健康人体内甲磺酸加替沙星对茶碱稳态药代动力学的影响

Influence of Gatifloxacin on Pharmacokinetics of Theophylline at Steady State in Healthy Volunteers

目的:研究甲磺酸加替沙星对健康人体内茶碱稳态药代动力学的影响。方法:采用HPLC法测定健康人体单独给药和合并甲磺酸加替沙星给药后茶碱的血药浓度,采用3P97药动学软件处理,选用非参数法计算药动学参数,Cmax和Tmax为实测值,AUC采用梯形法计算曲线下积分面积。主要药动学参数采用SPSS11.5软件进行统计分析。结果:单用和合用甲磺酸加替沙星后,茶碱的药动学参数Cmax、t1/2、CL、AUC0-12、AUC0-∞之间有显著性差异(P<0.01)。Cmax明显下降,t1/2明显减小,AUC0-12与AUC0-∞明显下降。结论:甲磺酸加替沙星对健康人体内茶碱稳态药动学有影响,两者合用可能降低茶碱疗效,提示两药合用应监测茶碱的血药浓度。

Objective： To study the effect of gatifloxacin on pharmacokinetics of theophylline in healthy volunteers.Methods： The concentration of theophylline in plasma was detected by high performance liquid chromatography（HPLC） before and after gatifloxacin administration.Pharmacokinetic parameters were evaluated by the 3P97 pharmacokinetics program.Statistical analysis was performed with the SPSS11.5 software.Results： After theophylline was used alone and in combination with gatifloxacin,the pharmacokinetic processes were simulated using the statistical models.Pharmacokinetic parameters of the two occasions,Cmax,t1/2,CL,AUC0-12,AUC0-∞ had significant differences（P0.05）.Conclusion： Gatifloxacin may influence the pharmacokinetic parameters of theophylline in healthy volunteers.The concentration of theophylline in plasma should be monitored when theophylline and gatifloxacin are co-administered.