Pharmaceutical compositions

Patent metadata

Field	Value
Publication number	US-10668018-B2
Application number	US-201916249133-A
Country	US
Kind code	B2
Filing date	Jan 16, 2019
Priority date	May 13, 2011
Publication date	Jun 2, 2020
Grant date	Jun 2, 2020

Abstract

A pharmaceutical solution for a medication delivery apparatus, especially a metered dose inhaler, is described. The pharmaceutical solution comprises: (a) a liquefied propellant component consisting essentially of and preferably consisting entirely of 1,1-difluoroethane (R-152a); (b) ethanol; and (c) a drug component dissolved in the propellant/ethanol mixture consisting of at least one drug selected from the group consisting of beclomethasone dipropionate (BDP) and fluticasone propionate (FP).

First claim

The invention claimed is:

1. A pharmaceutical composition comprising:
(a) a drug in an amount of 0.01 to 4.0 weight % based on the total weight of the pharmaceutical composition, wherein the drug comprises at least one corticosteroid;
(b) a propellant component consisting essentially of 1,1-difluoroethane (R-152a); and
(c) a first amount of ethanol;
wherein at least 95 weight % of the pharmaceutical composition is made up of the propellant component, the drug and the first amount of ethanol, the first amount of ethanol is an amount needed such that the pharmaceutical composition is in solution form, and the first amount of ethanol is less than a second amount of ethanol that is needed to dissolve the same amount of the drug where 1,1,1,2-tetrafluoroethane (R-134a) replaces the 1,1-difluoroethane (R-152a).

2. The composition of claim 1 , wherein at least 99 weight % of the pharmaceutical composition consists of the drug, the propellant component and ethanol.

3. The composition of claim 1 , wherein the pharmaceutical composition consists entirely of the drug, the propellant component and ethanol.

4. The composition of claim 1 , wherein the propellant component consists of 1,1-difluoroethane (R-152a).

5. A method of treating a patient suffering from a respiratory disorder responsive to a corticosteroid which comprises administering to the patient a therapeutically or prophylactically effective amount of the pharmaceutical composition of claim 1 .

6. A method of reducing an amount of ethanol required for dissolving a drug in a pharmaceutical solution comprising the drug, a propellant component, and ethanol, which method comprises mixing the propellant component, the drug in an amount of from 0.01 to 4.0 weight % based on a total weight of the pharmaceutical solution, and a first amount of ethanol needed to dissolve the drug and form the pharmaceutical solution;
wherein:
at least 95 weight % of the pharmaceutical solution is made up of the propellant component, the drug, and the ethanol,
the propellant component consists essentially of 1,1-difluoroethane (R-152a),
the first amount of ethanol is less than a second amount of ethanol that is needed to dissolve the same amount of the drug where 1,1,1,2-tetrafluoroethane (R-134a) replaces the 1,1-difluoroethane (R-152a), and
the drug comprises at least one corticosteroid.

7. The method of claim 6 , wherein at least 99 weight % of the pharmaceutical solution consists of the drug, the propellant component and ethanol.

8. The method of claim 6 , wherein the pharmaceutical solution consists entirely of the drug, the propellant component and ethanol.

9. The method of claim 6 , wherein the propellant component consists of 1,1-difluoroethane (R-152a).

10. A pharmaceutical solution for delivery using a medication delivery apparatus to treat a respiratory disorder comprising:
(a) a liquefied propellant component consisting essentially of 1,1-difluoroethane (R-152a);
(b) 1.0 to 20.0 weight % of ethanol based on a total weight of the pharmaceutical solution; and
(c) 0.01 to 4.0 weight % of a drug component dissolved in the pharmaceutical solution consisting of at least one corticosteroid.

11. The pharmaceutical solution of claim 10 , wherein at least 95 weight % of the solution is made up of components (a), (b) and (c).

12. The pharmaceutical solution of claim 11 , wherein at least 98 weight % of the solution is made up of components (a), (b) and (c).

13. The pharmaceutical solution of claim 12 , wherein at least 99 weight % of the solution is made up of components (a), (b) and (c).

14. The pharmaceutical solution of claim 10 , wherein the solution is made up entirely of components (a), (b) and (c).

15. The pharmaceutical solution of claim 10 , wherein the ethanol comprises from 1.0 to 12.0 weight % of the total weight of the pharmaceutical solution.

16. The pharmaceutical solution of claim 15 , wherein the ethanol comprises from 1.0 to 6.0 weight % of the total weight of the pharmaceutical solution.

17. The pharmaceutical solution of claim 10 which comprises from 93.0 to 98.0 weight % of the propellant component, from 1.0 to 6.0 weight % of the ethanol and from 0.01 to 2.0 weight % of the drug component.

18. The pharmaceutical solution of claim 10 , wherein the liquefied propellant component consists of 1,1-difluoroethane (R-152a).

19. A sealed container that contains a pharmaceutical solution as claimed in claim 10 .

20. A method for treating a patient suffering from a respiratory disorder responsive to a corticosteroid which comprises administering to the patient a therapeutically or prophylactically effective amount of a pharmaceutical solution as claimed in claim 10 .

21. The composition of claim 1 , wherein the corticosteroid is a halogenated corticosteroid.

Assignees

• Mexichem Amanco Holdings S A De C V
• Mexichem Amanco Holding Sa

Inventors

• Corr Stuart
• Noakes Timothy James

Classifications

• A61K9/008

  comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI] · CPC title

• A61K47/06

  Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite · CPC title

• A61K9/124 Primary

  characterised by the propellant · CPC title

• A61K31/56

  Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids · CPC title

• A61K31/573

  substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone · CPC title