# US 2014/0155425 A1 · Pharmaceutical formulation containing opioid agonist, opioid antagonist and irritant agent

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- Number: US 2014/0155425 A1
- Document ID: US20140155425A1
- Status: Published application
- Kind: A1
- Application number: 14/139,304
- Filed: 2013-12-23
- Published: 2014-06-05
- Earliest claimed: 2001-08-06
- Assignees: Purdue Pharma L.P.
- Applicants: Purdue Pharma L.P.
- Inventors: Richard Sackler
- Web page: https://patentgrep.com/patent/US20140155425A1

## CPC

- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/1617: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/1635: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/1647: {Polyesters, e.g. poly(lactide-co-glycolide)}
- A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)}
- 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 9/1694: {resulting in granules or microspheres of the matrix type containing more than 5% of excipient}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/205: {Polysaccharides, e.g. alginate, gums; Cyclodextrin}
- A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets}
- A61K 9/2081: {with microcapsules or coated microparticles according to A61K9/50}
- A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)}
- A61K 9/5078: {with drug-free core}
- A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/36: Opioid-abuse
- 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: 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

Disclosed in certain embodiments is an oral dosage form comprising: a therapeutically effective amount of an opioid analgesic; an opioid antagonist; and an irritant in an effective amount to impart an irritating sensation to an abuser upon administration of the dosage form after tampering.

## Claims

### Claim 1

An oral dosage form comprising: a therapeutically effective amount of an opioid analgesic; an opioid antagonist; and an irritant in an effective amount to impart a burning sensation to an abuser upon administration of said dosage form after crushing, shearing, grinding, chewing, dissolution in a solvent, heating, or any combination thereof.

### Claim 2 (depends on 1)

The oral dosage form of claim 1, wherein the irritant is selected from the group consisting of capsaicin, a capsaicin analog, and mixtures thereof.

### Claim 3 (depends on 1)

The oral dosage form of claim 1, wherein the irritant is a capsaicin analog selected from the group consisting of resiniferatoxin, tinyatoxin, heptanoylisobutylamide, heptanoyl guaiacylamide, other isobutylamides or guaiacylamides, dihydrocapsaicin, homovanillyl octylester, nonanoyl vanillylamide, and mixtures thereof.

### Claim 4 (depends on 1)

The oral dosage form of claim 1, wherein the irritant is capsaicin.

### Claim 5 (depends on 1)

The oral dosage form of claim 1, wherein the irritant is vanillylamide.

### Claim 6 (depends on 1)

The oral dosage form of claim 1, wherein the irritant is in a sequestered form.

### Claim 7 (depends on 1)

The oral dosage form of claim 1, wherein the antagonist is in a sequestered form.

### Claim 8 (depends on 1)

The oral dosage form of claim 1, wherein the antagonist and the irritant are both in sequestered forms.

### Claim 9 (depends on 1)

The oral dosage form of claim 1, wherein the irritant is in an amount of about 0.00125% to about 50% by weight of the dosage form.

### Claim 10 (depends on 1)

The oral dosage form of claim 1, wherein the irritant is in an amount of about 1 to about 7.5% by weight of the dosage form.

### Claim 11 (depends on 1)

The oral dosage form of claim 1, wherein the irritant is in an amount of about 1 to about 5% by weight of the dosage form.

### Claim 12 (depends on 1)

The oral dosage forms of claim 1, further comprising a pharmaceutically acceptable excipient.

### Claim 13 (depends on 12)

The oral dosages form of claim 12, wherein said excipient is a sustained release excipient.

### Claim 14 (depends on 12)

The oral dosage form of claim 12, said dosage form providing an analgesic effect for at least about 12 hours after oral administration to a human patient.

### Claim 15 (depends on 1)

The oral dosage form of claim 1, wherein said irritant is at least partially interdispersed with the opioid analgesic.

### Claim at position 16

16-17. (canceled)

### Claim 18 (depends on 1)

The oral dosage form of claim 1 wherein the antagonist is in an amount to attenuate a side effect of said opioid agonist selected from the group consisting of anti-analgesia, hyperalgesia, hyperexcitability, physical dependence, tolerance, and a combination of any of the foregoing.

### Claim at position 18

19-24. (canceled)

### Claim 25 (depends on 1)

The oral dosage form of claim 1, wherein the opioid antagonist is naloxone or a pharmaceutically acceptable salt thereof.

### Claim 26 (depends on 25)

The oral dosage form of claim 25, wherein the opioid analgesic is oxycodone or a pharmaceutically acceptable salt thereof.

### Claim 27 (depends on 26)

The dosage form of claim 26, wherein the dosage form is a controlled release oral dosage form.

### Claim 28 (depends on 27)

The dosage form of claim 27, wherein the dosage form provides effective pain relief for about 12 hours.