Patent ID: 8105631

Claim:
An oral dosage form comprising an orally therapeutically effective dose of an opioid agonist, wherein at least a portion of said dose is in an immediate release form, and an amount of an opioid antagonist selected from the group consisting of naltrexone, naloxone, nalmephene, cyclazocine, levallorphan, pharmaceutically acceptable salts and mixtures thereof, wherein part or all of said amount is in a sustained release form; the dosage form having a ratio of opioid antagonist to opioid agonist that provides a combination product which is analgesically effective when the combination is administered orally, but which (i) is aversive in physically dependent human subjects when administered at the same dose or at a higher dose than said therapeutically effective dose; and (ii) maintains an analgesic effect but does not increase analgesic efficacy of the opioid agonist relative to the same therapeutic dose of opioid agonist when administered to human patients without said opioid antagonist; wherein the ratio of the opioid antagonist to the opioid agonist is selected from the group consisting of from about 0.03:1 to about 0.27:1, based on the opioid antagonist being naltrexone or a pharmaceutically acceptable salt thereof and the opioid agonist being hydrocodone or a pharmaceutically acceptable salt thereof; from about 0.037:1 to about 0.296:1, based on the opioid antagonist being naltrexone or a pharmaceutically acceptable salt thereof and the opioid agonist being oxycodone or a pharmaceutically acceptable salt thereof; from about 0.148:1 to about 1.185:1, based on the opioid antagonist being naltrexone or a pharmaceutically acceptable salt thereof and the opioid agonist being hydromorphone or a pharmaceutically acceptable salt thereof; from about 0.278:1 to about 2.222:1, based on the opioid antagonist being naltrexone or a pharmaceutically acceptable salt thereof and the opioid agonist being levorphanol or a pharmaceutically acceptable salt thereof; from about 0.056:1 to about 0.444:1, based on the opioid antagonist being naltrexone or a pharmaceutically acceptable salt thereof and the opioid agonist being methadone or a pharmaceutically acceptable salt thereof; and from about 0.018:1 to about 0.148:1, based on the opioid antagonist being naltrexone or a pharmaceutically acceptable salt thereof and the opioid agonist being morphine or a pharmaceutically acceptable salt thereof.