[关键词]
[摘要]
药物共晶是指药物活性成分与共晶形成物在氢键或其他非共价键的作用下以一定化学计量比结合而成的一种新的固体形态,其不但可以改善药物的理化性质和生物利用度,且可突破专利保护,是目前药物研发的一个新的热点。药物共晶的出现也为中药难溶性有效成分的应用提供了新的契机。对黄酮类、生物碱类、萜类和多酚类难溶性有效成分的共晶及其理化性质和生物学性质进行了综述,为药物共晶在改善中药难溶性有效成分的溶解度及生物利用度方面的应用提供借鉴与参考。
[Key word]
[Abstract]
Co-crystal is a crystalline structure composed of at least two components, where the components may be active pharmaceutical ingredients (APIs) and co-formers in stoichiometric amounts. Co-crystal structure exhibits long range order and the components interact via non-covalent interaction such as hydrogen bonding, ionic interaction, vander-waals interaction, and π-π interaction. The intermolecular interaction and resulting crystal structure can generate physicochemical properties which differ from the properties of the individual components. Such properties include melting point, solubility, chemical stability, and mechanical properties. Meanwhile, co-crystal can break through patents protection of APIs. So co-crystal attracts more attention in pharmaceutical research and development field. With the development of pharmaceutical co-crystals, there may be an opportunity for improving the insoluble active ingredients of Chinese materia medica (CMM) in further development. This review has been organized around four categories: the co-crystals of flavonoids (I), alkaloids (II), terpenes (III), and polyphenols (IV) and their effects on physicochemical properties and bioavailability of those APIs, which provide a good reference for the application of pharmaceutical co-crystals in insoluble active ingredients of CMM.
[中图分类号]
[基金项目]