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Oral Bioavailability: Basic Principles, Advanced Concepts, and Applications



Oral Bioavailability: Basic Principles, Advanced Concepts, and Applications

Ming Hu (Editor), Xiaoling Li

ISBN: 978-1-118-06758-1 August 2011 560 Pages


Understand and assess the design, delivery, and efficacy of orally administered drugs

A practical guide to understanding oral bioavailability, one of the major hurdles in drug development and delivery, Oral Bioavailability: Basic Principles, Advanced Concepts, and Applications is designed to help chemists, biologists, life science researchers, pharmaceutical scientists, pharmacologists, clinicians, and graduate and students become familiar with the fundamentals and practices of the science of oral bioavailability.

The difference in rate and extent between a drug taken orally and the actual amount of a drug reaching the circulatory system, oral bioavailability is an essential parameter for determining the efficacy and adverse effects of new and developing medications, as well as finding an optimal dosing regimen.

This book provides a much-needed one-stop resource to help readers better understand and appreciate the many facets and complex problems of oral bioavailability, including the basic barriers to oral bioavailability, the methods used to determine relevant parameters, and the challenges of drug delivery.

In addition, this comprehensive book discusses biological and physicochemical methods for improving bioavailability, integrates physicochemistry with physiology and molecular biology, and includes several state-of-the-art technologies and approaches—Caco-2 cell culture model, MDCK, and other related cell culture models—which are used to study the science of oral bioavailability.




Chapter 1. Barriers to Oral Bioavailability-An Overview (Ming Hu and Xiaoling Li).

Chapter 2. Physicochemical Characterization of Pharmaceutical Solids (Smita Debnath).

Chapter 3. Solubility of Pharmaceutical Solids (Lauren Wiser, Xiaoling Gao, Bhaskara Jasti, and Xiaoling Li).

Chapter 4. In Vitro Dissolution of Pharmaceutical Solids (Josephine L. P. Soh and Paul W. S. Heng).

Chapter 5. Biological and Physiological Features of the Gastrointestinal Tract Relevant to Oral Drug Absorption (Paul C. Ho).

Chapter 6. Absorption of Drugs via Passive Diffusion and Carrier-Mediated Pathways (Miki Susanto Park and Jae H. Chang).

Chapter 7. In vitro-In vivo Correlation of Pharmaceutical Dosage Forms (Deliang Zhou and Yihong Qiu).

Chapter 8. Drug Metabolism in Gastroinestinal Tract (Rashim Singh and Ming Hu).

Chapter 9. Efflux of Drugs via Transporters: The “Anti-absorption” Pathways (Jae H. Chang, James A. Uchizono and Miki Susanto Park).

Chapter 10. Liver Drug Metabolism (Leslie M. Tompkins, and Hongbing Wang).

Chapter 11. Protein Binding of Drugs (Antonia Kotsiou and Christine Tesseromatis).

Chapter 12. Urinary Excretion of Drugs and Drug Reabsorption (Pankaj Gupta, Bo Feng and Jack Cook).

Chapter 13. Pharmacokinetic Behaviors of Orally Administered Drugs (Jaime A. Yáñez, Dion R. Brocks, M. Laird Forrest, and Neal M. Davies).

Chapter 14. Effects of Food on Drug Absorption (Venugopal P. Marasanapalle, Xiaoling Li, and Bhaskara R. Jasti).

Chapter 15. Drug-Drug Interactions and Drug-Dietary Chemical Interactions (Ge Lin, Zhong Zuo, Na Li, and Li Zhang).

Chapter 16. Anatomical and Physiological Factors Affecting Oral Drug Bioavailability in Rates, Dogs, and Humans (Ayman El-Kattan, Susan Hurst, Joanne Brodfuehrer, Cho-Ming Loi).

Chapter 17. Amino Acid Drug Transporters (Zhong Qiu Liu, and Ming Hu).

Chapter 18. Drug Transporters and Their Role in Absorption and Disposition of Peptides and Peptide Based Pharmaceuticals (David J. Lindley, Stephen M. Carl, Dea Herrera-Ruiz, Li F. Pan, Lori B. Ward, Jonathan M. E. Goole, Olafur S. Gudmundsson, and Gregory T. Knipp).

Chapter 19. Organic Anion and Cation Drug Transporters (Takashi Sekine and Hiroshi Kusuhara).

Chapter 20. Gastroretentive Drug Delivery Systems (John R. Cardinal and Avinash Nangia).

Chapter 21. Lipid Based and self-emulsifying Oral Drug Delivery Systems (Sravan Penchala, Anh-Nhan Pham, Ying Huang and Jeffrey Wang).

Chapter 22. Prodrug Strategies to Enhance Oral Drug Absorption (Sai H.S. Boddu, Deep Kwatra, and Ashim K. Mitra).

Chapter 23. Oral Delivery of Protein/Peptide Therapeutics (Puchun Liu and Steven Dinh).

Chapter 24. ABC Transporters in Intestinal and Liver Efflux (Marilyn E. Morris and Yash A. Gandhi).

Chapter 25. Interplay between Efflux Transporter and Metabolic Enzymes (Stephen Wang).

Chapter 26. Regulatory Considerations in Metabolism- and Transporter-Based Drug Interactions (Yuanchao (Derek) Zhang, Lei Zhang, John M. Strong, Shiew-Mei Huang).

Chapter 27. Caco-2 Cell Culture Model for Oral Drug Absorption (Kaustubh Kulkarni and Ming Hu).

Chapter 28. MDCK Cells and Other Cell Culture Models of Oral Drug Absorption (Deep Kwatra, Sai H. S. Boddu, Ashim K. Mitra).

Chapter 29. Intestinal Perfusion Methods for Oral Drug Absorption (Wei Zhu and Eun-Jung (Zenobia) Jeong).

Chapter 30. Liver Perfusion and Primary Hepatocytes for Studying Drug Metabolism and Metabolite Excretion (Cindy Q. Xia, Chuang Lu, and Suresh K. Balani).

Chapter 31. In vivo Methods for Oral Bioavailability Studies (Ana Ruiz-Garcia and Marival Bermejo).

Chapter 32. Determination of Regulation of Drug Metabolizing Enzymes and Transporters (Bin Zhang and Wen Xie).

Chapter 33. Computational and Pharmacoinformatic Approaches to Oral Bioavailability Prediction (Miguel Ángel Cabrera-Pérez, and Isabel González-Álvarez).


"This book comprehensively covers the topics and issues of oral bioavailability and applications in drug development. The book helps readers master the basic terminology of the field, understand the basic barriers to oral bioavailability, be acquainted with the methods used to determine relevant parameters, and comprehend the challenge associated with oral drug delivery." (Fort Mill Times, 18 October 2011)