Drug Bioavailability. Estimation of Solubility, Permeability, Absorption and Bioavailability. 2nd Edition. Methods and Principles in Medicinal Chemistry

  • ID: 2183188
  • Book
  • 649 Pages
  • John Wiley and Sons Ltd
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In order to reach its intended site of action, the drug molecules in every pill that we swallow must first be absorbed, transported via the bloodstream and evade various mechanisms that eliminate drugs from the body. Those drug properties that determine, for example, its stability in the gut or its ease of uptake into the bloodstream, are therefore of central importance in drug development. In fact, many potentially useful drugs fail because of insufficient availability at the biological target site.

This second edition of the gold standard for industrial research is thoroughly revised in line with current trends in the field, with all contributions extensively updated or rewritten. No other publication offers the same level of treatment on this crucial topic.

In 22 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 solubility and gastrointestinal absorption, while the second discusses in vitro and in vivo measurements of physicochemical properties, such as membrane permeability and solubility. Part III 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 new drug development approaches as well as delivery strategies.

Indispensable for all those working in the pharmaceutical industry, pharmaceutical and medicinal chemists, and toxicologists.

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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

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Han van de Waterbeemd
Bernard Testa
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