Effect of scutellarin on the metabolism and pharmacokinetics of clopidogrel in rats. (22nd October 2014)

• Record Type: Journal Article
• Authors: Chen, Xinmeng; Jin, Jing; Chen, Yaobin; Peng, Lingling; Zhong, Guoping; Li, Jiali; Bi, Huichang; Cai, Yefeng; Huang, Min
• Is Part Of: Biopharmaceutics & drug disposition. Volume 36:Number 1(2015:Jan.)
• Page Start: 64
• Page End: 68
• Publication Date: 2014-10-22
• Subjects: Biopharmaceutics -- Periodicals; Drugs -- Metabolism -- Periodicals; Pharmacology -- Periodicals; Biopharmaceutics -- Periodicals; Pharmaceutical Preparations -- metabolism -- Periodicals; 615.19
• DOI: 10.1002/bdd.1918
• Languages: English
• ISSNs: 0142-2782

Abstract

<abstract abstract-type="main"> <title>Abstract</title> <p> <italic>Erigeron breviscapus</italic> (Vant.) Hand‐Mazz, a traditional Chinese medicine, is often co‐prescribed with clopidogrel for the treatment of ischemic vascular diseases. Scutellarin is the representative bioactive flavonoid isolated from this herb. The aim of this study was to explore the effect of scutellarin on the metabolism and pharmacokinetics of clopidogrel. The <italic>in vitro</italic> studies using rat liver microsomes showed that scutellarin significantly inhibited the metabolism of clopidogrel. The IC<sub>50</sub> value was 2.1 µ<sc>m</sc>. Ten male rats were employed to investigate the effect of scutellarin on the pharmacokinetics of clopidogrel <italic>in vivo</italic>. After pretreatment with scutellarin, there were significant increases in the <italic>AUC</italic><sub>0–∞</sub> (from 0.9 ± 0.4 to 1.7 ± 0.6 ng/ml h; <italic>p</italic> <0.05) and <italic>C</italic><sub>max</sub> (from 0.4 ± 0.1 to 0.9 ± 0.1 ng/ml; <italic>p</italic> <0.05) of clopidogrel. The pharmacokinetic data for clopidogrel active metabolite showed significant decreases in <italic>AUC</italic><sub>0–∞</sub> (18.2 ± 5.6 to 11.4 ± 3.7 ng/ml h; <italic>p</italic> <0.05) and <italic>C</italic><sub>max</sub> (from 8.2 ± 1.2 to 4.3 ± 0.3 ng/ml; <italic>p</italic> <0.05) after pretreatment with scutellarin. Collectively, the metabolism and pharmacokinetics of clopidogrel were significantly affected by scutellarin. This study indicated that potential herb–drug interaction between scutellarin and clopidogrel should be taken into consideration in clinical use. Copyright © 2014 John Wiley & Sons, Ltd.</p> </abstract>