Regional pharmacokinetics of orally administered PET tracers

Positron emission tomography (PET) is currently the most useful imaging tec hnique for noninvasive measurement of drug pharmacokinetics regionally in a variety of tissues. Over the past decade, PET measurements have provided m any critical insights about the tissue distribution of several classes of d rugs; neuro leptics, antimicrobials, antineoplastics, etc. PET measurements can be performed after any route of drug administration, intravenous, inha lation or oral, however, intravenously administered drugs have been the mos t extensively evaluated. Studies of orally administered drugs are clearly o f great interest; however, formulation issues have precluded widespread app lications in these areas. In this report, we discuss the unique problems as sociated with studying orally administered drugs and review the results of recent studies performed in our laboratory.