FORMULATIONS CONTAINING NALBUPHINE AND USES THEREOF

• US 20130123294A1
• Filed: 08/18/2011
• Published: 05/16/2013
• Est. Priority Date: 08/20/2010
• Status: Abandoned Application

• Current Assignee: Debregeas ET Associes Pharma
• Original Assignee: Debregeas ET Associes Pharma
• Inventors: Lebon, Christophe, Suplie, Pascal, Paul, David Olivier
• Application Number:
  US13/810,358
• Publication Number:
  US 20130123294A1
• Time in Patent Office: Days
• US Class Current: 514/282
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61K 9/1676 having a drug-free core with discrete complete coating layer containing drug adsorbates of liquid drug formulations on inert powders without simultaneous granulation step A61K9/141; with further drug-free outer coating A61K9/5078; drug conjugated to non-active particles A61K47/6921
• 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 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/5047 Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/5078 with drug-free core
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/30 for treating abuse or dependence
• 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

Immediate release, oral, pharmaceutical formulation including nalbuphine or a pharmaceutically acceptable salt thereof, and at least one hydrophilic granulation carrier, one hydrophilic binder and one lubricant.

Claims

1. Immediate release, oral pharmaceutical formulation comprising nalbuphine or a pharmaceutically acceptable salt thereof, and at least one hydrophilic granulation carrier, one hydrophilic binder and one lubricant.

2. The pharmaceutical formulation according to claim 1, wherein it only contains nalbuphine or one of the pharmaceutically acceptable salts thereof.

3. The pharmaceutical formulation according to claim 1, wherein the hydrophilic granulation carrier is selected from the group consisting of mannitol, polyvinyl pyrrolidone or a derivative thereof, a polyol, lactose, a cellulose derivative, polyethylene glycol or a derivative thereof and a silica derivative.

4. The pharmaceutical formulation according to claim 1, wherein the hydrophilic granulation carrier is lactose.

5. The pharmaceutical formulation according to claim 1, wherein the hydrophilic binder is selected from the group consisting of polyvinyl pyrrolidone or a derivative thereof, a polyol, lactose, a cellulose derivative, polyethylene glycol or a derivative thereof, gums and carbomers.

6. The pharmaceutical formulation according to claim 1, wherein the hydrophilic binder is polyvinylpyrrolidone.

7. The pharmaceutical formulation according to claim 1, wherein the lubricant is selected from the group consisting of silicon dioxide, magnesium stearate, anhydrous colloidal silica, sodium stearyl fumarate and talcum.

8. The pharmaceutical formulation according to claim 1, wherein it comprises at least 45% by weight of hydrophilic granulation carrier, relative to the total weight of the formulation.

9. The pharmaceutical formulation according to claim 1, wherein it comprises less than 10% by weight of hydrophilic binder, relative to the total weight of the formulation.

10. The pharmaceutical formulation according to claim 1, wherein it comprises less than 10% by weight of lubricant, relative to the total weight of the formulation.

11. The pharmaceutical formulation according to claim 1, wherein it comprises less than 30% by weight of nalbuphine, relative to the total weight of the formulation.

12. The pharmaceutical formulation according to claim 1, wherein it further comprises:

at least one disintegrating agent; and

optionally

at least one excipient.

13. The pharmaceutical formulation according to claim 1, wherein it comprises:

from 4 to 30% by weight of nalbuphine;

from 45 to 70% by weight of lactose;

from 2 to 10% by weight of PVP; and

from 0.9 to 7% by weight of at least one lubricant.

14. The pharmaceutical formulation according to claim 1, wherein it is in solid form.

15. The pharmaceutical formulation according to claim 14, wherein it is in a form selected from the group consisting of tablets, granules, pellets, micro-granules, capsules and lozenges.

16. The pharmaceutical formulation according to claim 1, for its use in the treatment of pain.

17. The pharmaceutical formulation for use according to claim 16, wherein pain is generated by a treatment for opioid addiction.

18. The pharmaceutical formulation for use according to claim 1, its use in the treatment of opioid addiction.