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Pharmaceutical Chemistry Reference from C.H.I.P.S.

Drug Bioavailability:
Estimation of Solubility, Permeability, Absorption
and Bioavailability
edited by
H. van de Waterbeemd

Drug Bioavailability: Estimation of Solubility, Permeability, Absorption, and Bioavailability covers all aspects of the oral bioavailability of medicines. The focus is placed on methods for determining the parameters relevant to bioavailability. These range from modern physico-chemical techniques via biological studies in vitro and in vivo right up to computer-aided predictions.

Possibilities for optimizing bioavailability during the early screening stage for the active substance is specifically addressed. Its clear structure and comprehensive coverage make this book equally suitable for researchers and lecturers in industry and teaching.

Contents

  1. Studies of Membrane Permeability and Oral Absorption
    1. Physico-chemical Approaches to Drug Absorption
    2. High-throughput Measurement of log D and pKa
    3. High-throughput Measurement of Permeability Profiles
    4. Caco-2 and Emerging Alternatives for Prediction of Intestinal Drug Transport: A General Overview
    5. Cell Cultures in Drug Discovery: An Industrial Perspective
    6. Use of Animals for the Determination of Absorption and Bioavailability
    7. In Vivo Permeability Studies in the Gastrointestinal Tract of Humans
  2. Drug Dissolution and Solubility
    1. Gastrointestinal Dissolution and Absorption of Drugs
    2. Aqueous Solubility in Discovery, Chemistry, and Assay Changes
    3. Factors Influencing the Water Solubilities of Crystalline Drugs
  3. Role of Transporters and Metabolism in Oral Absorption
    1. Transporters in the GI Tract
    2. Hepatic Transport
    3. The Importance of Gut Wall Metabolism in Determining Drug Bioavailability
    4. Modified Cell Lines
  4. Computational Approaches to Drug Absorption and Bioavailability
    1. Intestinal Absorption: The Role of Polar Surface Area
    2. Calculated Molecular Properties and Multivariate Statistical Analysis in Absorption Prediction
    3. VOLSURF: A Tool for Drug ADME-properties Prediction
    4. Simulation of Absorption, Metabolism, and Bioavailability
    5. Prediction of Bioavailability
    6. Towards P-Glycoprotein Structure-Activity Relationships
  5. Drug Development Issues
    1. Application of the Biopharmaceutical Classification System Now and in the Future
    2. Prodrugs
    3. Modern Delivery Strategies: Physiological Considerations for Orally Administered Medications

Index

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Drug Bioavailability: Estimation of Solubility, Permeability, Absorption, and Bioavailability
edited by H. van de Waterbeemd et al
579 pages $194.00 + shipping
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