脂质饮食对加替沙星药动学的影响

Effect of Lipid Diet on Pharmacokinetics of Gatifloxacin

目的：研究脂质饮食对加替沙星药动学的影响。方法：8只Beagle犬随机交叉空腹或给予脂质饮食同时单次口服加替沙星胶囊17mg·kg^-1，采用高效液相色谱法测定血药浓度，用3p97软件计算两者的药动学参数，并评价脂质饮食对加替沙星药动学的影响。结果：空腹组和脂质饮食组的药-时曲线符合口服吸收一室模型，主要药动学参数t1/2Ke。分别为（4．00±0．84）、（7．87±1．54）h；tmax分别为（2．29±1．08）、（3．61±2．72）h；Cmax分别为（6．06±0．87）、（2．91±1．27）μg·mL^-1；AUC（0～t）分别为（56．74±10．80）、（45．35±10．81）μg·h·mL^-1，其中t1/2Ke、Cmax比较均有显著性差异（P〈0．05或P〈0．01）。结论：脂质饮食明显影响加替沙星药动学参数。

OBJECTIVE： To study the effect of lipid diet on the pharmacokinetics of gatifloxacin. METHODS： 8 Beagle dogs were randomly assigned to receive single oral dose of gatifloxacin capsules （17 mg·kg^-1） on empty stomach or in combination with lipid diet by a randomized crossover design plasma concentrations of gatifloxacin were measured by HPLC. The pharmacokinetic parameters were calculated by 3p97, and the effect of the lipid diet on the pharmacokinetics of gatifloxacin was evaluated. RESULTS： The concentration - time curves fitted one compartment model in empty stomach group and lipide diet group. The main pharmacokinetic parameters were as follows： t1/2ke were （4.00±0.84） and （7.87± 1.54） h; tmax （2.29± 1.08） and （3.61±2.72） h; Cmax （6.06±0.87） and （2.91± 1.27） μg ·mL^-1; AUC（0-t） （56.74± 10.80） and （45.35± 10.81） μg · h· mL^-1, respectively There were significant differences between the two groups in the t 1/2Ke and Cmax（P〈0.05 or P〈 0.01）. CONCLUSION： It showed that the lipid diet can markedly influence the pharmacokinetic parameters of gatifloxacin.