药物常见的固态形式有溶剂化物、亚稳定型、无定型和共晶型,这些不同的存在形式影响着药物的溶解度、溶出速率、生物利用度等,有的甚至引发毒副作用,关系着药物的临床疗效。因此,对药物多晶型的研究是进行药物质量控制和管理的重要内容,广受医药研发和管理领域的关注。本文着重综述了单晶X-射线衍射法和粉末X-射线衍射法在药物多晶型研究中的应用进展。
It is well known that pharmaceutical solids can exist in multiple crystalline solid forms,including solvates,metastable formation,amorphization and cocrystal formation.These different polymorphic forms have an impact on solubility,dissolution rate and bioavailability,et al,and may affect the clinical efficacy.In an extreme case,an undesired polymorph can even be toxic.Therefore,the research on drug polymorphism is of importance in the quality control and management of drugs,and it is strongly concerned in the field of drug research and development.This review briefly highlights advances of single crystal X-ray diffraction and powder X-ray diffraction in drug polymorphism research.