高蛋白饮食对犬体内司帕沙星药动学的影响

目的:研究高蛋白饮食对司帕沙星(SPFX)药动学的影响。方法:8只Beagle犬分别在空腹或高蛋白饮食状态下单次口服SPFX 10mg·kg-1,2周后交叉实验;采用高效液相色谱法测定不同时间血药浓度,用3p97软件计算二者的药动学参数并进行比较。结果:空腹和高蛋白饮食状态下SPFX的口服吸收分别符合二室、一室模型。主要药动学参数t1/2β/t1/2ke分别为(17.90±5.36)、(8.45±1.03)h;tmax分别为(3.28±1.32)、(7.70±1.33)h;Cmax分别为(0.70±0.19)、(0.84±0.27)μg·mL-1;AUC(0～t)分别为(11.66±3.77)、(20.63±4.22)μg·h·mL-1。除Cmax外,各药动学参数两两比较均有显著性差异(P<0.01)。结论:高蛋白饮食可延缓SPFX的吸收速度,增大吸收量,加快其排出速度,可明显影响司帕沙星药动学。

Effects of High Protein Diet on Pharmacokinetics of Sparfloxacin in Dog

OBJECTIVE： To study the effect of high protein diet on pharmacokinetics of sparfloxacin. METHODS： 8 beagle dogs with condition of fasting or high protein diet were given single oral dose of 10 mg·kg^-1 sparfloxacin for 2 weeks. A randomized crossover design was performed in 8 beagle dogs. Plasma concentration of sparfloxacin was measured by HPLC and pharmacokinetic parameters were calculated using 3p97 software. RESULTS： The concentration-time curves were coincided with one or two compartment model under condition of high protein diet and fasting in beagle dogs. Main pharmacokinetic parameters under condition of fasting vs. high protein diet were as follows： t1/2β/t1/2ke： （17.90±5.36）h vs. （8.45 ±1.03） h; tmax： （3.28 ± 1.32） h vs.（7.70±1.33） h; Cax： （0.70±0.19） μg·mL^-1 vs.（0.84±0.27）μg·mL^-1; AUC（0-1）：（11.66±3.77） μg·h·mL^-1 vs. （20.63±4.22）μg·h·mL^-1, respectively. There was significant difference in pharmacokinetic parameters between the two groups （P〈0：01） except of Cmax. CONCLUSION： High protein diet can infuence pharmacokinetic parameters of sparfloxacin by delaying the absorption rate, promoting absorption amount and speeding up secretion time of sparfloxacin.