脂质饮食对犬体内莫昔沙星药动学的影响

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。

Effect of Lipide Diet on the Pharmacokinetics of Moxifloxacin in Dogs

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.