Research ArticlesBioavailability of Orally Administered propiram (cas 15686-91-6) Fumarate in Humans

Add time:09/01/2019    Source:sciencedirect.com

propiram (cas 15686-91-6) bioavailability was determined in 10 healthy volunteers after a single oral administration of 50 mg (base equivalent) of propiram fumarate in tablet or solution dosage form in a randomized crossover design. The plasma drug concentration-time curve revealed a one-compartment open model with first-order absorption kinetics. There were no statistically significant differences (p > 0.05) between all of the measured pharmacokinetic parameters obtained from the tablet and the solution with the exception of the absorption lag time (tlag. where the tablet had a significantly longertlag. The drug given as a tablet, or solution was absorbed rapidly after oral administration with an apparent absorption rate constant of 3.7 hr−1 for both dosage forms. TheCmax value (308 ng/ml for the tablet and 342 ng/ml for the solution) was attained at ˜1 hr after oral administration. The elimination half-life was 5.2 hr for the tablet and 4.4 hr for the solution, and the apparent distribution volume was 2.31 liters/kg for the tablet and 1.94 liters/kg for the solution. Total body clearance was much greater than renal clearance, indicating extensive metabolic clearance for both dosage forms. The study showed that propiram administered as the tablet was bioequivalent to the solution.

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