目的:研究芎冰微乳制剂在兔体内的药动学特征。方法:芎冰微乳质量静脉注射给药后,采用高效液相测定不同时间点TMP的血药浓度,用DAS2.1数据处理软件计算药动学参数。结果:TMP体内质量浓度在0.062~12.4 mg.L-1(R2=0.998)呈良好的线性关系,其血药浓度曲线符合二室模型,其主要药动学参数t1/2α=15.617 mint,1/2β=49.171 min,V=0.509 L.kg-1,CL=0.014 L.min-1.kg-1,AUC(0-∞)=222 063.235μg.min.L-1,MRT(0-∞)=30.841 min。结论:本实验建立的方法简单,线性、精密度、回收率良好,专属性强,可用于川芎嗪体内药动学研究,并明确了芎冰微乳注射给药在新西兰兔体内的药动学特征。
Objective:To investigate pharmacokinetics of Xiongbing Microemulsion in rabbit blood.Method:The plasma concentration of tetramethylpyrazine(TMP) was determined by HPLC after i.v.The data were processed by DAS 2.1 software to calculate the pharmacokinetic parameters.Result:The calibration curve was linear in the range of 0.062-12.4 mg·L-1(R2=0.998).The measured pharmacokinetics of free TMP concentration fitted open two compartment model after i.v.The main pharmacokinetic parameters for TMP were as follows:t1/2α was 15.617 min;t1/2was 49.171 min;and V was 0.509 L·kg-1;CL was 0.014 L·min-1·kg-1;AUC(0-∞)was 222 063.235 μg·min·L-1;MRT(0-∞)was 30.841 min.Conclusion:With good linearity,precision and recovery,the method is sensitive and simple,and suitable for pharmacokinetic study and the research of TMP.The pharmacokinetic characteristics of TMP in rabbits were understood.