The effect of herbal medicine baicalin on pharmacokinetics of rosuvastatin, substrate of organic anion-transporting polypeptide 1B1
The effect of herbal medicine baicalin on pharmacokinetics of rosuvastatin, substrate of organic anion-transporting polypeptide 1B1
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DOI：
10.1038/sj.clpt.6100318
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发表时间：
2008-03-01
影响因子：
6.7
通讯作者：
Zhou, H-H
中科院分区：
文献类型：
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作者：
Fan, L.;Zhang, W.;Zhou, H-H
本研究的目的是探索黄芩苷和瑞舒伐他汀之间潜在的药物相互作用，瑞舒伐他汀是有机阴离子转运多肽1B1(OATP1B1)的典型底物，与不同的OATP1B1单倍型相关。选择18名具有不同OATP1B1单倍型(6例OATP1B1*1b/*1b、6例OATP1B1*1b/*15和6例OATP1B1*15/*15)的无血缘关系的健康志愿者作为研究对象。采用两阶段随机交叉试验，采用高效液相色谱质谱联用法测定口服罗舒伐他汀(20 mg口服)后，安慰剂与50 mg黄芩苷片(每日3次，连续14天)合用72 h后的药代动力学。治疗后，罗伐他汀在OATP1B1*1b/*1b、21.0+/-20.6%(P=0.035)、23.9+/-8.66%(P=0.004)的血药浓度-时间曲线下面积分别下降了47.0+/-11.0%(P=0.001)和41.9+/-7.19%(P=0.001)。OATP1B115/15分别为9.20+/-11.6%(P=0.077)和1.76+/-4.89%(P=0.36)。不同单倍型组间瑞舒伐他汀的AUC值((0.002-72))和AUC值((0-无穷大))均有显著差异(P=
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