Formulations containing nalbuphine and uses thereof

• US 10,441,585 B2
• Filed: 06/01/2016
• Issued: 10/15/2019
• Est. Priority Date: 08/20/2010
• Status: Active Grant

• Current Assignee: Debregeas ET Associes Pharma
• Original Assignee: Debregeas ET Associes Pharma
• Inventors: Lebon, Christophe, Suplie, Pascal, Paul, David Olivier
• Primary Examiner(s): Rosenthal, Andrew S
• Application Number:
  US15/170,033
• Publication Number:
  US 20160271124A1
• Time in Patent Office: 1,231 Days
• 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 comprising nalbuphine or a pharmaceutically acceptable salt thereof, and at least one hydrophilic granulation carrier, one hydrophilic binder and one lubricant.

Claims

1. An immediate release, oral pharmaceutical formulation comprising in percentage by weight:

20.55% nalbuphine/HCl,

22.02% lactose,

47.53% microcrystalline cellulose,

4.98% povidone,

0.50% magnesium stearate,

3.98% flavoring, and

0.44% coating.

2. The pharmaceutical formulation of claim 1, wherein

the formulation is in a form of a tablet.

3. The pharmaceutical formulation of claim 2, wherein

the tablet is a 50 mg tablet.

4. A method of treating of pain, comprising:

administering an effective amount of the pharmaceutical formulation of claim 1 to a patient in need thereof to treat pain generated by treatment for opioid addiction.

5. A method of treating pain generated by treatment for opioid addiction, comprising:

administering the pharmaceutical formulation of claim 3 to a patient in need thereof.

6. An immediate release, oral pharmaceutical formulation comprising in percentage by weight:

20.31% nalbuphine/HCl,

62.16% agglomerated α

-lactose-monohydrate,

6.65% povidone,

2.38% crospovidone,

1.76% microcrystalline cellulose,

0.10% silica,

0.48% magnesium stearate,

1.92% talc, and

4.81% coating.

7. The pharmaceutical formulation of claim 6, wherein

the formulation is in a form of a tablet.

8. The pharmaceutical formulation of claim 7, wherein

the tablet is a 30 mg tablet.

9. A method of treating of pain, comprising:

administering an effective amount of the pharmaceutical formulation of claim 6 to a patient in need thereof to treat pain generated by treatment for opioid addiction.

10. A method of treating pain generated by treatment for opioid addiction, comprising:

administering the pharmaceutical formulation of claim 8 to a patient in need thereof.