Pharmacokinetic interaction study between ligustrazine and valsartan in rats and its potential mechanism

Autor: Yang Liu, Jiaqi Zhang, Di Wu, Liran Cui
Jazyk: angličtina
Rok vydání: 2020
Předmět:
Zdroj: Pharmaceutical Biology, Vol 58, Iss 1, Pp 1299-1302 (2020)
Druh dokumentu: article
ISSN: 1388-0209
1744-5116
13880209
DOI: 10.1080/13880209.2020.1859554
Popis: Context Ligustrazine and valsartan are commonly used drugs in the treatment of cardiac and cardiovascular disease. Objective The interaction between ligustrazine and valsartan was studied to investigate the effect of ligustrazine on the pharmacokinetics of valsartan. Materials and methods The pharmacokinetics of valsartan (10 mg/kg) was investigated in Sprague–Dawley rats divided into three groups (with the pretreatment of 4 or 10 mg/kg/day ligustrazine for 10 days and without the pretreatment of ligustrazine as control) of six rats each. The in vitro experiments in rat liver microsomes were performed to explore the effect of ligustrazine on the metabolic stability of valsartan. Results Ligustrazine changed the pharmacokinetic profile of valsartan. In the presence of 4 mg/kg ligustrazine, the AUC(0–t) (385.37 ± 93.05 versus 851.64 ± 104.26 μg/L*h), t1/2 (5.46 ± 0.93 versus 6.34 ± 1.25 h), and Cmax (62.64 ± 9.09 versus 83.87 ± 6.15 μg/L) of valsartan was significantly decreased, and the clearance rate was increased from 10.92 ± 1.521 to 25.76 ± 6.24 L/h/kg and similar changes were observed in the group with 10 mg/kg ligustrazine (p
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