Drusano G L, Standiford H C, Bustamante C I, Forrest A, Rivera G, Tatem B, Schimpff S C
Eur J Clin Microbiol. 1984 Oct;3(5):468-70. doi: 10.1007/BF02017377.
The plasma pharmacokinetics of imipenem, a beta-lactam antibiotic of the new class of carbapenems, was evaluated by administering 1 g imipenem plus 1 g of the dehydropeptidase inhibitor cilastatin to six healthy male volunteers over 30 min. Subsequently intensive plasma sampling was done for 5.5 h. The volume of distribution of the central compartment was 0.16 +/- 0.04 1/kg; the volume of distribution (area) was 0.28 +/- 0.07 1/kg; the volume of distribution (steady state) was 0.23 +/- 0.03 1/kg. The mean plasma clearance was 10.1 +/- 1.0 1/h/1.73 m2. Model-independent analysis showed excellent agreement with these values. The terminal excretion half-life was short (1.3 +/- 0.4 h). For approximately 6 h after administration, the observed plasma levels were above those required to inhibit most nosocomial pathogens in vitro.
通过在30分钟内给6名健康男性志愿者静脉注射1克亚胺培南加1克脱氢肽酶抑制剂西司他丁，评估了新型碳青霉烯类β-内酰胺抗生素亚胺培南的血浆药代动力学。随后进行了5.5小时的密集血浆采样。中央室的分布容积为0.16±0.04升/千克；分布容积（面积）为0.28±0.07升/千克；分布容积（稳态）为0.23±0.03升/千克。平均血浆清除率为10.1±1.0升/小时/1.73平方米。非模型分析显示与这些值高度一致。终末排泄半衰期较短（1.3±0.4小时）。给药后约6小时内，观察到的血浆水平高于体外抑制大多数医院病原体所需的水平。
