Summary
The pharmacokinetics of a new tablet formulation of acenocoumarol racemate, an oral anticoagulant agent, has been investigated in 8 normal healthy subjects. The drug was given as a single oral dose of 12 mg. 12 blood samples were collected after administration. Plasma acenocoumarol concentrations were determined by a sensitive HPLC method. Areas under the plasma level-time curves for each subject were evaluated by means of the trapezoidal rule. The peak plasma concentration of 244.19–644.23 μg/l was reached 1–4 h after drug administration. The terminal phase half-life was 6.29–14.22 h and a systemic clearance was 1.86–5.62 l/h. The new tablet formulation of acenocoumarol seems to be bioequivalent when compared to the one used so far. For the prediction of systemic availability and estimation of the first-pass metabolism, from plasma level data, a hepatic blood flow rate limited model were used. The systemic availability was 94.22–98.01% and the elimination of the drug on its first-pass through the liver was 1.99–5.78%.
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Popović, J., Mikov, M. & Jakovljević, V. Pharmacokinetic analysis of a new acenocoumarol tablet formulation during a bioequivalence study. Eur. J. Drug Metab. Pharmacokinet. 19, 85–89 (1994). https://doi.org/10.1007/BF03188828
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DOI: https://doi.org/10.1007/BF03188828