新药研发中药物盐型的筛选策略  

Salt type selection strategy in research and development of new drugs

作　　者：秦雪[1,2] 王成港[2] 兰静[3] 任晓文[2] 

机构地区：[1]天津中医药大学,天津300193 [2]天津药物研究院释药技术与药代动力学国家重点实验室,天津300193 [3]天津市药品审评中心,天津300191

出　　处：《现代药物与临床》2012年第4期414-417,共4页Drugs & Clinic

基　　金：国家重点基础研究发展计划(973计划)课题(2012CB724000;2012CB724002);国家生物医药国际创新园(天津)创新药物孵化基地建设(2010ZX09401)

摘　　要：在新药研发早期阶段,将候选化合物成盐是一种重要手段,可改善候选化合物的理化性质,如溶解度、结晶度、吸湿性、熔点和固态稳定性等。药物盐型的筛选首先从反离子的选择开始,然后筛选结晶条件制备其相应的盐型,最后根据结晶度、熔点、吸湿性、物理化学稳定性和晶型等因素确定药物的最终盐型。药物盐型的筛选对选择具有适宜药学性质的固态剂型有重要的指导作用。During the early stage of new drug research and development, to make the candidate compounds be salt is an important method for developing new drug, which could modify the physicochemical properties, such as solubility, crystallinity, hygroscopicity, melting point, and solid state stability. Salt type screening starts with the selection of possible counter ions, followed by the screening of crystallization conditions and the preparation of different salts. The final salt is determined by the crystaUinity, melting point, hygroscopicity, physicochemical stability, crystal type, and some other factors. The salt type selection of new drugs could provide the guides for the selection of proper solid dosage forms with appropriate pharmaceutical properties.

关 键 词：新药 候选化合物 盐型 溶解度 生物利用度 晶型 

分 类 号：R97[医药卫生—药品]