SEQUESTERING SUBUNIT AND RELATED COMPOSITIONS AND METHODS

• US 20110014280A1
• Filed: 04/23/2010
• Published: 01/20/2011
• Est. Priority Date: 09/20/2002
• Status: Active Grant

• Current Assignee: Alpharma Pharmaceuticals LLC (Pfizer Inc.), Alpharma Incorporated (Zoetis Incorporated)
• Original Assignee: Alpharma Pharmaceuticals LLC (Pfizer Inc.), Alpharma Incorporated (Zoetis Incorporated)
• Inventors: Boehm, Garth
• Granted Patent: US 8,685,443 B2
• Time in Patent Office: Days
• US Class Current: 424/452
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer
• CPC Class Codes: A61K 9/5078 with drug-free core
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/36 Opioid-abuse
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

A sequestering subunit comprising an aversive agent and a blocking agent, wherein the blocking agent substantially prevents release of the aversive agent from the sequestering subunit in the gastrointestinal tract for a time period that is greater than 24 hours; a composition comprising a sequestering subunit in releasable form, wherein, optionally, the mechanical fragility of the sequestering subunit is the same as the mechanical fragility of the therapeutic agent in releasable form; a capsule or tablet comprising a sequestering subunit and a therapeutic agent; and a method of preventing abuse of a therapeutic agent.

Claims

1-38. -38. (canceled)

39. A method of treating pain in a human being comprising administering to the human being a plurality of composite subunits, each composite subunit comprising a sequestering subunit comprising naltrexone and a blocking agent comprising a surfactant wherein the blocking agent substantially prevents release of the naltrexone from the sequestering subunit in the gastrointestinal tract, the sequestering subunit being overcoated with an opioid agonist in releasable form.

42. The method of claim 39 wherein the blocking agent further comprises a pharmaceutically acceptable hydrophobic material.

43. The method of claim 42 wherein the pharmaceutically acceptable hydrophobic material is insoluble in the gastrointestinal tract.

44. The method of claim 39 wherein the pharmaceutically acceptable hydrophobic material is a copolymer of acrylic acid and methacrylic acid.

45. The method of claim 44 wherein the pharmaceutically acceptable hydrophobic material is Eudragit RSPO.

46. The method of claim 45 wherein the surfactant is sodium lauryl sulfate.

47. The method of claim 39 wherein the plurality of composite subunits are contained within a capsule.

48. The method of claim 39 wherein the plurality of composite subunits are contained within a capsule, the blocking agent comprises Eudragit RSPO, and the surfactant is sodium lauryl sulphate, and the opioid agonist is morphine.

40. The method of 39 wherein the opioid agonist is selected from the group consisting of morphine, hydromorphone, oxycodone, and hydrocodone.

41. The method of claim 40 wherein the opioid agonist is morphine.