title: Relative bioavailability of imipramine (Tofranil) coated tablets in healthy volunteers.
abstract: OBJECTIVE
  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.
  
  
  METHODS
  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.
  
  
  RESULTS
  The relative bioavailabilities of Tofranil 25 and Tofranil mite were 97% and 81%, respectively. The study medication was well tolerated.
  
  
  CONCLUSIONS
  A sufficiently high extent of absorption was found for the test formulations ensuring therapeutic efficacy.
authors: Institute for Medicines Research, Allensbach, Germany.
authors: U
authors: U
authors: Ullmann
authors: R
authors: R
authors: Lehnfeld
authors: H
authors: H
authors: Bliesath
authors: M
authors: M
authors: Birkel
authors: H
authors: H
authors: Gebbing
authors: M
authors: M
authors: Gräve
authors: H
authors: H
authors: Wolf
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000929:Antidepressive Agents, Tricyclic / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D018592:Cross-Over Studies; D003891:Desipramine / Q000493:pharmacokinetics; D006207:Half-Life; D006801:Humans; D007099:Imipramine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D013607:Tablets
chemical_list: D000929:Antidepressive Agents, Tricyclic; D013607:Tablets; D007099:Imipramine; D003891:Desipramine