甲磺酸帕珠沙星与替硝唑在家兔体内的药动学相互作用研究  

Pharmacokinetic Interaction of Pazufloxacin Mesilate and Tinidazole in Rabbits

作　　者：黄品芳[1] 王长连[1] 刘亦伟[1] 郭晓卫[2] 

机构地区：[1]福建医科大学附属第一医院药学部,福州市350005 [2]福建医科大学,福州市350005

出　　处：《中国药房》2007年第22期1697-1699,共3页China Pharmacy

摘　　要：目的:研究甲磺酸帕珠沙星(PZFX)和替硝唑(TNZ)联用在家兔体内的药动学变化。方法:采用高效液相色谱法测定家兔给药后不同时间PZFX和TNZ血药浓度。药-时数据用3p87程序拟合,计算药动学参数。结果:2药单用与合用时的体内过程均呈二室模型,药-时曲线形态基本一致。PZFX联用TNZ前、后的AUC分别为(620±82.2)、(570±107.9)mg.min.L-1,TNZ联用PZFX前、后的AUC分别为(5507±1013)、(5086±1197)mg.min.L-1;PZFX联用TNZ前、后的t1/2α分别为(7.2±1.4)、(9.9±3.0)min,TNZ联用PZFX前、后的t1/2α分别为(30.5±4.3)、(43.5±5.0)min;PZFX联用TNZ前、后的血浆清除率(CL)分别为(1.4±0.2)、(1.5±0.2)L.h-1,TNZ联用PZFX前、后的CL分别为(0.4±0.1)、(0.5±0.1)L.h-1。2药合用后PZFX可使TNZ的α值增加、t1/2α稍延长,但其余药动学参数比较均无显著性差异(P>0.05)。结论:PZFX与TNZ合用后体内过程未发现明显变化,提示可联合用药,但PZFX有延缓TNZ分布迹象,可能使TNZ起效滞后。OBJECTIVE： To study the pharmacokinetic changes of pazufloxacin mesilate （PZFX） and tinidazole （TNZ） and their pharmacokinetic interaction in rabbits. METHODS ： Concentrations of Pazufloxacin mesilate and Tinidazole in plasma at different time after administration were determined by HPLC. The fitting of concentration - time data were performed with 3P87 program, and the pharmacokinetic parameters were computed as well. RESULTS： The concentration time curves of PZFX and TNZ used either alone or in combination fitted two- compartment model, and the pharmacokinetic feature of which were similar on the whole. The AUC, t1/2a, and CL of PZFX before vs. after combination with TNZ were （620± 82.2） vs. （570±107.9）mg· min·L^-1, （7.2±1.4）vs. （9.9±3.0）min, （1.4±0.2）vs. （1.5_＋0.2）L· h^-1 respectively; and the AUC, tl/2a, and CL of tinidazole before vs. after combination with PZFX were （5 507± 1 013） vs. （5 086±1 197） mg · min · L^-1, （30.5±4.3）vs. （43.5±5.0）min, and （0.4±0.1） vs. （0.5±0.1）L·h^-1, respectively. The tl/2a was longer and α valuewas higher for tinidazole when used concomitantly with PZFX than used alone, however, there were no significant differences for all the other pharmacokinetic parameters （P 〉 0.05） . CONCLUSION： There was no marked change in the pharmacokinetic process in vivo when PZFX and TNZ were used concomitantly, suggesting that the two drugs can be used in combination. But PZFX could delay distribution of TNZ, which may delay the onset time of initial dose of TNZ.

关 键 词：甲磺酸帕珠沙星 替硝唑 药动学 相互作用 高效液相色谱 

分 类 号：R969.1[医药卫生—药理学] R969.2[医药卫生—药学]