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High throughput solubility measurement in drug discovery and development
1Preclinical Research, Pharma Division, F. Hoffmann-La Roche Ltd., CH-4002 Basle, Switzerland. Jochem.Alsenz@roche.com
Accurate drug solubility measurement is vital for drug discovery and development. This review covers experimental methods, focusing on high-throughput assays for kinetic and thermodynamic solubility, and discusses future trends.
Area of Science:
- Pharmacology
- Analytical Chemistry
- Drug Development
Background:
- Drug solubility is a critical parameter in pharmaceutical research and development.
- Accurate solubility determination influences compound selection and formulation strategies.
Purpose of the Study:
- To review current experimental approaches for measuring drug solubility.
- To highlight recent advances in high-throughput solubility assays.
- To compare solubility studies in discovery versus development settings.
Main Methods:
- Discussion of traditional and high-throughput experimental methods for solubility determination.
- Analysis of assay focus, setup, advantages, disadvantages, and limitations.
- Comparison of kinetic and thermodynamic (equilibrium) solubility measurements.
Main Results:
- Comprehensive overview of various drug solubility assays.
- Identification of trade-offs between measurement speed, quality, and quantity.
- Highlighting differences in solubility testing requirements for drug discovery and development.
Conclusions:
- Experimental drug solubility assessment is essential throughout the drug lifecycle.
- Advances in high-throughput methods improve efficiency in solubility determination.
- Future trends aim to enhance assay capabilities, addressing current bottlenecks.
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