# US 5,348,730 A · Method for preparing medicinal aerosol formulation containing coated medicament

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- Number: US 5,348,730 A
- Document ID: US5348730A
- Status: Granted
- Kind: A
- Application number: 07/838,747
- Filed: 1993-03-17
- Granted: 1994-09-20
- Earliest claimed: 1989-09-20
- Assignees: Minnesota Mining and Manufacturing Company
- Inventors: David J. Greenleaf; Tarlochan S. Purewal; Philip A. Jinks
- Web page: https://patentgrep.com/patent/US5348730A

## CPC

- A61K 9/008: {comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]}
- A61K 9/5015: {Organic compounds, e.g. fats, sugars}
- 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

A method for preparing a self-propelling, powder dispersing aerosol composition comprising at least 0.0001% by weight of a finely-divided solid medicament coated with a non-perfluorinated surface active dispersing agent which constitutes at least 0.0001% by weight of the coated solid material, and suspended in an aerosol propellant in which the non-perfluorinated surface-active dispersing agent is substantially insoluble. Propellant-insoluble non-perfluorinated surfactants are used to prepare stable dispersions of powdered medicament by way of pre-coating the medicament with the surfactant prior to admixture with propellant.

## Claims

### Claim 1

A method for preparing an aerosol composition comprising:
a) coating a finely divided solid drug with non-perfluorinated surface-active dispersing agent in a solvent in which the finely divided solid drug is substantially insoluble to afford a coated solid medicament,
(b) separating the coated solid medicament from the solvent,
(c) drying the coated solid medicament,
(d) dispersing the coated solid medicament in an aerosol propellant substantially free of chlorofluorocarbons and in which the surface active dispersing agent is substantially insoluble such that the aerosol composition comprises from 0,001% to 20% by weight of said coated solid medicament and 0,001% to 50% by weight of the coated solid medicament is the non-perfluorinated surface-active dispersing agent.

### Claim 2 (depends on 1)

A method according to claim 1, wherein the finely-divided solid medicament of step (a) has an average particle size of less than 10 microns in diameter.

### Claim 3 (depends on 1)

A method according to claim 1, wherein the dispersing agent of step (a) is selected from the group consisting of sorbitan trioleate, sorbitan mono-oleate, sorbitan monolaurate, polyoxyethylene (20) sorbitan monolaurate, polyoxyethylene (20) sorbitan mono-oleate, natural lecithin, oleyl polyoxyethylene (2) ether, stearyl polyoxyethylene (2) ether, lauryl polyoxyethylene (4) ether, block copolymers of oxyethylene and oxypropylene,
Oleic acid, Synthetic lecithin, Diethylene glycol dioleate, Tetrahydrofurfuryl oleate, Ethyl oleate, Isopropyl myristate, Glyceryl mono-oleate, Glyceryl monostearate, Glyceryl monoricinoleate, Cetyl alcohol, Stearyl alcohol, Polyethylene glycol 400 and Cetyl pyridinium chloride, olive oil, glyceryl monolaurate, corn oil, cotton seed oil and sunflower seed oil.

### Claim 4 (depends on 1)

A method according to claim 1, wherein the finely divided solid medicament of step (a) comprises a drug selected from the group consisting of an antiallergic, an analgesic, a bronchodilator, an antihistamine, a steroid, an antitussive, an anginal preparation, an antibiotic, an antiinflammatory, a hormone, a sulfonamide, and a therapeutic protein or peptide.

### Claim 5 (depends on 4)

A method according to claim 4, wherein the drug is selected from the group consisting of salbutamol and its salts, beclomethasone dipropionate, pirbuterol and its salts, adrenaline and its salts, and disodium cromoglycate.

### Claim 6 (depends on 1)

A method according to claim 1, wherein the propellant of step (d) comprises 1,1,1,2-tetrafluoroethane.

### Claim 7 (depends on 6)

A method according to claim 6, wherein the propellant of step (d) further comprises an adjuvant selected from the group consisting of perfluoropropane, perfluorobutane, octafluorocyclobutane, perfluoropentane, perfluorohexane, perfluorotributylamine, perfluoromethylcyclohexane and perfluorodecalin.

### Claim 8 (depends on 7)

A method according to claim 7, wherein the propellant of step (d) comprises from 5 to 50% by weight of adjuvant and from 50 to 95% by weight of 1,1,1,2-tetrafluoroethane.