巴洛沙星片在健康人体内的药动学

目的:研究中国健康志愿者单次和多次口服巴洛沙星片的药动学。方法:12名健康志愿者,男女各半,单次给药试验口服(100 mg、200 mg、400 mg)3个剂量,多次给药试验口服剂量为每次200 mg,每日1次,连续5 d。采用高效液相色谱-紫外检测法测定巴洛沙星血药浓度,用DAS 2.0软件计算药动学参数。结果:主要药动学参数如下,单剂量(100 mg)c_(max)(1.42±s 0.25)mg·L~(-1),t_(max)(0.8±0.4)h,t_(1/2)(7.4±2.7)h,AUC_(0～∞)(9.8±1.7)mg·h·L~(-1);单剂量(200 mg)c_(max)(2.9±0.6)mg·L~(-1),t_(max)(0.9±0.4)h,t_(1/2)(7.2±1.1)h,AUC_(0～∞)(21±3)mg·h·L~(-1);单剂量(400 mg)c_(max)(5.6±1.4)mg·L~(-1),t_(max)(1.2±0.4)h,t_(1/2)(8.4±2.2)h,AUC_(0～∞)(44±12)mg·h·L~(-1)。多剂量c_(max)(2.9±0.8)mg·L~(-1),t_(max)(0.83±0.19)h,t_(1/2)(8.2±2.0)h,AUC_(0～∞)(21±5)mg·h·L~(-1),FI(93.7±1.4)%。结论:巴洛沙星在人体内符合二室模型,一级动力学过程。

Pharmacokinetics of balofloxacin tablets in healthy volunteers

AIM:To study the pharmacokinetics of balofloxacin tablets alter single or multiple doses orally taken in Chinese healthy volunteers.METHODS:Twelve Chinese healthy volunteers (6 males,6 females) were given single splitting of oral doses of 100 mg,200 mg,400 mg and multiple oral doses (200 mg daily for 5 days) of balofloxacin tablets.The concentrations of balofloxacin in plasma were measured by HPLC-UV and the pharmacokinetic parameters were calculated by DAS 2.0 software.RESULTS:The main pharmacokinetic parameters of balofloxacin tablet as splitting single orally taken doses for 100 mg,200 mg and 400 mg were c_(max) (1.42±s0.25),(2.9±0.6) and (5.6±1.4) mg·L~(-1);t_(max) (0.8±0.4),(0.9±0.4) and (1.2±0.4) h;t_(1/2) (7.4±2.7),(7.2±1.1) and (8.4±2.2) h;AUC_(0-∞) (9.8±1.7),(21±3) and (44±12) mg·h·L~(-1), respectively.Those for multiple orally taken dose were c_(max) (2.9±0.8) mg·L~(-1),t_(max) (0.83±0.19) h,t_(1/2) (8.2±2.0) h,AUC_(0-∞) (21±5) mg·h·L~(-1) and FI (93.7±1.4)%.CONCLUSION:The plasma concententration-time data of balofloxacin in human being coincide with a two compartment model and a first order kinetic processes in disposition in Chinese volunteers.