摘要
为科学指导麻保沙星在家兔临床上的合理使用,采用单剂量静脉注射、多剂量肌肉注射麻保沙星2.5mg/kg,用高效液相色谱法测定血药浓度,通过WinNonlin 5.2药代动力学软件分析药时数据并用Acs-lXtreme1.4对药时曲线进行仿真模拟。结果显示,家兔静脉注射麻保沙星后药时数据符合二室开放模型,主要的药代动力学参数分别为:CL=0.71L/(h·kg)±0.29L/(h·kg),Vss=1.16L/kg±0.48L/kg,t1/2β=1.69h±1.09h,MRT=1.82h±1.15h。单次肌肉注射给药的药时曲线符合一级吸收一室开放模型,最后一次肌肉注射给药结束时,血药浓度已达到稳态。整个稳态过程的主要药代动力学参数为:R=1.18±0.2,Cavg=0.21μg/mL±0.05μg/mL,t1/2λz=7.98h±5.02h,MRT=6.77h±3.68h。多次肌肉注射过程的仿真模拟结果显示,每次给药后血浆药物浓度的重现性较好,模拟值与试验值吻合度高。上述试验结果表明,肌肉注射麻保沙星在家兔体内吸收迅速而完全,分布广泛,消除缓慢。
The pharmacokinetics of marbofloxacin was investigated after single intravenous（IV） administration and being repeated intramuscular（IM）administration for reasonable usage of marbofloxacin in rabbits,both at a dose of 2.5mg/kg BW,in six healthy domestic rabbits.The marbofloxacin concentration in plasma was determined by high performance liquid chromatography.The data were analyzed with the pharmacokinetics software WinNonlin 5.2and simulated the concentration-time course by AcslXtreme.In results,the concentration-time course of marbofloxacin after single IV administration fitted a two-compartment open model.The main pharmacokinetics parameters were as follows：CL=0.71L/（h·kg）±0.29 L/（h·kg）,Vss=1.16L/kg±0.48L/kg,t1/2β=1.69h±1.09h,MRT=1.82h±1.15h.After the first IM administration,the concentration-time course was described by a one-compartment open model with first-order absorption.Plasma concentration of marbofloxacin was at steady state after the last IM administration.The main pharmacokinetics parameters of the last dose were as follows：R=1.18±0.2,Cavg=0.21 μg/mL±0.05μg/mL,t1/2λz=7.98h±5.02h,MRT=6.77h±3.68h.Repeated intramuscular injection process simulation results show each drug concentration in plasma after administration was well reproduci- ble and better agreement with the test value.In conclusion,marbofloxacin in rabbits after IM administration was rapidly and completely absorbed,widely distributed,and slowly eliminated.
出处
《中国兽医科学》
CAS
CSCD
北大核心
2010年第10期1072-1075,共4页
Chinese Veterinary Science
