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Title

Analytical tools for the physicochemical profiling of drug candidates to predict absorption/distribution

Authors
Bard, Bruno
Published in Analytical and Bioanalytical Chemistry. 2009, vol. 394, no. 3, p. 707-729
Abstract The measurement of physicochemical properties at an early phase of drug discovery and development is crucial to reduce attrition rates due to poor biopharmaceutical properties. Among these properties, ionization, lipophilicity, solubility and permeability are mandatory to predict the pharmacokinetic behavior of NCEs (new chemical entities). Due to the high number of NCEs, the analytical tools used to measure these properties are automated and progressively adapted to high-throughput technologies. The present review is dedicated to experimental methods applied in the early drug discovery process for the determination of solubility, ionization constants, lipophilicity and permeability of small molecules. The principles and experimental conditions of the different methods are described, and important enhancements in terms of throughput are highlighted.
Keywords Physicochemical profilingSolubilityIonization constantLipophilicityPermeabilityExperimental models
Stable URL http://archive-ouverte.unige.ch/unige:1631
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PMID: 19184676
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Deposited on : 2009-05-15

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