The effect of herbal medicine baicalin on pharmacokinetics of rosuvastatin, substrate of organic anion-transporting polypeptide 1B1

被引：70

作者：

Fan, L. ^{[1
]}

Zhang, W. ^{[1
]}

Guo, D. ^{[1
]}

Tan, Z-R ^{[1
]}

Xu, P. ^{[2
]}

Li, Q. ^{[1
]}

Liu, Y-Z ^{[1
]}

Zhang, L. ^{[1
]}

He, T-Y ^{[1
]}

Hu, D-L ^{[1
]}

Wang, D. ^{[1
]}

Zhou, H-H ^{[1
]}

机构：

[1] Cent S Univ, Pharmacogenet REs Inst, Inst Clin Pharmacol, Changsha, Hunan, Peoples R China

[2] Cent S Univ, Affiliated Hosp 2, XiangYa Med Sch, Changsha, Hunan, Peoples R China

来源：

CLINICAL PHARMACOLOGY & THERAPEUTICS | 2008年 / 83卷 / 03期

关键词：

D O I：

10.1038/sj.clpt.6100318

中图分类号：

R9 [药学];

学科分类号：

1007 [药学];

摘要：

The aim of this study was to explore potential herb-drug interaction between baicalin and rosuvastatin, a typical substrate for organic anion-transporting polypeptide 1B1 (OATP1B1) related to different OATP1B1 haplotype groups. Eighteen unrelated healthy volunteers who were CYP2C9*1/*1 with different OATP1B1 haplotypes (six OATP1B1*1b/*1b, six OATP1B1*1b/* 15, and six OATP1B1*15/*15) were selected to participate in this study. Rosuvastatin (20mg orally) pharmacokinetics after coadministration of placebo and 50-mg baicalin tablets (three times daily orally for 14 days) were measured for up to 72 h by liquid chromatography-mass spectrometry in a two-phase randomized crossover study. After baicalin treatment, the area under the plasma concentration-time curve (AUC)((0-72)) and AUC((0-infinity)) of rosuvastatin decreased by 47.0 +/- 11.0% (P=0.001) and 41.9 +/- 7.19% (P=0.001) in OATP1B1*1b/*1b, 21.0 +/- 20.6% (P=0.035) and 23.9 +/- 8.66% (P=0.004) in OATP1B1*1b/* 15, and 9.20 +/- 11.6% (P=0.077) and 1.76 +/- 4.89% (P=0.36) in OATP1B1*15/*15, respectively. Moreover, decreases of both AUC((0-72)) and AUC((0-infinity)) of rosuvastatin among different haplotype groups were significantly different (P=0.002 and <0.001). Baicalin reduces plasma concentrations of rosuvastatin in an OATP1B1 haplotype-dependent manner.

引用

页码：471 / 476

页数：6

共 44 条

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ABE K, 1990, CHEM PHARM BULL, V38, P208, DOI 10.1248/cpb.38.208

[2]

Balicalin, the predominant flavone glucuronide of scutellariae radix, is absorbed from the rat gastrointestinal tract as the aglycone and restored to its original form [J].