Abstract
A sustained release capsule formulation of piretanide (6mg) pellets was compared with a standard 6 mg tablet formulation and placebo on a double blind, double dummy basis in 33 healthy volunteers. Pharmacokinetic as well as pharmacodynamic parameters were determined. The relative bioavailability of piretanide from the pellets as compared to the tablets was 81% based on AUC and 87% based on urinary recovery comparison of unchanged drug.
The sustained release formulation cuts down the peak diuresis observed with the tablets in the first 2-hour period by about 50%. The duration of the diuretic effect is more than doubled in comparison to the standard tablet without loss of overall pharmacodynamic activity (diuresis and saluresis). The potassium excretion with both formulations was in the order of magnitude of placebo.
