HIGH AND PROLONGED PULMONARY TISSUE CONCENTRATIONS OF AZITHROMYCIN FOLLOWING A SINGLE ORAL DOSE
HIGH AND PROLONGED PULMONARY TISSUE CONCENTRATIONS OF AZITHROMYCIN FOLLOWING A SINGLE ORAL DOSE
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DOI：
10.1007/bf01975842
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发表时间：
1991-10-01
影响因子：
4.5
通讯作者：
MORGAN, WE
中科院分区：
文献类型：
--
作者：
MORRIS, DL;DESOUZA, A;MORGAN, WE
在这项开放性研究中，研究了肺组织样本和血浆中的抗生素浓度。 29例择期肺手术患者在手术前24、72、96或120 h接受500 mg阿奇霉素单次口服给药; 2例患者接受250 mg b.i.d. 在切除前和切除时采集血液样本，并在手术期间获得组织。 采用高效液相色谱法和微生物生物测定法测定血浆和组织中阿奇霉素的浓度。 仅一名患者具有可检测的阿奇霉素血浆浓度（0.13 μ g/ml），在给药后24小时通过HPLC测量。 然而，在肺组织中发现了高水平和持续的水平：在24、72、96和120 h时，通过HPLC测量的平均浓度分别为3.10 μ g/g（SD +/- 2.17）、2.55 μ g/g（SD +/- 1.36）、3.94 μ g/g（SD +/- 2.40）和3.13 μ g/g（SD +/- 0.50）。 生物测定结果与HPLC测定结果相似。 总之，单次口服500 mg剂量后，肺组织中阿奇霉素水平保持接近3 μ g/g长达5天，而血浆水平要低得多。 发现肺浓度对许多敏感的呼吸道病原体具有抑制作用，因此，短期阿奇霉素治疗是可能的。
Antibiotic concentrations in pulmonary tissue samples and plasma were studied in this open investigation. Twenty-nine patients scheduled for elective pulmonary surgery received a single oral dose of 500 mg azithromycin 24, 72, 96 or 120 h prior to the operation; two patients received 250 mg b.i.d. Blood samples were taken before and at the time of resection, and tissue was obtained during surgery. Plasma and tissue concentrations of azithromycin were measured by high performance liquid chromatography (HPLC) and a microbiological bioassay. Only one patient had a detectable plasma concentration of azithromycin (0.13-mu-g/ml), measured 24 h post-dose by HPLC. However, high and sustained levels were found in lung tissue: mean concentrations measured by HPLC were 3.10-mu-g/g (SD +/- 2.17), 2.55-mu-g/g (SD +/- 1.36), 3.94-mu-g/g (SD +/- 2.40) and 3.13-mu-g/g (SD +/- 0.50) at 24, 72, 96 and 120 h, respectively. Bioassay results were similar to those for the HPLC assay. In summary, azithromycin levels in pulmonary tissue remained close to 3-mu-g/g for up to 5 days after a single oral 500 mg dose, in contrast to plasma levels which were much lower. The lung concentrations found are inhibitory for many sensitive respiratory pathogens and short-course azithromycin therapy is therefore a possibility.