芹菜素囊泡的体内药动学和组织分布研究

 目的使用非离子表面活性剂制备芹菜素囊泡,并对其进行大鼠体内药动学和小鼠体内组织分布的研究。方法采用乙醇注入法制备芹菜素囊泡,尾静脉注射芹菜素囊泡和自制芹菜素溶液,利用高效液相色谱法检测血浆和各组织中的芹菜素浓度,利用统计学方法计算芹菜素在大鼠体内的药动学参数及小鼠的组织分布参数。结果芹菜素囊泡包封率为(69.48±2.5)%,粒径为(148±5.03)nm。经尾静脉给予剂量为2mg·kg^-1的芹菜素注射液和芹菜素囊泡注射液,体内药动结果显示,与注射液组相比,芹菜素囊泡组t_1/2延长了2.02倍,AUC_0-∞增加了1.85倍,MRT_0-∞增加了2.16倍,组织分布结果显示,芹菜素囊泡在肝、肺、脑部AUQ(are under the amount of drug vs time curve,Q=C×V)显著增加,在心脏、肾脏AUQ减小。结论芹菜素囊泡明显延长了芹菜素在体内的循环时间,降低了药物在心、肾的蓄积,使得为临床提供安全有效的芹菜素制剂成为可能。

Pharmacokinetics and Tissue Distribution of Apigenin Niosomes

OBJECTIVE To study the preparation of apigenin niosomes and their pharmacokinetics in rats and tissue distribution in mice.METHODS Apigenin niosomes was prepared by ethanol injection method.The pharmacokinetics and tissue distribution of apigenin niosomes and apigenin solution were carried out in Wistar rats and KM mice by caudal vein injection, respectively.RESULTS The entrapment efficiency of the niosomes was(69.48±2.5)% , the average particle size was(148±5.03)nm.Compared with apigenin injection,the circulation time of apigenin niosomes in plasma was longer.The t_1/2 was increased by 2.02 fold ,the AUC_0-∞ was increased by 1.85 fold and MRT_0-∞ was increased by 2.16 fold.The AUCs_0-∞ of liver,lung and brain were much bigger,while less in heart and kidney.CONCLUSION Apigenin niosomes can prolong the circulation in vivo,and reduce the accumulation in heart and kidney,which can improve curative effects and reduce toxicity.