ZIPRASIDONE COMPOSITION

PROBLEM TO BE SOLVED: To formulate a ziprasidone free base or a ziprasidone hydrochloride into a composition having a readily handleable and reasonable grain size by using a commonly used method for formulation and apparatus. SOLUTION: This composition comprises crystalline ziprasidone free base or...

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Bibliographic Details
Main Authors ARENSON DANIEL RAY, RASADI BIJAN, FRANK ROBERT BUSCH, HAUSBERGER ANGELA CAROL GATLIN
Format Patent
LanguageEnglish
Published 09.01.2002
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:PROBLEM TO BE SOLVED: To formulate a ziprasidone free base or a ziprasidone hydrochloride into a composition having a readily handleable and reasonable grain size by using a commonly used method for formulation and apparatus. SOLUTION: This composition comprises crystalline ziprasidone free base or crystalline ziprasidone hydrochloride grains having about <=85 μm average grain size and a pharmaceutically acceptable diluent or carrier. Furthermore, the method for producing large crystals of the ziprasidone hydrochloride monhydrate comprises (1) a step of dissolving the ziprasidone free base in which THF and water are contained in a volume ratio of about 22-35 unit volume of the THF to about 1.5-8 volume of the water in a solvent, (2) a step of heating the solution obtained from the step (1), (3) a step of adding HCl to the solution obtained from the step (2), and (4) a step of cooling the solution obtained from the step (3).
Bibliography:Application Number: JP20010175276