单剂量和多剂量巴洛沙星片在健康人体内的药动学特征

Pharmacokinetics of balofloxacin in healthy volunteers after a single dose and multi-dose administration

目的研究巴洛沙星片在10名健康志愿者体内的药动学特征。方法5名男性、5名女性健康志愿者单剂量和多剂量口服巴洛沙星片100 mg,采用Waters OASISTMHLB固相萃取小柱提取样品,反相高效液相色谱法测定血药浓度。结果主要药动学参数:单剂量为女t1/2(7．26±2．02)h、ρmax(1 229．93±419．98)μg·L-1、AUC0→48(10 031．56±2 856．78)μg·h·L-1;男t1/2(10．21±1．93)h、ρmax(989．37±219．62)μg·L-1、AUC0→48(9 783．05±879．95)μg·h·L-1。多剂量为女t1/2(8．53±1．84)h,ρav (690．28±150．0)μg·L-1,AUCss(8 283．30±1 800．08)μg·h·L-1,DF(1．68±0．68);男t1/2(8．72±1．23)h、ρav(784．74±82．62)μg·L-1、AUCss(9 416．93±991．41)μg·h·L-1、DF(1．19±0．15)。结论用DAS 2．0软件进行房室模型拟合,巴洛沙星体内过程符合一级消除二室模型,每次100mg,bid连续5 d,可达到稳定有效血药浓度。

AIM To study the pharmacokinetics of balofloxacin in 10 healthy volunteers（5 males,5 females）. METHODS A single dose and multi-dose administration of 100 mg balofloxaein were given to 10 healthy volunteers. The concentrations in plasma were determined by HPLC method. RESULTS The main pharmaeokinetie parameters were as follows： t1/2 （7.26 ± 2.02）h,ρmax（1 229.93 ± 419.98）μg·L^-1 ,AUC0→48（10 031.56±2 856.78）μg·h·L^-1 for females in single dose; t1/2（10.21 ± 1.93）h,ρmax（989.37 ± 219.62）μg·L^-1 ,AUC0→48（9 783.05 ± 879.95）μg·h·L^-1 for males in single dese. t1/2（8.53 ± 1.84）h, ρav（690.28 ± 150.0）μg·L^-1,AUC,（8 283.30± 1 800.08）μg·h·L^-1, DF （1.68 ± 0.68） for females in multi-doses; t1/2 （8.72 ± 1.23） h,ρav （？84.74 ± 82.62） μg·L^-1, AUC, （9 416.93 ± 991.41）μg·h·L^-1,DF（ 1.19± 0.15） for males in multi-doses. CONCLUSION The pharmacokinetic parameters are determined by DAS 2.0 program. The results show that it is fit for two eompamnent model in vivo after oral administration of 100 nag balofloxaein tablets. The effective and stable drug eoneentration in vivo could achieved after a dose of 100 nag balotlaeine, bid for 5 d.