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目的:研究妥舒沙星对家兔氨茶碱药动学的影响。方法:将18只家兔随机等分为A、B、C三组,A组经耳缘iv给予单剂量氨茶碱12．5 mg·kg-1;B、C两组家兔分别灌服妥舒沙星(每日300 mg·kg-1及450 mg·kg-1,分3次灌服),共服3 d,于第4天灌服妥舒沙星1 h后,iv与A组相同剂量的氨茶碱。结果:A、B、C三组的K分别为:0．1753,0．1341,0．1280 h-1;t1/2: 3．847,4．885,5．766 h;Vd:0．543,0．534,0．524 L;CL:0．0979,0．0759,0．0630 L·h-1;AUC:125．4,167．9,200．2μg·h·ml-1。结论:妥舒沙星使茶碱的K降低,t1/2延长,AUC增大,CL下降,对茶碱代谢的影响呈剂量依赖性。临床上妥舒沙星与氨茶碱合用时应监测茶碱的血药浓度,及时调整氨茶碱的剂量,以免引起氨茶碱中毒。
Objective: To study the effect of tosufloxacin on aminophylline pharmacokinetics in rabbits. Methods: Eighteen rabbits were randomly divided into three groups (A, B and C). Group A received a single dose of aminophylline 12.5 mg · kg-1 via ear margin iv; rabbits in groups B and C were fed Tosufloxacin (300 mg · kg-1 and 450 mg · kg-1, 3 times a day) for 3 days, tosufloxacin 1 h on the 4th day, iv and A The same dose of aminophylline. Results: The K of three groups of A, B and C were: 0.1753,0.1341,0.1280 h-1; t1 / 2: 3.847,4.885,5.766 h; Vd: 0. 543, 0.534, 0.524 L; CL: 0.0979, 0.0759, 0.0630 L · h -1; AUC: 125.4, 167.9, 200.2 μg · h · ml -1. CONCLUSION: Toshusarcosine reduced the K of theophylline, prolonged t1 / 2, increased AUC and decreased CL, which showed a dose-dependent effect on theophylline metabolism. Clinic tosufloxacin and aminophylline should monitor the serum concentration of theophylline, and timely adjustment of the dose of aminophylline, so as not to cause aminophylline poisoning.