摘要
目的对近年来靶向寡肽转运体1(oligopeptide transporter 1,PepT1)的各类前药及相应特点加以介绍,进而概括总结靶向肠道PepT1前药的进展情况。方法参考近年来国内外文献28篇对靶向PepT1的各类前药进行了综述。结果寡肽转运体目前是药物转运体中研究最深入、应用最广泛的转运体。对于很多口服吸收差的药物,以肠道转运体PepT1为靶点,按照底物结构特征的要求对药物分子进行结构修饰,可大大提高药物的跨膜吸收,改善其体内药动学性质,进而提高生物利用度。结论靶向PepT1的前药策略能够有效提高难吸收性药物的生物利用度。
Objective To introduce the progress of various types of prodrugs targeting at oligopeptide transporter 1(PepT1) in recent years.Methods The progress of various types of prodrugs targeting at PepT1 was reviewed according to 28 published literatures.Results Oligopeptide transporter,which is located in the intestinal brush border membrane,provides a major pathway for protein absorption through the human intestine.The strategy of PepT1-targeted prodrug is currently widely used to facilitate the absorption of oligopeptide and a variety of poor absorption drugs from the intestinal cavity to the blood and improve their bioavailability.Conclusions This strategy has become an effective method to enhance oral bioavailability of poor absorption drug.
出处
《沈阳药科大学学报》
CSCD
北大核心
2017年第9期788-795,共8页
Journal of Shenyang Pharmaceutical University
基金
辽宁省教育厅高等学校创新团队项目(LT2014022)
关键词
寡肽转运体1
靶向前药
生物利用度
oligopeptide transporter 1
prodrug
oral bioavailability
