Symonds J, Bone M, Turner A, Javaid A
Department of Microbiology, Russels Hall Hospital, Dudley.
Drugs. 1987;34 Suppl 1:33-6. doi: 10.2165/00003495-198700341-00008.
The penetration of ofloxacin into bronchial secretions was evaluated in 16 patients after administration of a single oral dose of ofloxacin 400mg. Bronchial secretions were aspirated at bronchoscopy after 1 to 6 hours and serum was collected simultaneously. Ofloxacin concentrations were measured by a microbiological assay method. Considerable individual variations in serum and bronchial aspirate concentrations were recorded: bronchial aspirate concentrations varied between 1.1 mg/L and 4.5 mg/L but exceeded 1.5 mg/L in 14 of 16 patients between 1 and 6 hours. The ratio between simultaneous mean bronchial aspirate and serum concentrations ranged between 0.53 in the second hour and 0.92 in the fourth hour. It is likely that inhibitory activity will be sustained over at least 6 hours against most potential respiratory pathogens including Haemophilus influenzae, Branhamella catarrhalis, Gram-negative bacilli, Staphylococcus aureus, Legionella pneumophila and Mycoplasma pneumoniae. Streptococcus pneumoniae and Pseudomonas aeruginosa may have minimal inhibitory concentration (MIC) values lower than ofloxacin concentrations achieved in bronchial secretions, although some isolates are less sensitive. Clinical studies should establish the relevance of pharmacokinetic data to respiratory infections caused by organisms of borderline susceptibility.
在16例患者单次口服400mg氧氟沙星后，评估了氧氟沙星在支气管分泌物中的渗透情况。在1至6小时后通过支气管镜检查抽吸支气管分泌物，并同时采集血清。采用微生物测定法测量氧氟沙星浓度。记录到血清和支气管抽吸物浓度存在相当大的个体差异：支气管抽吸物浓度在1.1mg/L至4.5mg/L之间变化，但在16例患者中有14例在1至6小时内超过1.5mg/L。同时期支气管抽吸物平均浓度与血清浓度之比在第二小时为0.53，在第四小时为0.92。对于包括流感嗜血杆菌、卡他莫拉菌、革兰氏阴性杆菌、金黄色葡萄球菌、嗜肺军团菌和肺炎支原体在内的大多数潜在呼吸道病原体，抑制活性可能至少持续6小时。肺炎链球菌和铜绿假单胞菌的最低抑菌浓度（MIC）值可能低于支气管分泌物中达到的氧氟沙星浓度，尽管一些分离株敏感性较低。临床研究应确定药代动力学数据与由临界敏感性微生物引起的呼吸道感染之间的相关性。
