汉防己甲素肺靶向聚乳酸微球兔体内药动学的研究

Study on Pharmacokinetics of Lung Targeted Tetrandrine Polylactic Acid Microspheres in Rabbits

目的:为汉防己甲素肺靶向聚乳酸(TET -PLA)微球的体内代谢研究提供科学依据。方法:采用兔耳缘静脉注射给药、颈动脉取血方式,以反相高效液相色谱法测定血样中的汉防己甲素浓度;应用3p87药动学程序进行房室模型拟合,计算药动学参数。结果:汉防己甲素在家兔体内药动学过程呈二房室模型,t1/2β为(286. 49±237. 55)min ,AUC为(810. 33±287 .49) (μg·min)/ml。结论:TET -PLA微球在兔体内具有缓释作用。

OBJECTIVE:To provide scientific evidence for the microsphere's m etabolism in vivo of lung targeted tetranˉdrine polylactic acid(TET-PLA)microspheres.METHODS:Blood was sampled from carotid artery after microspheres were injected into rabbit through auricular vein,the concentration of TET in plasma was determined by RP-HPLC method;The pharmacokinetic parameters were obtained by using3p87program.RESULTS:Concentration-time curves of TET microˉspheres were fitted to a2-compartment model with t 1/2β of(286.49±237.55)min and AUC of(810.33±287.49)(μg·min)/ml.CONCLUSION:TET-PLA microspheres show sustained release effects in rabbits.