Variable-temperature X-ray powder diffraction analysis of the crystal transformation of the pharmaceutically preferred polymorph C of mebendazole

被引:44
作者
de Villiers, MM [1 ]
Terblanche, RJ
Liebenberg, W
Swanepoel, E
Dekker, TG
Song, M
机构
[1] Univ Louisiana Monroe, Sch Pharm, Monroe, LA 71209 USA
[2] NW Univ, Sch Pharm, Res Inst Ind Pharm, ZA-2520 Potchefstroom, South Africa
关键词
mebendazole; polymorph transformation; variable-temperature X-ray powder diffraction;
D O I
10.1016/j.jpba.2005.01.025
中图分类号
O65 [分析化学];
学科分类号
070302 ; 081704 ;
摘要
Mebendazole is a common benzimidazole anthelmintic that is water insoluble. It is reported to exist in three different polymorphic forms in the solid state, i.e. polymorph A, B and C. Form C is the pharmaceutically preferred form because of its increased aqueous solubility. This paper deals with the use of variable-temperature X-ray powder analysis (VTXRPD) to study the transformation of Form C. Results showed that Form C was stable and transformed to the more stable polymorph A at high temperature (> 180 degrees C). This transformation is a first-order process with activation energy of 238 +/- 116 kJ/mole. Further studies showed that compression did not cause any significant changes in the crystal structure of polymorph C. (c) 2005 Elsevier B.V. All rights reserved.
引用
收藏
页码:435 / 441
页数:7
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