# US 11,077,196 B2 · Abuse-deterrent pharmaceutical composition

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- Number: US 11,077,196 B2
- Document ID: US11077196B2
- Status: Granted
- Kind: B2
- Application number: 16/080,491
- Filed: 2017-02-28
- Published: 2019-02-28
- Granted: 2021-08-03
- Earliest claimed: 2016-02-29
- Assignees: G.L. Pharma GmbH
- Applicants: G.L. Pharma GmbH
- Inventors: Georg Guebitz; Katrin Greimel; Martin Brandauer; Daniela Huber; Klaus Bleymaier; Wolfgang Kroutil; Doris Lechner; Christof Wachter; Harald Wagner; Heimo Winkler
- Web page: https://patentgrep.com/patent/US11077196B2

## CPC

- A61K 47/42: Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein (oligopeptides having up to five amino acids {A61K47/183}; polyamino acids A61K47/34)
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 38/44: Oxidoreductases (1)
- A61K 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K 47/61: the organic macromolecular compound being a polysaccharide or a derivative thereof
- A61K 47/6903: {the form being semi-solid, e.g. an ointment, a gel, a hydrogel or a solidifying gel}
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/30: for treating abuse or dependence
- A61P 25/36: Opioid-abuse
- C12N 9/00: Enzymes; Proenzymes; Compositions thereof (preparations containing enzymes for cleaning teeth A61K8/66, A61Q11/00; medicinal preparations containing enzymes or proenzymes A61K38/43; enzyme containing detergent compositions C11D; {enzymes with nucleic acid structure, e.g. ribozymes, C12N15/113}); Processes for preparing, activating, inhibiting, separating or purifying enzymes (preparation of malt C12C1/00)
- C12N 9/0006: {acting on CH-OH groups as donors (1.1)}
- C12N 9/0065: {acting on hydrogen peroxide as acceptor (1.11)}
- C12N 9/0069: {acting on single donors with incorporation of molecular oxygen, i.e. oxygenases (1.13)}
- C12N 9/0071: {acting on paired donors with incorporation of molecular oxygen (1.14)}
- C12N 9/1025: {Acyltransferases (2.3)}
- C12N 9/1051: {Hexosyltransferases (2.4.1)}
- C12N 9/13: {transferring sulfur containing groups (2.8)}
- 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
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

Disclosed is an abuse-deterrent pharmaceutical composition comprising a drug with an enzyme-reactive functional group, wherein the drug has an abuse potential, and an enzyme capable of reacting with the enzyme-reactive functional group (a drug-processing enzyme), wherein the drug with the enzyme-reactive functional group is contained in the pharmaceutical composition in a storage stable, enzyme-reactive state and under conditions wherein no enzymatic activity acts on the drug.

## Claims

### Claim 1

An abuse-deterrent pharmaceutical composition comprising a drug with an enzyme-reactive functional group, wherein the drug has an abuse potential, and an enzyme capable of reacting with the enzyme-reactive functional group, wherein the drug with the enzyme-reactive functional group is contained in the pharmaceutical composition in a storage stable, enzyme-reactive state and under conditions wherein no enzymatic activity acts on the drug, wherein the enzyme catalyses O-dealkylation, N-dealkylation, keto-reduction, N-oxidation, epoxy-hydroxylation, esterification, de-amidation, or dehalogenation of the drug or addition of molecules to the drug, wherein the composition comprises a drug/enzyme combination selected from the group consisting morphine/laccase, tapentadol/laccase, oxymorphone/laccase, hydromorphone/laccase, pentazocine/laccase, buprenorphine/laccase, diacetylmorphine/hydrolase/laccase, levorphanol/laccase, and oxycodone/laccase/oxycodone-processing enzyme.

### Claim 2 (depends on 1)

The abuse-deterrent pharmaceutical composition according to claim 1, wherein the pharmaceutical composition is selected from a tablet, a mini-tablet, a coated tablet, a bi-layer tablet, a multi-layer tablet, a capsule, a pellet, a multiple unit pellet system, a granulate, and a powder.

### Claim 3 (depends on 1)

The abuse-deterrent pharmaceutical composition according to claim 1, further comprising another enzyme.

### Claim 4 (depends on 1)

A method of treating pain and/or drug addiction, comprising administering the abuse-deterrent pharmaceutical composition according to claim 1 to a subject in need thereof to treat pain and/or drug addiction.

### Claim 5 (depends on 1)

A method for manufacturing the abuse-deterrent pharmaceutical composition according to claim 1, comprising mixing the drug with the enzyme and finishing the mixture to a pharmaceutical composition.

### Claim 6 (depends on 1)

A method for manufacturing the abuse-deterrent pharmaceutical composition according to claim 1, comprising providing the drug and the enzyme in separated form and finishing the separated drug and enzyme to a pharmaceutical composition.