盐酸克林沙星在大鼠体内药代动力学的研究  

Study on the pharmacokinetics of clinafloxacin hydrochloride in rats

作　　者：许茜[1] 张建新[1] 石南宁[1] 王红芳[1] 

机构地区：[1]东南大学医学院公共卫生学院,江苏南京210009

出　　处：《南京铁道医学院学报》2001年第2期85-88,共4页Journal of Nanjing Railway Medical College

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、2 0mg·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 .0 3～ 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2 2 .1% ,其中给药 72h从尿排泄的原形药累积量相当于给药量的 2 0 .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.

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 抗菌药物 血药浓度 

分 类 号：R978.19[医药卫生—药品] R969.1[医药卫生—药学]