.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 7,144,587

« Back to Dashboard

Details for Patent: 7,144,587

Title:Pharmaceutical formulation containing opioid agonist, opioid antagonist and bittering agent
Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of an opioid analgesic; an opioid antagonist; and a bittering agent in an effective amount to impart a bitter taste to an abuser upon administration of the dosage form after tampering.
Inventor(s): Oshlack; Benjamin (New York, NY), Colucci; Robert (Newtown, CT), Wright; Curtis (Norwalk, CT), Breder; Christopher (Greenwich, CT)
Assignee: Euro-Celtique S.A. (Luxembourg, LU)
Filing Date:Aug 06, 2002
Application Number:10/213,921
Claims:1. An oral dosage form comprising: a therapeutically effective amount of an opioid analgesic; a sequestered opioid antagonist; and a sequestered bittering agent, which bittering agent and opioid antagonist are substantially released only upon tampering of the dosage form in an amount sufficient to impart a bitter taste to an abuser upon oral administration of said tampered dosage form.

2. The oral dosage form of claim 1, wherein the bittering agent is selected from the group consisting of flavor oils; flavoring aromatics; oleoresins; extracts derived from plants; sucrose derivatives; chlorosucrose derivatives; quinine sulphate; denatonium benzoate; and combinations thereof.

3. The oral dosage form of claim 1, wherein the bittering agent is a flavor oil selected from the group consisting of spearmint oil, peppermint oil, eucalyptus oil, oil of nutmeg, allspice, mace, oil of bitter almonds, menthol and combinations thereof.

4. The oral dosage form of claim 1, wherein the bittering agent is a fruit flavor selected from the group consisting of lemon, orange, lime, grapefruit, and mixtures thereof.

5. The oral dosage form of claim 1, wherein the bittering agent is denatonium benzoate.

6. The oral dosage form of claim 1, wherein said bittering agent is in an amount of less than about 50% by weight of the dosage form.

7. The oral dosage form of claim 1, wherein said bittering agent is in an amount of less than about 10% by weight of the dosage form.

8. The oral dosage form of claim 1, wherein said bittering agent is in an amount of less than about 5% by weight of the dosage form.

9. The oral dosage form of claim 1, wherein said bittering agent is in an amount of from about 0.1 to 1.0 percent by weight of the dosage form.

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

11. The oral dosage form of claim 10, wherein said excipient is a sustained release excipient.

12. The oral dosage form of claim 11, said dosage form providing an analgesic effect for at least about 12 hours after oral administration to a human patient.

13. The oral dosage form of claim 1 wherein said bittering agent is at least partially interdispersed with the opioid analgesic.

14. The oral dosage form of claim 1 having a ratio of opioid antagonist to opioid agonist that is analgesically effective when the combination is administered orally, but which is aversive in physically dependent human subjects when administered to physically dependent human subjects at the same amount or at a higher amount than said therapeutically effective amount.

15. The oral dosage form of claim 14 wherein said ratio of opioid antagonist to opioid agonist maintains an analgesic effect but does not increase analgesic efficacy of the opioid agonist relative to the same therapeutic amount of opioid analgesic when administered to human patients without said opioid antagonist.

16. The oral dosage form of claim 1, wherein the antagonist is in an amount effective 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 amount of antagonist released during the dosing interval enhances the analgesic potency of the opioid agonist.

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

19. A method of preparing a pharmaceutical oral dosage form comprising combining a therapeutically effective amount of an opioid analgesic and a sequestered opioid antagonist into an oral dosage form with a sequestered bittering agent, which sequestered bittering agent and sequestered opiod antagonist are substantially released only upon tampering of the oral dosage form in an amount sufficient to impart a bitter taste to an abuser upon oral administration of said tampered dosage form.

20. The method of claim 19, wherein said bittering agent is at least partially interdispersed with the opioid analgesic.

21. The oral dosage form of claim 1, wherein said bittering agent is present in multiparticulates individually coated with a material that prevents substantial release of the bittering agent.

22. The oral dosage form of claim 1, wherein said bittering agent is dispersed in a matrix comprising a sequestering material that prevents substantial release of the bittering agent.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc