This study aimed to examine the effects of Rifampin (RIF) on the pharmacokinetics of Salvianolic acid A (SAA) in rats.Compared to the control group given SAA alone, the concurrent use of RIF (5, 10, and 20mg/kg, i.v.) prior to the intravenous injection ofSAA (5mg/kg) increased the AUC and Cmax values by 71.7-192.7% and 41.2-110.7%, respectively; While the CLtotal and CLbile were significantly decreased by 22.3-84.1% and 39.2-96.1% respectively; and it did not affect the T1/2.The concentrations of SAA in plasma and bile were determined using a Shimadzu HPLC system coupled with a LC-MS-2010EV mass spectrometer.These results show that pretreatment with RIF prior to SAA intravenous injection could significantly decrease the total and bile elimination of SAA and alter its pharmacokinetic profiles.Given that SAA and RIF can interact with organic anion-transporting polypeptides (Oatps) expressed in liver,the present results show the potential drug interaction between SAA and RIF via the competition for the Oatp-mediated cellular transport during hepatic uptake of drugs.