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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t1/2延长了2.02倍,AUC0-∞增加了1.85倍,MRT0-∞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。
OBJECTIVE To prepare apigenin vesicles using nonionic surfactants and study their pharmacokinetics in vivo and tissue distribution in mice. Methods The apigenin vesicles were prepared by ethanol injection. The apigenin vesicles and self-made apigenin solution were injected into the tail vein. The concentrations of apigenin in plasma and tissues were determined by high performance liquid chromatography (HPLC) Pharmacokinetic parameters in mice and tissue distribution parameters in mice. Results The encapsulation efficiency of apigenin vesicles was (69.48 ± 2.5)% and the particle size was (148 ± 5.03) nm. The pharmacokinetics of apigenin injection and apigenin injection at a dose of 2 mg · kg-1 in the tail vein showed that t1 / 2 of apigenin-treated vesicles was 2.02 times longer than that of the injection group, AUC0-∞ increased by 1.85-fold and MRT0-∞ increased by 2.16-fold. Tissue distribution showed that apigenin vesicles in the liver, lung and brain AUQ (under the amount of drug vs time curve, Q = C × V) Significant increase in heart, kidney AUQ decreases. Conclusions Apigenin vesicles significantly prolong the circulation time of apigenin in the body and reduce the accumulation of drugs in the heart and kidney, making it possible to provide a safe and effective apigenin preparation for clinical use.