>
网站首页期刊介绍通知公告编 委 会投稿须知电子期刊广告合作联系我们
最新消息:
盐酸克林沙星在大鼠体内药代动力学的研究
作者:许茜 张建新 石南宁 王红芳 
单位:东南大学医学院公共卫生学院,
关键词:克林沙星 药代动力学 高效液相色谱-紫外可见分光光度法 大鼠 
分类号:R-332, R978.19, R969.1
出版年·卷·期(页码):2001·20·第二期(85-88)
摘要:

目的:了解盐酸克林沙星(clinafloxacin,CF)在大鼠体内的吸收、分布、排泄过程。方法:用高效液相色谱-紫外可见分光光度法,给大鼠灌胃5、10、20mg·kg-1CF后,测定在不同时间各组织和体液中CF含量。结果和结论:CF在大鼠体内药代动力学为一室模型,t1/2为2.03~2.17h,达峰时间tmax为1.0h,Cmax和曲线下积分面积AUC均随剂量的升高线性增大。给药后CF在组织中广泛分布,但几乎不存在于脑和脂肪组织。尿、粪及胆汁中原形药物总排出量约为给药量的22.1%,其中给药72h从尿排泄的原形药累积量相当于给药量的20.6%。在0.2~5.0mg·L-1浓度范围内,CF血浆蛋白结合率为90.2%~97.0%。

Objective  To study the absorption,distribution and excretion process of clinafloxacin hydrochloride(CF) in rats.Methods  The concentrations of CF in tissues and body fluids were determined by RP   HPLC  UV method after the rats had been administratered CF with the dosage of 5,10 and 20?mg·kg    -1   through disgestive tract.Results and Conclusion  The drug was found to conform to a one  compartment model.  t      max   was 1.0?h,  t      1/2   was in the range of 2.03?h to 2.17?h.The relationship between dose and AUC or   C      max   for CF was linear within the dosage range.CF was found in many  organs after a single oral dose of 10?mg·kg    -1  ,except brain and fat.After oral medication with 10?mg·kg    -1  ,cumulative urinary excretion of CF was   20.6  %±7.81% in 72 h,cumlative feces excretion of CF was 0.98%±0.23% in 72 h,cumulative biliary excretion of CF was 0.43%±0.09% in 24 h.From 90.2% to 97.0% of CF in plasma was shown to be bound to protein.

参考文献:

[1] Cohen M A. In vitro and in vivo activities of clinafloxacin,CI-990 (PD 131112),and PD 138312 versus enterococci, 1995(9)
[2] Tack K J, MCGUIRE N M, EISEMAN I A. Initial clinical experience with clinafloxacin in the treatment of serious infections. 1995(Suppl 2). doi:10.2165/00003495-199500492-00145
[3] Bron N J, DORR M B, MANT T G. The tolerance and pharmacokinetics of clinafloxacin (CI-960) in healthy subjects. 1996(6). doi:10.1093/jac/38.6.1023
[4] 许茜, 张建新, 石南宁. 大鼠血浆中克林沙星的RP-HPLC测定. 中国医药工业杂志2000(7). doi:10.3969/j.issn.1001-8255.2000.07.015
[5] EHRNEBO M. Age differerces in drug binding by plasma proteins:studies on human foetuses,neonates and adults, 1971 

服务与反馈:
文章下载】【发表评论】【查看评论】【加入收藏
提示:您还未登录,请登录!点此登录
您是第 413338 位访问者


copyright ©《东南大学学报(医学版)》编辑部
联系电话:025-83272481 83272483
电子邮件:
bjb@pub.seu.edu.cn

苏ICP备09058364