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黑种草和葫芦巴对高血压大鼠氨氯地平药代动力学和药效学的影响。

Effect of Nigella sativa and Fenugreek on the Pharmacokinetics and Pharmacodynamics of Amlodipine in Hypertensive Rats.

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.

出版信息

Curr Drug Metab. 2020;21(4):318-325. doi: 10.2174/1389200221666200514121501.

DOI:10.2174/1389200221666200514121501
PMID:32407268
Abstract

BACKGROUND

The present article is related to in-vitro and in-vivo herb-drug interaction studies.

OBJECTIVES

This study aimed to investigate the effect of Nigella sativa and fenugreek on the pharmacodynamics and pharmacokinetics of amlodipine.

METHOD

Hypertensive rats of group-I were treated with amlodipine and rats of group-II and III were treated with N. sativa, and N. sativa + amlodipine and fenugreek, and fenugreek + amlodipine, respectively. Systolic blood pressure (SBP), diastolic blood pressure (DBP) and mean blood pressure (MBP) of group-I, II and III rats were measured by the "tail-cuff system".

RESULTS

N. sativa, as well as fenugreek, reduced the SBP, DBP and MBP. Simultaneously, administration of fenugreek + amlodipine or N. sativa + amlodipine showed better control of BP. Individually, fenugreek, as well as N. sativa, showed a surprising reduction in the heart rate. There was no remarkable effect of any of these two herbs on Cmax, AUC0-t, Kel, and terminal elimination half-life of amlodipine, but fenugreek altered the Tmax of amlodipine significantly, from 2 ± 1.2h in control to 7.2 ± 1.7h in fenugreek treated group, probably by delaying the absorption.

CONCLUSION

Results of pharmacodynamics and pharmacokinetics studies suggested that simultaneous administration of fenugreek or N. sativa with amlodipine improved the pharmacological response of amlodipine in hypertensive rats, though there was no remarkable change in pharmacokinetic parameters (Cmax, Kel, elimination t1/2, and AUC0-t).

摘要

背景

本文涉及体内和体外草药-药物相互作用研究。

目的

本研究旨在探讨黑种草子和葫芦巴对氨氯地平药效学和药代动力学的影响。

方法

将第一组高血压大鼠用氨氯地平治疗,第二组和第三组大鼠分别用黑种草子、黑种草子+氨氯地平、葫芦巴和葫芦巴+氨氯地平治疗。采用“尾套系统”测量三组大鼠的收缩压(SBP)、舒张压(DBP)和平均血压(MBP)。

结果

黑种草子和葫芦巴均能降低 SBP、DBP 和 MBP。同时,给予葫芦巴+氨氯地平或黑种草子+氨氯地平,血压控制效果更好。单独使用葫芦巴或黑种草子,均能显著降低心率。这两种草药单独使用时,对氨氯地平的 Cmax、AUC0-t、Kel 和终末消除半衰期均无显著影响,但葫芦巴显著改变了氨氯地平的 Tmax,从对照组的 2±1.2h 延长至葫芦巴处理组的 7.2±1.7h,可能是通过延迟吸收。

结论

药效学和药代动力学研究结果表明,同时给予葫芦巴或黑种草子与氨氯地平可改善高血压大鼠中氨氯地平的药理反应,尽管药代动力学参数(Cmax、Kel、消除半衰期 t1/2 和 AUC0-t)无显著变化。

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