摘要
目的:研究乳糖化-去甲斑蝥素(lactosyl-norcantharidin,Lac-NCTD)水溶液及纳米粒2种制剂在大鼠体内药动学特征。方法:建立测定大鼠血浆中Lac-NCTD的HPLC检测法,并用3P97软件进行药动学拟合。结果:Lac-NCTD能与血浆中其他成分较好分离,在0.1～100μg/mL范围内线性关系良好。与Lac-NCTD水溶液相比,Lac-NCTD纳米粒的AUC及t1/2β显著增加,分别为Lac-NCTD水溶液的8.96倍和1.68倍,清除率显著降低(P<0.01)。结论:与水溶液相比,Lac-NCTD制备成纳米粒制剂后能显著改变药物在大鼠体内的药动学特征,延长了药物在体内的循环时间,有利于更好地发挥抗肿瘤效果。
Objective：To study the pharmacokinetics of Lactosyl-norcantharidin（Lac-NCTD） nanoparticals in rats.Methods：The plasma concentrations of Lac-NCTD were detected at various time points by the validated HPLC method.The data were processed with the pharmacokinetic software 3P97.Results：A good separation of Lac-NCTD from other substances in plasma was obtained.The assay was linear over the range of 0.1～100 μg/mL.Compared with Lac-NCTD solution,the AUC and t1/2β of Lac-NCTD were increased significantly （8.96 fold and 1.68 fold,respectively）and the total body clearance was decreased （P0.01）.Conclusion：Compared with reference injection,the narnoparticals can significantly improve the pharmacokinetic behavior of Lac-NCTD.
出处
《抗感染药学》
2010年第2期90-93,共4页
Anti-infection Pharmacy
基金
国家科技支撑计划课题资助(编号:2006BAI09B00)
国家科技部科技型中小企业技术创新基金(立项代码:07C26223201333)
江苏省"六大人才高峰"资助项目
国家大学生创新实践课题(编号:57315924)
