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

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. Content: Chapter 1 Physico?Chemical Approaches to Drug Absorption (pages 1–20): Prof. Dr. Han van de WaterbeemdChapter 2 High?Throughput Measurement of log D and pKa (pages 21–45): Dr. John E. A. ComerChapter 3 High?throughput Measurement of Permeability Profiles (pages 46–71): Dr. Alex AvdeefChapter 4 Caco?2 and Emerging Alternatives for Prediction of Intestinal Drug Transport: A General Overview (pages 72–89): Prof. Dr. Per Artursson and Dr. Staffan TavelinChapter 5 Cell Cultures in Drug Discovery: An Industrial Perspective (pages 90–131): Dr. Anna?Lena Ungell and Dr. Johan KarlssonChapter 6 Use of Animals for the Determination of Absorption and Bioavailability (pages 132–154): Dr. Chris LoganChapter 7 In Vivo Permeability Studies in the Gastrointestinal Tract of Humans (pages 155–188): Dr. Niclas Petri and Prof. Dr. Hans LennernasChapter 8 Gastrointestinal Dissolution and Absorption of Drugs (pages 189–214): Dr. Gladys E. Granero, Dr. Chandrasekharan Ramachandran and Prof. Dr. Gordon L. AmidonChapter 9 Aqueous Solubility in Discovery, Chemistry, and Assay Changes (pages 215–231): Dr. Chris LipinskiChapter 10 Factors Influencing the Water Solubilities of Crystalline Drugs (pages 232–242): Dr. James W. McFarland, Dr. Chau M. Du and Dr. Alex AvdeefChapter 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. AmidonChapter 12 Hepatic Transport (pages 288–310): Prof. Dr. Hiroshi Suzuki and Prof. Dr. Yuichi SugiyamaChapter 13 The Importance of Gut Wall Metabolism in Determining Drug Bioavailability (pages 311–328): Kevin BeaumontChapter 14 Modified Cell Lines (pages 329–338): Dr. Charles L. CrespiChapter 15 Intestinal Absorption: The Role of Polar Surface Area (pages 339–357): Prof. Dr. Per Artursson and Dr. Christel A. S. BergstromChapter 16 Calculated Molecular Properties and Multivariate Statistical Analysis in Absorption Prediction (pages 358–405): Dr. Ulf Norinder and Dr. Markus HaeberleinChapter 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 MannholdChapter 18 Simulation of Absorption, Metabolism, and Bioavailability (pages 420–443): Prof. Dr. Michael B. Bolger, Dr. Balaji Agoram, Dr. Robert Fraczkiewicz and Dr. Boyd SteereChapter 19 Prediction of Bioavailability (pages 444–460): Dr. Arun K. Mandagere and Dr. Barry JonesChapter 20 Towards P?Glycoprotein Structure–Activity Relationships (pages 461–492): PD Anna Seelig, Dr. Ewa Landwojtowicz, Dr. Holger Fischer and Dr. Xiaochun Li BlatterChapter 21 Application of the Biopharmaceutic Classification System Now and in the Future (pages 493–531): Dr. Bertil Abrahamsson and Prof. Dr. Hans LennernasChapter 22 Prodrugs (pages 532–546): Prof. Dr. Bente Steffansen, Dr. Anne Engelbrecht Thomsen and Prof. Dr. Sven FrokjaerChapter 23 Modern Delivery Strategies: Physiological Considerations for Orally Administered Medications (pages 547–568): Prof. Dr. Clive G. Wilson