# US 8,771,716 B2 · Modified release analgesic suspensions

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- Number: US 8,771,716 B2
- Document ID: US8771716B2
- Status: Granted
- Kind: B2
- Application number: 13/755,749
- Filed: 2013-01-31
- Published: 2013-06-06
- Granted: 2014-07-08
- Earliest claimed: 2006-11-21
- Assignees: McNeil-PPC, Inc.
- Applicants: McNeil-PPC, Inc.
- Inventors: Der-Yang Lee; Jen-Chi Chen; Vincent Chen; Robert Shen
- Web page: https://patentgrep.com/patent/US8771716B2

## CPC

- 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 9/0095: {Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006)}
- 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 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/585: {Ion exchange resins, e.g. polystyrene sulfonic acid resin}
- A61P 11/02: Nasal agents, e.g. decongestants
- 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 9/5026: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/5047: {Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose}
- A61K 9/5073: {having two or more different coatings optionally including drug-containing subcoatings}
- 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 pharmaceutical dosage form comprising non-steroidal-anti-inflammatory drugs, in particular propionic acid derivatives such as ibuprofen, along with a second active ingredient having a shorter therapeutically effective plasma concentration duration, such as phenylephrine, and methods of administering the same are provided. This method provides improved therapeutic effect, in particular pain relief along with decongestant relief, over extended time periods.

## Claims

### Claim 1

A liquid pharmaceutical dosage form comprising:
a) a first portion comprising ibuprofen and/or pharmaceutically acceptable salts thereof, wherein said ibuprofen is released from the dosage form in a substantially immediate manner upon contact of the dosage form with a dissolution medium; and
b) a second portion comprising:
i. a phenylephrine-ion exchange resin complex, said phenylephrine-ion exchange resin complex comprising phenylephrine complexed with a sulfonated co-polymer of styrene and divinylbenzene;
ii. a first coating layer comprising a semi-permeable coating comprising a polymer selected from the group consisting of cellulose acetate, ethylcellulose, non-enteric polymethacrylates and copolymers and mixtures thereof, wherein said semi-permeable coating substantially covers said phenylephrine-ion exchange resin complex; and
iii. a second coating layer comprising a protective coating, wherein said second coating layer covers said first coating layer,
wherein said phenylephrine is released from the dosage form in a substantially sustained release manner.

### Claim 2 (depends on 1)

The dosage form of claim 1, further comprising a liquid medium for the administration of the first portion and the second portion.

### Claim 3 (depends on 2)

The dosage form of claim 2, wherein the liquid medium comprises agents selected from the group consisting of solvents, structuring agents, swelling agents, suspending systems, surfactants, sweeteners, buffering agents, preservatives, bacteriostatic agents, colorants, flavoring agents, and mixtures thereof.

### Claim 4 (depends on 2)

The dosage form of claim 2 wherein the liquid medium is water.

### Claim 5 (depends on 2)

The dosage form of claim 2 wherein the liquid medium is mixtures of water with a pharmaceutically acceptable water-miscible co-solvent selected from the group consisting of glycols, alcohols, glycerol, and mixtures thereof.

### Claim 6 (depends on 1)

The dosage form of claim 1, wherein the weight ratio of the first coating layer to the second coating layer is about 10:90 to about 90:10.

### Claim 7 (depends on 1)

The dosage form of claim 1, wherein the second portion comprises, based upon the total dry weight of the second portion,
a) from about 5 percent to about 80 percent of the first coating layer;
b) from about 10 percent to about 90 percent of the second coating layer; and
c) from about 1 percent to about 50 percent of the phenylephrine-ion exchange resin complex.

### Claim 8 (depends on 1)

The dosage form of claim 1, further comprising, based upon the total weight of the dosage form, from about 0.1% to about 5% of the first portion; and from about 0.05% to about 5% of the second portion.

### Claim 9 (depends on 1)

The dosage form of claim 1 further comprising, based upon the total weight of the dosage form,
a) from about 0.1% to about 5% of-ibuprofen; and
b) from about 0.005% to about 1% of phenylephrine.

### Claim 10 (depends on 1)

A method for treating pain in a mammal in need thereof, comprising administering the dosage form of claim 1 in an amount effective for providing pain relief to the mammal for a time period of at least about four hours to about six hours after administration of the dosage form.

### Claim 11 (depends on 1)

A method for treating sinus congestion in a mammal in need thereof, comprising administering the dosage form of claim 1 in an amount effective for providing sinus congestion relief to the mammal for a time period of at least about four hours to about six hours after administration of the dosage form.

### Claim 12 (depends on 1)

The dosage form of claim 1, wherein said non-enteric polymethacrylates are selected from the group consisting of poly(ethyl acrylate, methyl methacrylate) 2:1; poly(methyl acrylate, methyl methacrylate, methacrylic acid) 7:3:1; poly(ethyl acrylate, methyl methacrylate, triethylammonioethyl methacrylate chloride) 1:2:0.2; poly(ethyl acrylate, methyl methacrylate, triethyleammonioethyl methacrylate chloride 1:2:0.1, and copolymers and mixtures thereof.

### Claim 13 (depends on 1)

The dosage form of claim 1, wherein the semi-permeable coating comprises a polymer selected from the group consisting of cellulose acetate, ethylcellulose, and mixtures thereof.

### Claim 14 (depends on 1)

The dosage form of claim 1, wherein the protective coating comprises a polymer selected from the group consisting of poly(methacrylic acid, methyl methacrylate) 1:2; poly(methacrylic acid, methyl methacrylate) 1:1; and poly(methacrylic acid, ethyl acrylate) 1:1.

### Claim 15 (depends on 1)

The dosage form of claim 1, wherein the protective coating comprises a polymer selected from the group consisting of hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate, cellulose acetate phthalate, polyvinylacetate phthalate, shellac and copolymers and mixtures thereof.

### Claim 16 (depends on 1)

The dosage form of claim 1, wherein the protective coating comprises a material selected from the group consisting of a fatty acid ester, a wax, or mixtures thereof.

### Claim 17 (depends on 16)

The dosage form of claim 16, wherein the fatty acid ester is selected from the group consisting of sucrose fatty acid esters; mono-di- and triglycerides; glyceryl behenate; glyceryl palmitostearate; glyceryl tristearate; glyceryl trilaurylate; glyceryl myristate; lauroyl macrogol-32 glycerides; stearoyl macrogol-32 glyceride; fatty acid esters having a fatty acid chain length of about C10-C40; and mixtures thereof.