川芎嗪在小鼠血、脑和肝中的药动学研究

Pharmacokinetics of ligustrazine in blood,brain,and liver of mice

目的研究川芎嗪在小鼠体内血、脑、肝中的药动学,比较川芎嗪微乳和水溶液在小鼠体内药动学特征。方法川芎嗪微乳与其水溶液分别尾iv给药,用HPLC法测定不同时间点小鼠血、脑、肝中的川芎嗪质量浓度,用药动学软件对药时曲线数据进行拟合。结果微乳组的主要药动学参数分别为血浆:tmax2.50 min、Cmax4.79μg/mL、AUC 115.70 min.μg/mL、MRT 20.88 min;脑tmax5.00 min、Cmax7.81μg/mL、AUC 259.51 min.μg/mL、MRT 23.09 min;肝tmax5.00 min、Cmax10.66μg/mL、AUC 305.81 min.μg/mL、MRT 21.88 min。水溶液组的主要药动学参数分别为血浆:tmax2.50 min、Cmax4.42μg/mL、AUC 72.74 min.μg/mL、MRT 12.54 min;脑tmax5.00min、Cmax4.14μg/mL、AUC 130.19 min.μg/mL、MRT 25.90 min;肝tmax2.50 min、Cmax6.33μg/mL、AUC182.51 min.μg/mL、MRT 23.03 min。结论微乳改变了川芎嗪在小鼠血浆、脑、肝中药动学行为,提高了川芎嗪在脑、血、肝,特别是脑中的分布。

Objective To study the pharmacokinetics of ligustrazine in blood, brain, and liver of mice. Methods Ligustrazine solution and microemulsion were iv administrated to caudal vein of mice. Ligustrazine concentration in plasma, brain, and liver was determined by HPLC method. The data were processed with the software. Results The main pharmacokinetic parameters of ligustrazine microemulsion were： plasma t 2.50 min, Cmax 4.79 μg/mL, AUC 115.70 min·μg/mL, MRT 20. 88 min; brain： tmax 5. 00 min, C 7.81μg/mL, AUC 259.51 min ·μg/mL, MRT 23.09 min; liver： t 5.00 min, Cmax 10. 66μg/mL, AUC 305.81 min·μg/mL, MRT 21.88 rnin. The main pharmacokinetic parameters of ligustrazine solution were： plasma tmax 2.50 min, Cmax 4.42 μg/mL, AUC 72.74 min · μg/mL, MRT 12.54 min; brain： tmax 5.00 min, Cmax 4.14 μg/mL, AUC 130.19 min ·μg/mL, MRT 25.90 min; liver： tmax 2.50 min, Cmax 6.33 μg/mL, AUC 182.51 min ·μg/mL, MRT 23.03 min. Conclusion The microemulsion could after the ligustrazJne distribution in plasma, brain, and liver of mice, especially in brain.