# US 7,611,694 B2 · Aerosol formulation for inhalation comprising an anticholinergic

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- Number: US 7,611,694 B2
- Document ID: US7611694B2
- Status: Granted
- Kind: B2
- Application number: 11/424,541
- Filed: 2006-06-15
- Published: 2006-10-05
- Granted: 2009-11-03
- Earliest claimed: 2002-08-14
- Assignees: Boehringer Ingelheim Pharma GmbH & Co. KG
- Inventors: Friedrich Schmidt
- Web page: https://patentgrep.com/patent/US7611694B2

## CPC

- A61K 9/0078: {for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions}
- A61K 31/33: Heterocyclic compounds
- A61K 31/4745: condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48)
- A61K 31/5375: 1,4-Oxazines, e.g. morpholine
- 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)

## Abstract

The present invention relates to a propellant-free, aqueous aerosol formulation for anticholinergics of formula 1 wherein X− denotes an anion.

## Claims

### Claim 1

An propellant-free aqueous pharmaceutical formulation for inhalation comprising at least one compound of formula 1 as the only active substance
wherein
X− is an anion selected from the group consisting of chloride, bromide, iodide, sulphate, phosphate, methanesulphonate, nitrate, maleate, acetate, citrate, fumarate, tartrate, oxalate, succinate, benzoate and p-toluenesulphonate,
at least one pharmacologically acceptable acid and water, which formulation is a liquid.

### Claim 2 (depends on 1)

The propellant-free aqueous pharmaceutical formulation according to claim 1 further comprising one or more pharmaceutically acceptable excipients or complexing agents or mixtures thereof.

### Claim 3 (depends on 1)

The propellant-free aqueous pharmaceutical formulation according to claim 1, containing at least one compound of formula 1 wherein X− is selected from the group consisting of chloride, bromide, 4-toluenesulphonate and methanesulphonate.

### Claim 4 (depends on 1)

The propellant-free aqueous pharmaceutical formulation according to claim 1, wherein the pharmacologically acceptable acid is selected from the inorganic acids hydrochloric acid, hydrobromic acid, nitric acid, sulphuric acid and phosphoric acid or from the organic acids ascorbic acid, citric acid, malic acid, tartaric acid, maleic acid, succinic acid, fumaric acid, acetic acid, formic acid and propionic acid.

### Claim 5 (depends on 3)

The propellant-free aqueous pharmaceutical formulation according to claim 3, characterised by a pH of 2.5 to 6.5.

### Claim 6 (depends on 2)

The propellant-free aqueous pharmaceutical formulation according to claim 2, wherein the pharmaceutical excipient is benzalkonium chloride.

### Claim 7 (depends on 6)

The propellant-free aqueous pharmaceutical formulation according to claim 6, characterised in that the content of benzalkonium chloride is from 1 to 50 mg per 100 ml of solution.

### Claim 8 (depends on 1)

The propellant-free aqueous pharmaceutical formulation according to claim 1, characterised in that a pharmacologically active cation of the compound of 1 is present in the formulation in an amount of about 4 to 2000 mg per 100 ml of formulation.

### Claim 9 (depends on 2)

The propellant-free aqueous pharmaceutical formulation according to claim 2, which comprises at least one complexing agent.

### Claim 10 (depends on 9)

The propellant-free aqueous pharmaceutical formulation according to claim 9, characterised in that the content of the complexing agent is 5 to 20 mg per 100 ml of formulation.

### Claim 11 (depends on 1)

The propellant-free aqueous pharmaceutical formulation according to claim 1 in an inhaler suitable for nebulising the formulation.