Identification, preparation, and characterization of several polymorphs and solvates of terazosin hydrochloride.
The phenomenon of polymorphism is prevalent in pharmaceuticals, yet it is unusual to identify more than three or four forms for any particular drug. Terazosin hydrochloride has been found to exist at room temperature in four solvent-free forms that can be isolated directly, one solvent-free form that can be prepared by desolvation of a methanolate, a methanol solvate, and a dihydrate. This study presents characterization and methods for preparation of each of these forms. Data are also presented demonstrating the relative stability of these forms.
Bauer
J
J
Abbott Laboratories, North Chicago, Illinois 60064-6293, USA. john.f.bauer@abbott.com
Morley
J
J
Spanton
S
S
Leusen
F J J
FJ
Henry
R
R
Hollis
S
S
Heitmann
W
W
Mannino
A
A
Quick
J
J
Dziki
W
W
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D003198:Computer Simulation; D018360:Crystallography, X-Ray; D004355:Drug Stability; D006813:Humidity; D009682:Magnetic Resonance Spectroscopy; D000432:Methanol / Q000737:chemistry; D008958:Models, Molecular; D015394:Molecular Structure; D044367:Phase Transition; D011224:Prazosin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D012997:Solvents / Q000737:chemistry*; D014867:Water / Q000737:chemistry
D000970:Antineoplastic Agents; D012997:Solvents; D014867:Water; C041226:Terazosin; D011224:Prazosin; D000432:Methanol