DIFFERENTIAL-EFFECTS OF FOOD ON THE BIOAVAILABILITY OF CONTROLLED-RELEASE OXYCODONE TABLETS AND IMMEDIATE-RELEASE OXYCODONE SOLUTION

The effects of a high-fat meal on the bioavailability of oxycodone hyd rochloride, administered as a recently developed 40 mg controlled-rele ase (CR) tablet or a 20 mg immediate-release (IR) solution, were evalu ated in a randomized crossover study in 22 normal male and female subj ects. Serial blood samples were collected for 36 h after dosing and an alyzed for oxycodone by a validated method using gas chromatography/ma ss spectrometry. There was no significant food effect with CR oxycodon e as judged by 90% confidence interval (CI) analysis of AUC(0-infinity ) and C-max values under fed and fasted conditions. For the IR solutio n, both oxycodone bioavailability and peak plasma oxycodone concentrat ion were significantly altered by consumption of the high-fat meal, wi th the mean value for AUC(0-infinity), increasing to 120% (CI = 109-13 2%) and the mean value for C-max decreasing to 82% (CI = 47-91%) of va lues observed in the fasted condition. Adverse events reported for bot h formulations were mostly mild to moderate in severity and typical of those observed with opioids.