摘要
目的:考察静脉注射9-硝基喜树碱脂质体后原形药物经大鼠胆汁的排泄。方法:建立了利用HPLC法测定大鼠胆汁中9-硝基喜树碱浓度的方法;测定了9-硝基喜树碱在大鼠空白胆汁中的内酯型浓度、总浓度和内酯型比例的变化;测定了静脉注射3mg.kg-19-硝基喜树碱溶液和脂质体后大鼠胆汁中原形药物的排泄情况。结果:9-硝基喜树碱内酯型结构在胆汁中不稳定,内酯型浓度和比例迅速下降但总浓度保持恒定。静脉注射9-硝基喜树碱溶液和脂质体后12h胆汁中原形药物的累积排泄量分别为给药剂量的7.9%和8.1%。
Objective ： To investigate the biliary excretion of 9-nitrocamptothecin （9-NC） after intravenous administration of 9-NC liposome to rats. Methods：The specific and accurate HPLC method was developed for quantifying 9-nitrocamptothecin in bile samples of rats. The lactone and total 9-NC concentraions as well as lactone percentage versus time profiles in blank bile in vitro were determined. The ratios of cumulative excretion in bile to the administered dose were determined at different time following intravenous administration of 3 mg-kg i 9-NC solution or liposome to rats. Results：Lactone stability in rat bile samples was so poor that lactone 9-NC concentration as well as lactone percentage decreased quickly with time in blank bile in vitro. But total 9-NC concentration remained unchanged. After intravenous administration of 9-NC solution or liposome, the ratios of cumulative excretion in bile to the administered dose were 7.9% and 8.1% , respectively. Conclusion：Liposomal encapsulation has little effect on biliary excretion of 9-NC after intravenous administration to rats.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2007年第17期1365-1368,共4页
Chinese Journal of New Drugs
