Drug Bioavailability : Estimation of Solubility, Permeability, Absorption and Bioavailability

by Editor: Han van de Waterbeemd (Hoffmann-La Roche, Basel, CH); Editor: Hans Lennernäs (Dept. of Pharmacy, Uppsala University, Sweden); Editor: Per Artursson (Dept. of Pharmacy, Uppsala University, Sweden); Series Editor: Raimund Mannhold (Univ. of

• ISBN13: 9783527304387
• ISBN10: 352730438X
• Format: Hardcover
• Copyright: 2003-08-01
• Publisher: Wiley-VCH
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Summary

The peroral application (swallowing) of a medicine means that the body must first resorb the active substance before it can begin to take effect. The efficacy of drug uptake depends on the one hand on the chemical characteristics of the active substance, above all on its solubility and membrane permeability. On the other hand, it is determined by the organism's ability to absorb pharmaceuticals by way of specific transport proteins or to excrete them. Since many pharmacologically active substances are poorly suited for oral intake, a decisive criterion for the efficacy of a medicine is its so-called bioavailability. Written by an international team from academia and the pharmaceutical industry, this book covers all aspects of the oral bioavailability of medicines. The focus is placed on methods for determining the parameters relevant to bioavailability. These range from modern physicochemical techniques via biological studies in vitro and in vivo right up to computer-aided predictions. The authors specifically address possibilities for optimizing bioavailability during the early screening stage for the active substance. Its clear structure and comprehensive coverage make this book equally suitable for researchers and lecturers in industry and teaching.

Table of Contents

Preface.

Foreword.

List of Authors.

I. STUDIES OF MEMBRANE PERMEABILITY AND ORAL ABSORPTION.

1. Physico-chemical Approaches to Drug Absorption (H. van de Waterbeemd).

2. High-throughput Measurement of log D and pKa   (J. Comer).

3. High-th