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Gastrointestinal Dissolution and Absorption of Class II Drugs 33 Arik S. Physicochemical Aspects of Drug Dissolution and Solubility 7ДЄqueous Solubility in Drug Discovery Chemistry, DMPK, and Biological Assays 9 Nicola Colclough, Linette Ruston, and Kin Tam Introduction 10 Deп¬Ѓnition of Aqueous Solubility 11 Aqueous Solubility in Different Phases of Drug Discovery 12 Aqueous Solubility in Hit Identiп¬Ѓcation 12 Aqueous Solubility from DMSO Solutions 13 Turbidimetric Methods 14 UV Absorption Methods 15 Alternative Detection Methodology 17 Application of DMSO-Based Solubility Assays 18Дў.1 2.1.1 2.1.2 2.2 2.2.1 2.2.1.1 2.2.1.2 2.2.1.3 2.2.1.4ДЈ 3.1 3.2 3.3 3.4 3.4.1 3.4.2 3.4.3 3.4.4 3.4.5 3.5 3.5.1 3.5.2 3.6 3.6.1 3.6.2 3.7ДЄqueous Solubility in Lead Identiп¬Ѓcation and Lead Optimization 18 Dried-Down Solution Methods 20 Solubility from Solid 21 Thermodynamic Solubility Assays with Solid-State Characterization 22 Solubility by Potentiometry 24 Application of Thermodynamic Solubility Data in LI and LO Conclusions 28 References 28 Introduction: The Why and How of Drug Bioavailability Research Han van de Waterbeemd and Bernard Testa Deп¬Ѓning Bioavailability 1 The Biological Context 1 A Pharmacokinetic Overview 3 Speciп¬Ѓc Issues 3 Presentation and Layout of the Book 4 References 6 Composition Thomson Digital, Noida, India Printing Strauss GmbH, MГ¶rlenbach Bookbinding Litges & Dopf GmbH, Heppenheim Cover Graп¬Ѓk-Design Schulz, FuГџgГ¶nheim Printed in the Federal Republic of Germany Printed on acid-free paper ISBN: 978-1-6Д¬ontents List of Contributors XIX Preface XXIII A Personal Foreword XXV used in this book, even when not speciп¬Ѓcally marked as such, are not to be considered unprotected by law. No part of this book may be reproduced in any form вЂ“ by photoprinting, microп¬Ѓlm, or any other means вЂ“ nor transmitted or translated into a machine language without written permission from the publishers. Hospital Centre Pharmacy Dept.-CHUV BH 04 46 Rue du Bugnon 1011 Lausanne Schweiz Cover Description Bioavailability involves the transfer of gut wall membranes in which a drug may encounter metabolising enzymes and transporters limiting or enhancing systemic drug levels.ДЄll rights reserved (including those of translation into other languages). Han van de Waterbeemd Current address Rue de la Rasclose 14 66690 Saint AndrГ© France Former address AstraZeneca LG DECS-GCS, 50S39 Mereside, Alderley Park Macclesп¬Ѓeld SK10 4TG United Kingdom Prof. Bibliographic information published by the Deutsche Nationalbibliothek Die Deutsche Nationalbibliothek lists this publication in the Deutsche Nationalbibliograп¬Ѓe detailed bibliographic data are available on the Internet at. Library of Congress Card No.: applied for British Library Cataloguing-in-Publication Data A catalogue record for this book is available from the British Library. Readers are advised to keep in mind that statements, data, illustrations, procedural details or other items may inadvertently be inaccurate.

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Nevertheless, authors, editors, and publisher do not warrant the information contained in these books, including this book, to be free of errors. Gerd Folkers Collegium Helveticum STW/ETH Zurich 8092 Zurich Switzerland ДЄll books published by Wiley-VCH are carefully produced. Hugo Kubinyi Donnersbergstrasse 9 67256 Weisenheim am Sand Germany Prof. Raimund Mannhold Molecular Drug Research Group Heinrich-Heine-UniversitГ¤t UniversitГ¤tsstrasse 1 40225 DГјsseldorf Germany Prof.

39 2008, ISBN 978-2-8Дrug Bioavailability Estimation of Solubility, Permeability, Absorption and Bioavailability 33 2006, ISBN 978-6-0ДЇragment-based Approaches in Drug Discovery

Pharmacophores and Pharmacophore SearchesД¬hirality in Drug Research Vol. High-Throughput Screening in Drug Discovery Vol.

Pharmacokinetics and Metabolism in Drug Design, 2nd Ed. Methods and Principles in Medicinal Chemistry Edited by R.

Edited by Han van de Waterbeemd and Bernard Testa