盐酸莫西沙星片的人体药动学研究

目的:研究盐酸莫西沙星片在我国健康人体内的药动学。方法:12名健康受试者单剂量口服盐酸莫西沙星片400mg后,采用高效液相色谱-紫外(HPLC-UV)法检测人血浆中莫西沙星的浓度,用DAS软件进行数据处理,采用非房室模型法评估药动学参数。结果:单剂量口服莫西沙星片400mg后,主要药动学参数分别为:AUC0～2(432.57±6.94)mg·h·L-1,AUC0～∞(40.55±8.71)mg·h·L-1,Cmax(3.06±0.42)mg·L-1,tmax(1.75±0.76)h,t1/(210.32±1.98)h,MRT0～2(48.55±0.30)h,MRT0～∞(14.59±2.32)h,V(d150.62±34.00)L,CLz/F(10.20±1.77)L·h-1。除2例有可耐受的胃肠道不适外,无明显不良反应发生。结论:建立的HPLC-UV法可用于莫西沙星药动学研究。我国健康志愿者口服莫西沙星具血药峰浓度高、半衰期长、耐受性好的特点,与国外人体药动学参数基本一致。

Pharmacokinetics of Moxifloxacin Hydrochloride Tablets in Healthy Volunteers

OBJECTIVE： To study the pharmacokinetics of moxifloxacin hydrochloride tablet in healthy volunteers. METHODS： 12 healthy volunteers were orally administered with a single dose of 400 mg moxifloxacin hydrochloride tablet. The plasma concentrations of moxifloxacin in human plasma were measured by HPLC-UV method. The data were processed with DAS software and non-compartment model was used to evaluate pharmacokinetic parameters. RESULTS： After giving single dose of 400 mg moxifloxacin hydrochloride tablet, main pharmacokinetic parameters were as follows： AUC0-24（32.57±6.94）mg·h·L^-1,AUC0-∞（40.55±8.71）mg·h·L^-1,Cmax（3.06±0.42）mg·L^-1,tmax（1.75±0.76）h,t1/2（10.32±1.98）h,MRT0-24（8.55±0.30）h,MRT0-∞（14.59±2.32）h,Vd（150.62±34.00）L,CL2/F（10.20±1.77）L·h^-1. No significant ADR was observed, except for tolerable gastrointestinal discomfort in 2 cases. CONCLUSION： The established HPLC-UV method could be used for the pharmacokinetic study of moxifloxacin. Moxifloxacin after oral administration is well tolerable in Chinese healthy volunteers and its pharmacokinetics was characterized with high peak concentration and long half-life. The pharmacokinetic parameters obtained from Chinese healthy volunteers are accordant with those from foreign populations.