# US 8,569,375 B2 · Compositions

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- Number: US 8,569,375 B2
- Document ID: US8569375B2
- Status: Granted
- Kind: B2
- Application number: 13/059,260
- Filed: 2009-08-18
- Published: 2011-08-18
- Granted: 2013-10-29
- Earliest claimed: 2008-08-22
- Assignees: Reckitt Benckiser Healthcare (UK) Limited
- Applicants: Alistair Campbell
- Inventors: Alistair Campbell
- Web page: https://patentgrep.com/patent/US8569375B2

## CPC

- A61J 1/035: {Blister-type containers (blisters in general B65D75/36)}
- A61K 9/0007: {Effervescent (A61K9/0065 takes precedence)}
- A61K 9/0056: {Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals}
- A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays}
- A61K 9/14: Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)}
- A61K 9/1611: {Inorganic compounds}
- A61K 9/1623: {Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules}
- A61K 9/1635: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 11/04: for throat disorders
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61J: CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
- 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

An ingestible particulate composition comprises: a) at least one compound selected from the group consisting of 2,4-dichlorobenzyl alcohol, amylmetacresol, cetylpyridinium chloride, hexitidine, hexylresorcinol, flurbiprofen, lidocaine, benzocaine, ibuprofen, paracetamol, pectin, menthol, and benzydamine; and b) one or more bioadhesive materials. Resulting particulate compositions have excellent flow characteristics, dust suppression, organoleptic properties and stability. They are highly suitable for administration direction into a patient's mouth, and ingested to alleviate the symptoms of a sore throat.

## Claims

### Claim 1

An ingestible particulate composition comprising:
at least one pharmaceutically active compound selected from the group consisting of 2,4-dichlorobenzyl alcohol, amylmetacresol, cetylpyridinium chloride, hexitidine, hexylresorcinol, flurbiprofen, lidocaine, benzocaine, ibuprofen, paracetamol, pectin, menthol, and benzydamine;
one or more bioadhesive materials present in an amount up to 10 wt %;
sodium bicarbonate; and
citric acid;
wherein a mean particle size of the particulate composition is not greater than 1.0 mm.

### Claim 2 (depends on 1)

A composition according to claim 1, wherein the composition is a flowable particulate.

### Claim 3 (depends on 1)

A composition as claimed in claim 1, wherein the at least one pharmaceutically active compound is selected from the group consisting of 2,4-dichlorobenzyl alcohol, amylmetacresol, hexylresorcinol, and flurbiprofen.

### Claim 4 (depends on 3)

A composition as claimed in claim 3, wherein the at least one pharmaceutically active compound is flurbiprofen.

### Claim 5 (depends on 1)

A composition as claimed in claim 1, wherein the one or more bioadhesive materials is a polymeric or oligomeric compound.

### Claim 6 (depends on 1)

A composition as claimed in claim 1, further comprising a flow-aid.

### Claim 7 (depends on 1)

A composition according to claim 1, for use in a method of treatment of a human or animal body by therapy.

### Claim 8 (depends on 1)

A single-pack dosage form comprising a single dose of a composition of claim 1, the single-pack dosage form being a targeted outlet pack which necessarily deposits the composition onto a small area within the mouth.

### Claim 9 (depends on 8)

A single-pack dosage form according to claim 8, being a stick-form sachet.

### Claim 10 (depends on 1)

A bulk pack comprising a bulk source of a composition of claim 1, together with dosage metering means or dosage information.

### Claim 11 (depends on 1)

A method of making a medicament for the treatment of sore throat comprising forming a composition according to claim 1 by combining at least one pharmaceutically active compound and one or more bioadhesive materials.

### Claim 12

A method of treating sore throat comprising:
administering a flowable particulate composition into a mouth of a patient, the composition comprising:
at least one pharmaceutically active compound selected from the group consisting of 2,4-dichlorobenzyl alcohol, amylmetacresol, cetylpyridinium chloride, hexitidine, hexylresorcinol, flurbiprofen, lidocaine, benzocaine, ibuprofen, paracetamol, pectin, menthol, and benzydamine;
one or more bioadhesive materials present in an amount up to 10 wt %;
sodium bicarbonate; and
citric acid;
wherein a mean particle size of the particulate composition is not greater than 1.0 mm.

### Claim 13

A method of making of a particulate composition suitable for pouring into a mouth of a patient comprising forming a composition comprising:
at least one pharmaceutically active compound selected from the group consisting of 2,4-dichlorobenzyl alcohol, amylmetacresol, cetylpyridinium chloride, hexitidine, hexylresorcinol, flurbiprofen, lidocaine, benzocaine, ibuprofen, paracetamol, pectin, menthol, and benzydamine;
one or more bioadhesive materials present in an amount up to 10 wt %;
sodium bicarbonate; and
citric acid;
wherein a mean particle size of the particulate composition is not greater than 1.0 mm.

### Claim 14

A targeted outlet pack containing a single dose of an ingestible flowable particulate composition, the targeted outlet pack being adapted to deposit the composition onto a small area within the mouth, the composition comprising:
at least one pharmaceutically active compound selected from the group consisting of 2,4-dichlorobenzyl alcohol, amylmetacresol, cetylpyridinium chloride, hexitidine, hexylresorcinol, flurbiprofen, lidocaine, benzocaine, ibuprofen, paracetamol, pectin, menthol, and benzydamine;
one or more bioadhesive materials present in an amount up to 10 wt %;
sodium bicarbonate; and
citric acid;
wherein a mean particle size of the particulate composition is not greater than 1.0 mm.

### Claim 15 (depends on 1)

A composition according to claim 1, wherein the composition further comprises an organic acid.

### Claim 16 (depends on 5)

A composition as claimed in claim 5, wherein the polymeric or oligomeric compound has high a molecular weight up to several million Daltons.

### Claim 17 (depends on 7)

A composition according to claim 7, for use in a method of treatment of sore throats.