左氧氟沙星经胃转运、分布特点的研究  

Transport and distribution of levofloxacin in stomach

作　　者：鲍峻峻[1] 许建明[2] 胡咏梅[2] 梅俏[2] 石海[2] 郑海伦[3] 李见春[4] 

机构地区：[1]安徽医科大学第一附属医院腔镜中心,安徽蚌埠233000 [2]安徽医科大学第一附属医院消化内科,消化病重点实验室,安徽合肥230022 [3]蚌埠医学院第一附属医院消化内科,安徽蚌埠233000 [4]蚌埠医学院药学院,安徽蚌埠233000

出　　处：《中国药理学通报》2014年第1期90-96,共7页Chinese Pharmacological Bulletin

基　　金：国家青年自然科学基金资助项目(No 81100269);安徽省青年自然科学基金资助项目(No 11040606Q24)

摘　　要：目的初步探讨左氧氟沙星在大鼠胃内转运、分布特点。方法Wistar大鼠80只随机分为左氧氟沙星50、100g·k^-1组。静脉给药后2h内按15min间隔取血处死动物，收集不同时点胃液、胃黏膜样本，检测左氧氟沙星浓度。结果比较2组不同时点各部位药物浓度发现，给药后45～60min起，胃液药物浓度逐渐高于血药浓度，不同时间点胃体、胃窦药物浓度均高于血药浓度及前胃药物浓度，但胃体和胃窦药物浓度无差异；给药后60～75min起，胃液（药物浓度／血药浓度）％高于胃体、胃窦（药物浓度／血药浓度）％，不同时间点胃液、胃体、胃窦（药物浓度／血药浓度）％均高于前胃（药物浓度／血药浓度）％，但胃体和胃窦（药物浓度／血药浓度）％无差异。左氧氟沙星50、100mg·kg^-1组胃内转运分数分别为2．36、2．52。结论①在大鼠体内，随给药时间延长胃液左氧氟沙星浓度高于血药浓度，提示左氧氟沙星胃内可能存在主动转运过程。②大鼠胃窦、胃体左氧氟沙星药物分布无差异。Aim To discuss the transport and distribu- tion characteristics of levofloxacin in stomach of rat. Methods 80 Wistar rats were randomly divided into 2 groups： levofloxacin 50 mg ·kg^-1 group and levo- floxacin 100 mg ·kg^-1 group. Within 2 hours after in- travenous administration, the serum, gastric juice, stomach mucosa samples were collected at an interval of 15min and the concentration of levofloxacin of all the samples was detected to find out the feature of transport and distribution of levofloxacin in stomach of rat. Resuits Through comparison of the drug concentration of levofloxacin 50 mg ·kg^-1 group and 100 mg ·kg^-1 group in each part at different time points, it was found, after administration for about 45 - 60 minutes, that the drug concentration of gastric juice was gradual- ly higher than the drug concentration of serum （P 〈 0. 05）, and the drug concentrations of gastric corpus, gastric antrum at different time points were higher than the drug concentration of serum and forestomach （P 〈 0. 0 5 ） . However , there was no difference in the drug concentration of gastric corpus and the gastric antrum （P 〉 0.05 ）. The levofloxacin transport fraction in the stomach for levofloxacin 50 mg ·kg^-1 group, and levo- floxacin 100 mg ·kg^-1 group was respectively 2. 36, 2.52. Conclusions （ 1 ） In the rat body, along with the extension of administration time, the levofloxacin concentration of gastric juice gets higher than the serum concentration, indicating that there may be an active transport process for the levofloxacin in the stomach. （2） There is no difference between the distribution of levofloxacin in gastric corpus and gastric antrum.

关 键 词：左氧氟沙星 幽门螺杆菌 转运 分布 清除率 转运 分数 

分 类 号：R-332[医药卫生] R322.44