【摘要】 用DMAP法制备氟苯尼考琥珀酸钠(Fl-SNa)。将6只家兔分别单剂量肌肉注射氟苯尼考和Fl-SNa,然后采用高效液相色谱(HPLC)法检测血药浓度;用DAS2.0药代动力学程序计算药代动力学参数。结果显示,成功制得Fl-SNa;给家兔单剂量注射氟苯尼考和Fl-SNa后,主要的药代动力学参数Cmax分别为8.863mg/L±0.254mg/L和7.363mg/L±0.085mg/L,tmax分别为1.0h和2.0h,AUC0-∞分别为28.851mg/L.h±0.494mg/L.h和39.187mg/L.h±0.413mg/L.h。结果表明,Fl-SNa达峰时间延长,峰浓度降低,生物利用度大大提高。证明高效液相色谱法准确、灵敏,适用于氟苯尼考血浆浓度的测定;制备的Fl-SNa与氟苯尼考相比生物利用度显著提高。更多还原

【Abstract】 Florfenicol sodium succinate(Fl-SNa) was prepared using 4-dimethylaminopyridine(DMAP) as catalyst.The blood samples from the rabbits intramuscularly-injected with a single dose of either florfenicol solution or Fl-SNa solution were collected to measure florfenicol concentrations in plasma by high performance liquid chromatography(HPLC).The pharmacokinetic parameters were analyzed with DAS2.0 software.In results,Fl-SNa was successfully prepared.The major pharmacokinetic parameters of florfenicol and Fl-SNa were shown as Cmax of 8.863 mg/L±0.254 mg/L vs.7.363 mg/L±0.085 mg/L,tmax of 1.0 h vs.2.0 h,and AUC0-∞ of 28.851 mg/L·h±0.494 mg/L·h vs.39.187 mg/L·h±0.413 mg/L·h,respectively.In conclusion,HPLC was suitable for the determination of florfenicol concentration in plasma of rabbits,and the Fl-SNa could significantly increase bioavailability of florfenicol in rabbits.更多还原