作者
Yi-Jing He, Wei Zhang, Yao Chen, Dong Guo, Jiang-Hua Tu, Lin-Yong Xu, Zhi-Rong Tan, Bi-Lian Chen, Zhi Li, Gan Zhou, Bang-Ning Yu, Julia Kirchheiner, Hong-Hao Zhou
发表日期
2009/7/1
期刊
Clinica Chimica Acta
卷号
405
期号
1-2
页码范围
49-52
出版商
Elsevier
简介
BACKGROUND
Both atorvastatin and rifampicin are substrates of OATP1B1 (organic anion transporting polypeptide 1B1) encoded by SLCO1B1 gene. Rifampicin is a potent inhibitor of SLCO1B1 (IC50 1.5 umol/l) and SLCO1B1 521T>C functional genetic polymorphism alters the kinetics of atorvastatin in vivo. We hypothesize that rifampicin might influence atorvastatin kinetics in a SLCO1B1 polymorphism dependent manner.
METHODS
Sixteen subjects with known SLCO1B1 genotypes (6 c.521TT, 6 c.521TC and 4 c.521CC) were divided into 2 groups (atorvastatin–placebo group, n=8; atorvastatin–rifampicin group, n=8) randomly. In this 2-phase crossover study, atorvastatin (40 mg single-oral dose) pharmacokinetics after co-administration of placebo and rifampicin (600 mg single-oral dose) were measured for up to 48 h by liquid chromatography–mass spectrometry (LC–MS). In the third phase, rifampicin (450 …
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