Intrapulmonary steady-state concentrations of clarithromycin and azithromycin in healthy adult volunteers

Intrapulmonary steady-state concentrations of clarithromycin and azithromycin in healthy adult volunteers
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健康成年志愿者中克拉霉素和阿奇霉素的肺内稳态浓度

DOI:
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发表时间:
1997
影响因子:
4.9
通讯作者:
R. Servi
R. Servi
中科院分区:
医学2区
文献类型:
--
作者:
K. Rodvold;M. Gotfried;M. Gotfried;L. Danziger;R. Servi

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将血浆中克拉霉素和阿奇霉素的稳态浓度与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肺内样本中获得的上皮细胞衬里液(ELF)和肺泡巨噬细胞(AM)中的伴随浓度进行比较。平均血浆克拉霉素、14-(R)-羟基克拉霉素和阿奇霉素浓度与先前报告的相似。克拉霉素广泛集中在ELF(平均+/-标准差浓度范围,4 h为34.4 +/- 29.3 μ g/ml至24 h为4.6 +/- 3.7 μ g/ml)和AM(4 h为480 +/- 533 μ g/ml至24 h为99 +/- 50 μ g/ml)中。ELF中阿奇霉素的浓度为1.01 +/- 0.45 μ g/ml(4 h)至1.22 +/- 0.59 μ g/ml(24 h),AM中阿奇霉素的浓度为42.7 +/- 28.7 μ g/ml(4 h)至41.7 +/- 12.1 μ g/ml(24 h)。AM中14-(R)-羟基克拉霉素的浓度范围为89.3 +/- 52.8 μ g/ml(4 h)至31.3 +/- 17.7 μ g/ml(24 h)。在给药后24 h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。
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.