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目的研究中国健康受试者单剂量静滴比阿培南后的药动学过程。方法30名健康受试者(男性15名,女性15名)按体重指数和性别随机分为3组,单剂量(0.15,0.3,0.6g)静滴比阿培南后,于不同时间分别从受试者肘静脉取血3mL,离心分离血浆,采用高效液相色谱法测定血浆中比阿培南浓度。用DAS(ver2.0.1)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,静滴低、中、高3个剂量比阿培南后的t1/2分别为(1.08±0.21),(1.04±0.09)和(1.12±0.08)h;ρmax分别为(8.02±0.94),(17.84±4.32)和(35.77±5.86)mg·L-1;AUC0-6h分别为(13.05±1.89),(26.33±4.93)和(52.02±8.55)mg·h·L-1;ρmax和AUC0-6h与给药剂量呈正相关,回归方程分别为ρmax=0.0614X-0.9505,r=0.9436(P<0.001)和AUC0-6h=0.0865X-0.2090,r=0.9467(P<0.001)。结论健康人单剂量静滴0.15,0.3和0.6g比阿培南后,体内药动学呈二房室模型,比阿培南在0.15~0.6g内药物呈一级消除动力学,ρmax和AUC与给药剂量线性相关;男、女性受试者静滴注射用比阿培南后的体内药动学过程无明显差异。
Objective To study the pharmacokinetics of single-dose biapenem in healthy Chinese subjects. Methods Thirty healthy subjects (15 males and 15 females) were randomly divided into 3 groups according to body mass index and sex. After a single dose of 0.15, 0.3 and 0.6 g intravenous infusion of biapenem, Subjects elbow venous blood 3mL, centrifuged plasma, using high performance liquid chromatography determination of plasma concentration of biapenem. DAS (ver2.0.1) pharmacokinetic software was used to determine the atrioventricular model and calculate pharmacokinetic parameters. RESULTS Biapenem had a two-compartment model in time-dependent manner, with t1 / 2 at low, middle and high doses of biapenem (1.08 ± 0.21), (1.04 ± 0.09) and (1.12 ± 0.08) h and (ρmax) were (8.02 ± 0.94), (17.84 ± 4.32) and (35.77 ± 5.86) mg · L -1, respectively; AUC0-6h were (13.05 ± 1.89), (26.33 ± 4.93) and ± 8.55) mg · h · L-1; ρmax and AUC0-6h were positively correlated with the dose, the regression equation was ρmax = 0.0614X-0.9505, r = 0.9436 (P <0.001) and AUC0-6h = 0.0865X- 0.2090, r = 0.9467 (P <0.001). Conclusion After single dose of 0.15, 0.3 and 0.6 g biapenem, the pharmacokinetics of the two drugs in vivo showed a two-compartment model. The first order elimination kinetics of biapenem in the range of 0.15-0.6 g, ρmax and AUC and There was no significant difference in the pharmacokinetics of biapenem between male and female subjects after intravenous injection of biapenem.