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平行人工膜渗透测定法(PAMPA)是一种用于发现的有用工具吗?

Is PAMPA a useful tool for discovery?

作者信息

Galinis-Luciani D, Nguyen L, Yazdanian M

机构信息

Worldwide Drug Development, Cephalon, Inc., 145 Brandywine Parkway, West Chester, Pennsylvania 19380, USA.

出版信息

J Pharm Sci. 2007 Nov;96(11):2886-92. doi: 10.1002/jps.21071.

Abstract

Experimental PAMPA data generated for 40 low molecular weight commercial drugs is reviewed in the context of its utility in the drug discovery process. Several experimental variables that have been introduced in the literature as additions or improvements to the PAMPA were also evaluated. The relationship between PAMPA data and both calculated and measured octanol/water distribution coefficients was examined. From this assessment, it was concluded that the PAMPA yields information about the lipophilicity as measured by the octanol/water partitioning of a compound, but that this same information could be derived in a simpler manner from calculated log D values.

摘要

对40种低分子量商业药物生成的实验性平行人工膜渗透实验(PAMPA)数据在药物发现过程中的效用背景下进行了综述。还评估了文献中作为对PAMPA的补充或改进而引入的几个实验变量。研究了PAMPA数据与计算和测量的正辛醇/水分配系数之间的关系。通过该评估得出结论,PAMPA可得出有关化合物正辛醇/水分配所测量的亲脂性信息,但相同信息可以从计算的log D值以更简单的方式得出。

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