title: Pharmacokinetics and tissue penetration of ceftibuten.
abstract: The pharmacokinetics of the cephalosporin ceftibuten were determined after the fifth and final dose of 200 mg given every 12 h. Concentrations in plasma and cantharidin-induced inflammatory fluid were determined by a microbiological assay. Samples for three volunteers were assayed by a high-performance liquid chromatographic procedure to determine levels for both cis and trans ceftibuten. The mean peak level of ceftibuten in serum was 10.9 micrograms/ml at a mean time of 1.8 h after administration, and the mean elimination half-life from plasma was 2.5 h. Penetration into the inflammatory fluid was good, the mean peak level being 9.2 micrograms/ml at a mean time of 3.7 h. The mean percent penetration into the inflammatory fluid was 113.4%. High-performance liquid chromatography analysis showed that the mean peak level of the trans isomer was 5.7% that of the cis isomer. This study suggests that twice-daily doses of ceftibuten should be sufficient to treat urinary or systemic infections caused by susceptible pathogens.
authors.affiliation: Department of Medical Microbiology, Dudley Road Hospital, Birmingham, United Kingdom.
authors.forename: R
authors.initials: R
authors.lastname: Wise
authors.forename: K
authors.initials: K
authors.lastname: Nye
authors.forename: P
authors.initials: P
authors.lastname: O'Neill
authors.forename: M
authors.initials: M
authors.lastname: Wostenholme
authors.forename: J M
authors.initials: JM
authors.lastname: Andrews
mesh_terms: D000328:Adult; D001681:Biological Assay; D001768:Blister / Q000139:chemically induced / Q000378:metabolism; D001826:Body Fluids / Q000378:metabolism; D000077722:Ceftibuten; D002511:Cephalosporins / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D008297:Male; D013237:Stereoisomerism
chemical_list: D002511:Cephalosporins; D000077722:Ceftibuten