单剂量氟苯尼考内服及肌注在家兔体内药代动力学研究

The pharmacokinetics of florfenico1 following a single oral and intramuscular administration to rabbits

健康新西兰白兔20只,随机分为A、B 2组,A组内服单剂量30 mg/kg氟苯尼考试验品,B组肌注单剂量30mg/kg氟苯尼考试验品。用高效液相色谱法测定血浆中的药物浓度,3p97药代动力学程序软件处理药-时数据,A组药-时数据符合一室开放模型(W=1/C2),主要药代动力学参数:T1/2Ka=(0.461±0.066)h,T1/2ke=(2.013±0.195)h,Tpeak=(1.180±0.123)h,Cmax=(7.332±1.000)mg/L,AUC=(31.445±3.566)mg.L-1.h,V/F=(2.995±0.330)L/kg;B组药-时数据也符合一室开放模型(W=1/C2),主要药代动力学参数:T1/2Ka=(0.802±0.098)h,T1/2ke=(2.317±0.136)h,Tpeak=(1.805±0.103)h,Cmax=(6.646±0.578)mg/L,AUC=(38.714±3.727)mg.L-1.h,V/F=(2.772±0.303)L/kg。试验结果表明,氟苯尼考在家兔体内主要药动学特征为:内服吸收迅速、分布快而广、消除较快;肌注吸收速度显著慢于内服,分布广泛,消除也较快。

Twenty healthy New Zealand White rabbits were a11ocated into two groups of 10 rabbits each.The rabbits in group A were orally administrated with single dose of florfenico1 at 30 mg/kg.The rabbits in group B were intramuscularly injected with single dose of florfenico1 at 30 mg/kg too.The plasma concentration of florfenico1 was determined by HPLC.Pharmacokinetics parameters were calculated by 3p97 computer program.Concentration-time data relating to group A were best described by a one-compartment open model and main parameters were as fo11ows：T1/2Ka=（0.461±0.066） h,T1/2ke=（2.013±0.195） h,Tpeak=（1.180±0.123） h,Cmax=（7.332±1.000） mg/L,AUC=（31.445±3.566） mg·L^-1·h ,V/F=（2.995±0.330） L/kg;Data relating to group B were also charactered of a one-compartment open model and main parameters were as fo11ows：T1/2Ka=（0.802±0.098） h,T1/2ke=（2.317±0.136） h,Tpeak=（1.805±0.103） h,Cmax=（6.646±0.578） mg/L,AUC=（38.714±3.727） mg·L^-1·h,V/F=（2.772±0.303） L/kg.Results suggested that the pharmacokinetic characteristics of florfenicol after oral administration were rapid absorption,rapid and wide distribution,less rapid elimination in rabbits.After intramuscular administration of florfeni-col in rabbits,the speed of absorption was significantly lower than that of oral administration,the distribution was wide,and the elimination was also rapid.