J. Shimada, S. Hori, T. Oguma
May 1, 1993
Citations
0
Influential Citations
12
Citations
Quality indicators
Journal
Journal of pharmaceutical sciences
Abstract
Isomerization of ceftibuten to trans-ceftibuten, a less active isomer of ceftibuten, was observed in human serum in vitro. Investigation of the isomerization mechanism in the serum clarified that albumin accelerated the isomerization. The isomerization rate constant correlated significantly with the percent of binding to albumin, suggesting the binding of ceftibuten to albumin might be the driving force for the isomerization under in vitro conditions. This isomerization was also observed in clinical studies in humans. Results of physiological model analysis indicate that the isomerization catalyzed by albumin contributes significantly to the overall isomerization in the human body following oral administration.