Controlled release hydrocodone

• US 9,060,940 B2
• Filed: 03/14/2014
• Issued: 06/23/2015
• Est. Priority Date: 10/30/2000
• Status: Expired due to Fees

• Current Assignee: Purdue Pharma L.P.
• Original Assignee: Purdue Pharma L.P.
• Inventors: Oshlack, Benjamin, Huang, Hua-Pin, Masselink, John K., Tonelli, Alfred
• Primary Examiner(s): Sasan, Aradhana
• Application Number:
  US14/210,565
• Publication Number:
  US 20140199394A1
• Time in Patent Office: 466 Days
• US Class Current: 1/1
• 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. A method of providing effective pain relief to a patient in need thereof comprising:

obtaining a serum profile of an opioid in the patient, having a plasma level with a C₂₄/C_max ratio of about 0.55 to about 1.0, by administering orally on a once-a-day basis a controlled release formulation of the opioid to the patient, wherein

the controlled release formulation releases an analgesically effective amount of the opioid at an effective rate to provide said serum profile of the opioid, and

the opioid is hydrocodone or a pharmaceutically acceptable salt thereof.

2. The method of claim 1, wherein the plasma level of the opioid provides a C₂₄/C_max ratio of 0.55 to 0.85.

3. The method of claim 1, wherein the plasma level of the opioid provides a C₂₄/C_max ratio of 0.55 to 0.75.

4. The method of claim 1, wherein the plasma level of the opioid provides a C₂₄/C_max ratio of 0.6 to 0.7.

5. The method of claim 1, wherein the plasma level of the opioid provides a C₂₄/C_max ratio of 0.7 to 0.85.

6. The method of claim 1, wherein the controlled release formulation comprises a controlled release material comprising a material selected from the group consisting of gums, cellulose ethers, acrylic resins, waxes, shellac and oils.

7. The method of claim 6, wherein the cellulose ether is an alkylcellulose, a hydroxyalkylcellulose, or a carboxyalkylcellulose.

8. The method of claim 1, wherein the controlled release formulation comprises a matrix comprising a hydrophobic material having a melting point of from about 30°

C. to about 200°

C.

9. The method of claim 1, wherein the controlled release formulation 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.

10. The method of claim 9, wherein the matrix comprises the glyceryl ester of a fatty acid.

11. The method of claim 1, wherein the controlled release formulation comprises a matrix comprising microcrystalline cellulose.

12. The method of claim 11, wherein the matrix further comprises hydroxypropylcellulose.

13. The method of claim 1, wherein the controlled release formulation is administered at the initiation of therapy.

14. The method of claim 1, wherein the controlled release formulation is administered at steady-state.

15. The method of claim 1, wherein from about 0.5 mg to about 1250 mg of hydrocodone is administered.

16. The method of claim 15, wherein from about 5 mg to about 60 mg of hydrocodone is administered.

17. The method of claim 1, wherein the pharmaceutically acceptable salt is a bitartrate salt.

18. A method of providing effective pain relief to a patient in need thereof comprising:

obtaining a serum profile of an opioid in the patient, having a plasma level of the opioid with a C₂₄/C_max ratio of about 0.55 to about 1.0, by administering orally on a once-a-day basis a controlled release formulation of the opioid to the patient, wherein

the controlled release formulation comprises an effective amount of a controlled release material to release an analgesically effective amount of the opioid at an effective rate to provide said serum profile of the opioid, and

the opioid is a bitartrate salt of hydrocodone.

19. A method of providing effective pain relief to a patient in need thereof comprising:

obtaining a serum profile of hydrocodone or a pharmaceutically acceptable salt thereof in the patient having a plasma level of the hydrocodone with a C₂₄/C_max ratio of about 0.55 to about 1.0, and a W₅₀ of the hydrocodone of between 4 and 22 hours by administering orally on a once-a-day basis a controlled release formulation of the hydrocodone or pharmaceutically acceptable salt to the patient, wherein

the controlled release formulation comprises an effective amount of a controlled release material to release an analgesically effective amount of the hydrocodone or pharmaceutically acceptable salt thereof at an effective rate to provide said serum profile of the hydrocodone and said W₅₀.

20. The method of claim 19, wherein the W₅₀ is at least 12 hours.