Advanced screening assays to rapidly identify solubility-enhancing formulations: High-throughput, miniaturization and automation

被引:50
作者
Dai, Wei-Guo [1 ]
Pollock-Dove, Crystal [1 ]
Dong, Liang C. [1 ]
Li, Shu [1 ]
机构
[1] ALZA Corp, Mountain View, CA 94039 USA
关键词
screening assay; formulation; high-throughput; miniaturization; automation; solubility;
D O I
10.1016/j.addr.2007.10.017
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Development of solubility-enhancing formulations for poorly water-soluble compounds always poses a challenge. Conventional formulation screening assays are potentially time-consuming and labor-intensive and, moreover, require a large amount of a compound; they are not ideal when compound availability and testing time are limited. In recent years, in-vitro screening assays that are rapid, inexpensive, minimally labor-intensive, and require only small quantities of a compound have become available. These advanced assays allow high-throughput automation, miniaturization, and parallel processing, thereby enabling scientists to rapidly identify solubility-enhancing formulations with milligram or sub-milligram quantities of an active pharmaceutical ingredient (API). This article reviews these assays for rapidly screening the aqueous solubility of lead Compounds and the solubility-enhancing formulations with limited quantities of API. (C) 2008 Published by Elsevier B.V.
引用
收藏
页码:657 / 672
页数:16
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