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Drug Bioavailability: Estimation of Solubility, Permeability, Absorption and Bioavailability, Volume 18

Han van de Waterbeemd (Editor), Hans Lennernas (Editor), Per Artursson (Editor), Raimund Mannhold (Series Editor), Hugo Kubinyi (Series Editor), Gerd Folkers (Series Editor)
ISBN: 978-3-527-60515-6
602 pages
March 2006
Drug Bioavailability: Estimation of Solubility, Permeability, Absorption and Bioavailability, Volume 18 (3527605150) cover image

Description

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.
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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-throughput Measurement of Permeability Profiles (A. Avdeef).

4. Caco-2 and Emerging Alternatives for Prediction of Intestinal Drug Transport: A General Overview (P. Artursson & S. Tavelin).

5. Cell Cultures in Drug Discovery: An Industrial Perspective (A. Ungell & J. Karlsson).

6. Use of Animals for the Determination of Absorption and Bioavailability (C. Logan).

7. In Vivo Permeability Studies in the Gastrointestinal Tract of Humans (N. Petri & H. Lennernäs).

II. DRUG DISSOLUTION AND SOLUBILITY.

8. Gastrointestinal Dissolution and Absorption of Drugs (G. Granero, et al.).

9. Aqueous Solubility in Discovery, Chemistry, and Assay Changes (C. Lipinski).

10. Factors Influencing the Water Solubilities of Crystalline Drugs (J. McFarland, et al.).

III. ROLE OF TRANSPORTERS AND METABOLISM IN ORAL ABSORPTION.

11. Transporters in the GI Tract (H. Shin, et al.).

12. Hepatic Transport (H. Suzuki & Y. Sugiyama).

13. The Importance of Gut Wall Metabolism in Determining Drug Bioavailability (K. Beaumont).

14. Modified Cell Lines (C. Crespi).

IV. COMPUTATIONAL APPROACHES TO DRUG ABSORPTION AND BIOAVAILABILITY.

15. Intestinal Absorption: The Role of Polar Surface Area (P. Artursson & C. Bergström).

16. Calculated Molecular Properties and Multivariate Statistical Analysis in Absorption Prediction (U. Norinder & M. Haeberlein).

17. VOLSURF: A Tool for Drug ADME-properties Prediction (G. Cruciani, et al.).

18. Simulation of Absorption, Metabolism, and Bioavailability (M. Bolger, et al.).

19. Prediction of Bioavailability (A. Mandagere & B. Jones).

20. Towards P-Glycoprotein Structure-Activity Relationships (A. Seelig, et al.).

V. DRUG DEVELOPMENT ISSUES.

21. Application of the Biopharmaceutical Classification System Now and in the Future (B. Abrahamsson & H. Lennernäs).

22. Prodrugs (B. Steffansen, et al.).

23. Modern Delivery Strategies: Physiological Considerations for Orally Administered Medications (C. Wilson).

Index.

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Reviews

"…this book would make a valuable resource for scientists working in drug discovery and early drug development…" (Pharmaceutical Research, June 2004)

"This monograph is without a doubt the most comprehensive and up to date publication on drug bioavailability available today...very highly recommended..." (Journal of Medicinal Chemistry, Vol. 47, No. 7)

"This is an excellent book, which is very well suited for both teachers and newcomers to the field, who can use it as a starting point for further in-depth studies of the relevant literature. Experienced researchers from different disciplines will get the rapid introduction they desire and learn about the various aspects connected to drug bioavailability."
—Sven Grüneberg, Stefan Güssregen, Chemistry, Computational Chemistry, Aventis Pharma Deutschland GmbH, Frankfurt a.M., (Angewandte Chemie and Angewandte Chemie International Edition, 2/04)

"This is an excellent book, which is very well suited for both teachers and newcomers to the field, who can use it as a starting point for further in-depth studies of the relevant literature. Experienced researchers from different disciplines will get the rapid introduction they desire and learn about the various aspects connected to drug bioavailability."
—Sven Grüneberg, Stefan Güssregen, Chemistry, Computational Chemistry, Aventis Pharma Deutschland GmbH, Frankfurt a.M., Angewandte Chemie and Angewandte Chemie International Edition, 2/04

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