Is PAMPA a useful too for discovery?

被引：27

作者：

Galinis-Luciani, D. ^{[1
]}

Nguyen, L. ^{[1
]}

Yazdanian, M. ^{[1
]}

机构：

[1] Cephalon Inc, Worldwide Drug Dev, W Chester, PA 19380 USA

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 2007年 / 96卷 / 11期

关键词：

oral absorption; permeability; passive diffusion; absorption potential; parallel artificial membrane permeability assay; PAMPA; in vitro models; log D; drug-like properties;

D O I：

10.1002/jps.21071

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2007 Wiley-Liss, Inc. and the American Pharmacists Association.

引用

页码：2886 / 2892

页数：7

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