# US 2016/0256451 A1 · Dosage of naloxone

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- Number: US 2016/0256451 A1
- Document ID: US20160256451A1
- Status: Published application
- Kind: A1
- Application number: 14/828,028
- Filed: 2015-08-17
- Published: 2016-09-08
- Earliest claimed: 2015-03-06
- Assignees: Develco Pharma Schweiz AG
- Applicants: Develco Pharma Schweiz AG
- Inventors: Helene Rey; Olaf Mundszinger; Isabelle Golfier; Silvia Jakob; Oliver Rusch
- Web page: https://patentgrep.com/patent/US20160256451A1

## CPC

- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/209: {containing drug in at least two layers or in the core and in at least one outer layer}
- A61P 1/10: Laxatives
- 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

The present invention relates to a pharmaceutical composition comprising a μ-receptor antagonist as an active substance, wherein the antagonist is prepared in an extended release formulation. The composition is intended for the treatment of patients with opioid-induced constipation, wherein the dosage of the μ-receptor agonist is independent of the opioid dosage. The preferred dosage of the μ-receptor antagonist of the composition is equivalent to a daily dosage of 20-70 mg naloxone.

## Claims

### Claim 1

A method comprising:
administering a composition comprising an extended release formulation of a μ-receptor antagonist in a dosage equivalent to a daily dosage of 20 mg to 70 mg of naloxone to a subject receiving an opioid treatment,
wherein the μ-receptor antagonist is administered independently of the opioid treatment.

### Claim 2 (depends on 1)

The method of claim 1, wherein the μ-receptor antagonist is naloxone, methylnaloxone, methylnaltrexone, naltexone, or pharmaceutically acceptable salts thereof.

### Claim 3 (depends on 1)

The method of claim 1, wherein the dosage of the μ-receptor antagonist is equivalent to a daily dosage of 24-48 mg of naloxone.

### Claim 4 (depends on 1)

The method of claim 1, wherein the composition is designed as a once-a-day formulation.

### Claim 5 (depends on 1)

The method of claim 1, wherein the composition is designed as a twice-a-day formulation.

### Claim 6 (depends on 1)

The method of claim 1, wherein the composition releases the μ-receptor antagonist independently of the ambient pH of the gastrointestinal tract.

### Claim 7 (depends on 1)

The method of claim 1, wherein the μ-receptor antagonist has an in vitro release rate measured using the paddle stirrer method at 75 rpm in 500 ml 0.1 N hydrochloric acid at 37° C., is 0% to 75% in 2 h, 3% to 95% in 4 h, 20% to 100% in 10 h, 30% to 100% in 16 h, 50% to 100% in 24 h, and of more than 80% in 36 h.

### Claim 8 (depends on 1)

The method of claim 1, wherein the composition is a solid oral composition.

### Claim 9 (depends on 2)

The method of claim 2, wherein the μ-receptor antagonist is naloxone.

### Claim 10 (depends on 1)

The method of claim 1, wherein the opioid treatment is a continuous opioid treatment.

### Claim 11 (depends on 1)

The method of claim 1, further comprising administering an opioid to the subject, wherein the μ-receptor antagonist is not naloxone.

### Claim 12 (depends on 1)

The method of claim 1, further comprising administering an opioid to the subject, wherein the opioid is not oxycodone.

### Claim 13 (depends on 12)

The method of claim 12, wherein the opioid is present in the composition comprising an extended release formulation of a μ-receptor antagonist.

### Claim 14 (depends on 1)

The method of claim 1 further comprising administering an opioid to the subject wherein the opioid: μ-receptor antagonist molar ratio is greater than about 2.1:1.

### Claim 15 (depends on 1)

The method of claim 1 further comprising administering an opioid to the subject wherein the opioid: μ-receptor antagonist molar ratio is less than about 2:1.

### Claim 16

A composition comprising an opioid and a μ-receptor antagonist, wherein the μ-receptor antagonist is not naloxone.

### Claim 17

A composition comprising an opioid and a μ-receptor antagonist, wherein the opioid is not oxycodone.

### Claim 18

A composition comprising an opioid and a μ-receptor antagonist, wherein there is greater than about a 2.1:1 molar ratio of opioid to μ-receptor antagonist.

### Claim 19

A composition comprising an opioid and a μ-receptor antagonist, wherein there is less than about a 2:1 molar ratio of opioid to μ-receptor antagonist.

### Claim 20 (depends on 11)

The method of claim 11, wherein the opioid is present in the composition comprising an extended release formulation of a μ-receptor antagonist