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目的评价芎冰微乳灌胃、静脉注射和鼻腔给药三种不同给药途径川芎嗪(TMP)在脑部的药动学特性。方法采用脑微透析取样技术,以清醒大鼠为实验模型,连续收集三种给药途径大鼠脑纹状体透析液,HPLC法测定TMP浓度,经回收率校正后,用DAS2.1药动学软件计算主要药动学参数。结果灌胃、静注和鼻腔给药TMP在脑内药动学过程均符合一室模型,MRT0-∞分别为73.7,38.8,70.6 min;Tmax分别为15,5,15 min;Cmax分别为249.2,2579.3,1175.1μg.L-1,AUC0-∞分别为19806.9,106410.7,62973.3μg.min.L-1,TMP在脑组织中的局部生物利用度显示,鼻腔给药为59.2%,灌胃给药为18.6%。结论芎冰微乳灌胃给药生物利用度较低;静脉注射TMP入脑迅速,生物利用度最高,但代谢迅速,作用时间短;鼻腔给药生物利用度较高,且脑内作用时间较长,具有一定的研究价值。
Objective To evaluate the pharmacokinetic properties of ligustrazine (TMP) in the brain of mice by intragastric, intravenous and intranasal administration of Xiong Bing microemulsion. Methods Brain microdialysis sampling technique was used in this study. The conscious rats were used as the experimental model, and the brain striatum dialysate of three administration routes were collected continuously. The concentration of TMP was determined by HPLC. After recoveries were corrected, Learning software calculates the main pharmacokinetic parameters. Results The intragastric administration of TMP administered intragastrically, intravenously and intranasally was in accordance with the one-compartment pharmacokinetic model. The MRT0-∞ were 73.7, 38.8 and 70.6 min, the Tmax were 15, 5 and 15 min, and the Cmax were 249.2 , 2579.3,1175.1μg.L-1, AUC0-∞ were 19806.9,106410.7,62973.3μg.min.L-1, the local bioavailability of TMP in brain tissue showed that nasal administration was 59.2%, intragastrically The medicine is 18.6%. Conclusion Xiongxiong microemulsified oral administration of bioavailability is low; intravenous injection of TMP rapidly into the brain, the highest bioavailability, but the rapid metabolism, short duration of action; nasal administration of bioavailability, and the role of brain time Long, with some research value.