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Claims for Patent: 8,822,487

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Claims for Patent: 8,822,487

Title:Opioid agonist/opioid antagonist/acetaminophen combinations
Abstract: The invention is directed in part to oral dosage forms comprising a combination of an opioid agonist, acetaminophen and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, "aversive" experience in physically dependent addicts (e.g., precipitated abstinence syndrome).
Inventor(s): Kaiko; Robert F. (Weston, CT), Colucci; Robert D. (Newton, CT)
Assignee: Purdue Pharma L.P. (Stamford, CT)
Application Number:13/708,736
Patent Claims: 1. A sustained release oral dosage form, comprising: (A) an opioid agonist present as an orally therapeutically effective dose of about 8 mg to about 50 mg hydrocodone or a pharmaceutically acceptable salt thereof, or about 2.5 mg to about 800 mg oxycodone or a pharmaceutically acceptable salt thereof; (B) an opioid antagonist selected from naltrexone, naloxone, nalmephene, cyclazocine, levallorphan, and mixtures thereof, or a pharmaceutically acceptable salt thereof; and (C) a sustained release carrier incorporated into a matrix that contains said opioid agonist and said opioid antagonist; said dosage form having a ratio of said opioid antagonist to said opioid agonist that provides a combination product which is analgesically effective when the combination is administered orally, but which is aversive in physically dependent human subjects when abused at a higher dose than said therapeutically effective dose.

2. The oral dosage form of claim 1, wherein the amount of antagonist included in the oral dosage form causes an aversive experience in a physically dependent addict taking about 2-3 times said therapeutically effective dose.

3. The oral dosage form of claim 1, wherein the opioid agonist is hydrocodone or a pharmaceutically acceptable salt thereof and the antagonist is naloxone or a pharmaceutically acceptable salt thereof.

4. The oral dosage form of claim 3, wherein said naloxone or a pharmaceutically acceptable salt thereof is present in an amount that corresponds to an equiantagonistic amount of naltrexone or a pharmaceutically acceptable salt thereof, and the ratio of the equiantagonistic amount of naltrexone or pharmaceutically acceptable salt thereof to hydrocodone or pharmaceutically acceptable salt thereof is from about 0.03:1 to about 0.27:1.

5. The oral dosage form of claim 4, wherein the ratio of the equiantagonistic amount of naltrexone or pharmaceutically acceptable salt thereof to hydrocodone or pharmaceutically acceptable salt thereof is from about 0.05:1 to about 0.20:1.

6. The oral dosage form of claim 1, wherein the opioid agonist is oxycodone or a pharmaceutically acceptable salt thereof.

7. The oral dosage form of claim 1, further comprising an additional non-opioid drug selected from the group consisting of an NSAID, a COX-2 inhibitor, aspirin, an NMDA receptor antagonist, a drug that blocks a major intracellular consequence of NMDA-receptor activation, dimenhydrinate or a pharmaceutically acceptable salt thereof, an antitussive, an expectorant, a decongestant, an antihistamine and mixtures thereof.

8. The oral dosage form of claim 1, further comprising one or more pharmaceutically acceptable inert excipients.

9. The oral dosage form of claim 6, wherein said opioid antagonist is naloxone or a pharmaceutically acceptable salt thereof.

10. The oral dosage form of claim 1, wherein said opioid antagonist is naloxone or a pharmaceutically acceptable salt thereof.

11. The oral dosage form of claim 1, wherein said sustained release carrier causes said opioid agonist to be released over a time period of about 8 to about 24 hours when orally administered to a human patient.

12. The oral dosage form of claim 1, wherein said opioid antagonist is naloxone or a pharmaceutically acceptable salt thereof present in an amount that corresponds to an equiantagonistic amount of naltrexone or a pharmaceutically acceptable salt thereof, and said opioid agonist is oxycodone or a pharmaceutically acceptable salt thereof, wherein the ratio of the equiantagonistic amount of naltrexone or pharmaceutically acceptable salt thereof to oxycodone or pharmaceutically acceptable salt thereof is from about 0.037:1 to about 0.296:1.

13. The oral dosage form of claim 12, wherein the ratio of the equiantagonistic amount of naltrexone or pharmaceutically acceptable salt thereof to oxycodone or pharmaceutically acceptable salt thereof is from about 0.056:1 to about 0.222:1.

14. The oral dosage form of claim 11, wherein the sustained release carrier further causes said opioid antagonist to be released over a time period of about 8 to about 24 hours when orally administered to a human patient.

15. The oral dosage form of claim 1, wherein the dosage form is formulated for twice-a-day or once-a-day administration.

16. The oral dosage form of claim 6, wherein the oxycodone or pharmaceutically acceptable salt thereof is present in the dosage form in an amount that is equianalgesic to about 8 mg to about 50 mg hydrocodone or a pharmaceutically acceptable salt thereof.

17. The oral dosage form of claim 16, wherein said opioid antagonist is naloxone or a pharmaceutically acceptable salt thereof.
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