Solubility of sparingly-soluble ionizable drugs |
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Authors: | Avdeef Alex |
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Affiliation: | pION INC, 5 Constitution Way, Woburn, MA 01801 USA. aavdeef@pion-inc.com |
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Abstract: | The experimental and computational basis of the pH-dependent measurement of solubility of sparingly-soluble ionizable drugs is reviewed. Recently described compound-sparing (but still accurate) approaches, suitable for application in preclinical development, and appropriate for the analysis of solubility of "problematic" molecules, are critically examined. A number of useful experimental methods are reviewed, including the miniaturized shake-flask microtitre plate, the micro solubility self-calibrating direct UV, potentiometric, and the micro dissolution methods. Several molecules were selected as case studies to illustrate important concepts, with re-analysis of literature data using recently established computational tools. |
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