目的研究枳壳对丁螺环酮在健康大鼠体内药物动力学的影响。方法将SD大鼠随机分为丁螺环酮组,丁螺环酮加枳壳低剂量组(15 g/kg),丁螺环酮加枳壳高剂量组(30 g/kg),测定给药后5、10、20、30、45、60、90、120、240、360、480、600 min丁螺环酮的血药浓度,计算并比较其药动学参数。结果与丁螺环酮组比较,丁螺环酮加枳壳低剂量组和高剂量组中丁螺环酮AUC(0-t)分别增加2.49和4.18倍,Cmax分别增加1.63和2.57倍,Tmax从0.28 h分别延长至0.52和1.06 h,t1/2从0.96 h分别延长至2.18和4.87 h,差异具有统计学意义(P〈0.05)。结论枳壳可增加同服药物丁螺环酮的AUC(0-t)和Cmax,提高丁螺环酮生物利用度,并有剂量依赖性趋势,枳壳与丁螺环酮发生显著的药动学相互作用。
Objective To investigate the effect of Fructus aurantii on the pharmacokinetics of buspirone in healthy rats.Methods SD rats were randomly divided into buspirone group, the low dose group of Fructus aurantii(15 g/kg) plus buspirone, and the high dose group of Fructus aurantii(30 g/kg) plus buspirone, respectively. The blood concentrations of buspirone were determined after 5, 10, 20, 30, 45, 60, 90, 120, 240, 360, 480, 600 min and their pharmacokinetic parameters were calculated. Results Compared with the buspirone group, the AUC(0-t)of the low dose group and high dose group were increased by 2.49 and 4.18 time and the Cmaxwere increased by 1.63 and 2.57 time, respectively. The Tmaxof the low dose group and high dose group were extended from 0.28 h to 0.52 h and 1.06 h and the t1/2were extended from 0.96 h to 2.18 h and 4.87 h, respectively. The differences were statistically significant(P〈0.05). Conclusion Fructus aurantii can increase the AUC(0-t)and Cmaxof buspirone, improve the bioavailability of buspirone, and the changs of parameters show the dependence trendency. Fructus aurantii and buspirone have significant pharmacokinetic interactions.