Abstract: AimTo develop a pharmacokinetic model for the enterohepatic circulation of mycophenolic acid (MPA). MethodsTwenty healthy volunteers were orally given a single dose of 500 mg mycophenolate mofetil. Plasma samples were collected during 48 hours and MPA concentration was measured by HPLC method. Pharmacokinetic (PK) model was established based on physiological and biopharmaceutical consideration and PK parameters were obtained using nonlinear mixed effect model. ResultsThe proposed model included an intestinal compartment and gall bladder compartment in addition to the central compartment. The predicted time-concentration curve and AUC0-t, C_max, T_max estimated by the established model were in agreement with the observations. ConclusionThe established model was well defined for the MPA disposition and could afford a useful approach for the further clinical investigation.