甲磺酸帕珠沙星注射液人体药动学研究_药学论文.docVIP

甲磺酸帕珠沙星注射液人体药动学研究_药学论文 甲磺酸帕珠沙星注射液人体药动学研究_药学论文 作者：沈奇 梁德荣 苗佳 余勤 梁茂植 徐楠 郑莉 罗柱 吴松泽【摘要】 目的 研究单次及多次静脉滴注甲磺酸帕珠沙星注射液的药动学特点。方法 筛选健康受试者12名，q12h静脉滴注甲磺酸帕珠沙星注射液每次500mg，连续5d，共9次；用反向高效液相色谱紫外法测定血药浓度，用DASver1.0软件拟合药动学参数。结果 受试者静脉滴注甲磺酸帕珠沙星注射液后体内过程符合二室模型；单次给药后的药动学参数：Tmax为(0.47±0.09)h，cmax为(13.71±1.81)mg/L，AUC0-t为(24.60±4.15)mg·h/L，t1/2为(1.46±0.64)h，MRT、CL和Vd分别为(2.14±0.33)h、(0.09±0.04)L/(h·kg)和(0.17±0.03)L/kg。q12h静脉滴注帕珠沙星500mg连续5d(共9次)，第2、3、4、5d晨测得谷浓度分别为0.13、0.16、0.17和0.14mg/L，提示血药浓度已达稳态。末剂给药后的药动学参数：Tmax为(0.48±0.10)h，cmax为(15.41±1.67)mg/L，AUC0-t为(28.42±4.90)mg·h/L，t1/2为(1.33±0.49)h，CL为(0.09±0.06L/)h，(css)av为(2.34±0.43)mg/L，DF为(99.48±0.38)%，以上参数与单次给药比较除cmax外均无统计学差异，且累积系数小，说明本品多次给药无体内蓄积。女性和男性受试者主要药动学参数比较均无统计学差异。受试者给药期间未出现严重不良反应。结论 500mg q12h静脉滴注，在人体内可达到有效血药浓度，可以作为临床应用的推荐方案。 【关键词】 甲磺酸帕珠沙星； 反向高效液相色谱紫外法； 药动学 　　Study on pharmacokinetics of pazufloxacin mesylate injection　in healthy volunteers 　　ABSTRACT Objective To investigate the pharmacokinetics of pazufloxacin mesylate injection after single and multiplenteers were administrated 500mg pazufloxacin mesylate twice a day for 5 days. The plasma concentrations were determined by RPHPLCUV method and the pharmacokinetic parameters were calculated by DASver1.0 software. Results The pharmacokinetics of pazufloxacin is fit to two compartment model. The pharmacokinetic parameters after single administration: Tmax was (0.47±0.09)h, cmax was (13.71±1.81)mg/L, AUC0-t was (24.60±4.15)mg·h/L, t1/2 was (1.46±0.64)h, MRT was (2.14±0.33)h, CL was (0.09±0.04)L/(h·kg) and Vd was (0.17±0.03)L/kg. The pharmacokinetic parameters after successive administration: Tmax was (0.48±0.10)h, cmax was (15.41±1.67)mg/L, AUC0-t was (8.42±4.90)mg·h/L, t1/2 was (1.33±0.49)h, CL was (0.09±0.06)L/h, (css)av was (2.34±0.43)mg/L, DF was (99.48±0.38)%. There were no significant differences in all pharmacokinetic parameters except cmax between the first and the last administraion of pazufloxacin and cumulation coefficient was very small. It suggested that there was no accumulati