# US 5,708,021 A · Debittered ranitidine preparation

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- Number: US 5,708,021 A
- Document ID: US5708021A
- Status: Granted
- Kind: A
- Application number: 08/574,340
- Filed: 1995-12-18
- Granted: 1998-01-13
- Earliest claimed: 1994-12-17
- Assignees: Roehm GmbH Chemische Fabrik
- Inventors: Manfred Assmus; Hans-Ulrich Petereit
- Web page: https://patentgrep.com/patent/US5708021A

## CPC

- 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 31/34: having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K 47/58: obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- 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

Ranitidine salts with polycarboxylic acids, such as copolymers of acrylic and/or methacrylic acid with their lower alkyl esters, are water-soluble salts with a very reduced bitter taste. The salts are suitable as liquid gastritis preparations.

## Claims

### Claim 1

A ranitidine composition in the form of an aqueous solution, said aqueous solution comprising a polycarboxylic acid salt of ranitidine, wherein said polycarboxylic acid has a weight average molecular weight of 1,000 D-200,000 D.

### Claim 2 (depends on 1)

The composition of claim 1, wherein said salt contains at least one equivalent of carboxyl groups of the polycarboxylic acid per mole of ranitidine.

### Claim 3 (depends on 1)

The composition of claim 1, wherein said polycarboxylic acid has a weight average molecular weight of 10,000-200,000 D.

### Claim 4 (depends on 3)

The composition of claim 3, wherein said molecular weight is 50,000-150,000 D.

### Claim 5 (depends on 1)

The composition of claim 1, wherein said polycarboxylic acid has a carboxyl equivalent weight of 72-800 D.

### Claim 6 (depends on 5)

The composition of claim 5, wherein said polycarboxylic acid has a carboxyl equivalent weight of 100-500 D.

### Claim 7 (depends on 1)

The composition of claim 1, wherein said polycarboxylic acid is an alkali-soluble polymer or copolymer of acrylic acid, methacrylic acid or a combination thereof.

### Claim 8 (depends on 7)

The composition of claim 7, wherein said polycarboxylic acid is a polymer or copolymer containing 10-100 wt. % monomer units of acrylic acid, methacrylic acid or a combination thereof and 90-0 wt. % monomer units of one or more lower alkyl esters of acrylic acid, methacrylic acid or a combination thereof.

### Claim 9 (depends on 8)

The composition of claim 8, wherein said polycarboxylic acid is a copolymer of methylmethacrylate and methacrylic acid or a copolymer of ethylacrylate and methacrylic acid.

### Claim 10 (depends on 1)

The composition of claim 1, having a bitter value below 1,000.

### Claim 11 (depends on 10)

The composition of claim 10, having a bitter value below 750.

### Claim 12 (depends on 1)

The composition of claim 1, having a solids content of about 1-60 wt. %.

### Claim 13

A ranitidine composition in the form of an aqueous solution, said aqueous solution comprising a polycarboxylic acid salt of ranitidine, wherein said polycarboxylic acid has a weight average molecular weight of 1,000 D-200,000 D, said aqueous solution having a pH of about 4-8.

### Claim 14

A ranitidine composition in the form of an aqueous solution, said aqueous solution comprising a polycarboxylic acid salt of ranitidine, wherein said polycarboxylic acid has a weight average molecular weight of 1,000 D-200,000 D, wherein said ranitidine composition is formed by mixing said polycarboxylic acid with an aqueous solution of free ranitidine base or with an aqueous solution of ranitidine hydrochloride and a base to form a mixture, and heating said mixture at a temperature of 40.degree.-80.degree. C. to form a solution having a pH of about 4-8.