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Last Updated: March 28, 2024

Details for Patent: 8,652,515


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Title:Pharmaceutical formulation containing an opioid agonist, opioid antagonist and irritant agent
Abstract: Disclosed in certain embodiments is an oral dosage form comprising: a therapeutically effective amount of an opioid analgesic; an opioid antagonist; and an irritant in an effective amount to impart an irritating sensation to an abuser upon administration of the dosage form after tampering.
Inventor(s): Sackler; Richard (Greenwich, CT)
Assignee: Purdue Pharma L.P. (Stamford, CT)
Filing Date:Sep 12, 2011
Application Number:13/230,185
Claims:1. An oral dosage form comprising: a therapeutically effective amount of an opioid analgesic selected from the group consisting of hydrocodone, morphine, hydromorphone, oxycodone, codeine, levorphanol, meperidine, methadone, oxymorphone, buprenorphine, fentanyl, dipipanone, salts thereof, and mixtures thereof; an opioid antagonist selected from the group consisting of naltrexone, naloxone, nalmefene, nalorphine, cyclazocine, levallorphan, pharmaceutically acceptable salts thereof, and mixtures thereof; and an irritant in an effective amount to impart an irritating sensation to an abuser upon administration of said dosage form after tampering.

2. The oral dosage form of claim 1, wherein the irritant is selected from the group consisting of capsaicin, a capsaicin analog, and mixtures thereof.

3. The oral dosage form of claim 1, wherein the irritant is a capsaicin analog selected from the group consisting of resiniferatoxin, tinyatoxin, heptanoylisobutylamide, heptanoyl guaiacylamide, other isobutylamides or guaiacylamides, dihydrocapsaicin, homovanillyl octylester, nonanoyl vanillylamide, and mixtures thereof.

4. The oral dosage form of claim 1, wherein the irritant is capsaicin.

5. The oral dosage form of claim 1, wherein the irritant is vanillylamide.

6. The oral dosage form of claim 1, wherein the irritant is in a sequestered form.

7. The oral dosage form of claim 1, wherein the antagonist is in a sequestered form.

8. The oral dosage form of claim 1, wherein the antagonist and the irritant are both in sequestered forms.

9. The oral dosage form of claim 1, wherein the irritant is in an amount of about 0.00125% to about 50% by weight of the dosage form.

10. The oral dosage form of claim 1, wherein the irritant is in an amount of about 1% to about 7.5% by weight of the dosage form.

11. The oral dosage form of claim 1, wherein the irritant is in an amount of about 1% to about 5% by weight of the dosage form.

12. The oral dosage form of claim 1, further comprising a pharmaceutically acceptable excipient.

13. The oral dosages form of claim 12, wherein said excipient is a sustained release excipient.

14. The oral dosage form of claim 12, said dosage form providing an analgesic effect for from about 12 hours to about 24 after oral administration to a human patient.

15. The oral dosage form of claim 1, wherein said irritant is at least partially interdispersed with the opioid analgesic.

16. The oral dosage form of claim 1 wherein the antagonist is in an amount to attenuate a side effect of said opioid agonist selected from the group consisting of anti-analgesia, hyperalgesia, hyperexcitability, physical dependence, tolerance, and a combination of any of the foregoing.

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

18. The oral dosage form of claim 17, wherein the opioid analgesic is oxycodone or a pharmaceutically acceptable salt thereof.

19. The dosage form of claim 18, wherein the dosage form is a controlled release oral dosage form.

20. The dosage form of claim 19, wherein the dosage form provides effective pain relief for from about 12 hours to about 24 hours after oral administration to a human patient.

21. The dosage form of claim 18, wherein the dosage form includes a controlled release material which is incorporated into a matrix along with the opioid analgesic and the opioid antagonist.

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