Poorly soluble marketed drugs display solvation limited solubility

被引:132
作者
Bergstroem, Christel A. S. [1 ]
Wassvik, Carola M. [1 ]
Johansson, Kajsa [1 ]
Hubatsch, Ina [1 ]
机构
[1] Uppsala Univ, Uppsala Biomed Ctr, Dept Pharm, SE-75123 Uppsala, Sweden
关键词
D O I
10.1021/jm0706416
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We determined the intrinsic aqueous solubility of 15 poorly soluble drugs with solubilities ranging from 2.9 nM to 1.1 mu M. We then analyzed the data from a physicochemical perspective, using experimentally determined solid-state properties and easily interpretable two-dimensional molecular descriptors, to better understand the factors underlying poor solubility. The analysis shows that poorly soluble drugs that have reached the market are solubility limited by solvation rather than by their solid state.
引用
收藏
页码:5858 / 5862
页数:5
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