ABSTRACT

INTRODUCTION Pharmacokinetics is arguably one of the most important disciplines in pharmaceutical development as it permits “windowsof opportunity” tomeasuredrug and/ormetabolite concentrations and link these measurements with pharmacological effect. In today’s pharmaceutical industry, the science of pharmacokinetics has evolved such that, when used in support of drug safety testing, it forms an indispensable discipline in the pursuit of new candidate drugs. The earliest concepts of pharmacokinetics probably beganwith Torsten Teorell, a Swedish physiologist, who in 1937 described the movement of drugs through various compartments of the body (1,2), but it was not until 1953 that the term “Pharmacokinetics” was first used by Friedrich Dost in his text “Kinetik de Konzentrationsabla¨ufe in der Kreislaufflu¨ssigkeit” (3). Despite these earliest descriptions, the use of pharmacokinetics as a routine discipline to study the movement of drugs in and out the body had to wait a further two decades until the development of specific, sensitive, and accurate chromatographic methods for the quantitative analysis of drugs became widely available for use in drug research.