Please use this identifier to cite or link to this item: http://localhost:80/xmlui/handle/123456789/13228
Title: Inhibitory effect of sesamin on ivabradine metabolism in rats
Authors: Xu, Ren-ai
Sun, Wei
Chen, Ruimin
Liu, Naihua
Huang, Chengke
Keywords: Ivabradine
N-desmethylivabradine
sesamin
drug interaction
pharmacokinetics
Issue Date: 10-Nov-2020
Publisher: Karachi:Pakistan Journal of Pharmaceutical Sciences, university of Karachi.
Citation: Xu, R. A., Sun, W., Chen, R., Liu, N., & Huang, C. (2020). Inhibitory effect of sesamin on ivabradine metabolism in rats. Pakistan Journal of Pharmaceutical Sciences, 33(6), 2543-2547.
Abstract: In this work, the aim of our study was to assess whether sesamin could influence the pharmacokinetics of ivabradine and its active metabolite N-desmethylivabradine in rats. At the begining, 12 healthy male Sprague-Dawley rats were randomly divided into two groups: The rats were received an oral administration of 1.0mg/kg ivabradine alone (the control group), and the rats were given 1.0mg/kg ivabradine co-administered with 50mg/kg sesamin by gavage (the test group). After that, blood samples were collected from the tail vein of rats, and ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) were used for determing the plasma concentrations of ivabradine and N-desmethylivabradine in rats. Finally, the pharmacokinetic parameters were estimated using DAS 2.0 software. As the results, the pharmacokinetic parameters (t1/2, Cmax, AUC(0-t) and AUC(0-∞)) of ivabradine in the control group were significantly lower than those in the test group (P<0.05). Moreover, sesamin significantly decreased t1/2, Cmax, AUC(0-t) and AUC(0-∞) of N-desmethylivabradine when compared to the control. These results demonstrated that sesamin increases plasma concentration of ivabradine and decreases N-desmethylivabradine conversely. Hence, our data indicated sesamin could influence the pharmacokinetic profile of ivabradine in rats, which might cause food-drug interaction in humans.
URI: http://142.54.178.187:9060/xmlui/handle/123456789/13228
ISSN: 1011-601X
Appears in Collections:Issue 6

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