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Details for Patent: 9,101,668

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Details for Patent: 9,101,668

Title:Pharmaceutical formulation 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 (Greenwhich, CT)
Assignee: Purdue Pharma L.P. (Stamford, CT) Purdue Pharmaceuticals L.P. (Wilson, NC) The P.F. Laboratories, Inc. (Totowa, NJ)
Filing Date:Aug 01, 2013
Application Number:13/956,467
Claims:1. An oral dosage form comprising: (a) an analgesically effective amount of an opioid agonist, (b) an opioid antagonist in an effective amount to attenuate a side effect of the opioid agonist, and (c) a gelling agent selected from the group consisting of polyethylene oxides, surfactants, emulsifiers and mixtures thereof, wherein a weight ratio of the gelling agent to the opioid agonist is from about 1:40 to about 40:1, and a portion of the gelling agent is combined 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 form particles consisting of said portion of the gelling agent, said one or more pharmaceutically acceptable hydrophobic material(s), and said one or more additional pharmaceutically acceptable excipient(s) and sequester said portion of the gelling agent such that the gelling agent is not released from the dosage form which is administered intact, but is released from the dosage form which is subjected to tampering by crushing, shearing, grinding and dissolution in from about 0.5 to about 10 ml of an aqueous liquid in an effective amount to form a gel having a viscosity of at least about 10 cP.

2. The oral dosage form of claim 1, wherein the opioid agonist is selected from the group consisting of oxycodone, codeine, hydrocodone, hydromorphone, levorphanol, meperidine, morphine, pharmaceutically acceptable salts thereof, and mixtures thereof.

3. The oral dosage form of claim 1, wherein the opioid antagonist is naloxone or a pharmaceutically acceptable salt thereof.

4. The oral dosage form of claim 1, wherein the opioid antagonist is in a substantially non-releasable form and does not substantially block the analgesic effect of the opioid agonist when the dosage form is orally administered intact.

5. The oral dosage form of claim 1, wherein a weight ratio of the opioid agonist and the opioid antagonist is from about 1:1 to about 10:1.

6. The oral dosage form of claim 1, wherein a weight ratio of the gelling agent to the opioid agonist is from about 1:1 to about 30:1.

7. An oral dosage form comprising: (a) an analgesically effective amount of an opioid agonist, (b) naloxone or a pharmaceutically acceptable salt thereof in an effective amount to attenuate a side effect of the opioid agonist, and (c) a gelling agent selected from the group consisting of polyethylene oxides, surfactants, emulsifiers and mixtures thereof, wherein a weight ratio of the gelling agent to the opioid agonist is from about 1:40 to about 40:1, and a portion of the gelling agent is combined 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 form particles consisting of said portion of the gelling agent, said one or more pharmaceutically acceptable hydrophobic material(s), and said one or more additional pharmaceutically acceptable excipient(s) and sequester said portion of the gelling agent such that the gelling agent is not released from the dosage form which is administered intact, but is released from the dosage form which is subjected to tampering by crushing, shearing, or grinding in an effective amount to form a viscous gel upon administration of the tampered dosage form to nasal passages and render the tampered dosage form unsuitable for nasal administration.

8. The oral dosage form of claim 7, wherein the opioid agonist is selected from the group consisting of oxycodone, codeine, hydrocodone, hydromorphone, levorphanol, meperidine, morphine, pharmaceutically acceptable salts thereof, and mixtures thereof.

9. The oral dosage form of claim 7, wherein the opioid antagonist is in a substantially non-releasable form and does not substantially block the analgesic effect of the opioid agonist when the dosage form is orally administered intact.

10. The oral dosage form of claim 7, wherein a weight ratio of the opioid agonist and the opioid antagonist is from about 1:1 to about 10:1.

11. The oral dosage form of claim 7, wherein a weight ratio of the gelling agent to the opioid agonist is from about 1:1 to about 30:1.

12. The oral dosage form of claim 7, wherein a weight ratio of the gelling agent to the opioid agonist is from about 2:1 to about 10:1.

13. The oral dosage form of claim 7, wherein the viscous gel has a viscosity of at least about 10 cP.

14. An oral dosage form comprising: (a) an analgesically effective amount of an opioid agonist, (b) naloxone or a pharmaceutically acceptable salt thereof in an effective amount to attenuate a side effect of the opioid agonist, and (c) a gelling agent selected from the group consisting of polyethylene oxides, surfactants, emulsifiers and mixtures thereof, wherein a weight ratio of the gelling agent to the opioid agonist is from about 1:40 to about 40:1, and a portion of the gelling agent is combined 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 form particles consisting of said portion of the gelling agent, said one or more pharmaceutically acceptable hydrophobic material(s), and said one or more additional pharmaceutically acceptable excipient(s) and sequester said portion of the gelling agent such that the gelling agent is not released from the dosage form which is administered intact, but is released from the dosage form which is subjected to tampering by crushing, shearing, grinding, chewing, dissolution in a solvent, heating or any combination thereof.

15. The oral dosage form of claim 14, wherein the opioid agonist is selected from the group consisting of oxycodone, codeine, hydrocodone, hydromorphone, levorphanol, meperidine, morphine, pharmaceutically acceptable salts thereof, and mixtures thereof.

16. The oral dosage form of claim 14, wherein the opioid antagonist is in a substantially non-releasable form and does not substantially block the analgesic effect of the opioid agonist when the dosage form is orally administered intact.

17. The oral dosage form of claim 14, wherein a weight ratio of the opioid agonist and the opioid antagonist is from about 1:1 to about 10:1.

18. The oral dosage form of claim 14, wherein a weight ratio of the gelling agent to the opioid agonist is from about 1:1 to about 30:1.

19. The oral dosage form of claim 14, wherein a weight ratio of the gelling agent to the opioid agonist is from about 2:1 to about 10:1.

20. The dosage form of claim 14, wherein the dosage form forms a mixture having a viscosity of at least 60 cP when crushed and dissolved in from 1 to about 5 ml of an aqueous liquid.

21. The dosage form of claim 14, wherein the gelling agent is in an effective amount to render the dosage form aversive to nasal administration.

22. The dosage form of claim 1, wherein said viscosity renders the dosage form unsuitable for nasal administration.
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