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J Med Chem. 2007 Nov 15;50(23):5858-62. Epub 2007 Oct 11.

Poorly soluble marketed drugs display solvation limited solubility.

Author information

1
Pharmaceutical Screening and Informatics, Department of Pharmacy, Uppsala University, Uppsala Biomedical Centre, Post Office Box 580, SE-751 23 Uppsala, Sweden. christel.bergstrom@farmaci.uu.se

Erratum in

  • J Med Chem. 2011 Apr 14;54(7):2528.

Abstract

We determined the intrinsic aqueous solubility of 15 poorly soluble drugs with solubilities ranging from 2.9 nM to 1.1 microM. 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.

PMID:
17929794
DOI:
10.1021/jm0706416
[Indexed for MEDLINE]

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