HPLC-荧光法测定莫西沙星在犬体内的血药浓度及其药动学研究

目的:建立测定犬血浆中莫西沙星浓度的方法,并研究其药动学特性。方法:取Beagle犬6只,单剂量灌服莫西沙星120mg,采用高效液相色谱-荧光法测定给药后72 h内血浆中莫西沙星的浓度,采用DAS软件计算药动学参数。色谱柱为HypersilBDS C18,流动相为乙腈-1.0 mol.L-1醋酸溶液(25∶75,pH=2.0),流速为1.0 mL.min-1,激发波长为273 nm,发射波长为488 nm。结果:莫西沙星检测浓度的线性范围为0.1～20.0μg.mL-(1r=0.999 2),平均相对回收率为89.5%～96.7%,日内和日间RSD均<6%。莫西沙星在犬体内的药动学特性符合二室模型,主要药动学参数cmax:(10.25±4.21)μg.mL-1,tmax:(3.0±1.0)h,t1/2β:(9.76±2.48)h,AUC0～24 h:(142.10±49.80)mg.h.L-1。结论:本方法准确、灵敏、快速,适用于莫西沙星的血药浓度测定和药动学研究。

Determination of Plasma Concentration of Moxifloxacin in Beagle Dogs by HPLC-fluorescent Method and Its Pharmacokinetic Study

OBJECTIVE: To establish the method for determining the plasma concentration of moxifloxacin in Beagle dogs,and to study pharmacokinetic characteristics of it.METHODS: 6 Beagle dogs were given a single dose of moxifloxacin 120 mg.The plasma concentration of moxifloxacin in samples within 72 h after administration was determined by HPLC-fluorescent method and pharmacokinetic parameters was calculated by using DAS software.The determination was performed on Hypersil BDS C18 column with mobile phase consisted of acetonitrile-1.0 mol·L-1 acetic acid solution(25 ∶ 75,pH=2.0) at the flow rate of 1.0 mL·min-1.The excitation wavelength was set at 273 nm and emission wavelength was set at 488 nm.RESULTS: The liner range of moxifloxacin was 0.1～20.0 μg·mL-1(r=0.999 2) with relative recovery rate of 89.5%～96.7%.The RSDs of intra-day and inter-day were less than 6%.The pharmacokinetics of moxifoxacin was fitted to two-compartment open pharmacokinetic model.The main pharmacokinetic parameters of moxifloxacin were as follows: cmax:(10.25±4.21) μg·mL-1,tmax:(3.0±1.0) h,t1/2β:(9.76±2.48) h,AUC0～24 h:(142.10±49.80) mg·h·L-1.CONCLUSION: The method is accurate,sensitive and rapid,and suitable for plasma concentration determination and pharmacokinetic study of moxifloxacin.