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Details for Patent: 8,524,275

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Details for Patent: 8,524,275

Title:Pharmaceutical formulations containing opioid agonist, opioid antagonist and gelling agent
Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of an opioid analgesic, an opioid antagonist and one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid.
Inventor(s): Oshlack; Benjamin (New York, NY), Wright; Curtis (Norwalk, CT), Breder; Christopher (Greenwich, CT)
Assignee: Purdue Pharma L.P. (Stamford, CT) The P.F Laboratories, Inc. (Totowa, NJ) Purdue Pharmaceuticals, L.P. (Wilson, NC)
Filing Date:Oct 21, 2010
Application Number:12/909,527
Claims:1. An oral dosage form comprising: a therapeutically effective amount of an opioid analgesic, an opioid antagonist, one or more pharmaceutically acceptable excipients, and particles of a gelling agent in a substantially non-releasable form, the particles consisting of the gelling agent formulated with effective amounts of (i) one or more pharmaceutically acceptable hydrophobic material(s) selected from the group consisting of cellulose polymers, acrylic polymers, polylactic acid, polyglycolic acid and a co-polymer of the polylactic acid and polyglycolic acid, and (ii) one or more additional pharmaceutically acceptable excipient(s) to sequester the gelling agent such that the gelling agent is not substantially released from the dosage form which is administered intact, but is released from the dosage form which is crushed in an effective amount to hinder, deter or prevent the administration of the crushed dosage form and form a viscous gel with a viscosity of at least about 10 cP when the crushed dosage form is mixed with from about 0.5 to about 10 ml of an aqueous liquid, wherein the opioid antagonist is in an effective amount to attenuate a side effect of the opioid analgesic, the gelling agent is selected from the group consisting of polyethylene oxides, surfactants, emulsifiers and mixtures thereof, and a weight ratio of the gelling agent to the opioid analgesic is from about 1:40 to about 40:1.

2. The oral dosage form of claim 1, wherein the dosage form provides pain relief for at least about 12 hours when orally administered intact to a human patient.

3. The oral dosage form of claim 1, wherein said opioid analgesic is selected from the group consisting of levorphanol, meperidine, dihydrocodeine, dihydromorphine, pharmaceutically acceptable salts thereof, and mixtures thereof.

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

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

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

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

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

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

10. The oral dosage form of claim 1, wherein said ratio of said gelling agent to said opioid analgesic is from about 1:1 to about 30:1.

11. The oral dosage form of claim 1, wherein said ratio of said gelling agent to said opioid analgesic is from about 2:1 to about 10:1.

12. The oral dosage form of claim 1, wherein said gelling agent is in an effective amount to impart a viscosity unsuitable for administration by a route selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the crushed dosage form is mixed with from about 1 to about 3 ml of the aqueous liquid.

13. A method of preventing abuse of an oral dosage form of an opioid analgesic comprising: preparing a dosage form comprising an analgesically effective amount of an opioid analgesic, an opioid antagonist, one or more pharmaceutically acceptable excipients, and particles wherein the particles consist of a gelling agent formulated with an effective amount(s) of one or more pharmaceutically acceptable hydrophobic material(s) and one or more additional pharmaceutically acceptable excipient(s) which sequester the gelling agent such that the gelling agent is not substantially released from the dosage form which is administered intact, but is released in an effective amount to impart a viscosity of at least about 10 cP to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid and which renders the solubilized mixture unsuitable for administration by a route selected from the group consisting of parenteral and nasal administration, wherein the gelling agent is selected from the group consisting of polyethylene oxides, surfactants, emulsifiers and mixtures thereof, and the one or more pharmaceutically acceptable hydrophobic material(s) are selected from the group consisting of cellulose polymers, acrylic polymers, polylactic acid, polyglycolic acid and a co-polymer of the polylactic acid and polyglycolic acid.

14. The method of claim 13, wherein the dosage form provides effective pain relief for at least about 12 hours when orally administered intact to a human patient.

15. The method of claim 13, wherein the solubilized mixture has a viscosity of at least about 60 cP.

16. The method of claim 13, wherein said opioid analgesic is selected from the group consisting of morphine, hydromorphone, hydrocodone, oxycodone, codeine, levorphanol, meperidine, dihydrocodeine, dihydromorphine, oxymorphone, pharmaceutically acceptable salts thereof and mixtures thereof.

17. A controlled release oral dosage form comprising: a therapeutically effective amount of an opioid analgesic, an opioid antagonist, one or more pharmaceutically acceptable excipients, and particles of a gelling agent in a substantially non-releasable form, the particles consisting of the gelling agent and one or more pharmaceutically acceptable hydrophobic material(s) and one or more additional pharmaceutically acceptable excipient(s), wherein the gelling agent is coated with a coating or dispersed in a matrix consisting of effective amounts of the one or more pharmaceutically acceptable hydrophobic materials(s) and one or more additional pharmaceutically acceptable excipient(s) to sequester the gelling agent such that the gelling agent is not substantially released from the dosage form which is administered intact, but is released from the dosage form which is crushed in an effective amount to impart a viscosity of at least about 10 cP to a solubilized mixture formed when the crushed dosage form is mixed with from about 0.5 to about 10 ml of an aqueous liquid and which renders the solubilized mixture unsuitable for administration by a route selected from the group consisting of parenteral and nasal administration, wherein the one or more pharmaceutically acceptable hydrophobic material(s) are selected from the group consisting of cellulose polymers, acrylic polymers, polylactic acid, polyglycolic acid and a co-polymer of the polylactic acid and polyglycolic acid, and said intact dosage form provides pain relief for at least about 12 hours when orally administered to a human patient.

18. A method of preventing abuse of an oral controlled release dosage form of an opioid analgesic comprising: preparing a dosage form with an analgesically effective amount of the opioid analgesic, an opioid antagonist, one or more pharmaceutically acceptable excipients, and particles consisting of a gelling agent and effective amounts of one or more pharmaceutically acceptable hydrophobic material(s) and one or more additional pharmaceutically acceptable excipient(s) to sequester the gelling agent such that the gelling agent is not substantially released from the dosage form which is administered intact, but is released from the dosage form which is crushed in an effective amount to impart a viscosity of at least about 10 cP to a solubilized mixture formed when the crushed dosage form is mixed with from about 0.5 to about 10 ml of an aqueous liquid and which renders the solubilized mixture unsuitable for administration by a route selected from the group consisting of parenteral and nasal administration, wherein the gelling agent is coated with a coating or dispersed in a matrix consisting of said effective amounts of one or more pharmaceutically acceptably hydrophobic material(s) and additional excipient(s), wherein the one or more pharmaceutically acceptable hydrophobic material(s) are selected from the group consisting of cellulose polymers, acrylic polymers, polylactic acid, polyglycolic acid and a co-polymer of the polylactic acid and polyglycolic acid, said intact dosage form providing effective pain relief for at least about 12 hours when orally administered to a human patient.

19. A method of treating pain comprising: administering to a patient a dosage form according to claim 1 wherein the dosage form is administered intact.

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

21. The oral dosage form of claim 1, wherein the side effect of said opioid analgesic is selected from the group consisting of anti-analgesia, hyperalgesia, hyperexcitability, physical dependence, tolerance, and a combination of any of the foregoing.

22. The oral dosage form of claim 1, wherein the amount of antagonist released during a dosing interval enhances the analgesic potency of the opioid analgesic.

23. The oral dosage form of claim 1, wherein the amount of the opioid antagonist is about 100 to about 1000 fold less than the amount of the opioid agonist.

24. The oral dosage form of claim 17 wherein the gelling agent is polyethylene oxide.

25. The dosage form of claim 1, wherein the gelling agent is coated with a coating consisting of the one or more pharmaceutically acceptable hydrophobic material(s) and one or more additional pharmaceutically acceptable excipient(s).

26. The dosage form of claim 17, wherein said viscosity is imparted when the crushed dosage form is mixed with from about 0.5 to about 10 ml of the aqueous liquid and thereafter heated.

27. The method of claim 18, wherein said viscosity is imparted when the crushed dosage form is mixed with from about 0.5 to about 10 ml of the aqueous liquid and thereafter heated.
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