药物共晶多晶型的研究进展

Research advances of polymorphism in pharmaceutical cocrystals

药物多晶型现象是影响药物稳定性和疗效的重要因素。近年来,越来越多的共晶体系被发现存在多晶型现象,而且不同晶型的共晶也表现出了性能上的差异。共晶多晶型的研究也因此受到了越来越多的关注。综述了近几年有关药物共晶多晶型的报道,解释了共晶多晶型的概念,并对其进行了分类(合成子多晶型、堆积多晶型、构象多晶型以及互变异构多晶型),重点介绍了目前共晶多晶型的筛选方法。此外,强调了共晶药物由于晶型不同而引起的性能差异。

Pharmaceutical polymorphism is a critical factor that affects the stability and efficacy of the drug. In recent years, a growing number of pharmaceutical cocrystals have been found to be polymorphic and different polymorphs do show different properties. Accordingly, the research of polymorphism in cocrystals is attracting greater attention. In this contribution, the studies which focus on polymorphic cocrystals are reviewed. The concept of polymorphic cocrystals is explained and its different types are iden- tified, including synthon polymorph, packing polymorph, conformational polymorph as well as tautomeric polymorph. The screening methods of polymorphic cocrystals are introduced in detail. Furthermore, the difference in the properties of pharmaceutical cocrystals due to different crystal forms is emphasized.