Abstract
Imipramine hydrochloride (IMI) was administered to 12 healthy volunteers on three occasions in random sequence: 12.5 mg IV, 50 mg orally after overnight fast, and 50 mg orally 30 min after eating a standardized breakfast. IMI concentrations were measured by gas-liquid chromatography using nitrogen-phosphorous detection and pharmacokinetic and bioavailability parameters determined by iterative nonlinear least-squares regression analysis. After IV administration, mean kinetic variables were: volume of distribution, 21.0 l/kg; total clearance, 12.8 ml/min per kg, and elimination half-life, 21.2 h. Mean absolute bioavailability of IMI in the fasting state was 43.6%. When IMI was administered immediately after the standardized meal, absolute bioavailability was 44.1%. After oral administration, the time to peak IMI level was not changed by concurrent food ingestion (2.8 vs 3.2 h after dosage), and the peak IMI concentration was no different (35 vs 30 ng/ml). Thus concurrent food ingestion has no effect on IMI absolute bioavailability, peak concentration attained after oral dosing, or the time to peak concentration.
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Abernethyl, D.R., Divoll, M., Greenblatt, D.J. et al. Absolute bioavailability of imipramine: Influence of food. Psychopharmacology 83, 104–106 (1984). https://doi.org/10.1007/BF00427432
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DOI: https://doi.org/10.1007/BF00427432