Arrigucci Silvia, Garcea Alessandro, Fallani Stefania, Cassetta Maria Iris, Canonico Giuseppe, Tonelli Francesco, Mazzei Teresita, Novelli Andrea
Department of Pharmacology, University of Florence, Firenze, Italy.
Int J Antimicrob Agents. 2009 Apr;33(4):371-3. doi: 10.1016/j.ijantimicag.2008.09.015. Epub 2008 Dec 20.
Ertapenem, a novel carbapenem, is approved for the treatment of mild to severe intra-abdominal infections (IAIs), although its in vivo concentrations in peritoneal fluid are unknown. The purpose of this study was to determine the peritoneal fluid concentration of ertapenem after a single 1 g intravenous dose. After informed consent, 21 patients (9 females and 12 males; mean+/-standard deviation (S.D.) age 50.2+/-17.7 years) requiring intra-abdominal surgery were enrolled. Plasma and peritoneal fluid samples were taken at fixed times during surgery. Drug concentrations were determined by high-performance liquid chromatography (HPLC) with ultraviolet detection. Mean+/-S.D. ertapenem peritoneal fluid concentrations were 64.3+/-23.4 mg/L at 1h and 31.3+/-26.5 mg/L at 3 h after administration. The mean tissue/plasma ratio ranged from 46.7% to 83.1%. The mean peritoneal fluid concentrations were well above the MIC(90) (minimum inhibitory concentration for 90% of the organisms) for susceptible bacteria found in IAIs, especially Escherichia coli, viridans streptococci, Enterobacteriaceae, Klebsiella spp. and Bacteroides fragilis, during the entire sampling time. These pharmacokinetic results support the assumption that ertapenem might be suitable for the treatment of IAIs.
厄他培南是一种新型碳青霉烯类抗生素，已被批准用于治疗轻至重度腹腔内感染（IAIs），但其在腹膜液中的体内浓度尚不清楚。本研究的目的是确定单次静脉注射1g厄他培南后腹膜液中的浓度。在获得知情同意后，纳入了21例需要进行腹腔手术的患者（9例女性和12例男性；平均±标准差（S.D.）年龄50.2±17.7岁）。在手术期间的固定时间采集血浆和腹膜液样本。通过高效液相色谱（HPLC）和紫外检测测定药物浓度。给药后1小时，厄他培南腹膜液平均浓度±标准差为64.3±23.4mg/L，3小时时为31.3±26.5mg/L。平均组织/血浆比值在46.7%至83.1%之间。在整个采样期间，腹膜液平均浓度远高于IAIs中常见的敏感细菌的MIC（90）（90%的菌株的最低抑菌浓度），尤其是大肠杆菌、草绿色链球菌、肠杆菌科、克雷伯菌属和脆弱拟杆菌。这些药代动力学结果支持厄他培南可能适用于治疗IAIs的假设。
