甲磺酸帕珠沙星氯化钠注射液在健康人体的药代动力学

Parmacokinetics of pazufloxacin mesilate sodium chloride injection in Chinese healthy volunteers

目的研究甲磺酸帕珠沙星氯化钠注射液在健康人体的药代动力学。方法8名健康受试者单次静脉滴注甲磺酸帕珠沙星300,600mg后,用高效液相色谱法测定体内帕珠沙星的血药浓度,用DAS统计软件进行数据处理。结果结果符合一级消除药代动力学的二室模型,300,600mg2个剂量组的药代动力学参数:Cmax分别为(7.38±0.85),(18.36±2.39)mg·L-1;AUC0-t分别为(31.34±5.67),79.20±18.43)mg·h·L-1;t1/2β分别为(1.63±0.31),(1.71±0.21)h;CL/F分别为(0.10±0.02),(0.08±0.01)L·kg·h-1,V/F分别为(0.23±0.03),(0.19±0.05)L·kg-1。24h尿药累积排泄率分别为(92.2±2.6)%和(93.2±3.0)%。结论甲磺酸帕珠沙星每日给药300mg,每日2次,可达到有效治疗浓度,在600mg内可安全耐受。

Objective To investigate the pharmacokinetics of pazufloxacin mesilate sodium chloride injection in Chinese healthy volunteers. Methods Eight healthy volunteers were divided into 2 groups randomly by latin me-thod. The serum samples collected from the volunteers after injecting 300, 600 mg pazufloxacin mesilate sodium chloride injection respectively by turns were determined by the HPLC method. The serum concentration were determined by the accompanity pazufloxacin-serum concentration standard curve and the pharmacokinetic paraments were calculated by DAS sofeware. Results The following pharmacokinetic parameters were obtained:C max were (7.38± 0.85)and (18.36±2.39)mg·L -1, AUC 0-t were (31.34± 5.67)and (79.20±18.43)mg·h ·L -1, t 1/2β were (1.63±0.31)and (1.71±0.21)h,CL/F were (0.10±0.02)and(0.08± 0.01)L·kg·h -1, V/F were (0.23±0.03)and (0.19±0.05)L·kg -1.Conclusion The results indicated that the injection can be given 600 mg safely.