甲磺酸帕珠沙星注射液单次给药在人体内的药物动力学研究

The pharmacokinetics of Pazufloxacin mesilate injection in healthy volunteers

目的建立测定甲磺酸帕珠沙星血浆药物浓度的HPLC-UV检测法,研究国产甲磺酸帕珠沙星氯化钠注射液在人体内的药物动力学。方法12名健康志愿受试者单次静滴甲磺酸帕珠沙星氯化钠注射液500 mg,以盐酸芦氟沙星为内标,测定血浆中帕珠沙星的浓度,用DAS 1.0软件处理经时血药浓度数据,计算主要药物动力学参数。结果单次静滴甲磺酸帕珠沙星氯化钠注射液500 mg后,于给药后0.50 h达到峰浓度9.83±2.52 mg.L-1,AUC0-t为18.99±4.15 mg.h.L-1,T1/2β为2.67±0.31 h,Cl/F和V/F分别为23.73±3.81 L.h-1和1.16±0.31 L.kg-1。结论单次静滴甲磺酸帕珠沙星氯化钠注射液的体内过程符合二室开放模型;除AUC外,男、女受试者的其余药动学参数比较,差异无统计学意义。

OBJECTIVE To develop an HPLC - UV method to determine Pazufloxacin mesilate in human plasma and study the pharmacokinetics profiles of domestic Pazufloxacin mesilate injections in healthy volunteers. METHODS A single dose of injection of domestic Pazufloxacin mesilate was given to 12 healty volunteers respectively. Pazufloxacin mesilate concentrations in plasma were determined by HPLC method. The pharmacokinetic pararaeters of Pazufloxacin mesilate were obtained by statistical analysis DAS 1.0.RESULTS The main pharmacokinetic parameters of single preparations were as follows： Cmax Was 9.83 ± 2.52 mg·L^-1, Tmax was 0.50 h, AUC0-tn Was 18.99±4. 15 mg·h·L^-1, T1/2β was 2.67±0.31 h,Cl/F was 23.73±3.81L·h^-1 and V/F was 1.16±0.31 L·kg^-1.CONCLUSION The procedure of single injection of Pazufloxacin mesilate in vivo followed two compartment model. There was no significant difference between male and female volunteers in pharmacokinetics parameters except AUC.