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对健康志愿者单次口服400毫克莫西沙星后,其血浆、尿液中的浓度以及在前列腺液和精液中的渗透情况。

Concentrations of moxifloxacin in plasma and urine, and penetration into prostatic fluid and ejaculate, following single oral administration of 400 mg to healthy volunteers.

作者信息

Wagenlehner F M E, Kees F, Weidner W, Wagenlehner C, Naber K G

机构信息

Department of Urology, Justus-Liebig-University of Giessen, Germany.

出版信息

Int J Antimicrob Agents. 2008 Jan;31(1):21-6. doi: 10.1016/j.ijantimicag.2007.08.025. Epub 2007 Dec 3.

DOI:10.1016/j.ijantimicag.2007.08.025
PMID:18054465
Abstract

The spectrum of chronic bacterial prostatitis (CBP) comprises Gram-negative, Gram-positive and atypical pathogens. Because of its broad spectrum of activity, moxifloxacin might be a suitable antibiotic for the treatment of CBP. In this pharmacokinetic study, plasma concentrations and the penetration of moxifloxacin into prostatic fluid and ejaculate were investigated. Twelve healthy male volunteers received a single oral dose of 400mg moxifloxacin and at the same time received 3.24 g of iohexol intravenously to assess urinary contamination of prostatic fluid and ejaculate. Plasma concentrations were determined at 0, 0.5, 1, 2, 3 and 4h and prostatic fluid and ejaculate (mean+/-standard deviation (S.D.)) were determined at 3.5+/-0.4h and 3.6+/-0.4h, respectively, following administration of drugs. Urinary concentrations were determined in the urine collected from 0-4.5h. Concentrations of moxifloxacin and iohexol in plasma, secretions and urine were determined by high-performance liquid chromatography. The mean+/-S.D. peak plasma concentration of moxifloxacin was 2.8+/-0.5 mg/L observed after 1.6+/-0.9h. In prostatic fluid, the concentration of moxifloxacin was 3.8+/-1.2 mg/L and the prostatic fluid/plasma ratio was 1.6+/-0.5. In ejaculate, the concentration was 2.5+/-0.7 mg/L and the ejaculate/plasma ratio was 1.0+/-0.2. Moxifloxacin concentrations in prostatic fluid were ca. 60% (P<0.05) higher than in plasma and concentrations in ejaculate were approximately the same as in plasma. Therefore, moxifloxacin might be a good alternative for the treatment of CBP, but further studies are warranted to establish this indication.

摘要

慢性细菌性前列腺炎(CBP)的病原体谱包括革兰氏阴性菌、革兰氏阳性菌和非典型病原体。由于莫西沙星具有广泛的抗菌活性,它可能是治疗CBP的一种合适抗生素。在这项药代动力学研究中,对莫西沙星的血浆浓度及其在前列腺液和精液中的渗透情况进行了研究。12名健康男性志愿者单次口服400mg莫西沙星,同时静脉注射3.24g碘海醇,以评估前列腺液和精液的尿液污染情况。给药后,分别于0、0.5、1、2、3和4小时测定血浆浓度,于3.5±0.4小时和3.6±0.4小时分别测定前列腺液和精液(均值±标准差(S.D.))。在0 - 4.5小时收集的尿液中测定尿液浓度。采用高效液相色谱法测定血浆、分泌物和尿液中莫西沙星和碘海醇的浓度。莫西沙星的平均±标准差血浆峰浓度在1.6±0.9小时后为2.8±0.5mg/L。在前列腺液中,莫西沙星浓度为3.8±1.2mg/L,前列腺液/血浆比值为1.6±0.5。在精液中,浓度为2.5±0.7mg/L,精液/血浆比值为1.0±0.2。前列腺液中的莫西沙星浓度比血浆中约高60%(P<0.05),精液中的浓度与血浆中的大致相同。因此,莫西沙星可能是治疗CBP的一个良好替代药物,但需要进一步研究来确立这一适应证。

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