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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。
To guide the rational use of marbofloxacin clinically in rabbits, a single dose intravenous injection of multiple doses of intramuscular injection of 2.5 mg / kg of mafenoxacin was used to determine plasma concentration by high performance liquid chromatography (HPLC). WinNonlin 5.2 Pharmacokinetics software analysis of drug-time data and Acs-lXtreme1.4 simulation of drug curve. The results showed that the data of rabbits intravenous injection of lefloxacin followed the two-compartment open model. The main pharmacokinetic parameters were: CL = 0.71L / (h · kg) ± 0.29L / (h · kg) , Vss = 1.16 L / kg ± 0.48 L / kg, t1 / 2 β = 1.69 h ± 1.09 h, MRT = 1.82 h ± 1.15 h. A single intramuscular injection of the drug curve in line with the first-absorption model of an open chamber, the last intramuscular injection at the end, the plasma concentration has reached steady-state. The main pharmacokinetic parameters of the whole steady-state process were: R = 1.18 ± 0.2, Cavg = 0.21μg / mL ± 0.05μg / mL, t1 / 2λz = 7.98h ± 5.02h, MRT = 6.77h ± 3.68h. The simulation results of multiple intramuscular injection procedures showed that the reproducibility of plasma drug concentration after each administration was good, and the simulated values were in good agreement with the experimental values. The above test results show that intramuscular injection of Marbofloxacin in rabbits quickly and completely absorbed, widely distributed, eliminate slowly.