Details for Patent: 9,561,225

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 (Boca Raton, FL), Wright; Curtis (Rockport, MA), Breder; Christopher (Greenwhich, CT)
Assignee:	Purdue Pharma L.P. (Stamford, CT) The P.F. Laboratories, Inc. (Totowa, NJ) Purdue Pharmaceuticals L.P. (Wilson, NC)
Filing Date:	Jul 07, 2015
Application Number:	14/793,174
Claims:	1. A controlled release oral dosage form comprising: a therapeutically effective amount of an opioid analgesic, from about 10 ng to 275 mg of an opioid antagonist, and particles consisting of a gelling agent, 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 one or more additional pharmaceutically acceptable excipient(s), wherein the gelling agent is releasable from said particles and a solubilized mixture having a viscosity of at least about 10 cP is formed when the dosage form is crushed and dissolved in from about 1 to about 5 ml of water, a weight ratio of the gelling agent to the opioid analgesic is from about 1:40 to about 40:1, and the gelling agent is polyethylene oxide. 2. The dosage form of claim 1, wherein the viscosity is 10 Cp. 3. The dosage form of claim 1, wherein the viscosity is at least 60 cP. 4. The dosage form of claim 1, wherein the viscosity is from 10 cP to 60 cP. 5. The 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. 6. The oral dosage form of claim 1, wherein the opioid analgesic is selected from the group consisting of oxycodone, codeine, hydrocodone, hydromorphone, levorphanol, meperidine, morphine, pharmaceutically acceptable salts thereof, and mixtures thereof. 7. The dosage form of claim 6, wherein the opioid analgesic is oxycodone or a pharmaceutically acceptable salt thereof. 8. The oral dosage form of claim 1, wherein the opioid antagonist is naloxone or a pharmaceutically acceptable salt thereof. 9. A controlled release oral dosage form comprising: (a) an analgesically effective amount of an opioid analgesic selected from the group consisting of oxycodone, codeine, hydrocodone, hydromorphone, levorphanol, meperidine, morphine, pharmaceutically acceptable salts thereof, and mixtures thereof, and (b) naloxone or a pharmaceutically acceptable salt thereof in an effective amount to attenuate a side effect of the opioid analgesic, and (c) particles consisting of polyethylene oxide, 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 (iv) one or more additional pharmaceutically acceptable excipient(s), wherein said polyethylene oxide is releasable from said particles and a solubilized mixture having a viscosity unsuitable for injection is formed when the dosage form is crushed and dissolved in from about 1 to about 5 ml of water. 10. The dosage form of claim 9, wherein the viscosity unsuitable for injection is at least 10 cP. 11. The dosage form of claim 9, wherein the viscosity unsuitable for injection is at least 60 cP. 12. The dosage form of claim 9, wherein the viscosity unsuitable for injection is from 10 cP to 60 cP. 13. The dosage form of claim 9, wherein the dosage form provides pain relief for at least about 12 hours when orally administered intact to a human patient. 14. The oral dosage form of claim 9, wherein the opioid analgesic is selected from the group consisting of oxycodone, hydrocodone, hydromorphone, morphine, pharmaceutically acceptable salts thereof, and mixtures thereof. 15. The dosage form of claim 14, wherein the opioid analgesic is oxycodone or a pharmaceutically acceptable salt thereof. 16. The oral dosage form of claim 1, wherein a weight ratio of the opioid analgesic and the opioid antagonist is from about 1:1 to about 10:1. 17. The oral dosage form of claim 1, wherein a weight ratio of the gelling agent to the opioid analgesic is from about 1:1 to about 30:1. 18. The oral dosage form of claim 1, wherein a weight ratio of the gelling agent to the opioid analgesic is from about 2:1 to about 10:1. 19. A controlled release oral dosage form comprising: a therapeutically effective amount of an opioid analgesic selected from the group consisting of oxycodone, codeine, hydrocodone, hydromorphone, levorphanol, meperidine, morphine, pharmaceutically acceptable salts thereof, and mixtures thereof, an opioid antagonist, and particles consisting of a gelling agent, 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 one or more additional pharmaceutically acceptable excipient(s), wherein the gelling agent is releasable from said particles and a solubilized mixture having a viscosity unsuitable for injection is formed when the dosage form is crushed and dissolved in from about 1 to about 5 ml of water, a weight ratio of the gelling agent to the opioid analgesic is from about 1:40 to about 40:1, and the gelling agent is polyethylene oxide. 20. The dosage form of claim 19, wherein the viscosity unsuitable for injection is from 10 cP to 60 cP.