克林沙星在大鼠体内的药代动力学和生物利用度  

PHARMACOKINETICS AND BIOAVAILABILITY OF CLINAFLOXACIN IN RATS

作　　者：周梅华[1] 郁韵秋[1] 段更利[1] 程务本[1] 许长江[2] 刘骁[2] 

机构地区：[1]上海医科大学药学院分析化学教研室 [2]药理学教研室,上海200032

出　　处：《药学学报》2001年第2期134-136,共3页Acta Pharmaceutica Sinica

摘　　要：目的　研究克林沙星在大鼠体内的药动学和生物利用度。方法　HPLC法测定大鼠ig和iv克林沙星后的血药浓度 ,计算药动学参数和生物利用度。色谱柱为C18柱 (5 μm) ,流动相为乙腈 0 0 5 mol·L-1柠檬酸三乙胺液(pH 2 5 ) (2 0∶80 ) ,流速为 1 0 mL·min-1,检测波长 30 0nm。结果　克林沙星 0 1- 2 0 μg·mL-1呈良好线性关系 ,在大鼠体内的药动学过程符合一室模型 ,大鼠ig 5 0和 10 0mg·kg-1后 ,Cmax和AUC均与剂量呈正比 ,T1/ 2 与剂量无关 ;绝对生物利用度 (F)为 42 %。结论　克林沙星 5 0 - 10 0mg·kg-1的吸收和消除呈一级动力学特征 。AIM To study the pharmacokinetics and bioavailability of clinafloxacin in rats. METHODS The drug concentration was determined by HPLC. The main pharmacokinetic parameters were obtained by 3P87 program. An RP C 18 was used as the stationary phase. The mobile phase was a mixture of acetonitrile 0 05 mol·L -1 citric acid triethylamine (pH 2 5) ( 20∶80 ). The flow rate was 1 0 mL·min -1 . The UV absorbance detector was set at 300 nm. RESULTS A good linearity was obtained from 0 03-20 μg·mL -1 of clinafloxacin in rat plasma with γ=0 9998. The plasma concentration time curve of clinafloxacin conformed to one compartment open model. After ig administration of 50 mg·kg -1 and 100 mg·kg -1 dose of clinafloxacin in six rats, mean C max and AUC values increased in proportion to dose. Mean T 1/2 appeared to be independent of dose. Mean AUC was 65±6 and 27±4 μg·h·mL -1 respectively after iv and ig adminostration of 100 mg·kg -1 dose. The extent of bioavailability ( F ) of clinafloxacin was 42%. CONCLUSION The results of the pharmacokinetic study of clinafloxacin showed that it exhibited first order kinetic characteristics and the bioavailability is low.

关 键 词：克林沙星 高效液相色谱法 药代动力学 生物利用度 

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