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Bioavailability and disposition of prednisone and prednisolone from prednisone tablets
Author(s) -
Rose James Q.,
Yurchak Anthony M.,
Nsko William J.,
Powell David
Publication year - 1980
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510010504
Subject(s) - bioavailability , prednisolone , prednisone , urine , pharmacokinetics , chemistry , pharmacology , corticosteroid , metabolite , active metabolite , glucocorticoid , high performance liquid chromatography , biopharmaceutics , dexamethasone , chromatography , medicine , pharmacognosy , biological activity , biochemistry , in vitro
The relative bioavailability of two 50 mg prednisone tablet formulations was determined in 18 healthy male volunteers who were not pretreated with dexamethasone. Plasma and urine samples were collected over a 24‐h period and their concentrations of prednisone and prednisolone were assayed by a specific and sensitive high pressure liquid chromatography (HPLC) method. Bioavailability was assessed by comparing the areas under the plasma concentration‐time curves and by the relative amounts of prednisone and prednisolone in urine. There were no significant differences between the bioavailability of the film‐coated and standard 50 mg tablets. Eight subjects subsequently received a 40 mg equivalent intravenous dose of prednisolone as prednisolone succinate to provide plasma concentrations of prednisolone similar to concentrations found after oral doses of prednisone. The systemic bioavailability of prednisolone, the active metabolite generated from film‐coated and standard prednisone tablets, was estimated to be 0·77±0·15 and 0·80±0·11, respectively. The nonlinear distribution, the interconversion, and the simultaneous elimination of these drugs, however, complicate any assessment of their relative and absolute bioavailability.