罗红霉素对兔体内稳态时氨茶碱药代动力学的影响

目的　观察 6只新西兰白兔灌服罗红霉素前后对氨茶碱稳态血药浓度及药代动力学的影响。方法　实验分二期 :Ⅰ期为d 1～ 4单独灌服氨茶碱至稳态 ;Ⅱ期为d 5～ 10合用罗红霉素与氨茶碱 ,血药浓度采用HPLC法测定。结果　各期测得氨茶碱药代动力学参数 ,与Ⅰ期比较 ,Ⅱ期的AUC、CL/Fs、Ka、Ke、T1/ 2 (ka) 、Tmax差异有显著性 (P <0 0 5 ,P <0 0 1) ,而Cmax、V/Fc、T1/ 2 (ke) 在两期间差异均无显著性(P >0 0 5 )。结论　长期合用罗红霉素和氨茶碱 ,罗红霉素能延缓氨茶碱在兔体内稳态时的吸收和消除 ,提示合并用药时应对氨茶碱进行临床给药监测。

Effect of roxithromycin on pharmacokinetics of aminophylline at steady state

AIM To investigate the effect of oral roxithromycin on serum concentrations at steady state and its pharmacokinetics of aminophylline in New Zealand rabbits. METHODS The experiment was divided into 2 stages: (Ⅰ) The subjects only received a four-day course of oral aminophylline until steady-state; (Ⅱ) aminophylline and roxithromycin were coadministrated from the d 5～10. After the last dose of aminophylline at the end of each study stage, serum theophylline concentrations were determined with HPLC. RESULTS Compared to stage Ⅰ, AUC、CL/Fs、 K a、 K e、 T 1/2(ka) 、 T max had significantly changed or very significantly changed at stage Ⅱ ( P <0 05, P <0 01), and there was no significant variation in modification of other pharmacokinetics parameters. CONCLUSION It is necessary to change the therapeutic dose of aminophylline when the drug is taken with roxithromycin.