氨溴索对罗红霉素血药浓度及药动学参数的影响

Effect of Ambroxol on Plasma Concentration and Pharmacokinetic Parameters of Roxithromycin

目的:研究氨溴索与罗红霉素合用时,氨溴索对罗红霉素血药浓度及药动学参数的影响。方法:24名健康男性志愿者,采用双周期交叉试验设计,交叉服用罗红霉素片、罗红霉素片加氨溴索片,服药后在不同时间点抽取静脉血,采用液-质联用(LC-MS)法测定血药浓度,计算药动学参数并将罗红霉素的药动学参数进行方差分析,以90%可信区间判定药物是否发生相互作用。结果:罗红霉素单用与合用氨溴索后的药动学参数分别为:tma(x1.67±0.32)、(1.67±0.41)h,Cma(x10.26±2.82)、(10.86±3.19)mg.L-1,AUC0～7(2110.19±35.18)、(113.42±38.72)mg.h.L-1,AUC0～∞(111.70±36.23)、(115.04±39.98)mg.h.L-1。结论:氨溴索对人体内罗红霉素的血药浓度和药动学参数无影响。

OBJECTIVE：To evaluate the effect of ambroxol on plasma concentration and pharmacokinetic parameters of roxithromycin when healthy volunteers received roxithromycin and ambroxol. METHODS： In double-period cross-over experiment, 24 healthy male volunteers received roxithromycin tablets or roxithromycin tablets combined with ambroxol tablets. Serial venous blood samples were collected at different time points after drug administration. Plasma concentrations of roxithromycin were measured by LC-MS. The pharmacokinetic parameters of roxithromycin were calculated and analyzed by variance analysis. Drug interaction was detected by 90% confidence interval. RESULTS： Main pharmacokinetic parameters of roxithromycin tablets and drug combination were as follows： tmax（1.67±0.32）h vs. （1.67±0.41）h; Cmax（10.26±2.82） mg·L-1 vs. （10.86±3.19） mg·L-1; AUC0～72（110.19±35.18） mg·h·L-1 vs. （113.42±38.72）mg·h·L-1; AUC0～∞（111.70±36.23） mg·h·L-1 vs. （115.04±39.98） mg·h·L-1. CONCLUSION：？ Ambroxol has no effect on the plasma concentration and pharmacokinetics of roxithromycin in healthy volunteers.