Читать книгу Biopharmaceutics - Группа авторов - Страница 2
Table of Contents
Оглавление1 Cover
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 (t½) 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 7 Biopharmaceutics to Inform Candidate Drug Selection and Optimisation 7.1 Introduction 7.2 Oral Product Design Considerations During Early Development 7.3 Biopharmaceutics in Drug Discovery 7.4 Biopharmaceutics Assessment 7.5 Output of Biopharmaceutics Assessment 7.6 Influence/Optimise/Design Properties to Inform Formulation Development 7.7 Conclusion References
14 8 Biopharmaceutics Tools for Rational Formulation Design 8.1 Introduction 8.2 Formulation Development to Optimise Drug Bioavailability 8.3 Traditional Formulation Strategies 8.4 Decision Trees to Guide Formulation Development 8.5 Computational Tools to Guide Formulation Strategies 8.6 Decision‐Making for Optimising Enabling Formulations 8.7 Decision Trees for Enabled Formulations 8.8 System‐Based Formulation Strategies 8.9 Biopharmaceutics Risk Assessment Roadmap (BioRAM) 8.10 Conclusions References
15 9 Biopharmaceutic Classification System 9.1 Description and History of the BCS 9.2 BCS‐Based Criteria for Solubility, Dissolution and Permeability 9.3 BCS‐Based Biowaivers 9.4 Regulatory Development of BCS‐Based Biowaivers 9.5 International Harmonisation of BCS‐Based Biowaiver Criteria – ICH M9 9.6 BCS as a Development Tool 9.7 Beyond the BCS 9.8 Conclusions References
16 10 Regulatory Biopharmaceutics 10.1 Introduction 10.2 Clinical Bioequivalence Studies 10.3 Design of Clinical Bioequivalence (BE) Studies 10.4 Implication of Bioequivalence Metrics 10.5 Bioequivalence Regulatory Guidelines 10.6 Biowaivers 10.7 Biopharmaceutics in Quality by Design 10.8 Control of Drug Product and Clinically Relevant Specifications 10.9 Establishing Clinically Relevant Dissolution Methods and Specifications 10.10 Application of In Silico Physiologically Based Biopharmaceutics Modelling (PBBM) to Develop Clinically Relevant Specifications 10.11 Additional Considerations for Establishing Dissolution Methods and Specifications 10.12 Common Technical Document (CTD) 10.13 Other Routes of Administration and Locally Acting Drug Products 10.14 Conclusion References
17 11 Impact of Anatomy and Physiology 11.1 Introduction 11.2 Influence of GI Conditions on Pharmacokinetic Studies 11.3 The Stomach 11.4 Small Intestine 11.5 The Colon/Large Intestine 11.6 Conclusions References
18 12 Integrating Biopharmaceutics to Predict Oral Absorption Using PBPK Modelling 12.1 Introduction 12.2 Mechanistic Models 12.3 Solubility Inputs 12.4 Dissolution Inputs 12.5 Permeability Inputs 12.6 Incorporation of Modelling and Simulation into Drug Development 12.7 Conclusions References
19 13 Special Populations 13.1 Introduction 13.2 Sex Differences in the Gastrointestinal Tract and Its Effect on Oral Drug Performance 13.3 Ethnic Differences in the Gastrointestinal Tract 13.4 Impact of Diet on Gastrointestinal Physiology 13.5 Pregnancy and Its Effect on Gastrointestinal Physiology 13.6 The Implication of Disease States on Gastrointestinal Physiology and Its Effect on Oral Drug Performance 13.7 Diseases that Affect the Gastrointestinal Tract 13.8 Infections in the Gastrointestinal Tract 13.9 Systemic Diseases that Alter GI Physiology and Function 13.10 Age‐related Influences on Gastrointestinal Tract Physiology and Function 13.11 Conclusion References
20 14 Inhalation Biopharmaceutics 14.1 Introduction 14.2 Structure of the Lungs 14.3 Molecules, Inhalation Devices, Formulations 14.4 Inhaled Drug Delivery and Models for Studying Inhalation Biopharmaceutics 14.5 Bioequivalence and an Inhalation Bioclassification System 14.6 Conclusion References
21 15 Biopharmaceutics of Injectable Formulations 15.1 Introduction 15.2 Subcutaneous Physiology and Absorption Mechanisms 15.3 Intramuscular Physiology and Absorption Mechanisms 15.4 In Vitro Performance and IVIVC 15.5 Bioequivalence of Injectable Formulations 15.6 Summary References
22 16 Biopharmaceutics of Topical and Transdermal Formulations 16.1 Introduction 16.2 Skin Structure 16.3 Active Pharmaceutical Ingredient Properties 16.4 Topical and Transdermal Dosage Forms 16.5 Measurement of In Vitro Drug Release 16.6 Measurement of Skin Permeation 16.7 Bioequivalence Testing of Topical/Transdermal Products 16.8 Conclusions References
23 17 Impact of the Microbiome on Oral Biopharmaceutics 17.1 Introduction 17.2 Microbiome Distribution in the GI Tract 17.3 Key Causes of Microbiome Variability 17.4 Microbiome Influence on Key GI Parameters 17.5 Enzymatic Degradation of Drugs by GI Microbiota 17.6 Exploitation of the GI Microbiome for Drug Delivery 17.7 Models of the GI Microbiome 17.8 Conclusion References
24 Index
