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This short text deals with the fundamentals of the two twin disciplines of biopharmaceutics and pharmacokinetics which have been developed with the objective of learning how drugs can be employed optimally in the treatment of disease through the understanding of the various procedures and advances in drug design, product development, therapeutic drug monitoring, etc. The major aim of compiling this text is to present the information in a lucid style to cater specifically the needs of undergraduate and postgraduate students of pharmacy, medicine. Wherever necessary, mathematical equations have been developed using simple integration and differentiation methods to enable the students to understand the concepts easily. Every effort has been exercised to present the concepts in a simple way. A concise description of the biovailabilty of a drug from its formulation has been included at a separate place in the text. Practice questions have been included at the end of chapter to help the students to understand the subject thoroughly. Contents : 1. Introduction 2. Drug Absorption 3. Distribution of Drugs 4. Protein Binding of Drugs 5. Metabolism and Clearance Concept 6. Drug Dissolution 7. Pharmacokinetics 8. Nonlinear Pharmacokinetics 9. Introduction to Pharmacodynamics 10. Bioavailability, Dosage Regimen and Single and Multiple Dosing 11. Bioequivalence Studies 12. In Vitro-In Vivo Correlation of Dissolution 13. Mean Residence Time (MRT) 14. Statistical Moment Theory 15. Laplace Transformation 16. Drug Dosing