# US 2014/0194456 A1 · Abuse-resistant controlled-release opioid dosage form

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- Number: US 2014/0194456 A1
- Document ID: US20140194456A1
- Status: Published application
- Kind: A1
- Application number: 14/205,204
- Filed: 2014-03-11
- Published: 2014-07-10
- Earliest claimed: 2001-05-11
- Assignees: Purdue Pharma L.P.
- Applicants: Purdue Pharma
- Inventors: Frank S. CARUSO; Huai-Hung KAO
- Web page: https://patentgrep.com/patent/US20140194456A1

## CPC

- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 9/0002: {Galenical forms characterised by the drug release technique; Application systems commanded by energy}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)}
- 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 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)}
- A61K 9/4858: {Organic compounds}
- A61K 9/4866: {Organic macromolecular compounds}
- A61K 31/46: 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/36: Opioid-abuse
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as a immediate release product as a single dose. The controlled release nature of the table prevents the accumulation of orally effective amounts of opioid antagonist when taken normally. The opioid antagonist is contained in a controlled-release matrix and released, over time, with the opioid.

## Claims

### Claim 1

A method of treating a patient with an opioid agonist comprising:
providing an analgesic composition in capsule form comprising, in % by weight:
opioid agonist; and
an opioid antagonist in an amount that is orally effective to block an opioid effect caused by the opioid agonist;
ammonio methacrylate copolymer, NF;
up to about 5% sodium lauryl sulfate, NF; and
up to about 5% magnesium stearate, NF;
wherein said composition comprises 1) a controlled release formulation containing the opioid agonist that controls the release rate of the opioid agonist such that therapeutic agonist levels are maintained and 2) a controlled release formulation containing the antagonist which is not released unless the capsule is crushed but is released as an immediate release formulation when the capsule is crushed;
maintaining the capsule substantially intact; and
orally administering the substantially intact capsule to a patient.

### Claim 2 (depends on 1)

The method according to claim 1, wherein said opioid agonist is selected from the group consisting of morphine, oxycodone, levorphenol, meperdine, hydrocodone, codeine, dihydrocodeine, hydromorphone, propoxyphene, methadone, and oxymorphone and the opioid antagonist is selected from the group consisting of naloxone, naltrexone, N-cyclopropylmethyl-7,8-dihydro-14-hydroxynormorphinone, and 2-cyclopropyl z, -(1-hydroxy-1-methylethyl)-6,14-endo-ethano-tetrayhydrooripavine (or diphenorphine) and the pharmaceutically-acceptable salts thereof.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the opioid agonist is a pharmaceutically acceptable morphine and said opioid antagonist is naltrexone.

### Claim 4 (depends on 1)

The method according to claim 1, wherein the opioid antagonist has a greater antagonistic effect when administered parenterally than when administered orally.