Study objective: To determine the penetration of ceftibuten into various re
spiratory tissues and fluids.
Design: Single-dose, open-label, pharmacokinetic study.
Setting: Veterans Administration Medical Center.
Patients: Twelve hospitalized men aged 34 to 75 years with a variety of non
infectious pulmonary symptoms/diseases,
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 ana results: Mean pharmacokinetic parameters for ceftibuten in
plasma were the following: maximum observed plasma concentration (Cmax), 8
.77 mu g/mL; time to reach Cmax, 2.2 h; area under the plasma concentration
-time curve extraploated to infinity, 49.21 mu g/h/mL; and terminal elimina
tion 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. M
ean penetration into BAL fluid was 81%, whereas penetration into lung tissu
e 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 infection
s.