高效液相色谱法测定人血浆中比阿培南的浓度及其药动学

目的研究比阿培南在健康受试者体内的药动学过程。方法20名健康受试者(男女各10名)随机分为2组,分别单剂量(0.3 g)和多剂量(0.3 g×9)静脉滴注(静滴)比阿培南后,采用高效液相色谱法测定血浆中比阿培南浓度。用DAS(ver 2.0.1)药动学软件进行房室模型判断并计算药动学参数。结果比阿培南的体内经时过程符合二房室模型,单剂量和多剂量静滴比阿培南后,t_(1/2)分别为(1.04±s 0.09)和(1.03±0.11)h;c_(max)分别为(18±4)和(16.1±2.9)mg·L~(-1);A UC_(0～6)分别为(26±5)和(24±4)mg·h·L~(-1);多剂量c_(as-cav)为(2.0±0.3)mg·L~(-1),c_(as-min)为0 mg·L~(-1)。结论比阿培南的体内经时过程符合二房室模型,每日2次,连续静滴比阿培南9次后,体内药物没有蓄积。

Pharmacokinetics and serum concentration of biapenem in healthy volunteers

AIM To investigate the pharmacokinetics process of biapenem following a single and multiple doses intravenous administration in healthy volunteers.METHODS Twenty healthy volunteers(10 males,10 females)were divided into two groups randomly,and received a single dose(0.3 g,iv,gtt)and multi-dose (0.3 g×9,iv,gtt)of biapenem drip infusion.Blood samples of 3 mL each time individually were collected from anteeubital vein at certain planned times.Biapenem concentration in plasma was determined by HPLC method,and the pharmacokinetic parameters were calculated and determined by DAS software.RESULTS The intracorporeal passing process of biapenem coincided with two-compartment mode.The single dose and multi-dose pharmacokinetic parameters were as follows:t_(1/2)(1.04±s 0.09)and(1.03±0.11)h,c_(max)(18±4)and(16.1±2.9)mg·L~(-1),AUC_(0-6)(26±5)and(24±4)mg·h·L~(-1),respectively.The multi-dose c_(as-cav) was(2.0±0.3)mg·L~(-1).CONCLUSION The plasma concentration-time curves of biapenem were fitted to a two-compartment mode with no accumulations in vivo after multi-dose infusion(0.3 g×9,iv,gtt).