Abstract: Pharmacokinetics is an important part of pharmacology, which is guide for drug using rationally, preventing adverse reactions, studying the mechanism of action and drug-drug interaction. PET molecular imaging technology is able to dynamically monitor physiological, biochemical and biological processes in vivo, and it can be applied to the study of pharmacokinetics, tissues distribution and drug-drug interaction. All of these will promote new drug development. This paper summarizes the applications of PET molecular imaging technology to pharmacokinetics in recent years.