头孢呋辛钠与头孢呋辛钠复方制剂在Beagle犬体内的药动学考察

目的研究头孢呋辛钠舒巴坦钠复方制剂中头孢呋辛在Beagle犬体内的药动学行为,并比较单组分头孢呋辛与复方制剂中头孢呋辛的药动学差异。方法采用高效液相色谱法(HPLC)测定Beagle犬静脉给予头孢呋辛钠复方制剂不同剂量和单独给予头孢呋辛钠后不同时刻血浆中头孢呋辛的浓度,计算主要药动学参数。结果犬静脉给予头孢呋辛钠复方制剂(等同于头孢呋辛57.0、142.6和356.5 mg.kg-1)3个剂量后,头孢呋辛的t1/2分别为(1.1±0.2)、(1.0±0.1)和(1.2±0.3)h;ke分别为(0.693±0.119)、(0.707±0.094)和(0.591±0.117)h-1;犬静脉给予头孢呋辛钠(等同于头孢呋辛57.0 mg.kg-1)后,头孢呋辛的t1/2和ke分别为(1.2±0.3)h和(0.615±0.133)h-1。结论 Beagle犬静脉给予头孢呋辛钠复方制剂低、中、高3种剂量后,头孢呋辛呈线性动力学特征,且复方制剂与单一制剂中头孢呋辛的药动学行为无显著差异。

Pharmacokinetics of single cefuroxime and cefuroxime compound preparation in Beagle dogs

Objective To study the pharmacokinetics of single cefuroxime and cefuroxime compound preparation in Beagle dogs and their mutual influences.Methods Single cefuroxime and cefuroxime compound preparations were given to six Beagle dogs separately.The concentration of cefuroxime in plasma was determined by HPLC,the concentration-time curve was drawn and the main pharmacokinetics parameters were calculated.Results After intravenous injection three dosages cefuroxime compound preparations to six Beagle dogs,the t1/2 values of cefuroxime were(1.1±0.2)h,(1.1±0.1)h,and(1.2±0.3)h,respectively.The ke values of cefuroxime were(0.693±0.119)h-1,(0.707±0.094)h-1 and(0.591±0.117)h-1,respectively.The ρmax and AUC0-t of cefuroxime were directly proportional to the dosage of intravenous injection.Six Beagle dogs were given single cefuroxime,the t1/2 and ke of cefuroxime were(1.2 ± 0.3)h and(0.615 ± 0.133)h-1,respectively.Conclusions The plasma drug concentration-time course in Beagle dogs is conformed to the two-compartment model and cefuroxime′s pharmacokinetics appeared to be linearity.The main pharmacokinetics parameters show no significant after intravenous injection single cefuroxime and cefuroxime compound preparation.