Drug Bioavailability: Estimation of Solubility, Permeability, Absorption and Bioavailability, Volume 40, Second Edition By Raimund Mannhold, Hugo Kubinyi, Gerd Folkers(eds.)
2008 | 632 Pages | ISBN: 3527320512 | PDF | 16 MB
The gold standard for industrial research now completely revised in line with current trends in the field, with all contributions extensively updated or rewritten. In 21 chapters readers can benefit from the key working knowledge of today's leading pharmaceutical companies, including Pfizer, AstraZeneca, and Roche. Drug developers from industry and academia present all the factors governing drug bioavailability, complete with practical examples and real-life data. Part I focuses on in vitro and in vivo measurements of physicochemical properties, such as membrane permeability and ionization. Part II discusses solubility and gastrointestinal absorption, while the third part is devoted to metabolism and excretory mechanisms. The much revised and expanded part IV surveys current in silico approaches to predict drug properties needed to estimate the bioavailability of any new drug candidate. The final part shows how poor bioavailability may be improved by various approaches during the development process. No other publication offers the same level of treatment on this crucial topic in modern drug development.Content: Chapter 1 Introduction: The Why and How of Drug Bioavailability Research (pages 1-6): Dr. Han van de Waterbeemd and Prof. Dr. Bernard TestaChapter 2 Aqueous Solubility in Drug Discovery Chemistry, DMPK, and Biological Assays (pages 7-31): Nicola Colclough, Linette Ruston and Kin TamChapter 3 Gastrointestinal Dissolution and Absorption of Class II Drugs (pages 33-51): Arik S. Dahan and Gordon L. AmidonChapter 4 In Silico Prediction of Solubility (pages 53-68): Andrew M. Davis and Pierre BruneauChapter 5 Physicochemical Approaches to Drug Absorption (pages 69-99): Dr. Han van de WaterbeemdChapter 6 High?Throughput Measurement of Physicochemical Properties (pages 101-132): Barbara P. MasonChapter 7 An Overview of Caco?2 and Alternatives for Prediction of Intestinal Drug Transport and Absorption (pages 133-159): Anna?Lena Ungell and Per ArturssonChapter 8 Use of Animals for the Determination of Absorption and Bioavailability (pages 161-184): Chris LoganChapter 9 In Vivo Permeability Studies in the Gastrointestinal Tract of Humans (pages 185-219): Niclas Petri and Hans LennernasChapter 10 Transporters in the Gastrointestinal Tract (pages 221-276): Pascale Anderle and Carsten U. NielsenChapter 11 Hepatic Transport (pages 277-332): Kazuya Maeda, Hiroshi Suzuki and Yuichi SugiyamaChapter 12 The Importance of Gut Wall Metabolism in Determining Drug Bioavailability (pages 333-357): Christopher KohlChapter 13 Modified Cell Lines (pages 359-372): Guangqing Xiao and Charles L. CrespiChapter 14 Calculated Molecular Properties and Multivariate Statistical Analysis (pages 373-408): Ulf NorinderChapter 15 Computational Absorption Prediction (pages 409-432): Christel A. S. Bergstrom, Markus Haeberlein and Ulf NorinderChapter 16 In Silico Prediction of Human Bioavailability (pages 433-451): David J. Livingstone and Dr. Han van de WaterbeemdChapter 17 Simulations of Absorption, Metabolism, and Bioavailability (pages 453-495): Michael B. Bolger, Robert Fraczkiewicz and Viera LukacovaChapter 18 Toward Understanding P?Glycoprotein Structure-Activity Relationships (pages 497-519): Anna SeeligChapter 19 Application of the Biopharmaceutics Classification System Now and in the Future (pages 521-558): Bertil Abrahamsson and Hans LennernasChapter 20 Prodrugs (pages 559-570): Prof. Dr. Bernard TestaChapter 21 Modern Delivery Strategies: Physiological Considerations for Orally Administered Medications (pages 571-595): Clive G. Wilson and Werner WeitschiesChapter 22 Nanotechnology for Improved Drug Bioavailability (pages 597-611): Marjo Yliperttula and Arto Urtti