Poorly Soluble Marketed Drugs Display Solvation Limited Solubility

We determined the intrinsic aqueous solubility of 15 poorly soluble drugs with solubilities ranging from 2.9 nM to 1.1 μM. We then analyzed the data from a physicochemical perspective, using experimentally determined solid-state properties and easily interpretable two-dimensional molecular descripto...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2007-11, Vol.50 (23), p.5858-5862
Main Authors: Bergström, Christel A. S, Wassvik, Carola M, Johansson, Kajsa, Hubatsch, Ina
Format: Article
Language:English
Subjects:
Biological and medical sciences
Calorimetry, Differential Scanning
Chemical Phenomena
Chemistry, Physical
Chromatography, High Pressure Liquid
FARMACI
General pharmacology
Medical sciences
Molecular Structure
Multivariate Analysis
Pharmaceutical Preparations - chemistry
Pharmacology. Drug treatments
PHARMACY
Physicochemical properties. Structure-activity relationships
Principal Component Analysis
Solubility
Tandem Mass Spectrometry
Thermodynamics
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Summary:We determined the intrinsic aqueous solubility of 15 poorly soluble drugs with solubilities ranging from 2.9 nM to 1.1 μM. 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.
ISSN:0022-2623
1520-4804
1520-4804
DOI:10.1021/jm0706416