Abstract
Concentrations of ceftibuten in bronchial mucosa, epithelial lining fluid (ELF) and alveolar macrophages were determined from samples taken from 15 subjects at bronchoscopy following a single 400 mg oral dose. Concentrations at all sites were determined using a microbiological assay method which was unaffected by the trans-isomer of ceftibuten. The time from dosage to bronchoscopy ranged from 1.4 to 20.3 h and the subjects were analysed in three groups according to time after dosing. Group A had a mean time since dosing of 1.9 h with mean serum, mucosal and ELF concentrations of 15.2 mg/l, 5.7 mg/kg and 1.6 mg/l. Group B had a mean time of 6.5 h after dosing with mean serum, mucosal and ELF concentration of 14.0 mg/l, 3.2 mg/kg and 1.6 mg/l. Group C had a mean time of 13.3 h with mean serum, mucosal and ELF levels of 4.1 mg/l, 1.8 mg/kg and 1.2 mg/l. Macrophage-related ceftibuten could only be detected in two subjects. These levels are related to the minimum inhibitory concentrations of ceftibuten against common respiratory pathogens with the exception of Strep. pneumoniae.
Published Version
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