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首页> 外文期刊>Journal of pharmaceutical sciences. >High throughput solubility measurement with automated polarized light microscopy analysis.
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High throughput solubility measurement with automated polarized light microscopy analysis.

机译:通过自动偏振光显微镜分析进行高通量溶解度测量。

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As a high throughput solubility assay, the solution-precipitation method using a dimethylsulfoxide (DMSO) sample stock solution (DMSO-SP) has been widely used in drug discovery. However, the solid form of the precipitant has not been investigated. In this study, we investigated the experimental conditions of the DMSO-SP, focusing on the solid form of the precipitant. The final concentration of DMSO was 1% (v/v). The precipitant of more than a half of the model compounds was observed as crystalline by polarized light microscopy analysis. When the incubation time was 20 h and the precipitant was crystalline, the DMSO-SP solubility was similar to the solubility from a powder material (PWD). However, when the incubation time was 10 min and/or the precipitant was not crystalline, the DMSO-SP solubility was higher than the PWD solubility. These results suggested that the information regarding the solid form of the precipitant is important in interpreting the solubility data. In addition, we developed an automated birefringence diagnose system for drug discovery usage. Association
机译:作为高通量溶解度测定,使用二甲基亚砜(DMSO)样品原液(DMSO-SP)的溶液沉淀法已广泛用于药物开发中。但是,尚未研究固体形式的沉淀剂。在这项研究中,我们研究了DMSO-SP的实验条件,重点是沉淀剂的固体形式。 DMSO的最终浓度为1%(v / v)。通过偏振光显微镜分析观察到超过一半的模型化合物的沉淀物为结晶。当孵育时间为20小时且沉淀剂为结晶时,DMSO-SP的溶解度类似于粉末材料(PWD)的溶解度。但是,当孵育时间为10分钟和/或沉淀剂不是结晶时,DMSO-SP的溶解度高于PWD的溶解度。这些结果表明,有关沉淀剂固体形式的信息对于解释溶解度数据很重要。此外,我们开发了用于药物发现用途的自动双折射诊断系统。协会

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