盐酸莫西沙星片在健康人体的药动学研究

Pharmacokinetics of Moxifloxacin Hydrochloride Tablet in Healthy Volunteers

目的:研究盐酸莫西沙星片在中国健康人体内的药动学,为临床用药提供参考。方法:10名健康志愿者单剂量口服400 mg盐酸莫西沙星片后,HPLC-UV法测定血浆药物浓度,采用F检验结合AIC判断法进行房室模型判别,用DAS软件进行数据处理,采用房室模型法评估药动学参数。结果:最佳房室模型为二房室模型,主要药动学参数如下:C_(max)=(3.06±0.42)mg·L^(-1),t_(max)=(1.75±0.76)h,t_(1/2β)=(11.38±1.80)h,AUC_(0-t)=(32.45±6.48)mg·h·L^(-1),AUC_(0-∞)=(40.63±8.40)mg·h·L^(-1),V_(1/F)=(116.58±31.91)L,CL=(10.16±1.72)L·h^(-1)。除2例受试者出现可耐受的胃肠道不适外,无其他明显不良反应发生。结论:中国健康志愿者单剂量口服莫西沙星片后,耐受性良好,药动学参数与国外人体药动学参数基本一致,1日1次单次给药可迅速达到并维持有效血药浓度。

Objective： To study the pharmacokinetics of moxifloxacin tablet in Chinese healthy volunteers. Method： Ten healthy vol- unteers were orally administered a single dose of 400 mg moxifloxacin chloride tablet. The plasma concentration of moxifloxacin was determined by a validated HPLC-UV method. The best compartment model was judged by AIC criteria and F test. The data were processed with DAS software and assessed with compartment model to obtain the pharmacokinetic parameters. Result： The optimized compartment model was two-compartment model. The pharmacokinetic parameters were as follows ： Cmax （3. 06 ±0. 42 ） mg. L- 1, tmax= （ 1.75 ± 0. 76） h, t1/2β （ 11.38 ± 1.80） h,AUCo4（32. 45 ±6. 48） mg·h·L-1 ,AUCo（40. 63±8.40） mg·h·L-1 ,V1/F（ 116. 58 ±31.91 ） L,CL （ 10. 16 ± 1.72） L·h-1. Except for tolerable gastrointestinal discomfort in two volunteers ,no clinical significant changes were observed. Conclusion： Moxifloxacin tablet is well tolerated in Chinese healthy volunteers. The pharmacokinetic parameters are accordant with those from foreign popu-lations. Once-daily administration of 400mg moxifloxacin can acquire rapidly and maintain the effective plasma concentration.