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Last Updated: March 19, 2024

Details for Patent: 8,936,808


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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)
Filing Date:Sep 18, 2014
Application Number:14/490,493
Claims:1. An immediate release oral dosage form, comprising: an opioid agonist present as an orally therapeutically effective dose of buprenorphine or a pharmaceutically acceptable salt thereof; and an opioid antagonist selected from naltrexone, naloxone, nalmephene, cyclazocine, levallorphan, and mixtures thereof, and pharmaceutically acceptable salts thereof; said dosage form having a ratio of said opioid antagonist to said opioid agonist that provides a combination product which is therapeutically effective when the combination is administered orally, but which is aversive in physically dependent human subjects when orally 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 orally taking about 2-3 times said therapeutically effective dose.

3. 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, acetaminophen, aspirin, an NMDA receptor antagonist, a drug that blocks a major intracellular consequence of NMDA-receptor activation, an antitussive, an expectorant, a decongestant, and an antihistamine and mixtures thereof.

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

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

6. The oral dosage form of claim 5, wherein the buprenorphine 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.

7. The oral dosage form of claim 5, wherein the buprenorphine or pharmaceutically acceptable salt thereof is present in the dosage form in an amount that is equianalgesic to about 2 mg to about 64 mg hydromorphone hydrochloride.

8. The oral dosage form of claim 5, wherein the buprenorphine or pharmaceutically acceptable salt thereof is present in the dosage form in an amount that is equianalgesic to about 2.5 mg to about 800 mg morphine or a pharmaceutically acceptable salt thereof.

9. The oral dosage form of claim 5, wherein the buprenorphine or pharmaceutically acceptable salt thereof is present in the dosage form in an amount that is equianalgesic to about 2.5 mg to about 800 mg oxycodone or a pharmaceutically acceptable salt thereof.

10. The oral dosage form of claim 5, wherein the buprenorphine or pharmaceutically acceptable salt thereof is present in the dosage form in an amount that is equianalgesic to about 25 mg to about 800 mg tramadol or a pharmaceutically acceptable salt thereof.

11. The oral dosage form of claim 5, wherein the dosage form comprises a cellulose ether.

12. The oral dosage form of claim 5, wherein the dosage form comprises a hydroxyalkylcellulose.

13. The oral dosage form of claim 5, wherein the dosage form comprises hydroxypropylmethylcellulose.

14. The oral dosage form of claim 5, wherein the dosage form comprises polyethylene glycol.

15. The oral dosage form of claim 5, wherein the dosage form includes a carbohydrate.

16. The oral dosage form of claim 5, wherein the dosage form is in the form of an oral suppository.

17. The oral dosage form of claim 5, wherein the dosage form is in the form of a buccal tablet.

18. The oral dosage form of claim 5, wherein the dosage form is formulated for sublingual administration.

19. A method of reducing oral abuse of an oral opioid formulation comprising administering the oral dosage form of claim 1 to a subject in need thereof.

20. The method of claim 19, wherein said opioid antagonist is naloxone or a pharmaceutically acceptable salt thereof.

21. The method of claim 20, wherein the buprenorphine or pharmaceutically acceptable salt thereof is present in the dosage form in an amount that is equianalgesic to about 2 mg to about 64 mg hydromorphone hydrochloride.

22. The method of claim 20, wherein the buprenorphine or pharmaceutically acceptable salt thereof is present in the dosage form in an amount that is equianalgesic to about 2.5 mg to about 800 mg morphine or a pharmaceutically acceptable salt thereof.

23. The method of claim 20, wherein the buprenorphine or pharmaceutically acceptable salt thereof is present in the dosage form in an amount that is equianalgesic to about 2.5 mg to about 800 mg oxycodone or a pharmaceutically acceptable salt thereof.

24. The method of claim 20, wherein the buprenorphine or pharmaceutically acceptable salt thereof is present in the dosage form in an amount that is equianalgesic to about 25 mg to about 800 mg tramadol or a pharmaceutically acceptable salt thereof.

25. The method of claim 20, wherein the dosage form comprises a cellulose ether.

26. The method of claim 20, wherein the dosage form comprises a hydroxyalkylcellulose.

27. The method of claim 20, wherein the dosage form comprises hydroxypropylmethylcellulose.

28. The method of claim 20, wherein the dosage form comprises polyethylene glycol.

29. The method of claim 20, wherein the dosage form is in the form of an oral suppository or a buccal tablet.

30. The method of claim 20, wherein the dosage form is administered sublingually.

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