| Description |
1 online resource (742 pages) |
| Contents |
ABSORPTION AND DRUG DEVELOPMENT; CONTENTS; PREFACE; PREFACE TO THE FIRST EDITION; ABBREVIATIONS; NOMENCLATURE; COMMERCIAL TRADEMARKS; INTRODUCTION; 1.1 BULLDOZER SEARCHING FOR A NEEDLE IN A HAYSTACK?; 1.2 AS THE PARADIGM TURNS; 1.3 SCREEN FOR THE TARGET OR ADME FIRST?; 1.4 ADME AND MULTIMECHANISM SCREENS; 1.5 ADME AND THE MEDICINAL CHEMIST; 1.6 THE "ABSORPTION" IN ADME; 1.7 IT IS NOT JUST A NUMBER, IT IS A MULTIMECHANISM; REFERENCES; 2: TRANSPORT MODEL; 2.1 PERMEABILITY-SOLUBILITY-CHARGE STATE AND; 2.2 PROPERTIES OF THE GASTROINTESTINAL TRACT (GIT); 2.3 PH MICROCLIMATE; 2.4 INTRACELLULAR |
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2.5 TIGHT JUNCTION COMPLEX2.6 STRUCTURE OF OCTANOL; 2.7 BIOPHARMACEUTICS CLASSIFICATION SYSTEM; REFERENCES; 3: pKa DETERMINATION; 3.1 CHARGE STATE AND THE pKa; 3.2 METHODS OF CHOICE FOR THE DETERMINATION OF THE pKa; 3.3 TITRATION WITH A GLASS-MEMBRANE; 3.4 EQUILIBRIUM EQUATIONS AND THE IONIZATION CONSTANT; 3.5 "PURE SOLVENT" ACTIVITY SCALE; 3.6 IONIC STRENGTH AND DEBYE-HÜCKEL/ DAVIES EQUATION; 3.7 "CONSTANT IONIC MEDIUM" ACTIVITY SCALE; 3.7.1 Constant Ionic Medium Activity Scale, fX?; 3.7.2 Example of the Constant Ionic Medium Activity Scale Treatment; 3.8 TEMPERATURE DEPENDENCE OF pKa VALUES |
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3.8.1 Thermodynamics of Temperature Dependence of pKa3.8.2 Predicting pKa at 37°C from Measured Values at 25°C; 3.9 ELECTRODE CALIBRATION AND STANDARDIZATION; 3.9.1 Overview: From Millivolts to pH to pcH; 3.9.2 One-Buffer Operational Calibration of Electrode and Automatic Temperature Compensation; 3.9.3 Four-Parameter Procedure for Standardizing pH Electrode:; 3.9.3.1 Blank Titration; 3.9.3.2 Buffer-Capacity Enhanced Standardization Titrations; 3.9.4 Blank Titrations Assess the State of the Measurement System; 3.9.5 Frequency of Electrode Standardizations; 3.9.6 Effects of Ionic Strength on |
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3.9.7 Effects of Temperature on3.10 BJERRUM PLOT: MOST USEFUL GRAPHICAL TOOL IN pKa ANALYSIS; 3.10.1 Derivation of the Bjerrum Function; 3.10.2 Diagnostic Uses of the Bjerrum Plots; 3.10.2.1 Confirming the Number of pKa and the Value of nH; 3.10.2.2 Correcting Residual Acidity/Basicity Error; 3.10.2.3 Correcting Sample Concentration Error; 3.10.2.4 Recognizing Electrode Calibration Errors; 3.10.2.5 Errors in Titrant Concentration; 3.10.2.6 Consequences of Errors in Ionic Strength; 3.10.2.7 Evidence of Precipitation; 3.10.2.8 pKa "Ghosts"; 3.10.2.9 Overlapping pKa Values |
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3.10.3 More Than One Substance: Subtracting Effects of Dissolved Carbon Dioxide3.10.4 Case Examples; 3.10.5 Bjerrum's Lasting Contribution; 3.11 COSOLVENT METHODS FOR pKa DETERMINATION OF PRACTICALLY INSOLUBLE SUBSTANCES; 3.11.1 Traditional Cosolvent Extrapolation Procedure: psKa versus wt% Cosolvent; 3.11.2 Yasuda-Shedlovsky Cosolvent Extrapolation Procedure:psKa + log[H2O] versus 1/e; 3.11.3 Which Method Is Better to Use: Traditional or Yasuda-Shedlovsky?; 3.11.4 Precipitation in Mixed-Solvent Titration; 3.11.5 Electrode Standardization in Mixed Solvents |
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3.11.6 Yasuda-Shedlovsky Ancillary Data |
| Summary |
This book explains how to examine a compound's pharmaceutical properties, emphasizing oral absorption, detailing different physicochemical methods and how to interpret results for analyzing drug candidates. Now in a new edition, this updated volume now includes more case examples, more entries into properties data tables, updated references, and extensive compilations of solubility, permeability, and pKas. With over 600 references and 100 drawings, this book is well-suited for the practical pharmaceutical chemist and those seeking a better understanding of physicochemical measurements |
| Bibliography |
Includes bibliographical references and index |
| Notes |
Print version record |
| Subject |
Drugs -- Design.
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Drugs -- Metabolism.
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Drug development.
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Absorption.
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Drug Design
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absorption (physicochemical processes)
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Absorption
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Drug development
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Drugs -- Design
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Drugs -- Metabolism
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| Form |
Electronic book
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| ISBN |
9781118285961 |
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1118285964 |
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