High throughput physicochemical profiling for drug discovery

被引：253

作者：

Kerns, EH ^{[1
]}

机构：

[1] Wyeth Ayerst Res, Princeton, NJ 08543 USA

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 2001年 / 90卷 / 11期

关键词：

discovery; physicochemical; profiling; high throughput; methods;

D O I：

10.1002/jps.1134

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The drug development bottlenecks of attrition and development time are being addressed by acquiring a profile of the candidate's physicochemical and physiological properties during early discovery phases. This information assists selection and optimization of pharmaceutical properties in parallel with activity. High throughput methods to measure the properties: solubility, permeability, lipophilicity, pKa, stability and integrity are described and compared in this article. The underlying discovery requirements, needs and application strategies are discussed. (C) 2001 Wiley-Liss, Inc. and the American Pharmaceutical Association.

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页码：1838 / 1858

页数：21

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