Study objective: To determine the penetration of
ceftibuten into various respiratory tissues and fluids.
Design: Single-dose, open-label, pharmacokinetic
Setting: Veterans Administration Medical
Patients: Twelve hospitalized men aged 34 to
75 years with a variety of noninfectious pulmonary
Interventions: Patients received a
single oral dose of ceftibuten, 200 mg, prior to undergoing diagnostic
fiberoptic bronchoscopy. Plasma samples for the determination of
ceftibuten concentrations were collected pretreatment and up to 12
h postdosing. Nasal secretions, tracheal secretions, BAL fluid, and
lung tissue from a biopsy were obtained at bronchoscopy from 2 to
7 h postdosing.
Measurements and results: Mean
pharmacokinetic parameters for ceftibuten in plasma were the following:
maximum observed plasma concentration (Cmax), 8.77 μg/mL; time to
reach Cmax, 2.2 h; area under the plasma concentration-time curve
extraploated to infinity, 49.21 μg/h/mL; and terminal
elimination half-life, 3.17 h. These parameters were similar to
those obtained in studies using healthy volunteers. Mean penetration of
ceftibuten into nasal, tracheal, and bronchial secretions was 47%,
50%, and 30%, respectively. Mean penetration into BAL fluid
was 81%, whereas penetration into lung tissue was 39%. No patient
experienced any adverse effects related to ceftibuten.
Conclusions: Ceftibuten penetrates well into various
tissues and fluids of the upper and lower respiratory tracts. The
results support the activity of ceftibuten in the treatment of upper
and lower respiratory tract infections.