CONTROLLED RELEASE HYDROCODONE

• US 20130158061A1
• Filed: 12/20/2012
• Published: 06/20/2013
• Est. Priority Date: 10/30/2000
• Status: Active Grant

• Current Assignee: Purdue Pharma L.P.
• Original Assignee: Purdue Pharma L.P.
• Inventors: Oshlack, Benjamin, HUANG, Hua-Pin, Masselink, John K., Tonelli, Alfred
• Granted Patent: US 8,551,520 B2
• Time in Patent Office: Days
• US Class Current: 514/282
• CPC Class Codes: A61K 31/194 having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
• CPC Class Codes: A61K 31/46 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61K 9/141 Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers (co) spray-dried products A61K9/16, (co) lyophilised products A61K9/19; the carrier being chemically bound to the active ingredient A61K47/50
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/205 Polysaccharides, e.g. alginate, gums; Cyclodextrin
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2072 characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms A61K9/0004, A61K9/0056, A61K9/0065 take precedence
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/2086 Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat active cores with a complete drug-free outer coat A61K9/28
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.

Claims

1-38. -38. (canceled)

39. A solid oral controlled-release dosage form comprising a matrix comprising an analgesically effect amount of hydrocodone or a pharmaceutically acceptable salt thereof and an amount of a controlled release material sufficient to render the dosage form suitable for once-a-day administration, wherein the matrix is compressed into a tablet, and the dosage form provides

an in-vitro release rate of hydrocodone or a pharmaceutically acceptable salt thereof, when measured by the USP Basket Method at 100 rpm in 900 ml aqueous buffer at a pH of between 1.6 and 7.2 at 37°

C., of from 0% to about 35% at 1 hour, from about 10% to about 70% at 4 hours, from about 20% to about 75% at 8 hours, from about 30% to about 80% at 12 hours, from about 40% to about 90% at 18 hours, and greater than about 60% at 24 hours, and,

after a first administration to an individual patient or a patient population, a C₂₄/C_max ratio of about 0.55 to about 1.0.

40. The dosage form of claim 39, which provides a C₂₄/C_max ratio of 0.55 to 0.85 after said administration.

41. The dosage form of claim 39, which provides a C₂₄/C_max ratio of 0.55 to 0.85 after said administration.

42. The dosage form of claim 39, which provides a C₂₄/C_max ratio of 0.6 to 0.7 after said administration.

43. The dosage form of claim 39, which provides a C₂₄/C_max ratio of 0.7 to 0.85 after said administration.

44. The dosage form of claim 39, wherein the controlled release material comprises a material selected from the group consisting of gums, cellulose ethers, acrylic resins, waxes, shellac and oils.

45. The dosage form of claim 44, wherein the cellulose ether is an alkylcellulose, a hydroxyalkylcellulose, or a carboxyalkylcellulose.

46. The dosage form of claim 39, wherein the matrix further comprises a hydrophobic material having a melting point of from about 30°

C. to about 200°

C.

47. The dosage form of claim 39, wherein the matrix further comprises a fatty acid, a fatty alcohol, a glyceryl ester of fatty acid, a wax, a polyalkylene glycol, or a mixture of any of the foregoing materials.

48. The dosage form of claim 47, wherein the matrix comprises the glyceryl ester of a fatty acid.

49. The dosage form of claim 39, wherein the matrix further comprises microcrystalline cellulose.

50. The dosage form of claim 49, wherein the matrix further comprises hydroxypropylcellulose.

51. The dosage form of claim 39, wherein said C₂₄/C_max ratio is provided after the first administration to the individual patient.

52. The dosage form of claim 39, wherein said C₂₄/C_max ratio is provided after the first administration to the patient population.

53. A solid oral controlled-release dosage form comprising a matrix comprising hydrocodone bitartrate in an amount equivalent to from about 0.5 mg to about 1250 mg of hydrocodone and an amount of a controlled release material sufficient to render the dosage form suitable for once-a-day administration, wherein the matrix is compressed into a tablet, and the dosage form provides

an in-vitro release rate of hydrocodone bitartrate, when measured by the USP Basket Method at 100 rpm in 900 ml aqueous buffer at a pH of between 1.6 and 7.2 at 37°

C., of from 0% to about 35% at 1 hour, from about 10% to about 70% at 4 hours, from about 20% to about 75% at 8 hours, from about 30% to about 80% at 12 hours, from about 40% to about 90% at 18 hours, and greater than about 60% at 24 hours, and, after a first administration to an individual patient or a patient population,

a C₂₄/C_max ratio of about 0.55 to about 1.0.

54. The dosage form of claim 53, which provides a C₂₄/C_max ratio of 0.55 to 0.85 after said administration.

55. The dosage form of claim 53, wherein the controlled release material comprises a material selected from the group consisting of gums, cellulose ethers, acrylic resins, waxes, shellac and oils.

56. A solid oral controlled-release dosage form comprising a matrix comprising hydrocodone bitartrate in an amount equivalent to from about 0.5 mg to about 1250 mg of hydrocodone and an amount of a controlled release material sufficient to render the dosage form suitable for once-a-day administration, wherein the matrix is compressed into a tablet, and the dosage form provides

an in-vitro release rate of hydrocodone bitartrate, when measured by the USP Basket Method at 100 rpm in 900 ml aqueous buffer at a pH of between 1.6 and 7.2 at 37°

C., of from 0% to about 35% at 1 hour, from about 10% to about 70% at 4 hours, from about 20% to about 75% at 8 hours, from about 30% to about 80% at 12 hours, from about 40% to about 90% at 18 hours, and greater than about 60% at 24 hours.

57. The dosage form of claim 56, which provides a C₂₄/C_max ratio of 0.55 to 0.75 after a first administration to an individual patient or a patient population.