Buccal and oral bioavailability of naloxone and naltrexone in rats

Abstract

The opioid antagonists naloxone and naltrexone are both known to undergo extensive first-pass metabolism after oral dosing. The buccal route was investigated as a potential alternative to oral administration. Oral and buccal bioavailabilities of naloxone and naltrexone were determined in rats. Less than 1 % of oral naloxone or naltrexone was bioavailable, but buccal administration resulted in approximately 70% bioavailability for each drug. © 1987.