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自乳化载药系统中脂质和表面活性剂的消化对水难溶性药物在胃肠道内溶出和吸收的影响
引用本文:杨茜,张志伟,高立军,全东琴.自乳化载药系统中脂质和表面活性剂的消化对水难溶性药物在胃肠道内溶出和吸收的影响[J].国际药学研究杂志,2016(5):899-904.
作者姓名:杨茜  张志伟  高立军  全东琴
作者单位:100850 北京,军事医学科学院毒物药物研究所,抗毒药物与毒理学国家重点实验室
基金项目:国家自然科学基金资助项目(81102390)
摘    要:自乳化载药系统(SEDDS)是提高水难溶性药物(PWSD)口服生物利用度的重要方法。SEDDS改善药物吸收可能通过多种机制,而高PWSD在消化道内的溶出是其中最重要的因素。本文介绍了预测SEDDS体内溶出的体外评价方法,包括分散实验和脂解实验,并综述了体外评价结合体内生物利用度实验研究SEDDS中的脂质和表面活性剂的消化对药物在小肠内溶出和吸收的影响,期望对SEDDS的处方研究起到一定的指导作用。

关 键 词:药物吸收  脂质  表面活性剂  溶出  消化

Effect of lipid and surfactant digestion on poorly water-soluble drug solubilization and absorption in gastrointestinal tract using self-emulsifying drug delivery systems
Abstract:Self-emulsifying drug delivery systems(SEDDS)are a vital tool in solving low oral bioavailability of poorly soluble drugs(PWSD). SEDDS may improve oral absorption via several mechanisms,however,enhancement of gastrointestinal solubilization of PWSD remains the most important factor of absorption enhancement. This review introduces the methods including dispersion tests and lipolysis tests in vitro as the indicators of potential performance in vivo. The use of these methods in vitro combined with oral bio?availability study is subsequently described,with particular focus on recent data which suggest that the digestion of lipid and surfac?tants present in SEDDS formulations impact on formulation performance in vivo. This review is expected to provide some guiding princi?ples on formulation design of SEDDS.
Keywords:drug absorption  lipid  surfactant  solubilisation  digestion
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