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Details for Patent: 7,157,103

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Details for Patent: 7,157,103

Title:Pharmaceutical formulation containing irritant
Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse; and an effective amount of an irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering.
Inventor(s): Sackler; Richard (Greenwich, CT)
Assignee: Euro-Celtique S.A. (Luxembourg, LU)
Filing Date:Aug 06, 2002
Application Number:10/214,410
Claims:1. An oral dosage form comprising: a therapeutically effective amount of an opioid analgesic; and an effective amount of a sequestered irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering, wherein said sequestered irritant is in the form of multiparticulates individually coated with a material that substantially prevents release of the irritant.

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 said opioid analgesic is morphine, codeine, tramadol, or a pharmaceutically acceptable salt thereof.

7. The oral dosage form of claim 1, wherein said opioid analgesic is hydromorphone or a pharmaceutically acceptable salt thereof.

8. The oral dosage form of claim 1, wherein said opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof.

9. The oral dosage form of claim 1, wherein said opioid analgesic is oxycodone or a pharmaceutically acceptable salt thereof.

10. The oral dosage form of claim 1, wherein said administration of said dosage form after tampering is oral administration.

11. The oral dosage form of claim 1, wherein said administration of said dosage form after tampering is nasal administration.

12. The oral dosage form of claim 1, wherein said administration of said dosage form after tampering is parenteral administration.

13. 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.

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

15. 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.

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

17. The oral dosage form of claim 16, wherein said excipient is a sustained release excipient.

18. The oral dosage form of claim 17, wherein said dosage form provides an analgesic effect for at least about 12 hours after oral administration to a human patient.

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

20. A method of treating pain comprising administering to a patient an oral dosage form of claim 1.

21. A method of preparing a pharmaceutical dosage form comprising combining a therapeutically effective amount of an opioid analgesic in a dosage form with an effective amount of a sequestered irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering wherein said sequestered irritant is in the form of multiparticulates individually coated with a material that substantially prevents release of the irritant.

22. The method of claim 21 wherein said irritant is at least partially interdispersed with the drug susceptible to abuse.

23. A method of preparing a pharmaceutical dosage form comprising combining an opioid analgesic in a dosage form with an effective amount of a sequestered irritant to impart an irritating sensation to an abuser upon administration, of said dosage form after tampering, wherein said sequestered irritant is in a matrix comprising a sequestering material that substantially prevents release of the irritant.

24. An oral dosage form comprising: a therapeutically effective amount of an opioid analgesic; and an effective amount of a sequestered irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering, wherein said sequestered irritant is in a matrix comprising a sequestering material that substantially prevents release of the irritant.

25. The oral dosage form of claim 24, wherein the irritant is selected from the group consisting of capsaicin, a capsaicin analog, and mixture thereof.

26. The oral dosage form of claim 24, wherein the irritant is a capsaincin analog selected from the group consisting of resiniferatoxin, tinyatoxin, heptanoyl isobutylamide, heptanoyl guaiacylamide, other isobutylamides or guaiacylamides, dihydrocapsaicin, homovanillyl octylester, nanonoyl vanillylamide, and mixture thereof.

27. The oral dosage form of claim 24, wherein the irritant is capsaicin.

28. The oral dosage form of claim 24, wherein the irritant is vanillylamide.

29. The oral dosage form of claim 24, wherein said opioid analgesic is morphine, codeine, tramadol or pharmaceutically acceptable salt thereof.

30. The oral dosage form of claim 24, wherein said opioid analgesic is hydromorphone or a pharmaceutically acceptable salt thereof.

31. The oral dosage form of claim 24, wherein said opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof.

32. The oral dosage form of claim 24, wherein said opioid analgesic is oxycodone or a pharmaceutically acceptable salt thereof.

33. The oral dosage form of claim 24, wherein said administration of said dosage form after tampering is oral administration.

34. The oral dosage form of claim 24, wherein said administration of said dosage form after tampering is nasal administration.

35. The oral dosage form of claim 24, wherein said administration of said dosage form after tampering is parenteral administration.

36. The oral dosage form of claim 24, wherein the irritant is in an amount of about 0.00125% to about 50% by weight of the dosage form.

37. The oral dosage form of claim 24, wherein the irritant is in an amount of about 1% to about 7.5% by weight of the dosage form.

38. The oral dosage form of claim 24, wherein the irritant is in an amount of about 1% to about 5% by weight of the dosage form.

39. The oral dosage forms of claim 24, further comprising a pharmaceutically acceptable excipient.

40. The oral dosage form of claim 39, wherein said excipient is a sustained release excipient.

41. The oral dosage form of claim 40, wherein said dosage form provides an analgesic effect for at least about 12 hours after oral administration to a human patient.

42. The oral dosage form of claim 24, wherein said irritant is at least partially interdispersed with the opioid analgesic.

43. A method of treating pain comprising administering to a patient an oral dosage form of claim 24.
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