生物碱类化合物共晶的研究进展

Research Progress in Cocrystal of Alkaloids

共晶技术的出现为解决难溶性天然药物临床应用的局限性带来了希望。药物共结晶的优势是在不改变药物活性成分的基础上,使药物的溶解度和溶出速率得到改善,从而提高药物的生物利用度,增强疗效。药物共晶是指药物中的活性成分与共晶配体之间通过氢键或者其他非共价键连接形成的一种具有不同理化性质的晶体物质。生物碱类药物是难溶性天然药物,本文主要对生物碱类天然药物共晶的制备、理化性质的表征和临床应用进行综述,旨在为生物碱类化合物共晶在药物中的应用提供依据。

The emergence of cocrystal technology has brought hope to solve the limitations of clinical applications of many insoluble pharmaceutical ingredients. The advantage of cocrystal is the improvement of drug’s solubility in body without changing the active ingredient of drug,thereby improving the bioavailability and the therapeutic effect. Pharmaceutical cocrystals refer to a crystalline substance with different physicochemical properties formed by hydrogen bonding or other non-covalent interaction between active pharmaceutical ingredients(APIs) and cocrystal formers(CCFs). Alkaloids are one of poorly soluble drugs. This review focused on the preparation,characterization and research progress in alkaloid pharmaceutical co-crystals to provide reference for the clinical application of alkaloid co-crystals in pharmaceutical preparations.