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Adv Drug Deliv Rev. 2007 Jul 30;59(7):546-67. Epub 2007 May 29.

High throughput solubility measurement in drug discovery and development.

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Preclinical Research, Pharma Division, F. Hoffmann-La Roche Ltd., CH-4002 Basle, Switzerland.


Measurement of drug solubility in various solvents is one of the key elements of compound characterization during the whole discovery and development process. This review summarizes current experimental approaches and addresses recent advances in the experimental methods used to determine drug solubility in drug discovery and early development. This paper focuses on high throughput methods designed to determine kinetic and thermodynamic (equilibrium) solubility but traditional methods are also presented. The focus, positioning, experimental setup, pros and cons, and limitations of individual assays are discussed and differences in solubility studies in discovery and development environments are highlighted. Finally, future needs and trends in solubility assay development designed to overcome current bottlenecks and trade-offs between speed and quality/quantity of measurements are addressed.

[Indexed for MEDLINE]

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