Identification, preparation, and characterization of several polymorphs and solvates of terazosin hydrochloride

被引:15
作者
Bauer, J [1 ]
Morley, J
Spanton, S
Leusen, FJJ
Henry, R
Hollis, S
Heitmann, W
Mannino, A
Quick, J
Dziki, W
机构
[1] Abbott Labs, N Chicago, IL 60064 USA
[2] Accelrys Ltd, Cambridge CB4 0WN, England
关键词
terazosin; polymorphs; dehydrate; methanolate; molecular modeling; X-ray diffraction;
D O I
10.1002/jps.20425
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 2006 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 95:917-928, 2006.
引用
收藏
页码:917 / 928
页数:12
相关论文
共 37 条
[1]  
ABRAHAM PA, 1985, PHARMACOTHERAPY, V5, P285
[2]  
[Anonymous], SOLID STATE CHEM DRU
[3]   Sulfathiazole polymorphism studied by magic-angle spinning NMR [J].
Apperley, DC ;
Fletton, RA ;
Harris, RK ;
Lancaster, RW ;
Tavener, S ;
Threlfall, TL .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1999, 88 (12) :1275-1280
[4]  
BAUER J, 1994, Patent No. 5362730
[5]  
BERNSTEIN J, 2002, POLYM MOL CRYSTALS
[6]  
Brittain H. B., 2002, AM PHARM REV, V5, P74
[7]  
BURGER A, 1979, MIKROCHIM ACTA, V2, P273
[8]   ANTIHYPERTENSIVE EFFECTIVENESS OF TERAZOSIN - A NEW LONG-ACTING ALPHA-ADRENERGIC INHIBITOR [J].
CHRYSANT, SG ;
BAL, IS ;
JOHNSON, B ;
MCPHERSON, MA .
CLINICAL CARDIOLOGY, 1985, 8 (09) :486-489
[9]   DISAPPEARING POLYMORPHS [J].
DUNITZ, JD ;
BERNSTEIN, J .
ACCOUNTS OF CHEMICAL RESEARCH, 1995, 28 (04) :193-200
[10]  
GRAHAM RM, 1984, AM J CARDIOL, V53, pA16, DOI 10.1016/0002-9149(84)90829-4