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首页> 外文期刊>Pulmonary pharmacology & therapeutics >Pharmacokinetics of telithromycin using bronchoscopic microsampling after single and multiple oral doses.
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Pharmacokinetics of telithromycin using bronchoscopic microsampling after single and multiple oral doses.

机译：单次和多次口服给药后，使用支气管镜微量采样法测定泰利霉素的药代动力学。

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OBJECTIVES: Bronchoscopic microsampling (BMS) is a new technique for repeated sampling of bronchial epithelial lining fluid (ELF) to obtain the pharmacokinetic profile of drugs. We analyzed the time versus concentration profiles of telithromycin in bronchial ELF obtained by BMS and compared these finding to those in plasma and alveolar ELF obtained by bronchoalveolar lavage (BAL). METHODS: Bronchial ELF samples were obtained from five healthy subjects using BMS probe at 0, 2, 3, 4, 6, 10 and 24h after single or multiple oral doses of 600mg of telithromycin. Alveolar ELF was also obtained by BAL 3h after single or multiple oral doses of 600mg of telithromycin. RESULTS: The areas under the concentration-time curve from 0 to 24h (AUC0-24) of telithromycin in plasma and bronchial ELF were 2.86+/-0.60 and 19.5+/-10.4mgh/l after single treatment and 3.60+/-0.49 and 42.2+/-22.7mgh/l after multiple treatments, respectively. Single and multiple oral doses of telithromycin produced significantly (p<0.05) higher AUC0-24 in bronchial ELF compared to those in plasma. While concentrations in bronchial ELF obtained by BMS were significantly lower than those in alveolar ELF obtained by BAL, they tended to be higher than those in plasma after multiple administration. The telithromycin concentrations obtained by BMS method were very consistent in bronchial ELF at different bronchi at one time point and at the same bronchus at different time points. CONCLUSIONS: Using the BMS technique, we could describe the pharmacokinetics of telithromycin in bronchial ELF. Furthermore, BMS was reasonably validated and reconfirmed to be a feasible and reliable method for measuring antimicrobial concentrations in bronchial ELF.
机译：目的：支气管镜显微采样（BMS）是一种用于反复采样支气管上皮衬里液（ELF）以获得药物药代动力学特征的新技术。我们分析了通过BMS获得的支气管ELF中telithromycin的时间与浓度曲线，并将这些发现与通过支气管肺泡灌洗（BAL）获得的血浆和肺泡ELF中的发现进行了比较。方法：单次或多次口服600 mg泰利霉素后0、2、3、4、6、10和24h，使用BMS探针从5名健康受试者中获取支气管ELF样本。单次或多次口服600 mg泰利霉素后3小时，BAL也可得到肺泡ELF。结果：血浆和支气管ELF中telithromycin在0至24h（AUC0-24）浓度-时间曲线下的面积分别为单次治疗后2.86 +/- 0.60和19.5 +/- 10.4mgh / l，3.60 +/- 0.49和多次处理后分别为42.2 +/- 22.7mgh / l。与血浆中的剂量相比，单次和多次口服泰利霉素在支气管ELF中产生的AUC0-24显着更高（p <0.05）。虽然通过BMS获得的支气管ELF中的浓度明显低于通过BAL获得的肺泡ELF中的浓度，但在多次给药后它们往往高于血浆中的浓度。通过BMS方法获得的telithromycin浓度在一个时间点的不同支气管和同一时间的同一支气管的支气管ELF中非常一致。结论：使用BMS技术，我们可以描述泰利霉素在支气管ELF中的药代动力学。此外，BMS已得到合理验证和确认，是测量支气管ELF中抗菌素浓度的可行且可靠的方法。

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