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Prediction of Drug-Drug Interaction between Tacrolimus and Principal Ingredients of Wuzhi Capsule in Chinese Healthy Volunteers Using Physiologically-Based Pharmacokinetic Modelling 期刊论文

编号：

4cca24c9-0bf1-4d51-b487-7d0c78f22750
作者：

Zhang, Hongyan^[1];Bu, Fengjiao^[1];Li, Lei^[1];Jiao, Zheng^[2];Ma, Guo(马国)^[1]Cai, Weimin(蔡卫民)^[1]Zhuang, Xiaomei^[3];Lin, HaiShu^[4];Shin, JaeGook^[5];Xiang, Xiaoqiang(相小强)*^[1]
语种：

English
期刊：

BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY ISSN：1742-7835 2018 年 122 卷 3 期 (331 - 340) ; MAR
收录：
摘要：

Schisantherin A and schisandrin A, the most abundant active ingredients of Wuzhi capsule, are known to inhibit tacrolimus metabolism by inhibiting CYP3A4/5. We aimed to predict the contribution of schisantherin A and schisandrin A to drug-drug interaction (DDI) between Wuzhi capsule and tacrolimus using physiologically-based pharmacokinetic (PBPK) modelling. Firstly, the inhibition mechanism of schisantherin A and schisandrin A on CYP3A4/5 was investigated. Thereafter, PBPK models of schisantherin A, schisandrin A and tacrolimus were established. Finally, tacrolimus pharmacokinetics were evaluated after the combined use with schisantherin A or schisandrin A. The blood area under the curve (AUC) of tacrolimus increased 1.77- and 2.61-fold after a single dose and multiple doses of schisantherin A, respectively. Meanwhile, schisandrin A inhibited tacrolimus metabolism to a smaller extent. Also, it showed that mechanism-based inhibition (MBI) played a more important role in DDI than reversible inhibition after long-term administration, while reversible inhibition was comparable to MBI after single-dose administration. In conclusion, we utilized PBPK modelling to quantify the contribution of schisantherin A and schisandrin A to DDI between tacrolimus and Wuzhi capsule. This may provide more insights for the rational use of this drug combination.
推荐引用方式
GB/T 7714：

Zhang Hongyan,Bu Fengjiao,Li Lei, et al. Prediction of Drug-Drug Interaction between Tacrolimus and Principal Ingredients of Wuzhi Capsule in Chinese Healthy Volunteers Using Physiologically-Based Pharmacokinetic Modelling [J].BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY,2018,122(3):331-340.
APA：

Zhang Hongyan,Bu Fengjiao,Li Lei,Jiao Zheng,&Xiang Xiaoqiang.(2018).Prediction of Drug-Drug Interaction between Tacrolimus and Principal Ingredients of Wuzhi Capsule in Chinese Healthy Volunteers Using Physiologically-Based Pharmacokinetic Modelling .BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY,122(3):331-340.
MLA：

Zhang Hongyan, et al. "Prediction of Drug-Drug Interaction between Tacrolimus and Principal Ingredients of Wuzhi Capsule in Chinese Healthy Volunteers Using Physiologically-Based Pharmacokinetic Modelling" .BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY 122,3(2018):331-340.

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