# US 10,441,585 B2 · Formulations containing nalbuphine and uses thereof

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- Number: US 10,441,585 B2
- Document ID: US10441585B2
- Status: Granted
- Kind: B2
- Application number: 15/170,033
- Filed: 2016-06-01
- Published: 2016-09-22
- Granted: 2019-10-15
- Earliest claimed: 2010-08-20
- Assignees: Debregeas Et Associes Pharma
- Applicants: Debregeas Et Associes Pharma
- Inventors: Christophe Lebon; Pascal Suplie; David Olivier Paul
- Web page: https://patentgrep.com/patent/US10441585B2

## CPC

- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/2009: {Inorganic compounds}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/30: for treating abuse or dependence
- A61P 25/36: Opioid-abuse
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- 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)}
- A61K 9/5047: {Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose}
- A61K 9/5078: {with drug-free core}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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

### Claim 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.

### Claim 2 (depends on 1)

The pharmaceutical formulation of claim 1, wherein
the formulation is in a form of a tablet.

### Claim 3 (depends on 2)

The pharmaceutical formulation of claim 2, wherein
the tablet is a 50 mg tablet.

### Claim 4 (depends on 1)

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.

### Claim 5 (depends on 3)

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.

### Claim 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.

### Claim 7 (depends on 6)

The pharmaceutical formulation of claim 6, wherein
the formulation is in a form of a tablet.

### Claim 8 (depends on 7)

The pharmaceutical formulation of claim 7, wherein
the tablet is a 30 mg tablet.

### Claim 9 (depends on 6)

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.

### Claim 10 (depends on 8)

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.