Drug Bioavailability (eBook)

I. STUDIES OF MEMBRANE PERMEABILITY AND ORAL ABSORPTION
Physicochemical Approaches to Drug Absorption
High Throughput Measurement of Membrane Permeability
Biosensors to Study Intestinal Drug Absorption
Cell Cultures in Drug Discovery: An Industrial Perspective
In Vivo Permeability Studies in the GI Tract
II. DRUG DISSOLUTION AND SOLUBILITY
Gastrointestinal Dissolution and Absorption of Drugs
Solubility Screening in Drug Discovery
Impact of Salt/Crystal Forms on Solubility and Permeability
Prediction of Solubility
III. ROLE OF TRANSPORTERS AND METABOLISM IN ORAL ABSORPTION
Transporters in the GI Tract
Role of Transporters in Liver Extraction of Drugs
Gut Wall Metabolism
IV. COMPUTATIONAL APPROACHES TO DRUG ABSORPTION AND BIOAVAILABILITY
2D and 3D Molecular Descriptors in ADME prediction
Simulation of the Absorption Process
Prediction of Bioavailability
V. DRUG DEVELOPMENT ISSUES
Biopharmaceutical Classification System
Prodrugs
(partial contents) I. STUDIES OF MEMBRANE PERMEABILITY AND ORAL ABSORPTION
Physicochemical Approaches to Drug Absorption
High Throughput Measurement of log D and pKa
High Throughput Measurement of Membrane Permeability
Biosensors to Study Intestinal Drug Absorption
Cell Cultures of Caco-2, MDCK and Other Cell Lines: General Overview
Cell Cultures in Drug Discovery: An Industrial Perspective
Role of Animals in Absorption and Bioavailability Estimation
In Vivo Permeability Studies in the GI Tract
II. DRUG DISSOLUTION AND SOLUBILITY
Gastrointestinal Dissolution and Absorption of Drugs
Solubility Screening in Drug Discovery
Impact of Salt/Crystal Forms on Solubility and Permeability in Drug Development
Prediction of Solubility
III. ROLE OF TRANSPORTERS AND METABOLISM IN ORAL ABSORPTION
Transporters in the GI Tract
Role of Transporters in Liver Extraction of Drugs
Gut Wall Metabolism
Modified Cell Lines
IV. COMPUTATIONAL APPROACHES TO DRUG ABSORPTION AND BIOAVAILABILITY
Intestinal Absorption: The Role of Polar Surface Area
Calculated Molecular Properties and Multivariate Statistical Analysis in Absorption Prediction
2D and 3D Molecular Descriptors in ADME prediction
Simulation of the Absorption Process
Prediction of Bioavailability
Towards P-gp Structure-Activity Relationships
V. DRUG DEVELOPMENT ISSUES
Biopharmaceutical Classification System: How Important Are Solubility and Permeability?
Prodrugs

"This is an excellent book, which is very well suited for both teachers and newcomers to the field, who can use it as a starting point for further in-depth studies of the relevant literature. Experienced researchers from different disciplines will get the rapid introduction they desire and learn about the various aspects connected to drug bioavailability."

Sven Grüneberg, Stefan Güssregen, Chemistry, Computational Chemistry, Aventis Pharma Deutschland GmbH, Frankfurt a.M.
Angewandte Chemie + Angewandte Chemie International Edition 2/04

"This monograph is without a doubt the most comprehensive and up to date publication on drug bioavailability available today...very highly recommended..."

Journal of Medicinal Chemistry, Vol. 47, No. 7

"...liegt hier ein ausgezeichnetes Buch vor, das sowohl für Lehrende als auch für Neulinge auf dem Gebiet, die es als Ausgangspunkt für tiefer gehende Studien in der entsprechenden Spezialliteratur nutzen können, geeignet ist. Erfahrene Forscher erhalten eine schnelle, prägnante Einführung und eine umfassenden Überblick über die zahlreichen Bereiche der Forschung zur Bioverfügbarkeit von Arzneistoffen."

Sven Grüneberg, Stefan Güssregen, Chemistry, Computational Chemistry, Aventis Pharma Deutschland GmbH, Frankfurt a.M.
Angewandte Chemie + Angewandte Chemie International Edition 2/04