Absorption and Drug Development Solubility, Permeability, and Charge State

Profiling compounds for drug–like properties

Of the hundreds of thousands of compounds synthesized each year, most have almost no chance of becoming drugs. This problem exists because most molecules lack eht drug–like poperties necessary to enable them to be effective in vivo. To address this issue, Alex Avdeef s Absorption and Drug Development shows the reader how to examine a compound s pharmaceutical properties, emphasizing oral absorption. This book explains the different physiochemical methods currently used to analyze drug candidates and how to interpret these methods. Topics discussed include:

• The physicochemical needs of pharmaceutical research and development
• The flux model in terms of solubility, permeability, and charge state (pH)
• Ionization constants
• Experimental methods of measuring partition coefficients, log P and log D
• Partition coefficients where the lipid phase is made of liposomes formed from vesicles of bilayers of phospholipids
• PAMPA (parallel artificial membrane permeability assays)

Also included are physicochemical data for over 200 commercial drugs. With over 600 references and 100 drawings, this book is suitable for the practical pharmaceutical chemist and those seeking a better understanding of physiochemical measurements.