Abstract
Recently, it became clear that drug transporters are closely related to pharmacokinetics, and it has been recognized that the transporters are the important factor for determining drug bioavailability. On the other hand, in a viewpoint of drug delivery system, drug pharmacokinetics are thought to be controllable by manipulating the function of transporters. This review introduces how intestinal active drug influx or efflux transport system is concerned with drug pharmacokinetics, with a focus on the transporters of intestine. In addition, the possibility to control oral bioavailability by manipulating the function of transporters will be discussed.
