摘要
随着新药研发水平的提高,每类药物的候选化合物增多,研究工作量明显增加,对化合物进行快速筛选的方法已经成为研究的重点之一。平行人工膜渗透模型(PAMPA)作为药物筛选的有力工具,已用于药物研究中。该模型主要以人工磷脂作为生物膜来模拟药物跨膜的屏障,用于药物的膜渗透研究。本文介绍了平行人工膜渗透模型的建立、特点和研究进展,概述了利用PAMPA进行药物筛选等方面内容。通过调整人工磷脂膜的配比,PAMPA能够作为肠道、血脑屏障和皮肤吸收等体外模型。作为药物被动转运模型,PAMPA能够对药物进行高通量快速筛选,具有成本低、灵活、用药量少和重现性好等特点。
With the development of drug discovery,more and more candidate compounds need to be studied.Methods that can screen compound rapidly received significant attention.Parallel artificial membrane perme-ability assay（PAMPA） as a powerful tool has been applied to drug studies.It uses an artificial lipid membrane to mimic the barrier for drug permeability studies.This article introduces the establishment and characteristics of PAMPA,as well as its applications in screening compounds.It can be used as models（e.g.predicting the ability of compound in gastro-intestinal absorption,blood-brain barrier transportation and skin penetration） by changing the component of artificial lipid membrane.PAMPA has advantages in high throughput selection of valuable compound with low cost,versatile,low dose,and good reproducibility.
出处
《药学学报》
CAS
CSCD
北大核心
2011年第8期890-895,共6页
Acta Pharmaceutica Sinica
基金
国家自然科学基金资助项目(30940090)
甘肃省中医药重点项目(GZK-2009-1)
关键词
平行人工膜渗透模型
磷脂
被动扩散
parallel artificial membrane permeability assay
phospholipid
passive diffusion
