Aerosol formulation containing a particulate medicament

• US 6,306,368 B1
• Filed: 11/24/1998
• Issued: 10/23/2001
• Est. Priority Date: 11/09/1990
• Status: Expired due to Fees

• Current Assignee: Glaxo Group Limited (GSK plc)
• Original Assignee: Glaxo Group Limited (GSK plc)
• Inventors: Burnell, Patricia Kwong Phieu, Taylor, Anthony James
• Primary Examiner(s): Bawa, Raj
• Application Number:
  US09/198,463
• Time in Patent Office: 1,064 Days
• Field of Search: 424/45, 424/46, 514/826, 514/937
• US Class Current: 424/45
• CPC Class Codes: A61K 9/008 comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
• CPC Class Codes: A61K 9/124 characterised by the propellant
• CPC Class Codes: A61K 9/5015 Organic compounds, e.g. fats, sugars

Abstract

Aerosol formulations comprising:

(A) A medicament in particulate form and having a surface coating of a surfactant;

(B) A hydrogen-containing fluorocarbon or chlorofluorocarbon propellant; and

(C) A cosolvent having higher polarity than the propellant which cosolvent is present in an amount of up to 5% w/w based upon propellant;

and methods for their preparation.

Claims

1. An aerosol formulation comprising:

(i) a hydrogen-containing fluorocarbon or chlorofluorocarbon propellant which is selected from the group consisting of CH₂ClF, CClF₂—

CHClF, CF₃—

CHClF, CHF₂—

CClF₂, CHClF—

CHF₂, CF₃—

CH₂Cl, CHF₂—

CHF₂, CF₃—

CH₂F, CClF₂—

CH₃, CHF₂—

CH₃ and CF₃CHFCF₃;

(ii) a cosolvent having higher polarity than the propellant, which cosolvent is present in an amount of less than 1% w/w based upon the weight of propellant; and

(iii) a medicament in particulate form, said medicament having a particle size of less than 100 μ

m and having a surface coating of a surfactant in an amount of from 0.05 to 5% w/w based upon the weight of the medicament, and wherein said surfactant has no affinity for said propellant.

2. A formulation as claimed in claim 1 wherein the propellant comprises 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoropropane.

3. A formulation as claimed in claim 1 wherein the propellant comprises 1,1,1,2-tetrafluoroethane.

4. A formulation as claimed in claim 1 which is substantially free of chlorofluorocarbons.

5. A formulation as claimed in claim 1 wherein the cosolvent is selected from the group consisting of an aliphatic alcohol or a polyol.

6. A formulation as claimed in claim 1 wherein the surfactant is selected from the group consisting of benzalkonium chloride, lecithin, oleic acid and sorbitan trioleate.

7. A formulation as claimed in claim 1 wherein the medicament is selected from the group consisting of salbutamol, salmeterol, beclomethasone esters or fluticasone esters.