不同剂量左氧氟沙星在大鼠胆汁药物浓度分布情况探讨

目的在大鼠模型上,研究不同剂量左氧氟沙星在大鼠胆汁药物浓度分布的情况,并初步探讨左氧氟沙星用于胆道感染的剂量问题。方法选择32只Wistar大鼠分为20,40,50,100 mg.kg-14个剂量组。在给药后30 min,1,2,3,4,5,6,8,10,12 h分别收集血标本和胆汁标本,经HPLC方法检测药物含量,并计算相关药代动力学参数。结果通过比较各组不同时点的血药浓度发现,各时点血药浓度差异均有显著性(P<0.05);而比较各剂量组胆汁药物浓度后发现,20和40 mg.kg-1剂量组各时点均无差异;1～5 h,50和100 mg.kg-1剂量组胆汁药物浓度显著高于其它剂量组;6～8 h,50和40 mg.kg-1剂量组相比差异无显著性,但10～12 h,两剂量组差异具有显著性;10～12 h,50和100 mg.kg-1剂量组相比浓度相差较大,但差异无显著性(P=0.053)。结论由动物模型结果推测,400 mg.d-1剂量用于治疗胆道感染可以满足临床需要,但500 mg.d-1剂量可能更合适临床用药。

Distribution of levofloxacin in rate bile after intravenous administration at different doses

Objective To determine the distribution of levofloxacin in rat bile after intravenous administration at different doses and if the dose of levofloxacin for treating the biliary tract administered infection is reasonable in China.Methods Thirty-two Wistar rats were divided into 4 groups randomly,and the drugs were respectively at a dose of 20,40,50,100 mg·kg-1.The blood and bile samples were collected in 30 min,1,2,3,4,5,6,8,10,12 h separately for assay by HPLC.Results By comparing of the plasma concentration in each group at each time point,it was found that the plasma concentration of each group at each time point was different（P0.05）.Comparing data of different times in each group,no significant difference was found between 20 mg·kg-1 and 40 mg·kg-1 groups.There was no distinct difference between 40 mg·kg-1 and 50 mg·kg-1 groups between 6 h and 8 h,while significant difference existed between 40 mg·kg-1 and 50 mg·kg-1 groups but no difference between 50 mg·kg-1 and 100 mg·kg-1 groups between 10 h and 12 h.Conclusion As for the dose of levofloxacin for curing biliary infection in China,400 mg·d-1 is basically able to meet the clinical requirement,but 500 mg·d-1 may be more suitable.