Effect of P-Glycoprotein Inhibitor Verapamil on Pharmacokinetics of Loureirin A B C in Rats

被引：0
作者：
Li Y.-J. [1 ]
Kang L.-T. [1 ]
Guo J.-J. [1 ]
Wang S.-B. [1 ]
Li Y.-Z. [2 ]
Wang J.-P. [2 ]
Gao J.-Y. [2 ]
机构：
[1] School of Life Science, Beijing Institute of Technology, Beijing
[2] China Astronaut Research and Training Centre, Beijing
来源：
Li, Yu-Juan (lylyjlzh2006@163.com) | 1600年 / Beijing Institute of Technology卷 / 40期
关键词：
Dragon's Blood; P-glycoprotein; Pharmacokinetic; Verapamil;
D O I：
10.15918/j.tbit1001-0645.2018.289
中图分类号：
学科分类号：
摘要：
To study how P-glycoprotein inhibitor verapamil affect pharmacokinetics of the active constituents Loureirin A, B and C in rat plasma after oral administration of Dragon's Blood, SD rats were randomly put into different group: control group and inhibitor group. A single dose of 5 g/kg of Dragon's Blood was orally administered to rats in control group, and rats in the inhibitor group were given verapamil (1 mg/kg) and Dragon'Blood (5 g/kg). Plasma samples were collected from the two groups in the same series of time. A HPLC-MS/MS method was used to determine the content of Loureirin A, B and C in rat plasma, and the plasma samples pharmacokinetic parameters were calculated. Comparing the area under curve (AUC0-t) of the rats in the inhibitor group with the control group, it increased by 109.4%, 78.5%, 22.8%. And the peak concentration(Cmax) of Loureirin A, B and C increased by 69.6%, 115.0%, and 42.1%. The time of Loureirin A and B reaching peak concentration (tmax) was prolonged, while the tmax of Loureirin C was unchanged. All three biological half-life (t0.5) decreased. It indicates that P-glycoprotein inhibitor can significantly change the plasma pharmacokinetic parameters of Loureirin A, B and C in rats. Loureirin A, B and C may be potential substrates of P-glycoprotein. This article provides basic data for the subsequent in-depth study of the relationship between P-glycoprotein and transportation of Dragon's Blood in the intestinal tract of rats. © 2020, Editorial Department of Transaction of Beijing Institute of Technology. All right reserved.
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页码：105 / 110
页数：5
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