【摘要】 目的研究替加氟磁性长循环脂质体经肝动脉给药的药代动力学和组织靶向性。方法采用高效液相色谱仪检测大鼠生物样品中替加氟的浓度。结果磁控并加热的替加氟磁性长循环脂质体组的肝内8h药时曲线下面积(AUC)是游离替加氟组的17.4倍,是替加氟长循环脂质体组的3.9倍;其肝外组织血浆和肾的AUC比游离替加氟组低。其肝靶向效率达到73.9%。结论替加氟磁性长循环脂质体经肝动脉给药能显著增加药物的肝脏靶向性,可能降低其肾毒性。更多还原

【Abstract】 AIM To study liver targeting and pharmacokinetics of tegafur magnetic long-circulating liposomes (TMLCL) which were given rats by hepatic artery. METHODS The concentration in biological specimens of rats was detected with high performance liquid chromatography. RESULTS Area under concentration-time curve of 8 h at liver in TMLCL group was 17.4 times of that in tegafur group,and 3.9 times of that in tegafur long-circulating liposome group. Tegafur concentrations in plasma and kidney were lower than those in tegafur group and its liver-targeted ratio was 73.9%. CONCLUSION TMLCL by hepatic artery can markedly increase the liver targeting for tegafur and decrease nephrotoxicity in rats.更多还原