周梅华, 郁韵秋, 段更利, 程务本, 许长江, 刘骁. 克林沙星在大鼠体内的药代动力学和生物利用度J. 药学学报, 2001, 36(2): 134-136.
引用本文: 周梅华, 郁韵秋, 段更利, 程务本, 许长江, 刘骁. 克林沙星在大鼠体内的药代动力学和生物利用度J. 药学学报, 2001, 36(2): 134-136.
ZHOU Mei-hua, YU Yun-qiu, DUAN Geng-li, CHENG Wu-ben, XU Chang-jiang, LIU Xiao. PHARMACOKINETICS AND BIOAVAILABILITY OF CLINAFLOXACIN IN RATSJ. Acta Pharmaceutica Sinica, 2001, 36(2): 134-136.
Citation: ZHOU Mei-hua, YU Yun-qiu, DUAN Geng-li, CHENG Wu-ben, XU Chang-jiang, LIU Xiao. PHARMACOKINETICS AND BIOAVAILABILITY OF CLINAFLOXACIN IN RATSJ. Acta Pharmaceutica Sinica, 2001, 36(2): 134-136.

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

  • 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(5μm),流动相为乙腈-0.05mol·L-1柠檬酸三乙胺液(pH2.5)(20∶80),流速为1.0mL·min-1,检测波长300nm。结果 克林沙星0.1-20μg·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ig50和100mg·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50-100mg·kg-1的吸收和消除呈一级动力学特征,在大鼠体内的生物利用度低。

     

    Abstract: 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-C18 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-1and 100 mg·kg-1 dose of clinafloxacin in six rats, mean Cmax and AUC values increased in proportion to dose. Mean T1/2 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.

     

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