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Drug Bioavailability: Estimation of Solubility, Permeability, Absorption and Bioavailability, 2nd Edition

Drug Bioavailability: Estimation of Solubility, Permeability, Absorption and Bioavailability, 2nd Edition


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.

Part I. Physicochemical Aspects of Drug Dissolution and Solubility

Aqueous Solubility in Discovery Chemistry, DMPK and Biological Assays
Gastrointestinal Dissolution and Absorption of Class II Drugs
In Silico Prediction of Aqueous Solubility

Part II. Physicochemical and Biological Studies of Membrane Permeability and Oral Absorption

Physico-chemical Approaches to Drug Absorption
High-throughput Measurement of Physicochemical Properties (pKa, solubility, log D, permeability)
Cell Cultures for Permeability Assessment in Drug Discovery
Use of Animals for the Determination of Absorption and Bioavailability
In vivo Permeability Studies in the GI Tract of Humans

Part III Role of Transporters and Metabolism in Oral Absorption

Transporters in the GI Tract
Hepatic Drug Transport
The Importance of Gut Wall Metabolism in Determining Drug Bioavailability
Modified Cell Lines to Assess Active Transport and Metabolism during Absorption

Part IV Computational Approaches to Drug Absorption and Bioavailability

Calculated Molecular Properties and Multivariate Statistical Analysis
Computational Absorption Prediction
In Silico Prediction of Bioavailability
Simulation of Absorption, Metabolism, and Bioavailability
P-Glycoprotein Structure-Activity Relationships

Part V Drug Development Issues

Application of the Biopharmaceutical Classification System Now and in the Future
Modern Delivery Strategies: Physiological Considerations for Orally Administered Medications
The Promise of Nanotechnology in Drug Delivery
"The book covers a wide range of topics and, as such, it will serve as a valuable reference for pharmaceutical scientists, toxicologists, academicians, and the graduate students." (Doody's, May 2009)