固体药物的转晶现象  

Polymorph transformation of solid drugs

作　　者：张奇 梅雪锋 

机构地区：[1]中国科学院上海药物研究所,上海200203

出　　处：《药学学报》2015年第5期521-527,共7页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81273479;81402898)

摘　　要：在药物开发过程中,有些药物的稳定晶型可能会存在某些缺陷,如溶解度太差等,从而不得不考虑将一些动力学上可以稳定存在的亚稳晶型作为药用晶型开发上市。使用亚稳晶型存在晶型转变的风险。对固体药物转晶现象的研究可以帮助这些使用亚稳晶型的药物选择合适的生产和储存条件,避免因转晶而获得不需要的晶型。For the minimized phase transforming risk, the most stable polymorph is generally considered as the desirable solid form for pharmaceutical applications. However, occasionally, the stable form may have some shortcomings such as low solubility, dissolution rate and bioavailability, etc. In that case, the metastable form which is kinetically stable at room or lower temperature could be selected. Using metastable form may result in polymorph transformation in pharmaceutical manufacture and storage. Hence, the knowledge of the transformation between solid forms is essential to the development of the drug materials. In this paper, we will review the recent studies in the area of crystal conversion of polymorphs and hydrates, to illustrate some cases to introduce the types, conditions and mechanisms of the crystalline solid transformation.

关 键 词：药物稳定性 多晶型 转晶 

分 类 号：R943[医药卫生—药剂学]