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不同内酯型比例9-硝基喜树碱对胆汁排泄的影响
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.
作者姓名:陆姗姗  胡蓉蓉  顾薇  陈军  杨希雄
作者单位:南京中医药大学药学院药物制剂研究室,南京 210023,南京中医药大学药学院药物制剂研究室,南京 210023,南京中医药大学药学院药物制剂研究室,南京 210023,南京中医药大学药学院药物制剂研究室,南京 210023,荆楚理工学院靶向抗肿瘤药物湖北省协同创新中心,湖北 荆门 448000
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)
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
收稿时间:2014/7/15 0:00:00
修稿时间:2014/10/25 0:00:00

Effect of Different Lactone Percentage of 9-nitrocamptothecin to Biliary Excretion
LU Shanshan,HU Rongrong,GU Wei,CHEN Jun and YANG Xixiong.Effect of Different Lactone Percentage of 9-nitrocamptothecin to Biliary Excretion[J].The Chinese Journal of Modern Applied Pharmacy,2015,32(4):446-449.
Authors:LU Shanshan  HU Rongrong  GU Wei  CHEN Jun and YANG Xixiong
Institution:Laboratory of Pharmaceutics, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China,Laboratory of Pharmaceutics, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China,Laboratory of Pharmaceutics, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China,Laboratory of Pharmaceutics, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China and Hubei Collaborative Innovation Center of Targeted Antitumor Drug, Jingchu University of Technology, Jingmen, 448000, China
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.
Keywords:9-nitrocamptothecin  lactone  carboxylate  biliary excretion
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