Pharmacokinetic profiles of two tablet formulations of piroxicam

Abstract

There is considerable interest in developing new non-steroidal anti-inflammatory drugs (NSAIDs) formulations with faster onset of analgesic action like fast dissolving tablets. An open-label, randomized, single dose, crossover study with a 18 days washout period was conducted in 16 healthy volunteers to compare the pharmacokinetic profile of 20 mg piroxicam freeze-dried tablet (Proxalyoc ®, Cephalon) with that of 20 mg piroxicam capsule (Feldène ®, Pfizer). T lag with freeze-dried tablet was three times shorter than with capsule (21.6 min versus 59.4 min). Mean AUC 0–30 min , mean AUC 0–1 h , mean plasma concentrations at 15 min, 30 min and 1 h post-dose were significantly higher with the freeze-dried tablet than with the capsule, indicating that piroxicam was more rapidly absorbed from the freeze-dried tablet with higher plasma concentrations achieved at shorter intervals after dosing. The 90% confidence intervals of the ratios of means C max, AUC 0– t , AUC 0– ∞ and T 1/2 all fell within the acceptance range of 0.8–1.25, demonstrating the bioequivalence of the two formulations. Although the bioavailability of the two formulations was similar, the administration of piroxicam as a freeze-dried tablet gave a much faster absorption rate during the first hour after dosing than the capsule formulation. This faster absorption is an obvious advantage for the treatment of acute episodes of pain.