不同内酯型比例9-硝基喜树碱对胆汁排泄的影响

Effect of Different Lactone Percentage of 9-nitrocamptothecin to Biliary Excretion

摘要: 目的考察9-硝基喜树碱(9-nitrocamptothecin，9-NC)不同形式(内酯型或羧酸盐型)给药对胆汁排泄的影响。方法建立HPLC测定胆汁中9-NC浓度的方法，比较不同内酯型比例的9-NC溶液以4 mg?kg^-1剂量静脉注射后大鼠胆汁中原形药物的排泄量。结果静脉注射100%，75%，50%，25%，0%内酯型比例的9-NC在8 h内的胆汁累积排泄百分数分别为(7.03±2.23)%，(13.36±0.83)%，(22.68±4.83)%，(28.01±6.71)%，(32.65±2.82)%。结论 9-NC羧酸盐型更易经胆汁途径排泄。

Abstract: OBJECTIVE To investigate the effect of administered 9-nitrocamptothecin(9-NC) forms (lactone or carboxylate form) on biliary excretion. METHODS The accurate HPLC method was developed for quantifying 9-NC in bile samples of rats. Then the ratios of cumulative excretion in bile were determined at different time following intravenous administration of 4 mg?kg^-1 9-NC solution with different lactone percentages to rats. RESULTS Following injection of 9-NC solution of 100%, 75%, 50%, 25% and 0% lactone ratios, the ratios of cumulative excretion in bile to the dose were determined to be (7.03±2.23)%, (13.36±0.83)%, (22.68±4.83)%, (28.01±6.71)%, (32.65±2.82)%, respectively. CONCULSION 9-NC in carboxylate form is easily excreted in bile compared to lactone form.