ABSTRACT

I. INTRODUCTION Pharmacokinetics is one of the many disciplines that contribute to the discov­ ery and development of drugs. This was not always the case. Although the basic mathematics of pharmacokinetics were described in some detail almost 60 years ago [1,2], about 30years went by before pharmacokinetics and the closely related discipline of drug metabolism started to make an appreciatable con­ tribution to the understanding and management of drug action and also to the contents of applications to regulatory authorities for drug marketing. The rapid advances in the disciplines of pharmacokinetics and drug metabolism during the 1960s were a result of the combined influences of improved analytical methodology and the increased awareness by health care providers of the fun­ damental importance of pharmacokinetics in drug development and therapy. The major leap forward in pharmacokinetics during that period was due also to the ingenuity, foresight, and entrepreneurial skills of a number of scientists, predominantly in the United States, including Benet [3], Garrett [4], Gibaldi [5], Levy [6], Riegelman [7], and Wagner [8]. The combined influence of these individuals, and some others, provided a considerable driving force for the rapid evolution of pharmacokinetics.