| 引用本文: | 陆姗姗,胡蓉蓉,顾薇,陈军,杨希雄.不同内酯型比例9-硝基喜树碱对胆汁排泄的影响[J].中国现代应用药学,2015,32(4):446-449. |
| LU Shanshan,HU Rongrong,GU Wei,CHEN Jun,YANG Xixiong.Effect of Different Lactone Percentage of 9-nitrocamptothecin to Biliary Excretion[J].Chin J Mod Appl Pharm(中国现代应用药学),2015,32(4):446-449. |
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| 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。 |
| 关键词: 9-硝基喜树碱 内酯型 羧酸盐型 胆汁排泄 |
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| 基金项目:湖北省自然科学基金项目(2012FFA083)；湖北省教育厅自然科学类重点科研项目(D20114301)；江苏省教育厅高校青蓝工程资助项目(苏教师〔2014〕23号) |
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| Effect of Different Lactone Percentage of 9-nitrocamptothecin to Biliary Excretion |
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LU Shanshan1, HU Rongrong1, GU Wei1, CHEN Jun1, YANG Xixiong2
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1.Laboratory of Pharmaceutics, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China;2.Hubei Collaborative Innovation Center of Targeted Antitumor Drug, Jingchu University of Technology, Jingmen, 448000, China
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| 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. |
| Key words: 9-nitrocamptothecin lactone carboxylate biliary excretion |
