Zomepirac kinetics in healthy males

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Abstract
Kinetics of zomepirac [ZP], an oral, nonnarcotic analgesic, were studied in healthy [human] males in 3 clinical experiments. ZP 100 mg was taken as tablet, capsule and solution. Bioavailability of ZP from the 3 dosage forms was much the same, ZP absorption was rapid, peak plasma concentrations being reached within 1-2 h. Plasma concentration profile could be described by the 2-comaprtment oral absorption model with an absorption rate constant of 7.66/h (t 1/2 = 0.09 h), a rapid disposition rate constant of 0.75/h (t 1/2 = 0.94 h) and a slow disposition rate constant of 0.16/h (t 1/2 = 4.3 h). Safety and acceptability were established with 100 mg 4 times/day for 14 days followed by 150 mg 4 times/day for 14 days. ZP plasma levels indicated attainment of steady state within less than 3 days of treatment. There was little drug accumulation on the regimens studied. There was no change in plasma kinetics after 14 days on either regimen. Dose/bioavailability response was followed at 50, 100 and 200 mg dose levels. There were linear correlations between dose and peak plasma concentration, area under the plasma concentration-time curve and urinary excretion of intact and total (intact + glucuronide conjugate) ZP during the 12 h following drug administration.

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