Non-chlorofluorocarbon aerosol formulations

• US 5,474,759 A
• Filed: 12/09/1993
• Issued: 12/12/1995
• Est. Priority Date: 06/10/1991
• Status: Expired due to Term

• Current Assignee: Merck Sharp & Dohme Corporation (Merck & Co., Inc.)
• Original Assignee: Schering Corporation (Merck & Co., Inc.)
• Inventors: Chaudry, Imtiaz A., Sequeira, Joel A., Fassberg, Julianne, Kopcha, Michael
• Primary Examiner(s): GRIFFIN, RONALD
• Application Number:
  US08/157,182
• Time in Patent Office: 733 Days
• Field of Search: 424/45, 424/46, 422/34, 422/37, 514/826
• US Class Current: 424/45
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• 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: A61P 11/08 Bronchodilators
• CPC Class Codes: A61P 11/14 Antitussive agents
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: C09K 3/30 for aerosols aerosol containers B65D83/14

Abstract

Aerosol formulations substantially free of chlorofluorocarbons for oral and/or nasal administration are described. The formulations comprise 1,1,1,2,3,3,3-heptafluoropropane, a medicament, optionally an excipient and optionally a surfactant. Methods of treatment utilizing the formulations are also described.

Claims

1. An aerosol formulation consisting essentially of:

A. an effective amount of a medicament;

B. 1,1,1,2,3,3,3-heptafluoropropane;

C. optionally, an excipient selected from the group consisting of a propylene glycol diester of a medium chain fatty acid and a triglyceride ester of a medium chain fatty acid, a surfactant being optionally present together with the excipient; and

D. optionally, one or more components selected from one or more of the following;

preservatives;

buffers;

antioxidants;

sweeteners; and

taste masking agents.

2. The formulation of claim 1 wherein the medicament is selected from the group consisting of:

albuterol;

mometasone furoate;

beclomethasone dipropionate;

isoproterenol;

heparin;

terbutaline;

rimiterol;

pirbuterol;

disodium cromoglycate;

isoprenaline, adrenaline, pentamidine;

ipratropium bromide; and

salts and clathrates thereof.

3. The formulation of claim 1 wherein the medicament is selected from the group consisting of:

albuterol;

albuterol sulfate;

beclomethasone dipropionate;

beclomethasone dipropionate clathrates; and

mometasone furoate.

4. The formulation of claim 1 containing 0.01 to 1 percent by weight medicament.

5. The formulation of claim 1 containing 0.03 to 0.7 percent by weight medicament.

6. The formulation of claim 1 containing 0.05 to 0.5 percent by weight medicament.

7. The formulation of claim 1 wherein the medicament is a powder having a mean particle size of 1 to 5 microns.

8. An aerosol formulation consisting essentially of:

A. a medicament selected from the group consisting of albuterol, mometasone furoate, beclomethasone dipropionate, and salts and clathrates thereof;

B. 1,1,1,2,3,3,3-heptafluoropropane;

C. optionally, an excipient selected from the group consisting of a propylene glycol diester of a medium chain fatty acid and a triglyceride ester of a medium chain fatty acid, a surfactant being optionally present together with the excipient; and

D. optionally, one or more components selected from one or more of the following;

preservatives;

buffers;

antioxidants;

sweeteners; and

taste masking agents.

9. An aerosol formulation consisting essentially of:

A. an effective amount of mometasone furoate;

B. 1,1,1,2,3,3,3-heptafluoropropane; and

C. optionally, one or more components selected from at least one of the following;

excipients;

surfactants; and

additives which are;

preservatives;

buffers;

antioxidants;

sweeteners; and

taste masking agents.

10. The formulation of claim 9 containing the following:

space="preserve" listing-type="tabular">______________________________________ Component Weight Percent ______________________________________ Mometasone Furoate 0.01-1 1,1,1,2,3,3,3-Heptafluoropropane 25-99.99 Excipient 0-75 Surfactant 0-3. ______________________________________

11. The formulation of claim 10 containing the following:

space="preserve" listing-type="tabular">______________________________________ Component Weight Percent ______________________________________ Mometasone Furoate 0.03-0.7 1,1,1,2,3,3,3-Heptafluoropropane 50-99.97 Excipient 0-50 Surfactant 0-2. ______________________________________

12. The formulation of claim 11 containing the following:

space="preserve" listing-type="tabular">______________________________________ Component Weight Percent ______________________________________ Mometasone Furoate 0.05-0.5 1,1,1,2,3,3,3-Heptafluoropropane 50-99.95 Excipient 0-50 Surfactant 0-1. ______________________________________

13. The formulation of claim 9 which is substantially free of chlorofluorocarbons.