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

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

Editor(s): Han van de Waterbeemd, Hans Lennernäs, Per Artursson

Published Online: 23 FEB 2004

Print ISBN: 9783527304387

Online ISBN: 9783527601479

DOI: 10.1002/3527601473

Series Editor(s): Raimund Mannhold, Hugo Kubinyi, Gerd Folkers

About this Book

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

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  1. Part I: Studies of Membrane Permeability and Oral Absorption

  2. Part II: Drug Dissolution and Solubility

    1. Chapter 8

      Gastrointestinal Dissolution and Absorption of Drugs (pages 189–214)

      Dr. Gladys E. Granero, Dr. Chandrasekharan Ramachandran and Prof. Dr. Gordon L. Amidon

  3. Part III: Role of Transporters and Metabolism in Oral Absorption

    1. Chapter 11

      Transporters in the GI Tract (pages 243–287)

      Dr. Ho-Chul Shin, Dr. Christopher P. Landowski, Dr. Duxin Sun and Prof. Dr. Gordon L. Amidon

    2. Chapter 12

      Hepatic Transport (pages 288–310)

      Prof. Dr. Hiroshi Suzuki and Prof. Dr. Yuichi Sugiyama

  4. Part IV: Computational Approaches to Drug Absorption and Bioavailability

    1. Chapter 17

      VOLSURF: A Tool for Drug ADME-Properties Prediction (pages 406–419)

      Prof. Dr. Gabriele Cruciani, Dr. Mirco Meniconi, Dr. Emanuele Carosati, Dr. Ismael Zamora and Prof. Dr. Raimund Mannhold

    2. Chapter 18

      Simulation of Absorption, Metabolism, and Bioavailability (pages 420–443)

      Prof. Dr. Michael B. Bolger, Dr. Balaji Agoram, Dr. Robert Fraczkiewicz and Dr. Boyd Steere

    3. Chapter 20

      Towards P-Glycoprotein Structure–Activity Relationships (pages 461–492)

      PD Anna Seelig, Dr. Ewa Landwojtowicz, Dr. Holger Fischer and Dr. Xiaochun Li Blatter

  5. Part V: Drug Development Issues

    1. Chapter 22

      Prodrugs (pages 532–546)

      Prof. Dr. Bente Steffansen, Dr. Anne Engelbrecht Thomsen and Prof. Dr. Sven Frokjaer

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