盐酸头孢噻呋对苦参碱大鼠体内药动学的影响

Effect of ceftiofur hydrochloride on pharmacokinetics of matrine in rats

目的:研究盐酸头孢噻呋对苦参碱在大鼠体内药动学的影响。方法:采用HPLC-UV测定苦参碱单独给药组与盐酸头孢噻呋和苦参碱联合给药组中苦参碱在大鼠体内的血药浓度,用DAS2.1.1药动学程序处理苦参碱的血药浓度-时间数据对,比较两者的药动学参数。结果:苦参碱单独给药组苦参碱的Cmax为21.113 9 mg.L-1,Tmax为0.75 h,t1/2α为1.34 h,t1/2β为3.509 h,AUC0～t为90.984 mg.h-1.L-1,AUC0～∞为100.346 mg.h-1.L-1。盐酸头孢噻呋和苦参碱联合给药组苦参碱的Cmax为11.707 mg.L-1,Tmax为0.917 h,t1/2α为1.598 h,t1/2β为3.247 h,AUC0～t为53.28 mg.h-1.L-1,AUC0～∞为60.035mg.h-1.L-1。结论:苦参碱与盐酸头孢噻呋联合给药时苦参碱的血药浓度、生物利用度显著降低,在外周室的分布减少,中央室的分布增加,体内清除率亦有所增加。

Objective： To investigate the effect of ceftiofur hydrochloride on the pharmacokinetics of matrine in rats.Method： The rats were divided into two groups： one group was administrated with matrine only（control group） and the other was administrated with matrine in combination with ceftiofur hydrochloride.HPLC-UV method was used for determining the plasma concentration of matrine in both groups.The pharmacokinetic parameters were calculated from the plasma concentration-time data using the DAS 2.1.1 software program.Result： The main pharmacokinetic parameters for the control group were Cmax=21.113 9 mg·L-1,Tmax=0.75 h,t1/2α=1.34 h,t1/2β=3.509 h,AUC0～t=90.984 mg·h-1·L1 and AUC0～∞=100.346 mg·h-1·L-1,and the data for the combination group were Cmax=11.707 mg·L-1,Tmax=0.917 h,t1/2α=1.598 h,t1/2β=3.247 h,AUC0～t=53.28 mg·h-1·L-1 and AUC0～∞=60.035 mg·h-1·L-1.Conclusion： The plasma concentration of matrine and bioavailability in combination group were significantly lower than those of the control group.In combination group,matrine had a higher clearance and volume of distribution in the central compartments,as well as a lower volume of distribution in the peripheral compartments.