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目的:研究灌服磷酸川芎嗪对大鼠体内硝苯地平的药动学过程影响。方法:24只雄性Wistar大鼠随机分为4组,分别灌服纯化水,20,40,80mg.kg-1磷酸川芎嗪,连续5d灌服10mg.kg-1硝苯地平,于0,0.10,0.25,0.50,0.75,1.0,2.0,4.0,6.0,8.0,10.0h取血,采用HPLC-MS/MS法测定血浆硝苯地平浓度,采用DAS2.0计算药动学参数。结果:与单独灌服硝苯地平相比,大鼠连续5d灌服40mg.kg-1和80mg.kg-1磷酸川芎嗪,硝苯地平AUC0-10h分别增加41.8%(P<0.05)和77.3%(P<0.01),MRT0-10h延长15.3%(P<0.05)和10.4%(P<0.05),Cl降低31.5%和45.0%。结论:40mg.kg-1和80mg.kg-1磷酸川芎嗪可增加硝苯地平的生物利用度,减慢硝苯地平的体内消除。
Objective: To study the effects of ligustrazine phosphate on the pharmacokinetics of nifedipine in rats. Methods: Twenty-four male Wistar rats were randomly divided into 4 groups. The rats were infused with purified water, ligustrazine phosphate 20,40,80mg.kg-1, nifedipine 10mg.kg-1 for 5 days, , 0.25,0.50,0.75,1.0,2.0,4.0,6.0,8.0,10.0h blood plasma was determined by HPLC-MS / MS nifedipine plasma concentration, using the DAS2.0 pharmacokinetic parameters. RESULTS: Compared with nifedipine alone, rats were administered with 40 mg.kg-1 and 80 mg.kg-1 Ligustrazine Phosphate every 5 days, and nifedipine AUC0-10h increased by 41.8% (P <0.05) and 77.3 (P <0.01). MRT0-10h was prolonged by 15.3% (P <0.05) and 10.4% (P <0.05), Cl decreased by 31.5% and 45.0%, respectively. Conclusion: Ligustrazine phosphate 40mg · kg-1 and 80mg · kg-1 can increase the bioavailability of nifedipine and reduce the elimination of nifedipine in vivo.