Drug Bioavailability

Introduction

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
Prodrugs
Modern Delivery Strategies: Physiological Considerations for Orally Administered Medications
The Promise of Nanotechnology in Drug Delivery