title: Effects of danshen ethanol extract on the pharmacokinetics of fexofenadine in healthy volunteers.
abstract: This study investigated the effect of multidose administration of danshen ethanol extract on fexofenadine pharmacokinetics in healthy volunteers. A sequential, open-label, two-period pharmacokinetic interaction design was used. 12 healthy male volunteers received a single oral dose of fexofenadine (60 mg) followed by danshen ethanol extract (1 g orally, three times a day) for 10 days, after which they received 1 g of the danshen extract with fexofenadine (60 mg) on the last day. The plasma concentrations of fexofenadine was measured by LC-MS/MS. After 10 days of the danshen extract administration, the mean AUC and C max⁡ of the fexofenadine was decreased by 37.2% and 27.4% compared with the control, respectively. The mean clearance of fexofenadine was increased by 104.9%. The in vitro study showed that tanshinone IIA and cryptotanshinone could induce MDR1 mRNA. This study showed that multidose administration of danshen ethanol extract could increase oral clearance of fexofenadine. The increased oral clearance of fexofenadine is attributable to induction of intestinal P-glycoprotein.
authors.affiliation: Laboratory of Clinical Pharmacokinetics, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Furong
authors.initials: F
authors.lastname: Qiu
authors.affiliation: Laboratory of Clinical Pharmacokinetics, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Jin
authors.initials: J
authors.lastname: Zeng
authors.affiliation: Laboratory of Clinical Pharmacokinetics, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Songcan
authors.initials: S
authors.lastname: Liu
authors.affiliation: Laboratory of Clinical Pharmacokinetics, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Min
authors.initials: M
authors.lastname: He
authors.affiliation: Laboratory of Clinical Pharmacokinetics, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Leilei
authors.initials: L
authors.lastname: Zhu
authors.affiliation: Laboratory of Clinical Pharmacokinetics, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Yujie
authors.initials: Y
authors.lastname: Ye
authors.affiliation: Laboratory of Clinical Pharmacokinetics, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Ping
authors.initials: P
authors.lastname: Miao
authors.affiliation: Laboratory of Clinical Pharmacokinetics, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Shujiao
authors.initials: S
authors.lastname: Shen
authors.affiliation: Laboratory of Clinical Pharmacokinetics, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Jian
authors.initials: J
authors.lastname: Jiang