Hu Ming., Li Xiaoling. Oral Bioavailability. Basic Principles, Advanced Concepts, and Applications

John Wiley, 2011. — 544 p.Understand and assess the design, delivery, and efficacy of orally administered drugsA 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.Barriers to Oral Bioavailability — An Overview
Physicochemical Characterization of Pharmaceutical Solids
Solubility of Pharmaceutical Solids
In Vitro Dissolution of Pharmaceutical Solids
Biological and Physiological Features of the Gastrointestinal Tract Relevant to Oral Drug Absorption
Absorption of Drugs via Passive Diffusion and Carrier-Mediated Pathways
In Vitro–In Vivo Correlations of Pharmaceutical Dosage Forms
Drug Metabolism in Gastrointestinal Tract
Efflux of Drugs via Transporters — The Antiabsorption Pathway
Liver Drug Metabolism
Protein Binding of Drugs
Urinary Excretion of Drugs and Drug Reabsorption
Pharmacokinetic Behaviors of Orally Administered Drugs
Effects of Food on Drug Absorption
Drug–Drug Interactions and Drug–Dietary Chemical Interactions
Anatomical and Physiological Factors Affecting Oral Drug Bioavailability in Rats, Dogs, and Humans
Amino Acid Drug Transporters
Drug Transporters and Their Role in Absorption and Disposition of Peptides and Peptide-Based Pharmaceuticals
Organic Anion and Cation Drug Transporters
Gastric Retentive Drug Delivery Systems
Lipid-Based and Self-Emulsifying Oral Drug Delivery Systems
Prodrug Strategies to Enhance Oral Drug Absorption
Oral Delivery of Protein/Peptide Therapeutics
ABC Transporters in Intestinal and Liver Efflux
Interplay Between Efflux Transporters and Metabolic Enzymes
Regulatory Considerations in Metabolism- and Transporter-Based Drug Interactions
Caco-2 Cell Culture Model for Oral Drug Absorption
MDCK Cells and Other Cell-Culture Models of Oral Drug Absorption
Intestinal Perfusion Methods for Oral Drug Absorptions
Liver Perfusion and Primary Hepatocytes for Studying Drug Metabolism and Metabolite Excretion
In vivo Methods for Oral Bioavailability Studies
Determination of Regulation of Drug-Metabolizing Enzymes and Transporters
Computational and Pharmacoinformatic Approaches to Oral Bioavailability Prediction