高效液相色谱荧光检测法测定人血浆中氟罗沙星浓度及其药代动力学研究

目的建立测定人血浆中氟罗沙星浓度的高效液相色谱方法，并用于其药代动力学研究。方法氟罗沙星血浆样品经甲醇沉淀蛋白后直接进样。色谱柱为Diamonsil C18柱，流动相为1％三乙胺（磷酸调pH至4．8）／乙腈（80／20，V／V），流速1．0mL·min^-1。采用荧光检测器，激发波长290nm，发射波长458nm。氟罗沙星药代动力学研究采用双周期交叉试验设计。结果氟罗沙星血浆浓度在0．025～8．00μg·L^-1范围内线性关系良好，低、中、高浓度质控样品的日内、日间精密度不超过5．16％，方法精密度99．1％～100．9％，提取回收率86．7％～92．0％。健康志愿者口服400mg氟罗沙星试验及参比制剂后主要药代动力学参数分别为：Cmax5．08±0．78和5．38±1．40μg·mL^-1，tmax 1．72±0．79和1．82±0．78h，t1/2 11．68±1．27和11．38±1．51h^-1，AUC0-∞ 78．44±11．44和76．53±13．24μg·mL^-1·h。结论该方法灵敏度高、定量准确，适用于氟罗沙星人体药代动力学研究。

Determination of fleroxacin in human plasma by HPLC with fluorescence detection and the pharmacokinetic study

Aim To develop a sensitive and acctLrate HPLC methodfor the determination of fleroxacin in human plasma,and study its pharmacokinetics in healthy subjects.Methods The analytes were isolated from plasma by simple protein precipitation with methanol,separated on a Diamonsil C18 column by isocratic elution with the mobile phase consisted of 1%triethylamine at pH 4.8(adjusted with phosphofic acid)and acetonitrile(80/20,V/V) at a flow rate of 1.0 mL min-1,and analyzed by fluorescence detector with an excitation at 290 nm and emission 458 nm.The pharmacokinefic studv of fleroxacin was performed according to a double period crossover design.Results The weighted (1/x)calibration curve was linear over the plasma concentration railge of and extraction recoveries at three concentrations ranged from 99.1% to 100.9%,and 86.7%to 92.O%,respectively.FoUowing oral administration at a dose of 400 mg fleroxaein,the main pharmacokinetic parameters for test and reference capsules were for human pharmacokinetic study of fleroxacin.