# US 2013/0158061 A1 · Controlled release hydrocodone

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- Number: US 2013/0158061 A1
- Document ID: US20130158061A1
- Status: Published application
- Kind: A1
- Application number: 13/721,293
- Filed: 2012-12-20
- Published: 2013-06-20
- Earliest claimed: 2000-10-30
- Assignees: Purdue Pharma L.P.
- Inventors: Benjamin Oshlack; Hua-Pin HUANG; John K. Masselink; Alfred Tonelli
- Web page: https://patentgrep.com/patent/US20130158061A1

## CPC

- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 9/0004: {Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/141: {Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers ((co) spray-dried products A61K9/16, (co) lyophilised products A61K9/19; the carrier being chemically bound to the active ingredient A61K47/50)}
- A61K 9/2009: {Inorganic compounds}
- 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 9/2031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers}
- A61K 9/205: {Polysaccharides, e.g. alginate, gums; Cyclodextrin}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2072: {characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms (A61K9/0004, A61K9/0056, A61K9/0065 take precedence)}
- A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets}
- A61K 9/2086: {Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat (active cores with a complete drug-free outer coat A61K9/28)}
- A61K 31/194: having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
- 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 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- 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

A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.

## Claims

### Claim at position 1

1-38. (canceled)

### Claim 39

A solid oral controlled-release dosage form comprising a matrix comprising an analgesically effect amount of hydrocodone or a pharmaceutically acceptable salt thereof and an amount of a controlled release material sufficient to render the dosage form suitable for once-a-day administration, wherein the matrix is compressed into a tablet, and the dosage form provides
an in-vitro release rate of hydrocodone or a pharmaceutically acceptable salt thereof, when measured by the USP Basket Method at 100 rpm in 900 ml aqueous buffer at a pH of between 1.6 and 7.2 at 37° C., of from 0% to about 35% at 1 hour, from about 10% to about 70% at 4 hours, from about 20% to about 75% at 8 hours, from about 30% to about 80% at 12 hours, from about 40% to about 90% at 18 hours, and greater than about 60% at 24 hours, and,
after a first administration to an individual patient or a patient population, a C24/Cmax ratio of about 0.55 to about 1.0.

### Claim 40 (depends on 39)

The dosage form of claim 39, which provides a C24/Cmax ratio of 0.55 to 0.85 after said administration.

### Claim 41 (depends on 39)

The dosage form of claim 39, which provides a C24/Cmax ratio of 0.55 to 0.85 after said administration.

### Claim 42 (depends on 39)

The dosage form of claim 39, which provides a C24/Cmax ratio of 0.6 to 0.7 after said administration.

### Claim 43 (depends on 39)

The dosage form of claim 39, which provides a C24/Cmax ratio of 0.7 to 0.85 after said administration.

### Claim 44 (depends on 39)

The dosage form of claim 39, wherein the controlled release material comprises a material selected from the group consisting of gums, cellulose ethers, acrylic resins, waxes, shellac and oils.

### Claim 45 (depends on 44)

The dosage form of claim 44, wherein the cellulose ether is an alkylcellulose, a hydroxyalkylcellulose, or a carboxyalkylcellulose.

### Claim 46 (depends on 39)

The dosage form of claim 39, wherein the matrix further comprises a hydrophobic material having a melting point of from about 30° C. to about 200° C.

### Claim 47 (depends on 39)

The dosage form of claim 39, wherein the matrix further comprises a fatty acid, a fatty alcohol, a glyceryl ester of fatty acid, a wax, a polyalkylene glycol, or a mixture of any of the foregoing materials.

### Claim 48 (depends on 47)

The dosage form of claim 47, wherein the matrix comprises the glyceryl ester of a fatty acid.

### Claim 49 (depends on 39)

The dosage form of claim 39, wherein the matrix further comprises microcrystalline cellulose.

### Claim 50 (depends on 49)

The dosage form of claim 49, wherein the matrix further comprises hydroxypropylcellulose.

### Claim 51 (depends on 39)

The dosage form of claim 39, wherein said C24/Cmax ratio is provided after the first administration to the individual patient.

### Claim 52 (depends on 39)

The dosage form of claim 39, wherein said C24/Cmax ratio is provided after the first administration to the patient population.

### Claim 53

A solid oral controlled-release dosage form comprising a matrix comprising hydrocodone bitartrate in an amount equivalent to from about 0.5 mg to about 1250 mg of hydrocodone and an amount of a controlled release material sufficient to render the dosage form suitable for once-a-day administration, wherein the matrix is compressed into a tablet, and the dosage form provides
an in-vitro release rate of hydrocodone bitartrate, when measured by the USP Basket Method at 100 rpm in 900 ml aqueous buffer at a pH of between 1.6 and 7.2 at 37° C., of from 0% to about 35% at 1 hour, from about 10% to about 70% at 4 hours, from about 20% to about 75% at 8 hours, from about 30% to about 80% at 12 hours, from about 40% to about 90% at 18 hours, and greater than about 60% at 24 hours, and, after a first administration to an individual patient or a patient population,
a C24/Cmax ratio of about 0.55 to about 1.0.

### Claim 54 (depends on 53)

The dosage form of claim 53, which provides a C24/Cmax ratio of 0.55 to 0.85 after said administration.

### Claim 55 (depends on 53)

The dosage form of claim 53, wherein the controlled release material comprises a material selected from the group consisting of gums, cellulose ethers, acrylic resins, waxes, shellac and oils.

### Claim 56

A solid oral controlled-release dosage form comprising a matrix comprising hydrocodone bitartrate in an amount equivalent to from about 0.5 mg to about 1250 mg of hydrocodone and an amount of a controlled release material sufficient to render the dosage form suitable for once-a-day administration, wherein the matrix is compressed into a tablet, and the dosage form provides
an in-vitro release rate of hydrocodone bitartrate, when measured by the USP Basket Method at 100 rpm in 900 ml aqueous buffer at a pH of between 1.6 and 7.2 at 37° C., of from 0% to about 35% at 1 hour, from about 10% to about 70% at 4 hours, from about 20% to about 75% at 8 hours, from about 30% to about 80% at 12 hours, from about 40% to about 90% at 18 hours, and greater than about 60% at 24 hours.

### Claim 57 (depends on 56)

The dosage form of claim 56, which provides a C24/Cmax ratio of 0.55 to 0.75 after a first administration to an individual patient or a patient population.