| Effect of organic anion transporting polypeptide 1B1 inhibition on the pharmacokinetics of rosuvastatin via HNF1a by ursodeoxycholic acid in vivo |
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| 引用本文： | HE Yi-jing ZHANG Wei TU Jiang-hua JULIA Kirchheiner CHENG Yao GUO Dong LI Qin LI Zhong-yu CHENG Hao HU Dong-li WANG Dan ZHOU Hong-hao. Effect of organic anion transporting polypeptide 1B1 inhibition on the pharmacokinetics of rosuvastatin via HNF1a by ursodeoxycholic acid in vivo[J]. 中国临床药理学与治疗学, 2007, 12(10): 1179-1179 |
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| 作者姓名： | HE Yi-jing ZHANG Wei TU Jiang-hua JULIA Kirchheiner CHENG Yao GUO Dong LI Qin LI Zhong-yu CHENG Hao HU Dong-li WANG Dan ZHOU Hong-hao |
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| 作者单位： | [1]Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University, Changsha 410078, Hunan, China [2]Institute of Natural Product and Clinical Pharmacology, Ulm University, Helmholtzstr, Ulm 89081, Germany |
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| 摘 要： | AIM： The inhibition of organic anion transporting polypeptide 1B1 （OATP1B1） on the pharmacokinetics of rosuvastatin is unknown. Hence, the effect of ursodeoxycholic acid （UDCA） on the kinetics of rosuvastatin in healthy volunteers is to be investigated. METHODS： The inhibition effect of long term use of UDCA on rosuvastatin kinetics was studied in 12 subjects in a randomized, crossover study. Each subject received 500 mg UDCA once daily continuously for 14 days. A single oral dose of 20 mg rosuvastatin was given on study day 15 and 34 separated by 2 weeks. Plasma concentrations of rosuvastatin were above the limits of quantitation for up to 72 h after dosing. RESULTS： UDCA significantly increased AUC0-72 and AUC0-∞ of rosuvastatin to 146% ± 55% （P = 0.008） and 167% ± 73% （ P = 0.004） compared with those of the control group and CL/F decreased 75% ± 19% （P = 0. 003）. The results confirmed the in vitro study that UDCA inhibited OATP1B1 activity via hepatic nuclear factor 1a （HNF1a）.[第一段]
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| 关 键 词： | 熊脱氧胆酸 罗苏伐他汀 药物代谢动力学 HNF1a 抑制作用 |
Effect of organic anion transporting polypeptide 1B1 inhibition on the pharmacokinetics of rosuvastatin via HNF1a by ursodeoxycholic acid in vivo |
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| Abstract: | |
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| Keywords: | OATP1B1 HNF1a UDCA rosuvastatin inhibition |
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