Ceftibuten is a broad-spectrum oral cephalosporin exhibiting antimicro
bial activity against a wide range of gram-negative and some gram-posi
tive pathogens. Pharmacokinetic studies have shown that the molecule h
as an oral bioavailability higher than 90% of the administered dose (r
eaching peak serum concentrations of 5-19 mg/l after a single dose of
200 and 400 mg). Moreover, ceftibuten has been shown to be useful in t
he treat ment of acute lower respiratory tract infections. This study
was performed to determine the distribution of ceftibuten in bronchial
secretions from patients affected by the exacerbation of chronic bron
chitis. Patients were treated with a single 400-mg oral dose of ceftib
uten. Blood and bronchial-secretion samples were obtained just before,
and at 0.5, 1, 2, 4, 8, 12, 16 and 24 h after dosing. Cells were sepa
rated from bronchial secretions by centrifugation. Ceftibuten in dupli
cate samples of both serum and bronchial secretion was quantified by H
PLC. Ceftibuten reached peak levels 2 and 4 h after oral administratio
n in serum and in bronchial secretions, respectively (18.12 +/- 2.13 a
nd 9.19 +/- 3.1 mg/l, respectively). Falling curves after the peaks sh
owed a monoexponential decay. The absorption was very rapid both in se
rum and bronchial secretions, but elimination was slower in bronchial
secretions than in serum.