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Details for Patent: 8,980,305

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Details for Patent: 8,980,305

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)
Filing Date:Mar 13, 2013
Application Number:13/799,310
Claims:1. A method of treating pain in a subject in need thereof comprising transmucosally administering 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 the group consisting of fentanyl, alfentanil, sufentanil, remifentanil and buprenorphine, and the opioid antagonist is selected from the group consisting of nalmefene, methylnaltrexone, naltrexone and naloxone.

2. The method of claim 1, wherein said pain is selected from the group consisting of severe pain, acute pain and breakthrough pain.

3. The method of claim 1, wherein the opioid analgesic is fentanyl.

4. The method of claim 1, wherein the opioid analgesic is in the form of microparticles.

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

6. The method 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 method of claim 6 wherein the range is about 1% to about 7%.

8. The method 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 method of claim 8, wherein the amount is between about 5 .mu.g and about 15 mg.

10. The method of claim 1, wherein the opioid antagonist is naloxone.

11. The method or claim 1, wherein the total amount of opioid antagonist that is employed is in the range of about 1% to about 99.9995% by weight based upon the total weight of the composition.

12. The method of claim 11, wherein the range is about 10% to about 98%.

13. The method of claim 1, wherein the amount of opioid antagonist that is present is sufficient to provide a dose per unit dosage form of between about 0.1 mg and about 10 mg.

14. The method of claim 13, wherein the amount is between about 1 and about 5 mg.

15. The method of claim 1, wherein the carrier particles are of a size that is between about 50 and about 1,000 .mu.m.

16. The method of claim 15, wherein the carrier particles are of a size that is between about 100 and about 800 .mu.m.

17. The method 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.

18. The method of claim 17, wherein the bioadhesion or mucoadhesion promoting agent is a polymeric substance with a weight average molecular weight above 5,000.

19. The method of claim 17, wherein the hioadhesion 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 guru, poly co-(methylvinyl ether/maleic anhydride) and crosscarmellose, or a mixture thereof.

20. The method of claim 17, wherein the hioadhesion 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.

21. The method of claim 17, wherein the bioadhesion or mucoadhesion promoting agent is crosscarmellose sodium or crosslinked polyvinylpyrrolidone.

22. The method of claim 17, 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.

23. The method of claim 17, 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.

24. The method of claim 17, wherein the bioadhesion or mucoadhesion promoting agent has a particle size in the range of about 1 to about 100 .mu.m.

25. The method of claim 1, 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.

26. The particulate transmucosal pharmaceutical composition of claim 25, 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, crosslinked polyvinylpyrrolidone or a mixture thereof.

27. The particulate transmucosal pharmaceutical composition of claim 25, wherein the pharmaceutically-acceptable substance comprises mannitol, microcrystalline cellulose, cellulose, crosslinked polyvinylpyrrolidone or a mixture thereof.

28. The method 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.

29. The method of claim 28, 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.

30. The method of claim 28, wherein the disintegrating agent may also function as a bioadhesion or mucoadhesion promoting agent.

31. The method of claim 28, wherein the disintegrating agent is: (a) presented between carrier particles; (b) attached to, adhered to and/or associated with the surfaces of carrier particles; (c) presented within carrier particles.

32. The method of claim 28, wherein the disintegrating agent is selected from the group consisting of crosslinked polyvinylpyrrolidone, carboxymethyl starch, natural starch and mixtures thereof.

33. The method of claim 28, wherein the amount of disintegrating agent is between about 2% and about 7% by weight based upon the total weight of the composition.

34. The method of claim 1, wherein said composition is resistant to abuse by an opioid dependent individual.

35. The method of claim 1, wherein said patient is an opioid dependent individual.
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