This publication explains the principles of the techniques used in disposition and metabolism studies in animals, in man, and in vitro. It includes methods for studying routes and rates of absorption, distribution, metabolism, and excretion of novel compounds and their metabolites. Relevant surgical, whole-body autoradiographic and pharmacokinetic procedures are discussed, together with techniques for separating and identifying metabolites and metabolic path-ways. Information on when the procedures are appropriate, and examples of what they represent, are presented in order to illustrate the value of such studies.

SECTION 1: INTRODUCTION, Chapter 1 The Rationale for and Timing of Drug Metabolism Studies, SECTION 2: IN VIVO BIOLOGICAL STUDIES, Chapter 2 Aims, Chapter 3 Balance Studies, Chapter 4 Whole Body Autoradiography, Chapter 5 Surgical Techniques Used in Disposition and Metabolism Studies, Chapter 6 Afterword, SECTION 3: EXTRAPOLATION OF DATA AND STUDIES IN MAN, Chapter 7 Studies in Man with Potential Therapeutic Agents, Chapter 8 Pharmacokinetics and Its Application to Drug Development, SECTION 4: METABOLITE IDENTIFICATION AND IN VITRO STUDIES, Chapter 9 Analytical Procedures for Metabolites: Metabolite Profiling and the Isolation and Identification of Metabolitesm, Chapter 10 In Vitro Studies on Metabolism, Chapter 11 Biochemical Studies on Induction, Inhibition, and Activation, Index