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Claims for Patent: 8,658,198

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Claims for Patent: 8,658,198

Title:Non-abusable pharmaceutical composition comprising opioids
Abstract: There is provided pharmaceutical compositions for the treatment of pain comprising a pharmacologically-effective amount of an opioid analgesic, or a pharmaceutically-acceptable salt thereof, presented in particulate form upon the surfaces of carrier particles comprising a pharmacologically-effective amount of an opioid antagonist, or a pharmaceutically-acceptable salt thereof, which carrier particles are larger in size than the particles of the opioid analgesic. The compositions are also useful in prevention of opioid abuse by addicts.
Inventor(s): Pettersson; Anders (Kode, SE)
Assignee: Orexo AB (Uppsala, SE)
Application Number:13/799,117
Patent Claims: 1. A particulate transmucosal pharmaceutical composition in the form of a tablet suitable for sublingual or buccal administration comprising a pharmacologically-effective amount of an opioid analgesic, or a pharmaceutically-acceptable salt thereof, in the form of particles, which particles are attached to, are adhered to, or are associated with surfaces of carrier particles comprising a pharmacologically-effective amount of an opioid antagonist, or a pharmaceutically-acceptable salt thereof, which carrier particles are larger in size than the particles of the opioid analgesic, wherein both of said opioid analgesic and said opioid antagonist are delivered transmucosally, wherein the opioid analgesic is selected from fentanyl, alfentanil, sufentanil, remifentanil and buprenorphine, and the opioid antagonist is selected from nalmefene, methylnaltrexone, naltrexone and naloxone, and wherein the carrier particles further comprise a pharmaceutically-acceptable substance selected from a carbohydrate, a pharmaceutically-acceptable inorganic salt or a polymer, or a mixture thereof.

2. The particulate transmucosal pharmaceutical composition of claim 1, wherein the pharmaceutically-acceptable substance comprises sugar, mannitol, lactose, sodium chloride, calcium phosphate, dicalcium phosphate hydrate, dicalcium phosphate dehydrate, tricalcium phosphate, calcium carbonate, barium sulfate; microcrystalline cellulose, cellulose, cross linked polyvinylpyrrolidone or a mixture thereof.

3. The particulate transmucosal pharmaceutical composition of claim 1, wherein the pharmaceutically-acceptable substance comprises mannitol, microcrystalline cellulose, cellulose, cross linked polyvinylpyrrolidone or a mixture thereof.

4. The particulate transmucosal pharmaceutical composition of claim 1, wherein the opioid analgesic is in the form of microparticles.

5. The particulate transmucosal pharmaceutical composition of claim 4, wherein the microparticles have a weight based mean diameter of less than about 15 .mu.m.

6. The particulate transmucosal pharmaceutical composition of claim 1, wherein the total amount of opioid analgesic that is employed is in the range of about 0.0005% to about 20% by weight based upon the total weight of the composition.

7. The particulate transmucosal pharmaceutical composition of claim 6 wherein the range is about 1% to about 7%.

8. The particulate transmucosal pharmaceutical composition of claim 1, wherein the amount of opioid analgesic that is present is sufficient to provide a dose per unit dosage form of between about 1 .mu.g and about 20 mg.

9. The particulate transmucosal pharmaceutical composition of claim 8, wherein the amount is between about 5 .mu.g and about 15 mg.

10. The particulate transmucosal pharmaceutical composition of claim 1, wherein the opioid antagonist is naloxone.

11. The particulate transmucosal pharmaceutical composition of claim 1, wherein the carrier particles are of a size that is between about 50 and about 1,000 .mu.m.

12. The particulate transmucosal pharmaceutical composition of claim 1, wherein the carrier particles are of a size that is between about 100 and about 800 .mu.m.

13. The particulate transmucosal pharmaceutical composition of claim 1, which further comprises a bioadhesion or a mucoadhesion promoting agent, which agent is, at least in part, presented on the surfaces of the carrier particles.

14. The particulate transmucosal pharmaceutical composition of claim 13, wherein the bioadhesion or mucoadhesion promoting agent is a polymeric substance with a weight average molecular weight above 5,000.

15. The particulate transmucosal pharmaceutical composition of claim 13, wherein the bioadhesion or mucoadhesion promoting agent is selected from a cellulose derivative, a starch derivative, an acrylic polymer, polyvinylpyrrolidone, polyethylene oxide, chitosan, a natural polymer, scleroglucan, xanthan gum, guar gum, poly co-(methylvinyl ether/maleic anhydride) and crosscarmellose, or a mixture thereof.

16. The particulate transmucosal pharmaceutical composition of claim 13, wherein the bioadhesion or mucoadhesion promoting agent is selected from hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, methyl cellulose, ethyl hydroxyethyl cellulose, carboxymethyl cellulose, modified cellulose gum, sodium carboxymethyl cellulose, moderately cross-linked starch, modified starch, sodium starch glycolate, carbomer or a derivative thereof, crosslinked polyvinylpyrrolidone, polyethylene oxide, chitosan, gelatin, sodium alginate, pectin, scleroglucan, xanthan gum, guar gum, poly co-(methylvinyl ether/maleic anhydride) and crosscarmellose sodium, or a mixture thereof.

17. The particulate transmucosal pharmaceutical composition of claim 13, wherein the bioadhesion or mucoadhesion promoting agent is crosscarmellose sodium or crosslinked polyvinylpyrrolidone.

18. The particulate transmucosal pharmaceutical composition of claim 13, wherein the amount of bioadhesion or mucoadhesion promoting agent present is in the range of about 0.1 to about 25% by weight based upon the total weight of the composition.

19. The particulate transmucosal pharmaceutical composition of claim 13, wherein the amount of bioadhesion or mucoadhesion promoting agent present is in the range of about 1 to about 15% by weight based upon the total weight of the composition.

20. The particulate transmucosal pharmaceutical composition of claim 13, wherein the bioadhesion or mucoadhesion promoting agent has a particle size in the range of about 1 to about 100 .mu.m.

21. The particulate transmucosal pharmaceutical composition of claim 1, wherein the composition further comprises a disintegrating agent, which is capable of accelerating to a measurable degree the disintegration or dispersion of a composition of the invention or the carrier particles.

22. The particulate transmucosal pharmaceutical composition of claim 21, wherein said disintegrating agent is capable of swelling and/or expanding when placed in contact with water and/or mucous or saliva, thus causing the composition and/or carrier particles to disintegrate when so wetted.

23. The particulate transmucosal pharmaceutical composition of claim 21, wherein the disintegrating agent may also function as a bioadhesion or mucoadhesion promoting agent.

24. The particulate transmucosal pharmaceutical composition of claim 23, wherein the disintegrating agent is: (a) presented between carrier particles; (b) attached to, adhered to and/or associated with the surfaces of carrier particles; and/or (c) presented within carrier particles.

25. The particulate transmucosal pharmaceutical composition of claim 21, wherein the disintegrating agent is selected from the group consisting of crosslinked polyvinylpyrrolidone, carboxymethyl starch, natural starch and mixtures thereof.

26. The particulate transmucosal pharmaceutical composition of claim 21, wherein the amount of disintegrating agent is between about 2 and about 7% by weight based upon the total weight of the composition.

27. A method which comprises sublingual or buccal administration of the composition of claim 1 to a patient.

28. The method of claim 27, wherein said composition is resistant to abuse by an opioid dependent individual.

29. The method of claim 27, wherein said patient is an opioid dependent individual.

30. A method of reversing one or more of the pharmacological effects of an opioid analgesic, which method comprises providing for sublingual or buccal administration to a patient the composition of claim 1.

31. The method of claim 30, wherein the pharmacological effect is euphoria.

32. A method of reversing the euphoric effects that may be produced by injection of a composition comprising an opioid analgesic, which method comprises providing for sublingual or buccal administration to a patient the composition of claim 1.

33. A method of treating narcotic drug overdose or diagnosing suspected opioid addiction, which method comprises administering the composition of claim 1 to a patient.
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