# US 11,433,030 B2 · Extended relief dosage form

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- Number: US 11,433,030 B2
- Document ID: US11433030B2
- Status: Granted
- Kind: B2
- Application number: 16/714,856
- Filed: 2019-12-16
- Published: 2020-04-16
- Granted: 2022-09-06
- Earliest claimed: 2016-09-26
- Assignees: The Procter & Gamble Company
- Applicants: The Procter & Gamble Company
- Inventors: Mark Edward Stella; John Richard Entwisle; Baltej Ludher; Jonathan E. Clark; Daren K. Anness; Guhan Balan; Andrew Nicholas Carr
- Web page: https://patentgrep.com/patent/US11433030B2

## CPC

- 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 9/0002: {Galenical forms characterised by the drug release technique; Application systems commanded by energy}
- A61K 9/2004: {Excipients; Inactive ingredients}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/209: {containing drug in at least two layers or in the core and in at least one outer layer}
- A61K 9/2095: {Tabletting processes}
- A61K 9/4808: {characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release (capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084)}
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 29/02: without antiinflammatory effect
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- 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

A dosage form with a first portion and a second portion. The first portion can be an immediate release portion and can comprise a pain reliever, which can be naproxen or naproxen sodium. The second portion can be an extended release portion and can comprise pseudoephedrine or a pharmaceutically acceptable salt thereof and/or dextromethorphan or a pharmaceutically acceptable salt thereof. The dosage form can optionally comprise a stabilizing agent. The dosage form can be adapted to maintain a therapeutically effective amount of pain reliever, pseudoephedrine, or a pharmaceutically acceptable salt thereof, and/or dextromethorphan, or a pharmaceutically acceptable salt thereof, for at least eight hours.

## Claims

### Claim 1

A dosage form comprising:
a. a first portion comprising a pain reliever selected from the group consisting of acetaminophen, ibuprofen, ketoprofen, diclofenac, aspirin, naproxen, pharmaceutically acceptable salts thereof, and combinations thereof; wherein the first portion is an immediate release portion;
b. a second portion comprising pseudoephedrine or a pharmaceutically acceptable salt thereof; a chelating agent; dextromethorphan or a pharmaceutically acceptable salt thereof; a basic buffering agent sufficient to achieve a pH of about 6.0 to about 8.0; and a hydrophilic polymer;
wherein the second portion is an extended release portion;
wherein the dosage form comprises less than about 0.01%, by weight of the dosage form, methcathinone;
wherein the dosage form comprises less than about 0.2%, by weight of the dosage form, 10-keto-dextromethorphan.

### Claim 2 (depends on 1)

The dosage form of claim 1 wherein the hydrophilic polymer is a hydroxypropyl methylcellulose with a viscosity of from about 10,000 cP to about 250,000 cP.

### Claim 3 (depends on 1)

The dosage form of claim 1 wherein the basic buffering agent is selected from the group consisting of meglumine, glycine, sodium carbonate, calcium carbonate, sodium bicarbonate, phosphate buffer, magnesium hydroxide, and combinations thereof.

### Claim 4 (depends on 1)

The dosage form of claim 1 wherein the second portion comprises from about 0.5% to about 3% of the chelating agent.

### Claim 5 (depends on 4)

The dosage form of claim 4 wherein the chelating agent is selected from the group consisting of EDTA, citric acid, malic acid, tartaric acid, lactic acid, aspartic acid, glutamic acid, lysine, sodium hexametaphosphate, salts thereof, and combinations thereof.

### Claim 6 (depends on 1)

The dosage form of claim 1 wherein the second portion further comprises from about 0.1% to about 1% of the antioxidant.

### Claim 7 (depends on 6)

The dosage form of claim 6 wherein the antioxidant is selected from the group consisting of ascorbyl palmitate, ascorbic acid, propyl gallate, alpha-tocopherol, butylated hydroxytoluene, butylated hydroxyanisole, tert-butyl hydroquinone, acetyl cysteine, and combinations thereof.

### Claim 8 (depends on 1)

The dosage form of claim 1 wherein the dosage form comprises less than about 2 ppm iron.

### Claim 9

A dosage form comprising:
a. a first portion comprising a pain reliever selected from the group consisting of acetaminophen, ibuprofen, ketoprofen, diclofenac, aspirin, naproxen, pharmaceutically acceptable salts thereof, and combinations thereof; wherein the first portion is an immediate release portion;
b. a second portion comprising pseudoephedrine or a pharmaceutically acceptable salt thereof; a stabilizing agent selected from the group consisting of a chelating agent, an antioxidant, and combinations thereof;
a basic buffering agent sufficient to achieve a pH of about 6.0 to about 8.0; and a hydrophilic polymer;
wherein the second portion is an extended release portion;
wherein the dosage form comprises less than about 0.01%, by weight of the dosage form, methcathinone.

### Claim 10 (depends on 9)

The dosage form of claim 9, wherein the dosage form comprises a ratio of pseudoephedrine or a pharmaceutically acceptable salt thereof to hydrophilic polymer of from about 0.10 to about 3.0 on a weight basis.

### Claim 11 (depends on 9)

The dosage form of claim 9 wherein the antioxidant is selected from the group consisting of ascorbyl palmitate, ascorbic acid, propyl gallate, alpha-tocopherol, butylated hydroxytoluene, butylated hydroxyanisole, tert-butyl hydroquinone, acetyl cysteine, and combinations thereof.

### Claim 12 (depends on 11)

The dosage form of claim 11 wherein the second portion comprises from about 0.001% to about 3% of the antioxidant.

### Claim 13 (depends on 12)

The dosage form of claim 12 wherein the second portion comprises from about 0.01% to about 1.5% of the antioxidant.

### Claim 14 (depends on 12)

The dosage form of claim 12 wherein the second portion comprises from about 0.01% to about 8% of a chelating agent.

### Claim 15 (depends on 14)

The dosage form of claim 14 wherein the chelating agent is selected from the group consisting of EDTA, citric acid, malic acid, tartaric acid, lactic acid, aspartic acid, glutamic acid, lysine, sodium hexametaphosphate, salts thereof, and combinations thereof.

### Claim 16 (depends on 15)

The dosage form of claim 15 wherein the chelating agent is EDTA.

### Claim 17 (depends on 9)

The dosage form of claim 9 wherein the second portion further comprises dextromethorphan or a pharmaceutically acceptable salt thereof.

### Claim 18 (depends on 9)

The dosage form of claim 9 wherein the hydrophilic polymer is a hydroxypropyl methylcellulose with a viscosity of from about 10,000 cP to about 250,000 cP.

### Claim 19 (depends on 9)

The dosage form of claim 9 wherein the dosage form comprises less than about 0.005%, by weight of the dosage form, methcathinone.