Poorly soluble marketed drugs display solvation limited solubility
Poorly soluble marketed drugs display solvation limited solubility
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DOI：
10.1021/jm0706416
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发表时间：
2007-11-15
影响因子：
7.3
通讯作者：
Hubatsch, Ina
中科院分区：
文献类型：
--
作者：
Bergstroem, Christel A. S.;Wassvik, Carola M.;Hubatsch, Ina
我们测定了15种溶解度范围为2.9 nM至1.1 μ M的难溶性药物的固有水溶性。然后，我们从物理化学的角度分析了数据，使用实验确定的固态特性和易于解释的二维分子描述符，以更好地了解溶解度差的因素。分析表明，已上市的难溶性药物的溶解度受溶剂化作用的限制，而不是受其固体状态的限制。
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.