摘要
药物的肠道渗透性是口服药物发挥药效的决定性因素之一,如何准确高效地评估化合物的渗透性已成为新药研发时的一大挑战。本文简介了几种常用的肠道渗透性预测模型的原理、优缺点和最新进展,重点介绍准确度和效率较高的尤斯灌流和平行人工膜渗透模型,并对未来渗透性模型的发展趋势进行展望,以期为先导化合物的渗透性评价提供借鉴。
Intestinal permeability is one of key factors determing absorption of oral drug products. It is a big challenge to assess permeability of compounds with high accuracy and high efficacy during research and development process. In this review, the principles, strengths, weaknesses and advances of common intestinal permeability models are summarized, with focus on Ussing chamber and parallel artificial membrane permeability assay. In addition, future trends of permeability models are briefly discussed. This review may provide a reference to accessing permeability of lead compounds.
作者
沈青青
江振洲
张陆勇
黄鑫
SHEN Qing-qing;JIANG Zhen-zhou;ZHANG Lu-yong;HUANG Xin(Institute of Pharmaceutical Sciences;Jiangsu Key Laboratory of Drug Screening;Key Laboratory of Drug Quality Control and Pharmacovigilance, Ministry of Education, China Pharmaceutical University, Nanjing 210009, China;Center for Drug Screening and Pharmacodynamics Evaluation, School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China)
出处
《药学学报》
CAS
CSCD
北大核心
2018年第5期727-734,共8页
Acta Pharmaceutica Sinica
基金
国家自然科学基金面上项目(81673684)
国家自然科学基金青年项目(81303301)
国家自然科学基金重大国际(地区)合作研究项目(81320108029)
江苏省研究生培养创新工程(KYCX17-0718)
关键词
肠道渗透性
在体单向肠灌流
外翻肠囊
尤斯灌流
CACO-2
平行人工渗透膜
intestinal permeability
single-pass intestinal perfusion in vivo
everted intestinal sac
Ussing chamber
Caco-2
parallel artificial membrane permeability assay
