通过差示扫描量热法（DSC）和热重分析法（TG）测定药物悬浮液中氯硝柳胺溶剂化物的物理转变

Physical transformation of niclosamide solvates in pharmaceutical suspensions determined by DSC and TG analysis.

作者信息

de Villiers M M, Mahlatji M D, Malan S F, van Tonder E C, Liebenberg W

机构信息

Department of Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana at Monroe, 71209, USA.

出版信息

Pharmazie. 2004 Jul;59(7):534-40.

PMID:15296091

Abstract

This study reports the preparation of four niclosamide solvates and the determination of the stability of the crystal forms in different suspension vehicles by DSC and TG analysis. Thermal analysis showed that the niclosamide solvates were extremely unstable in a PVP-vehicle and rapidly changed to monohydrated crystals. A suspension in propylene glycol was more stable and TG analysis showed that crystal transformation was less rapid. In this vehicle, the crystals transformed to the anhydrate, rather than the monohydrate, since the vehicle was non-aqueous. The TEG-hemisolvate was the most stable in suspension and offered the best possibility of commercial exploitation.

摘要

本研究报告了四种氯硝柳胺溶剂化物的制备，以及通过差示扫描量热法（DSC）和热重分析（TG）测定不同混悬剂中晶型的稳定性。热分析表明，氯硝柳胺溶剂化物在聚乙烯吡咯烷酮（PVP）混悬剂中极不稳定，并迅速转变为一水合物晶体。丙二醇混悬剂更稳定，TG分析表明晶体转变较慢。在这种溶剂中，晶体转变为无水物而非一水合物，因为该溶剂为非水性。三甘醇半溶剂化物在混悬剂中最稳定，具有最佳的商业开发可能性。