脂质饮食对犬体内莫昔沙星药动学的影响

Effect of Lipide Diet on the Pharmacokinetics of Moxifloxacin in Dogs

目的:研究脂质饮食对莫昔沙星药动学的影响。方法:8只Beagle犬分别在空腹或脂质饮食状态下灌服莫昔沙星胶囊17mg·kg-1,1周后交叉实验;采用高效液相色谱法测定不同时间(72h内)血药浓度,用3p97软件计算二者的药动学参数并进行比较。结果:Beagle犬空腹组和脂质饮食组的药-时曲线分别符合二室模型和一室模型;空腹和脂质饮食状态下莫昔沙星主要药动学参数t1/2(βt1/2ke)分别为(24.89±6.77)、(12.32±2.96)h,tmax分别为(2.00±0.76)、(9.00±1.85)h,Cmax分别为(7.07±0.67)、(4.16±1.32)μg·mL-1,AUC0～t分别为(84.30±10.86)、(85.78±27.38)μg·h·mL-1;除AUC0～t外,其余各参数两两比较均有显著性差异(P<0.01)。结论:脂质饮食可明显延迟莫昔沙星的吸收,不利于其抗菌作用的发挥。

OBJECTIVE：To study the effect of lipide diet on pharmacokinetics of moxifloxacin.METHODS：In randomized crossover experiment,8 Beagle dogs were given moxifloxacin 17 mg·kg^-1 at the condition of empty stomach or after lipide diet for 1 week.Plasma concentration of moxifloxacin was determined by HPLC at different time（during 72 h）.The pharmacokinetic parameters were calculated by 3p97 software.RESULTS：The plasma concentration-time curves were two or one compartment model at the condition of empty stomach or after lipide diet.Main pharmacokinetic parameters were as follows：t1/2β（t1/2ke）：（24.89±6.77） h vs.（12.32±2.96） h;tmax：（2.00±0.76） h vs.（9.00±1.85） h;Cmax：（7.0±0.67） μg·mL^-1 vs.（4.16±1.32） μg·mL^-1;AUC0～t：（84.30±10.86） μg·h·mL^-1 vs.（85.78±27.38） μg·h·mL^-1,respectively.There were significant differences in pharmacokinetic parameters except for AUC0～t（P0.01）.CONCLUSION：Lipide diet can delay the absorption of moxifloxacin and inhibit its antibacterial activity.