heating the solution resulting from step (1);
- 3) adding HCl to the solution resulting from step (2);
- and
- 4) cooling the solution resulting from step (3).
Dependencies are inferred from the claim text.