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一种使用酶标仪中的激光散射比浊法测定药物水溶解度的高通量筛选方法。

A high-throughput screening method for the determination of aqueous drug solubility using laser nephelometry in microtiter plates.

作者信息

Bevan C D, Lloyd R S

机构信息

Physical Sciences, GlaxoWellcome Research and Development, Stevenage, Hertfordshire, UK.

出版信息

Anal Chem. 2000 Apr 15;72(8):1781-7. doi: 10.1021/ac9912247.

Abstract

The determination of aqueous solubility in a high-throughput screening environment is invaluable in the selection of the most promising potential drug candidates. We describe a fast method based on laser nephelometry that can determine the solubility of potential drug candidates (usually from combinatorial chemistry) supplied as dimethyl sulfoxide (DMSO) solutions in 96-well plates. In the sample, the percent DMSO is kept constant allowing direct comparison of results. The nephelometric method has been shown to produce results equivalent to those produced by an HPLC method and to be largely unaffected by colored solutions.

摘要

在高通量筛选环境中测定水溶性对于选择最有前景的潜在药物候选物非常重要。我们描述了一种基于激光散射比浊法的快速方法,该方法可以测定以二甲基亚砜(DMSO)溶液形式提供在96孔板中的潜在药物候选物(通常来自组合化学)的溶解度。在样品中,DMSO的百分比保持恒定,从而可以直接比较结果。已证明散射比浊法产生的结果与HPLC方法产生的结果相当,并且在很大程度上不受有色溶液的影响。

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