Panteix G, Harf R, Desnottes J F, Gosselet H, Leclercq M, Diallo N, Couprie N, Desbos A, Perrin Fayolle M, Ballereau M
Institut Pasteur de Lyon, Laboratoire Micro-Analyse et Nutrition, France.
J Antimicrob Chemother. 1994 May;33(5):979-85. doi: 10.1093/jac/33.5.979.
The in-vivo pulmonary disposition of pefloxacin in alveolar macrophages alveolar macrophages and in the alveolar epithelial lining fluid recovered by bronchoalveolar lavage was studied in 10 healthy volunteers. Bronchoalveolar lavage was performed either 2 or 4 h after oral intake of 800 mg of the drug. The recovered fluid was immediately centrifuged and processed for the assays. Pefloxacin was assayed by High Pressure Liquid Chromatography (HPLC) and by a microbiological method. The mean concentrations of pefloxacin assayed by HPLC were 106 +/- 11.1 mg/L in alveolar macrophages and 88.2 +/- 10 mg/L in the epithelial lining fluid, whereas the mean serum concentration was 6.67 +/- 0.47 mg/L. Therefore, pefloxacin accumulated rapidly in human alveolar macrophages. The high epithelial lining fluid concentrations may be attributed to lipophilicity of the drug and to rapid diffusion from blood, pulmonary cells and interstitium during the bronchoalveolar lavage procedure. The substantial accumulation of pefloxacin in alveolar components (alveolar macrophages and epithelial lining fluid) endorses its use in the treatment of intracellular bacterial infections such as legionellosis; for these diseases, pefloxacin represents an alternative to the macrolide antibiotics.
在10名健康志愿者中研究了培氟沙星在肺泡巨噬细胞以及通过支气管肺泡灌洗回收的肺泡上皮衬液中的体内肺部处置情况。在口服800毫克该药物后2小时或4小时进行支气管肺泡灌洗。回收的液体立即离心并进行分析测定。培氟沙星通过高压液相色谱法（HPLC）和微生物学方法进行测定。通过HPLC测定的培氟沙星在肺泡巨噬细胞中的平均浓度为106±11.1毫克/升，在上皮衬液中的平均浓度为88.2±10毫克/升，而血清平均浓度为6.67±0.47毫克/升。因此，培氟沙星在人肺泡巨噬细胞中迅速蓄积。上皮衬液中的高浓度可能归因于该药物的亲脂性以及在支气管肺泡灌洗过程中从血液、肺细胞和间质的快速扩散。培氟沙星在肺泡成分（肺泡巨噬细胞和上皮衬液）中的大量蓄积支持其用于治疗细胞内细菌感染，如军团病；对于这些疾病，培氟沙星是大环内酯类抗生素的一种替代药物。
