氟苯尼考微囊在猪体内的药物动力学研究

Studies on the Pharmacokinetics of Florfenicol Microcapsules in Pigs

为了给兽医临床合理用药提供依据,分析氟苯尼考微囊(Florfenicol Microcapsules,FM)和氟苯尼考原粉(Florfenicol,FF)在猪体内的药物代谢动力学过程。猪单剂量分别灌服FF和FM 30 mg.kg-1,36 h不同时间16次前腔静脉采血,高效液相色谱法测定血药质量浓度。结果表明,FM和FF在猪体内的药物动力学配置均符合有吸收因素一室开放模型,其药-时曲线最佳方程分别为ρFM=3.772 7(e-0.047t-e-0.847 7t)和ρFF=0.375 9(e-0.258 1t-e-4.670 9t)。吸收半衰期(t1/2Ka)分别为(0.944 6±0.507 5)h,(0.155 0±0.030 1)h;消除半衰期(t1/2Ke)分别为(15.214 0±3.024 9)h,(2.694 5±0.169 5)h;药-时曲线下面积(AUC)为(77.3111±13.312 7)mg.L-1.h,(1.374 7±0.606 0)mg.L-1.h;峰质量浓度(ρmax)为(2.937 1±0.232 2)mg.L-1,(0.298 3±0.023 9)mg.L-1;达峰时间(tmax)为(3.951 0±1.533 9)h,(0.675 3±0.104 6)h。结果表明,氟苯尼考微囊口服给药吸收较慢但完全,达峰时间较长,消除缓慢,能够发挥长效作用。

Pharmacokinetic parameters of florfenicol microcapsules（FM） and florfenicol powder（FF） in 6 pigs were calculated.Pigs were treated with a single oral dosage of FF and FM（30 mg·kg-1） respectively,and the blood samples were collected from precaval vein for 16 times within 36 hours after giving drug.The concentrations of FF in serum were determined by high performance liquid chromatography（HPLC）.The result showed that the one-compartment open model with first-order absorption factor adequately describes concentrations of FM and FF in serum disposition and best concentration-time equations are： ρFM=3.772 7（e-0.047t-e-0.847 7t）,ρFF=0.375 9（e-0.258 1t-e-4.670 9t）.The primary pharmacokinetic parameters of FM and FF are： t1/2Ka=（0.944 6±0.507 5） h and（0.155 0±0.030 1） h,t1/2Ke=（15.214 0±3.024 9） h and（2.694 5±0.169 5） h,AUC=（77.311 1± 13.312 7） mg·L-1·h and（1.374 7±0.606 0） mg·L-1·h,ρmax=（2.937 1±0.232 2） mg·L-1 and（0.298 3±0.023 9） mg·L-1·h,tmax=（3.951 0±1.533 9）h and（0.675 3±0.104 6）.It will be seen that florfenicol microcapsules was completely absorbed with a slowly absorption rate,and which was eliminated slowly in the blood after single oral administration.