Relative bioavailability of imipramine (Tofranil) coated tablets in healthy volunteers

Imipramine is a tricyclic antidepressant drug with a considerable hepatic first-pass metabolism resulting in highly variable pharmacokinetic characteristics and desipramine as active major metabolite. This study describes the bioavailability of 3 formulations of imipramine. In a randomized, three-pe...

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Bibliographic Details
Published inInternational journal of clinical pharmacology and therapeutics Vol. 39; no. 6; p. 271
Main Authors Ullmann, U, Lehnfeld, R, Bliesath, H, Birkel, M, Gebbing, H, Gräve, M, Wolf, H
Format Journal Article
LanguageEnglish
Published Germany 01.06.2001
Subjects
Administration, Oral
Adult
Antidepressive Agents, Tricyclic - administration & dosage
Antidepressive Agents, Tricyclic - pharmacokinetics
Area Under Curve
Cross-Over Studies
Desipramine - pharmacokinetics
Half-Life
Humans
Imipramine - administration & dosage
Imipramine - pharmacokinetics
Male
Tablets
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Summary:Imipramine is a tricyclic antidepressant drug with a considerable hepatic first-pass metabolism resulting in highly variable pharmacokinetic characteristics and desipramine as active major metabolite. This study describes the bioavailability of 3 formulations of imipramine. In a randomized, three-period crossover study, 18 healthy male Caucasian subjects received single oral doses of Tofranil 25, Tofranil mite (10 mg) and an aqueous solution containing 25 mg imipramine-HCl. Serum concentrations of imipramine-HCl and its main metabolite desipramine were measured. The pharmacokinetic characteristics, Cmax, AUC, t1/2 and tmax were determined and the relative bioavailability of the two coated tablet formulations was calculated with the aqueous solution as reference. Safety and tolerability were assessed using vital signs, ECG, clinical laboratory and adverse event recording. The relative bioavailabilities of Tofranil 25 and Tofranil mite were 97% and 81%, respectively. The study medication was well tolerated. A sufficiently high extent of absorption was found for the test formulations ensuring therapeutic efficacy.
ISSN:0946-1965