Monday , 8 August 2022

ABSORPTION AND DRUG DEVELOPMENT (Solubility, Permeability, and Charge State)

ALEX AVDEEF
This is useful for the practicing pharmaceutical scientist involved in absorption–distribution–metabolism–excretion measurements who needs to communicate with medicinal chemists persuasively, so that newly synthesized molecules will be more ‘‘drug-like.’’ ADME is all about ‘‘a day in the life of a drug molecule’’ (absorption, distribution, metabolism, and excretion). Specifically, this book attempts to describe the state of the art in measurement of ionization constants (pKa), oil–water partition coefficients (log P/log D), solubility, and permeability (artificial phospholipid membrane barriers). Permeability is covered in considerable detail, based on a newly developed methodology known as parallel artificial membrane permeability assay (PAMPA). These physical parameters form the major components of physicochemical profiling (the ‘‘A’’ in ADME) in the pharmaceutical industry, from drug discovery through drug development. But, there are opportunities to apply the methodologies in other fields, particularly the agrochemical and environmental industries. Also, new applications to augment animal-based models in the cosmetics industry may be interesting to explore.

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