Clinical bioavailability evaluation of a controlled release formulation of diazepam

A controlled release formulation of diazepam was compared to equal daily dose of the trade tablet under single day and steady-state conditions. Virtually no differences were found in the mean steady-state concentrations of diazepam or its metabolites, N-desmethyldiazepam, when the subjects received...

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Bibliographic Details
Published inJournal of pharmacokinetics and biopharmaceutics Vol. 9; no. 6; p. 679
Main Authors Gustafson, J H, Weissman, L, Weinfeld, R E, Holazo, A A, Khoo, K C, Kaplan, S A
Format Journal Article
LanguageEnglish
Published United States 01.12.1981
Subjects
Adult
Biological Availability
Biopharmaceutics
Delayed-Action Preparations
Diazepam - administration & dosage
Diazepam - metabolism
Humans
Nordazepam - metabolism
Time Factors
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Summary:A controlled release formulation of diazepam was compared to equal daily dose of the trade tablet under single day and steady-state conditions. Virtually no differences were found in the mean steady-state concentrations of diazepam or its metabolites, N-desmethyldiazepam, when the subjects received the 5 mg trade table three times daily or the 15 mg controlled release formulation once daily. Similarly, there was no difference in mean diazepam or N-desmethyldiazepam plasma concentrations when single doses of the controlled release formulation were give to fed or fasted volunteers. These data indicate that the controlled release formulation produces plasma concentrations of diazepam and N-desmethyldiazepam comparable to those achieved with the same daily dose of the trade product given three times daily, suggesting that these regimens can be used interchangeably.
ISSN:0090-466X
DOI:10.1007/BF01070900