title: Influence of rifampicin on the pharmacokinetics of salvianolic acid B may involve inhibition of organic anion transporting polypeptide (Oatp) mediated influx.
abstract: This article studied the possible effect of rifampicin (RIF), an inhibitor of organic anion transporting polypeptide (Oatp), on the pharmacokinetics of salvianolic acid B (SAB) in rats. Rifampicin was administered intravenously 15 min prior to SAB (5 mg/kg) in rats at doses of 0, 5.0, 10.0 and 20.0 mg/kg, respectively. The concentrations of SAB in plasma and bile were determined using a Shimadzu HPLC system coupled to a LC-MS-2010EV mass spectrometer. Compared with the control group, the AUC(0-t) and C(max) values of SAB were increased significantly, while the CL(total) and CL(bile) were decreased significantly. These results suggested that pretreatment with rifampicin prior to SAB administration could decrease significantly the total and bile elimination of SAB and alter its pharmacokinetic profiles. The influence of rifampicin on the pharmacokinetics of SAB may be attributed to the inhibition of Oatp-mediated influx.
authors.affiliation: Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, Jiangsu 210009, PR China.
authors.forename: Di
authors.initials: D
authors.lastname: Zhao
authors.forename: Zi-dong
authors.initials: ZD
authors.lastname: Gao
authors.forename: De-en
authors.initials: DE
authors.lastname: Han
authors.forename: Ning
authors.initials: N
authors.lastname: Li
authors.forename: Yong-jie
authors.initials: YJ
authors.lastname: Zhang
authors.forename: Yang
authors.initials: Y
authors.lastname: Lu
authors.forename: Ting-ting
authors.initials: TT
authors.lastname: Li
authors.forename: Xi-jing
authors.initials: XJ
authors.lastname: Chen
mesh_terms: D000818:Animals; D019540:Area Under Curve; D001572:Benzofurans / Q000097:blood / Q000378:metabolism / Q000493:pharmacokinetics*; D001646:Bile / Q000378:metabolism*; D001692:Biological Transport / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D002853:Chromatography, Liquid; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D041743:Herb-Drug Interactions; D008297:Male; D013058:Mass Spectrometry; D027361:Organic Anion Transporters / Q000037:antagonists & inhibitors*; D010936:Plant Extracts / Q000097:blood / Q000378:metabolism / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012293:Rifampin / Q000494:pharmacology*; D027561:Salvia miltiorrhiza / Q000737:chemistry*; D053630:Depsides
chemical_list: D001572:Benzofurans; D004791:Enzyme Inhibitors; D027361:Organic Anion Transporters; D010936:Plant Extracts; D012293:Rifampin; C076944:salvianolic acid B; D053630:Depsides