# US 2003/0114391 A1 · Carbinoxamine tannate

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- Number: US 2003/0114391 A1
- Document ID: US20030114391A1
- Status: Published application
- Kind: A1
- Application number: 10/326,349
- Filed: 2002-12-20
- Published: 2003-06-19
- Earliest claimed: 2001-12-14
- Assignees: Jame Fine Chemicals, Inc.
- Inventors: Sham N. Redkar; Dina Donatiello; Timothy N. Truong; Vilas M. Chopdekar
- Web page: https://patentgrep.com/patent/US20030114391A1

## CPC

- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 31/7024: Esters of saccharides
- A61P 21/02: Muscle relaxants, e.g. for tetanus or cramps
- 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

The invention pertains to carbinoxamine tannate and to a method for preparing carbinoxamine tannate by reacting carbinoxamine free base at a temperature of about 50 to about 150° C. with tannic acid neat or as an aqueous slurry containing about 5 to about 30 wt. % water.

## Claims

### Claim 1

A composition comprising carbinoxamine tannate.

### Claim 2

A therapeutic antihistamine composition comprising a pharmaceutically effective amount of an active ingredient comprising carbinoxamine tannate.

### Claim 3 (depends on 2)

A therapeutic composition as claimed in claim 2 in tablet form.

### Claim 4 (depends on 2)

A therapeutic composition as claimed in claim 2 in suspension form.

### Claim 5 (depends on 2)

A therapeutic composition as claimed in claim 2 in syrup form

### Claim 6 (depends on 2)

A therapeutic composition as claimed in claim 2 further comprising one or more antitussive, expectorant and/or antihistamine compositions.

### Claim 7 (depends on 6)

The composition of claim 6 wherein the antitussive, expectorant and/or antihistamine compositions are selected from the group consisting of dextromethorphan, guaifenesin, chlorpheniramine, dextrochlorpheniramine, brompheniramine, pyrilamine, phenylephrine, ephedrine, pseudoephedrine and carbetapentane.

### Claim 8

A method for suppressing the production of histamines in a human being which comprises orally administering to such human being a therapeutic amount of a composition comprising an active ingredient comprising carbinoxamine tannate.

### Claim 9 (depends on 8)

A method as claimed in claim 8 wherein said composition is in tablet form.

### Claim 10 (depends on 8)

A method as claimed in claim 8 wherein said composition is in suspension form.

### Claim 11 (depends on 8)

A method as claimed in claim 8 wherein said composition is in syrup form.

### Claim 12

A method for preparing carbinoxamine tannate comprising reacting carbinoxamine free base with tannic acid at a temperature of about 50 to about 150° C. and thereafter recovering the resultant carbinoxamine tannate.

### Claim 13 (depends on 12)

The method of claim 12 wherein the reaction is carried out at a temperature of 70 to 120° C.

### Claim 14 (depends on 12)

The method of claim 12 wherein the carbinoxamine free base is employed in an amount of about 4 to about 8 moles of the free base per mole of tannic acid.

### Claim 15 (depends on 14)

The method of claim 14 wherein the carbinoxamine free base is employed in an amount of 5 to 6 moles of the free base per mole of tannic acid.

### Claim 16 (depends on 12)

The method of claim 12 wherein the reaction is carried out in the additional presence of about 5 to about 30 wt. % water.

### Claim 17 (depends on 12)

The method of claim 12 wherein the recovered carbinoxamine tannate is subsequently died under vacuum at a temperature of about 50 to about 75° C. for a period of 1 to 10 hours or more.

### Claim 18 (depends on 12)

The method of claim 12 wherein the recovered carbinoxamine tannate is dried by sparging with nitrogen for a period of 1 to 10 hours or more.

### Claim 19 (depends on 12)

The method of claim 12 wherein the recovered carbinoxamine tannate is milled to provide a free flowing powder.

### Claim 20 (depends on 19)

The method of claim 19 wherein the powder has a particle size in the range of about 50 to about 200 mesh.