# US 8,784,888 B2 · Controlled release and taste masking oral pharmaceutical composition

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- Number: US 8,784,888 B2
- Document ID: US8784888B2
- Status: Granted
- Kind: B2
- Application number: 13/617,138
- Filed: 2012-09-14
- Published: 2013-01-24
- Granted: 2014-07-22
- Earliest claimed: 1999-06-14
- Assignees: Cosmo Technologies Limited
- Applicants: Roberto Villa; Massimo Pedrani; Mauro Ajani; Lorenzo Fossati
- Inventors: Roberto Villa; Massimo Pedrani; Mauro Ajani; Lorenzo Fossati
- Web page: https://patentgrep.com/patent/US8784888B2

## CPC

- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/1617: {Organic compounds, e.g. phospholipids, fats}
- 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 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets}
- A61K 9/209: {containing drug in at least two layers or in the core and in at least one outer layer}
- A61K 9/28: Dragees; Coated pills or tablets {, e.g. with film or compression coating (A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209)}
- A61K 9/2806: {Coating materials}
- A61K 9/2813: {Inorganic compounds}
- A61K 9/282: {Organic compounds, e.g. fats}
- A61K 9/2846: {Poly(meth)acrylates}
- A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/12: Antihypertensives
- A61P 11/08: Bronchodilators
- A61P 11/14: Antitussive agents
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/22: Anxiolytics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/04: Antibacterial agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)}
- A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- 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

Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.

## Claims

### Claim 1

A controlled release oral pharmaceutical composition consisting essentially of:
(1) a tablet core consisting essentially of:
a) budesonide in an amount effective to treat intestinal inflammatory disease; and
b) a macroscopically homogeneous composition comprising at least one lipophilic excipient, at least one amphiphilic excipient, and at least one hydrogel-forming hydrophilic excipient other than a gum, wherein said budesonide is dispersed in said macroscopically homogeneous composition; and
(2) a coating on said tablet core, said coating consisting essentially of a gastro-resistant film.

### Claim 2 (depends on 1)

A controlled release oral pharmaceutical composition according to claim 1, wherein said at least one hydrogel-forming hydrophilic excipient comprises at least one hydroxyalkyl cellulose.

### Claim 3 (depends on 1)

A controlled release oral pharmaceutical composition according to claim 1, wherein said gastro-resistant film consists essentially of at least one methacrylic acid polymer.

### Claim 4 (depends on 3)

A controlled release oral pharmaceutical composition according to claim 3, wherein said at least one hydrogel-forming hydrophilic excipient comprises at least one hydroxyalkyl cellulose.

### Claim 5 (depends on 1)

A controlled release oral pharmaceutical composition according to claim 1, wherein said at least one lipophilic excipient comprises stearic acid or magnesium stearate.

### Claim 6 (depends on 5)

A controlled release oral pharmaceutical composition according to claim 5, wherein said at least one hydrogel-forming hydrophilic excipient comprises at least one hydroxyalkyl cellulose.

### Claim 7 (depends on 1)

A controlled release oral pharmaceutical composition according to claim 1, wherein said at least one amphiphilic excipient comprises lecithin.

### Claim 8 (depends on 7)

A controlled release oral pharmaceutical composition according to claim 7, wherein said at least one hydrogel-forming hydrophilic excipient comprises at least one hydroxyalkyl cellulose.

### Claim 9 (depends on 7)

A controlled release oral pharmaceutical composition according to claim 7, wherein said at least one lipophilic excipient comprises stearic acid or magnesium stearate.