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

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.