A high-throughput screening method for the determination of aqueous drug solubility using laser nephelometry in microtiter plates
A high-throughput screening method for the determination of aqueous drug solubility using laser nephelometry in microtiter plates
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DOI：
10.1021/ac9912247
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发表时间：
2000-04-15
影响因子：
7.4
通讯作者：
Lloyd, RS
中科院分区：
文献类型：
--
作者：
Bevan, CD;Lloyd, RS
在高通量筛选环境中测定水溶性对于选择最有前途的潜在候选药物是非常宝贵的。我们描述了一种基于激光散射比浊法的快速方法，该方法可以确定在96孔板中作为二甲基亚砜（DMSO）溶液供应的潜在候选药物（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，以便直接比较结果。已证明比浊法产生的结果与HPLC法产生的结果相当，并且基本上不受有色溶液的影响。
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.