Progress on transformation and manipulation of drug polymorphism

doi:10.3969/j.issn.0438-1157.2013.02.001

Abstract

Abstract: The drug polymorphism has a profound effect on the quality, safety and efficiency of the drug product.The Twelfth Five-Year Development Plan of China's Pharmaceutical Industry puts forward one of the major development tasks and technologies focused on the improvement in drug polymorphism study to enhance the quality and safety of the drugs.In this paper, the solubility behavior coupled with the solid state and solution mediated transformation of drug polymorphs are introduced and analyzed.In addition, solvent and additive/template play a critical role in the manipulation of drug crystal form.In many cases, physical field (ultrasound, microwave and high gravity-field)-assisted crystallization gives different results for the manipulation of drug crystal form by specific mechanism.Meanwhile, with the rapid development of process analytical technologies, process optimization and control are enhanced through getting more knowledge of drug polymorphism transformation.In the future, the research of transformation and manipulation of pharmaceutical drug polymorphism will focus on the molecular assembly and regulation, process analysis and structure-activity relationship of drugs.

Key words: drug polymorphism, transformation, manipulation

摘要： 药物晶型可显著影响药品质量、安全性和有效性,国家"医药工业十二五发展规划"将药物晶型研究列为提升药物质量安全的主要任务和重点技术。本文介绍了药物多晶型的溶解度行为以及晶型转化的液相和固相介导机理,溶剂、添加剂/模板剂对药物晶型的控制有着重要的作用,而物理场效应(超声波、微波、超重力场等)对晶型转化过程起强化效应;过程分析技术的快速发展为晶型转化机理的研究以及过程优化、控制提供了先进手段。未来药物晶型转化与控制的研究将聚焦分子的组装与调控行为、过程分析以及药物的构效关系等方面。

关键词: 药物多晶型, 转化, 控制

CLC Number:

TQ460.6

GONG Junbo, WANG Qi, DONG Weibing, WANG Jingkang. Progress on transformation and manipulation of drug polymorphism[J]. CIESC Journal, 2013, 64(2): 385-392.

龚俊波, 王琦, 董伟兵, 王静康. 药物晶型转化与控制的研究进展[J]. 化工学报, 2013, 64(2): 385-392.

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