摘要
由于高通量筛选技术在药物开发上的广泛应用,涌现了越来越多水难溶性的新化合物。注射剂在临床治疗中发挥着重要的作用,但水溶性低却成了这些化合物开发成注射剂的一个主要难题。本文综述了微乳、亚微乳、前药、环糊精包合物、纳米混悬剂和聚合物胶束系统等在难溶性药物注射给药方面的应用,以期能通过比较各给药系统的优缺点,为产品的开发提供思路。
An increasing number of slightly water-soluble new chemical compounds have been generated,with the widespread application of high-throughput screening technology in drug discovery.Injections are of great importance in clinical therapy.However,their poor solubility represents a major challenge for formulation of these compounds in parenteral drug delivery.This paper reviews the application for parenteral delivery systems of slightly water-soluble drugs,including microemulsions,submicron emulsions,prodrugs,nanosuspensions,cyclodextrin inclusion compounds and polymeric micelles.We are trying to provide some ideas for product development by comparing both advantages and disadvantages of various systems.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2010年第11期856-863,共8页
Chinese Journal of Pharmaceuticals
基金
上海市优秀学科带头人计划(08XD14225)
上海市纳米科技专项(0952nm04500)
国家“重大新药创制”科技重大专项资助(2009ZX09301-007)
关键词
微乳
亚微乳
前药
环糊精包合物
纳米混悬剂
聚合物胶束
难溶性药物
综述
microemulsion
submicron emulsion
prodrug
cyclodextrin inclusion compound
nanosuspension
polymeric micelle
slightly water-soluble drug
review