# US 2019/0167663 A1 · Abuse Resistant Pharmaceutical Compositions

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- Number: US 2019/0167663 A1
- Document ID: US20190167663A1
- Status: Published application
- Kind: A1
- Application number: 16/124,899
- Filed: 2018-09-07
- Published: 2019-06-06
- Earliest claimed: 2014-09-12
- Assignees: Recro Gainesville LLC
- Applicants: Recro Gainesville LLC
- Inventors: Gurvinder Singh Rekhi; Richard Sidwell
- Web page: https://patentgrep.com/patent/US20190167663A1

## CPC

- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/1635: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/1641: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers}
- 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 9/48: 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 9/5084: {Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs (tablets containing such a mixture A61K9/2077)}
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- 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 composition comprising pharmaceutical active ingredients which are susceptible to, or have potential for, abuse. The invention provides an oral pharmaceutical composition comprising a first population of beads and a second population of beads. The first bead population comprises a pharmaceutically active ingredient susceptible to, or having the potential for, abuse. The second bead population comprises a gelling agent and a coating substantially surrounding the gelling agent, but containing no pharmaceutically active ingredient. The first bead population and the second bead population are physically separable, but visually indistinguishable to the naked eye. Upon ingress of water into the second population of beads, the gelling agent is caused to swell forming a viscous mass inhibiting or preventing the extraction of the active ingredient.

## Claims

### Claim at position 1

1-15. (canceled)

### Claim 16

A method of preparing an oral dosage form comprising a population of immediate release beads comprising an opioid and a population of gelling agent-containing beads comprising polyethylene oxide and a permeable or semi-permeable coating polymer, the method comprising the steps of:
a) independently preparing a solution comprising an opioid selected from the group consisting of benzylmorphine, bezitramide, buprenorphine, butorphanol, carfentanil, clonitazene, codeine, desomorphine, dextromoramide, dezocine, diacetylmorphine, diampromide, diamorphone, dihydrocodeine, dihydromorphine, dimenoxadol, dimepheptanol, dimethylthiambutene, diphenoxylate, dioxaphetyl butyrate, diprenorphine, dipipanone, eptazocine, ethoheptazine, ethylmethylthiambutene, ethylmorphine, etonitazene, etorphine, dihydroetorphine, fentanyl, hydrocodone, hydromorphone, β-hydroxy-3-methylfentanyl, hydroxypethidine, isomethadone, ketobemidone, levo-α-acetylmethadol, levorphanol, levophenacylmorphan, lofentanil, meperidine, meptazinol, metazocine, methadone, metopon, morphine, myrophine, nalmefene, narceine, nicomorphine, norlevorphanol, normethadone, nalorphine, nalbuphene, normorphine, norpipanone, o-methylnaltrexone, opium, oxycodone, oxymorphone, papaveretum, pentazocine, pethidine, phenadoxone, phenomorphan, phenazocine, phenoperidine, piminodine, piritramide, propheptazine, promedol, properidine, propoxyphene, remifentanil, sufentanil, tilidine, and tramadol, or pharmaceutically acceptable salts thereof;
b) applying sufficient amounts of the solution of step a) onto sufficient amounts of sugar spheres to produce an immediate release population of the opioid;
c) independently forming a binder solution by dissolving a binder in a solvent mixture comprising alcohol and water;
d) applying the binder solution and a sufficient amount of polyethylene oxide powder onto sufficient amounts of sugar spheres to produce polyethylene oxide layered sugar spheres;
e) independently forming a coating polymer mixture by mixing the permeable or semi-permeable polymer in a solvent mixture comprising alcohol, acetone and water;
f) applying the coating polymer mixture onto polyethylene oxide layered sugar spheres of step e) to form a population of polymeric coated polyethylene oxide layered sugar spheres; and
g) mixing the immediate release beads and the polymeric coated polyethylene oxide layered sugar spheres in different proportions to form the dosage form.

### Claim 17 (depends on 16)

The method of claim 16, wherein the opioid is selected from the group consisting of codeine, dihydrocodeine, hydrocodone, methadone, morphine and oxycodone.

### Claim 18 (depends on 16)

The method of claim 16, wherein the opioid is hydrocodone bitartrate.

### Claim 19 (depends on 16)

The method of claim 16, wherein the oral dosage form is a capsule.

### Claim 20 (depends on 19)

The method of claim 19, wherein the capsule comprises from 5 to 250 mg of hydrocodone.

### Claim 21 (depends on 20)

The method of claim 20, wherein the capsule comprises 20 mg of hydrocodone bitartrate.

### Claim 22 (depends on 20)

The method of claim 20, wherein the capsule comprises 50 mg of hydrocodone bitartrate.

### Claim 23 (depends on 19)

The method of claim 19, wherein the capsule comprises at least about 20 mg of polyethylene oxide.

### Claim 24 (depends on 16)

The method of claim 16, wherein the binder is povidone.

### Claim 25 (depends on 16)

The method of claim 16, wherein the semi-permeable polymer is selected from the group consisting of an ammonio methacrylate copolymer, and a methacrylic acid copolymer, or a combination thereof.