甲磺酸帕珠沙星与其它抗生素联用于大鼠模型的药动学研究

Comparison on pharmacokinetics of pazufloxacin mesilate co-administered with cefoperazone sulbactam sodium or azithromycin in rats

目的:对甲磺酸帕珠沙星与其它抗生素联合应用的大鼠药代动力学进行对比研究,评价药物间的相互作用及联合用药的合理性。方法:采用一个剂量组,3种用药方案分别单次给药。用药方案:帕珠沙星45 mg/kg;帕珠沙星45 mg/kg加头孢哌酮/舒巴坦180 mg/kg;帕珠沙星45 mg/kg加阿奇霉素45 mg/kg。采用反相HPLC-UV法测定大鼠血药浓度,用DAS软件估算药动学参数,进行统计学分析及临床药效评价。结果:甲磺酸帕珠沙星单用及与头孢哌酮/舒巴坦或阿奇霉素联用的主要药动学参数t1/2、Cmax、tmax、AUC无显著性差异,但帕珠沙星与阿奇霉素联用后清除率(CL)降低及体内驻留时间(MRT)延长,具有统计学意义。结论:帕珠沙星与头孢哌酮/舒巴坦,帕珠沙星与阿奇霉素联用是可行的用药方案。

Objective ：To estimate the results of coadministered drug interaction, the effects of cefoperazone sulbactam sodium and azithromycin separately on the pharmacokinetics of pazufloxacin （PZFX） mesilate in rats were studied. Method： There are three dosage regimens group to administrate rats separately as follow： （i） the control group, PZFX administered at a dose of 45mg/kg through tail vein, （ii） PZFX 45 mg/kg and cefoperazone sulbactam sodium （CPZ/SBT） 180 mg/kg, （ iii ） the PZFX 45 mg/kg and azithromycin （AZM） 45 mg/kg. The plasma concentrations were measured by reversed phase HPLC-UV. Result： There is no distinct difference in t1/2, Cmax tmax and AUC between control group and the coadministrate groups of PZFX. But there is statistical significance in decrease of CL and prolonged MRT when combined using PZFX and azithromycin. Conclusion： Co-adminlstrating PZFX with cefoperazone sulbactam sodium or azithromycin is available and rationally therapeutic regimens.