# US 2014/0193492 A1 · Method for the preparation of a pharmaceutical composition comprising 5-aminosalicylic acid for use in treatment of ulcerative colitis and crohn's disease

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- Number: US 2014/0193492 A1
- Document ID: US20140193492A1
- Status: Published application
- Kind: A1
- Application number: 14/133,934
- Filed: 2013-12-19
- Published: 2014-07-10
- Earliest claimed: 2001-10-15
- Assignees: Ferring B.V.
- Applicants: Ferring B.V.
- Inventors: Svenn Kluver Jepsen
- Web page: https://patentgrep.com/patent/US20140193492A1

## CPC

- A61K 9/2081: {with microcapsules or coated microparticles according to A61K9/50}
- A61J 3/00: Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
- A61K 9/1694: {resulting in granules or microspheres of the matrix type containing more than 5% of excipient}
- 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 31/606: having amino groups
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61K 9/1635: {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)
- 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
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention concerns a new method of preparing granules comprising 5-aminosalicylic acid and a new method of preparing a pharmaceutical composition for the treatment of ulcerative colitis or Crohn's disease by oral administration comprising as active ingredient 5-aminosalicylic acid.

## Claims

### Claim at position 1

1-27. (canceled)

### Claim 28

A composition comprising dry extruded strong, smooth non-spherical granules comprising 5-aminosalicylic acid (5-ASA) and a pharmaceutically acceptable binder, wherein:
the weight ratio of the binder to 5-ASA in the granules is up to 6.5:100 and
the granules are made by a process comprising extruding a wet mass comprising the binder, 5-ASA, and a solvent comprised of at least 50% w/w water through an extruder.

### Claim 29 (depends on 28)

The composition of claim 28, wherein the weight ratio of the binder to 5-ASA in the granules is up to 5:100.

### Claim 30 (depends on 28)

The composition of claim 28, wherein the binder is selected from the group consisting of polyvinylpyrrolidone, pregelatinized cornstarch, and cellulose derivative binders.

### Claim 31 (depends on 28)

The composition of claim 28, wherein the binder comprises polyvinylpyrrolidone.

### Claim 32 (depends on 28)

The composition of claim 28, wherein the solvent is comprised of at least 85% w/w water.

### Claim 33 (depends on 28)

The composition of claim 28, wherein more than 85% of the granules have a particle size of 850 to 1000 μm as measured by sieve analysis.

### Claim 34 (depends on 28)

The composition of claim 28, wherein the granules exhibit a strength that makes them resistant to wear during further processing.

### Claim 35 (depends on 34)

The composition of claim 34, wherein the percent of granules in the composition having a particle size of 850 to 1000 μm as measured by sieve analysis before and after processing for one hour in a laboratory fluid bed does not differ by more than 1%.

### Claim 36 (depends on 28)

The composition of claim 28, wherein the granules exhibit a smoothness that permits a reproducible coating process to achieve a target dissolution rate profile.

### Claim 37 (depends on 28)

The composition of claim 28, wherein the granules are provided with a pharmaceutically acceptable coating.

### Claim 38 (depends on 37)

The composition of claim 37, wherein the coating is selected from the group consisting of enteric coatings and delayed release coatings.

### Claim 39 (depends on 37)

The composition of claim 37, wherein the coating provides a dissolution rate-limiting barrier on the granules.

### Claim 40 (depends on 39)

The composition of claim 39, wherein the barrier is semipermeable.

### Claim 41 (depends on 38)

The composition of claim 38, wherein the coating comprises a polymer selected from the group consisting of polymethacrylate polymers and ethyl cellulose polymers.

### Claim 42 (depends on 28)

A tablet formed from the granules of claim 28.

### Claim 43 (depends on 37)

A tablet formed from the granules of claim 37.