BIOPHARMACEUTICAL CHARACTERIZATION OF A LOW-DOSE (75 MG) CONTROLLED-RELEASE ASPIRIN FORMULATION

The release of aspirin from a 75 mg controlled-release formulation, de signed to inhibit maximally thromboxane A2 production while sparing st imulated prostacyclin biosynthesis, was characterised in healthy subje cts. The calculated in vivo release rate of aspirin matched the design goal of approximately 10 mg h-1. The C(max) of aspirin associated wit h the controlled-release formulation was lowered 15-fold relative to a solution formulation of the same dose. The bioavailability of aspirin (based on salicylate concentrations) from the controlled-release form ulation was approximately 90% relative to the solution, and drug relea se was not affected by co-administration of a standard breakfast.