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莫西沙星在腹膜炎中的药代动力学及腹膜穿透性

Pharmacokinetics and peritoneal penetration of moxifloxacin in peritonitis.

作者信息

Stass H, Rink A D, Delesen H, Kubitza D, Vestweber K-H

机构信息

Pharma Research Centre Bayer AG, Wuppertal, Germany.

出版信息

J Antimicrob Chemother. 2006 Sep;58(3):693-6. doi: 10.1093/jac/dkl305.

Abstract

OBJECTIVES

To investigate the penetration of moxifloxacin into peritoneal exudate in patients with complicated intra-abdominal infections (cIAIs).

PATIENTS AND METHODS

Patients (n = 10) with evidence of peritonitis who required surgery with drainage of the abdominal cavity received a single intravenous infusion of moxifloxacin, 400 mg, over 1 h. Plasma and peritoneal exudate samples were obtained over 24 h, and moxifloxacin concentrations were measured by HPLC with fluorescence detection.

RESULTS

Plasma moxifloxacin concentrations decreased from a geometric mean of 3.61 mg/L at 1 h to 0.36 mg/L at 24 h. Concentrations in peritoneal exudate were highest 2 h after the start of the infusion, reaching a geometric mean of 3.32 mg/L, and declined to a geometric mean of 0.69 mg/L at 24 h. The exudate/plasma concentration ratio rose from 1.45 at 2 h to 1.91 at 24 h; the 95% confidence intervals for the ratio excluded unity at all time points, suggesting that moxifloxacin penetrates and accumulates in peritoneal exudate. The area under the concentration-time curve (AUC) tended to be greater in exudate; the time to peak concentrations (T(max)) was longer in exudate than in plasma, as were half-life and mean residence time (MRT).

CONCLUSIONS

Following intravenous administration, moxifloxacin penetrated peritoneal exudate in patients with peritonitis, achieving and maintaining concentrations that exceed the MICs for pathogens commonly isolated in cIAIs. These findings support the clinical use of moxifloxacin as treatment for cIAIs.

摘要

目的

研究莫西沙星在复杂性腹腔内感染(cIAIs)患者腹腔渗出液中的渗透情况。

患者和方法

10例有腹膜炎证据且需行腹腔引流手术的患者接受单次静脉输注400mg莫西沙星,输注时间为1小时。在24小时内采集血浆和腹腔渗出液样本,采用高效液相色谱荧光检测法测定莫西沙星浓度。

结果

血浆莫西沙星浓度从输注1小时时的几何均值3.61mg/L降至24小时时的0.36mg/L。腹腔渗出液中的浓度在输注开始后2小时最高,达到几何均值3.32mg/L,并在24小时时降至几何均值0.69mg/L。渗出液/血浆浓度比值从2小时时的1.45升至24小时时的1.91;该比值的95%置信区间在所有时间点均不包括1,表明莫西沙星可渗透并在腹腔渗出液中蓄积。浓度-时间曲线下面积(AUC)在渗出液中往往更大;渗出液中的达峰时间(T(max))比血浆中的长,半衰期和平均驻留时间(MRT)也是如此。

结论

静脉给药后,莫西沙星可渗透至腹膜炎患者的腹腔渗出液中,达到并维持超过cIAIs中常见病原体MICs的浓度。这些发现支持莫西沙星用于cIAIs的临床治疗。

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