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The Effects of Verapamil on the Pharmacokinetics of Paeoniflorin in Rats 期刊论文

编号：

8332ffcc-0582-42dd-9862-a67b1d37733c
作者：

Liu, Lu(刘璐)#^[1]Li, Xiaohua^[1];Yuan, Yawei^[2];Li, Pihong^[3,4];
语种：

英文
期刊：

LATIN AMERICAN JOURNAL OF PHARMACY ISSN：0326-2383 2019 年 38 卷 2 期 (329 - 334)
收录：
关键词：

Caco-2 cells CYP450 oral absolute bioavailability paeoniflorin P-gp verapamil
摘要：

Paeoniflorin, a Chinese herbal medicine, has been widely used in clinical practice in China because of its numerous pharmacological activities. This study investigates the effects of verapamil on the pharmacokinetics of paeoniflorin in rats and clarify its potential mechanism. First, the pharmacokinetics of paeoniflorin (20 mg/kg) in rats with or without pretreatment with verapamil (10 mg/kg) were determined using a sensitive and reliable LC-MS method. Then the effects of verapamil on the transport and metabolic stability of paeoniflorin were investigated using Caco-2 cell transwell model and rat liver microsome incubation systems. The results showed that verapamil could significantly increase the peak plasma concentration (from 137.68 +/- 12.48 to 185.25 +/- 21.01 ng/mL) and AUC(0-t) (from 990.35 +/- 110.25 to 1472.48 +/- 243.52 ng.h/mL) of paeoniflorin. The Caco-2 cell experiments indicated that the efflux ratio of paeoniflorin was 2.90 (P-appAB 6.35 +/- 0.52 x 10(-7) ; P-appBA 1.84 +/- 032 x 10(-6) cm/s), P-gp might be involved in the transport of paeoniflorin, and verapamil could inhibit the efflux of paeoniflorin and increase the absorption of paeoniflorin significantly in the Caco-2 cell monolayer. Additionally, the rat liver microsome incubation experiments indicated that verapamil could significantly increase the metabolic stability of paeoniflorin from 31.5 to 46.8 min. Those results indicated that verapamil could significantly change the pharmacokinetic profiles of paeoniflorin in rats, the poor absorption due to P-gp mediated efflux in intestine and high intrinsic clearance rate in rat liver may be the main reason for its poor oral absolute bioavailability of paeoniflorin.
推荐引用方式
GB/T 7714：

Liu Lu,Li Xiaohua,Yuan Yawei, et al. The Effects of Verapamil on the Pharmacokinetics of Paeoniflorin in Rats [J].LATIN AMERICAN JOURNAL OF PHARMACY,2019,38(2):329-334.
APA：

Liu Lu,Li Xiaohua,Yuan Yawei,Li Pihong.(2019).The Effects of Verapamil on the Pharmacokinetics of Paeoniflorin in Rats .LATIN AMERICAN JOURNAL OF PHARMACY,38(2):329-334.
MLA：

Liu Lu, et al. "The Effects of Verapamil on the Pharmacokinetics of Paeoniflorin in Rats" .LATIN AMERICAN JOURNAL OF PHARMACY 38,2(2019):329-334.
入库时间：

1/1/2019 12:00:00 AM
更新时间：

1/1/2019 12:00:00 AM

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