Oral Bioavailability Assessment Basics and Strategies for Drug Discovery and Development

AYMAN F. EL-KATTAN, B. Pharm, PhD, is Associate Research Fellow in Pfizer's Pharmacokinetics, Dynamics, and Metabolism Department, Cambridge Laboratories and an Adjunct Professor at College of Pharmacy-University of Rhode Island in Rhode Island, US. Dr. El-Kattan is a reviewer for several journals and is an active member of the American Association of Pharmaceutical Scientists (AAPS). He serves on the executive committee of the Drug Transporter focus group. He has been invited speaker 50 times at national/international conferences and has published over 100 papers in peer-reviewed Journals, book chapters, and proceedings.

1 Drug Pharmacokinetics and Toxicokinetics 1

2 GIT Anatomy and Physiology and Drug Oral Bioavailability: Impact of Species Differences 35

3 Drug Routes of Excretion 77

4 Physicochemical and Biopharmaceutical Properties that Affect Drug Absorption of Compounds Absorbed by Passive Diffusion 139

5 Physicochemical and Biopharmaceutical Factors Affecting Hepatic/Intestinal First-Pass Effect 173

6 Impact of Intestinal Efflux Transporters on Oral Absorption 203

7 Impact of Influx Transporters on Drug Absorption 269

8 Extended Clearance Classification System (ECCS) and its Utility in Predicting Clearance Rate-Determining Step in Drug Discovery 309

9 In Vitro and In Situ Approaches to Measure Intestinal Permeability and Efflux Transporters 331

10 In Silico Approaches to Predict Intestinal Permeability 347

11 In Vivo Preclinical Approaches to Deconvolute The Contribution of First-Pass Effect from Oral Absorption 357

12 In Vitro Approaches to Assess Hepatic Metabolism and First-Pass Effect 377

13 The Utility of ECCS as a Roadmap to Improve Oral Bioavailability of New Molecular Entities: Industrial Perspective 387

INDEX 431

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