Biopharmaceutics. Группа авторов

      

      Table of Contents

      1  Cover

      2  Series Page

      3  Title Page

      4  Copyright Page

      5  List of Contributors

      6  Foreword

      7  1 An Introduction to Biopharmaceutics 1.1 Introduction 1.2 History of Biopharmaceutics 1.3 Key Concepts and Definitions Used Within Biopharmaceutics 1.4 The Role of Biopharmaceutics in Drug Development 1.5 Conclusions References

      8  2 Basic Pharmacokinetics 2.1 Introduction 2.2 What is ‘Pharmacokinetics’? 2.3 Pharmacokinetic Profile 2.4 Bioavailability 2.5 Drug Distribution 2.6 Volume of Distribution 2.7 Elimination 2.8 Elimination Half‐Life (t_½) 2.9 Elimination Rate Constant 2.10 Area Under the Curve (AUC) 2.11 Bioequivalence 2.12 Steady State 2.13 Compartmental Concepts in Pharmacokinetics 2.14 Concept of Linearity in Pharmacokinetics 2.15 Conclusions Further Reading

      9  3 Introduction to Biopharmaceutics Measures 3.1 Introduction 3.2 Solubility 3.3 Dissolution 3.4 Permeability 3.5 Absorptive Flux 3.6 Lipinsky's Rule of 5 References

      10  4 Solubility 4.1 Definition of Solubility 4.2 The Importance of Solubility in Biopharmaceutics 4.3 What Level of Solubility Is Required? 4.4 Solubility‐Limited Absorption 4.5 Methods to Assess Solubility 4.6 Brief Overview of Forces Involved in Solubility 4.7 Solid‐State Properties and Solubility 4.8 pH and Drug Solubility 4.9 Solvents 4.10 Risk of Precipitation 4.11 Solubility and Link to Lipophilicity 4.12 Conclusions References

      11  5 Permeability 5.1 Introduction 5.2 Enzymes, Gut Wall Metabolism, Tissue Permeability and Transporters 5.3 Applications and Limitations of Characterisation and Predictive Tools for Permeability Assessment 5.4 In Vivo Tools 5.5 Conclusion References

      12  6 Dissolution 6.1 Introduction 6.2 Purpose of Dissolution Testing 6.3 History of Dissolution Testing 6.4 Compendial (Pharmacopeial) Dissolution Apparatus 6.5 Dissolution Media Selection 6.6 Dissolution Agitation Rates 6.7 Reporting Dissolution Data 6.8 In Vitro In Vivo Relationships and Correlations (IVIVR/IVIVC) 6.9 Evolution of Biorelevant Dissolution Testing 6.10 Conclusions References

      13