ABSTRACT

The pharmacokinetics of drugs intended for systemic use has been extremely useful in the design of an improved therapeutic agent. Specifically, pharmacokinetics has aided in the design of new chemical structures with optimal transport characteristics. The individual processes of pharmacokinetics are absorption, distribution, metabolism, and excretion (ADME). The lack of success in applying classical pharmacokinetic modeling to the eye is a result of a number of limitations, all unique to the eye. The compartmental scheme used to explain the ocular pharmacokinetics of fluorescein following the instillation of a 10% solution by iontophoresis shows aqueous humor reversibly connected with the cornea and a single exit pathway to plasma. A pharmacokinetic model was developed which described pilocarpine pharmacokinetics as a four-compartmental model in series. Cefotaxime is very water soluble and therefore expected to possess pharmacokinetic behavior similar to fluorescein. The noncompartmental approach was adapted for systemic pharmacokinetic use in the 1970s and obviated the necessity for compartments to determine ADME.