Rodvold K A, Gotfried M H, Danziger L H, Servi R J
College of Pharmacy, University of Illinois, Chicago 60612, USA.
Antimicrob Agents Chemother. 1997 Jun;41(6):1399-402. doi: 10.1128/AAC.41.6.1399.
The steady-state concentrations of clarithromycin and azithromycin in plasma were compared with concomitant concentrations in epithelial lining fluid (ELF) and alveolar macrophages (AM) obtained in intrapulmonary samples during bronchoscopy and bronchoalveolar lavage from 40 healthy, nonsmoking adult volunteers. Mean plasma clarithromycin, 14-(R)-hydroxyclarithromycin, and azithromycin concentrations were similar to those previously reported. Clarithromycin was extensively concentrated in ELF (range of mean +/- standard deviation concentrations, 34.4 +/- 29.3 microg/ml at 4 h to 4.6 +/- 3.7 microg/ml at 24 h) and AM (480 +/- 533 microg/ml at 4 h to 99 +/- 50 microg/ml at 24 h). The concentrations of azithromycin in ELF were 1.01 +/- 0.45 microg/ml at 4 h to 1.22 +/- 0.59 microg/ml at 24 h, and those in AM were 42.7 +/- 28.7 microg/ml at 4 h to 41.7 +/- 12.1 microg/ml at 24 h. The concentrations of 14-(R)-hydroxyclarithromycin in the AM ranged from 89.3 +/- 52.8 microg/ml at 4 h to 31.3 +/- 17.7 microg/ml at 24 h. During the period of 24 h after drug administration, azithromycin and clarithromycin achieved mean concentrations in ELF and AM higher than the concomitant concentrations in plasma.
对40名健康、不吸烟的成年志愿者在支气管镜检查和支气管肺泡灌洗期间获取的肺内样本中的上皮衬液（ELF）和肺泡巨噬细胞（AM）中的克拉霉素和阿奇霉素稳态浓度与血浆中的伴随浓度进行了比较。血浆中克拉霉素、14-(R)-羟基克拉霉素和阿奇霉素的平均浓度与先前报道的相似。克拉霉素在ELF中大量富集（平均±标准差浓度范围，4小时时为34.4±29.3μg/ml至24小时时为4.6±3.7μg/ml），在AM中也大量富集（4小时时为480±533μg/ml至24小时时为99±50μg/ml）。阿奇霉素在ELF中的浓度在4小时时为1.01±0.45μg/ml至24小时时为1.22±0.59μg/ml，在AM中的浓度在4小时时为42.7±28.7μg/ml至24小时时为41.7±12.1μg/ml。AM中14-(R)-羟基克拉霉素的浓度范围为4小时时89.3±52.8μg/ml至24小时时31.3±17.7μg/ml。在给药后的24小时内，阿奇霉素和克拉霉素在ELF和AM中的平均浓度高于血浆中的伴随浓度。
