莫西沙星在中国健康受试者体内的药代动力学研究  

Pharmcokinetics of moxifloxacin in Chinese healthy volunteers

作　　者：刘银萍[1] 秦玉花[1] 白楠[2] 唐铭婧[2] 王睿[2] 赵红伟[1] 

机构地区：[1]河南省人民医院药学部,郑州450003 [2]解放军总医院药物临床研究中心,北京100853

出　　处：《中国临床药理学杂志》2015年第13期1255-1257,共3页The Chinese Journal of Clinical Pharmacology

基　　金：国家科技部十二五重大专项基金资助项目(2012ZX09303004)

摘　　要：目的评价中国健康受试者连续4 d单剂量口服盐酸莫西沙星片400 mg的药代动力学。方法开放、随机、平行、单次、单周期试验设计。48名健康受试者,男女各半,单剂量口服盐酸莫西沙星片400 mg,连续4 d,用高效液相色谱串联质谱法测定血药浓度,用Win Nonlin 5.2.1程序计算药代动力学参数。结果有6例受试者中途退出,其余42名健康受试者口服莫西沙星后的主要药代动力学参数如下,t1/2为(11.71±3.53)h,Cmax为(0.51±0.19)×10-4ng·m L-1,tmax为(2.94±1.41)h,MRT0-24 h为(18.02±4.45)h,CLz/F为(0.84±0.75)×10-4m L·h-1,AUC0-24 h为(5.82±1.82)×10-4ng·m L-1·h。结论我国健康受试者口服莫西沙星血药浓度高、半衰期长、耐受性好,可参照国外剂量,并且服用同等剂量的莫西沙星时,女性的血药浓度比男性略高。Objective To study the pharmacokinetics of oral administration of moxifloxacin in Chinese healthy volunteers.Methods The study was designed as an open,randomized,parallel and single-dose cycle study.The volunteers were administered with a single dose of moxifloxacin 400 mg for consistent four days,respectively.The plasma concentrations of moxifloxacin were determined by LC-MS / MS method.The pharmacokinetic parameters of moxifloxacin were calculated by Win Nonlin 5.2.1 software.Results Six subjects quit from the study,and the main pharmacokinetic parameters of the remaining 42 subjects were as follows：t1 /2was（11.71 ± 3.53） h,Cmaxwas（0.51 ± 0.19） × 10-4ng·m L-1,tmaxwas（2.94 ± 1.41） h,MRT0-24 hwas（18.02 ± 4.45） h,CLz /F was（0.84 ± 0.75） × 10-4m L · h-1,AUC0-24 hwas（5.82 ± 1.82） × 10-4ng·m L-1·h.Conclusion The characteristics of oral moxifloxacin 400 mg has shown a high blood concentration,long half-life time and it can be well tolerated.The doses adopted in foreign study is recommended.There was a gender difference in volunteers when with same dose of moxifloxacin.

关 键 词：盐酸莫西沙星 高效液相色谱质谱联用法 药代动力学 

分 类 号：R978.1[医药卫生—药品] R969.6[医药卫生—药学]