Essentials of Biopharmaceutics and Pharmacokinetics

CONTENTS

Section 1 Biopharmaceutics and Pharmacokinetics: What Do They Mean? 1

Chapter 1

Introduction to Biopharmaceutics and Pharmacokinetics 3

1. Introduction 3

2. Historical Perspective of Biopharmaceutics 3

3. Extravascular Administration of a Drug 6

4. Scope of Biopharmaceutics 7

5. Variants in Biopharmaceutics 7

6. Pharmacokinetics 8

7. Clinical Pharmacokinetics 10

8. Pharmacodynamics 12

9. Toxicokinetics and Clinical Toxicology 13

10. Bioavailability 13

11. Bioequivalence 17

Section 2 Biopharmaceutics 23

Chapter 2

Biopharmaceutics 25

1. Introduction 25

2. Biopharmaceutics Classifi cation System (BCS) 29

3. In Vitro–In Vivo Correlation (IVIVC): An Introspection 30

4. Passage of Drugs across Biological Barrier 33

5. Factors Infl uencing Drug Absorption 43

6. Mechanisms of Drug Absorption 58

7. Drug Absorption vs. Bioavailability 72

Section 3 Pharmacokinetics 121

Chapter 3

Pharmacokinetics 123

1. Introduction 123

2. Clinical Signifi cance of Plasma Protein Drug Concentration

Measurement 124

3. Pharmacokinetic Models 133

4. Pharmacokinetics of Drug Absorption 154

5. Volume of Distribution and Distribution Coeffi cient 170

6. Organ-Specifi c Clearance 173

7. Non-Linear Pharmacokinetics 195

8. Pharmacokinetic Profi les of Some Specifi c Examples

from Various Classes of Drugs 206

Section 4 Clinical Pharmacokinetics 215

Chapter 4

Clinical Pharmacokinetics 217

1. Introduction 217

2. Dosage Regimens: Design, Modalities and Implementation 221

3. Single Dose Bioequivalence Study: Design and Relevant Statistics 248

4. Pharmacokinetic Drug Interaction: Signifi cance in Combination Therapy 275

Section 5 Bioavailability and Bioequivalence 283

Chapter 5

Bioavailability and Bioequivalence 285

1. Introduction 285

2. Bioavailability 291

3. Bioequivalence 327

4. Bioanalytical Method Development and Validation for Bioavailability and Bioequivalence Studies 336

Index 347