Pharmaceutical compositions

Patent metadata

Field	Value
Publication number	US-10258568-B2
Application number	US-201615250319-A
Country	US
Kind code	B2
Filing date	Aug 29, 2016
Priority date	May 13, 2011
Publication date	Apr 16, 2019
Grant date	Apr 16, 2019

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 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 is 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 beclomethasone dipropionate (BDP) and/or fluticasone propionate (FP).

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

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

4. The method of claim 1 , wherein the drug is beclomethasone dipropionate (BDP).

5. The method of claim 1 , wherein the drug is fluticasone propionate (FP).

6. A pharmaceutical composition comprising:
a) a drug in an amount of 0.01 to 4.0 weight % based on a total weight of the pharmaceutical composition, wherein the drug comprises beclomethasone dipropionate (BDP) and/or fluticasone propionate (FP);
b) a propellant component, wherein the propellant component is 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).

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

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

9. The composition of claim 6 , wherein the drug is beclomethasone dipropionate (BDP).

10. The composition of claim 6 , wherein the drug is fluticasone propionate (FP).

11. A method of treating a patient suffering from a respiratory disorder responsive to BDP or FP which comprises administering to the patient a therapeutically or prophylactically effective amount of the pharmaceutical composition of claim 6 .

12. A pharmaceutical composition comprising:
(a) a drug in an amount of 0.01 to 4.0 weight % based on a total weight of the pharmaceutical composition, wherein the drug comprises beclomethasone dipropionate (BDP) and/or fluticasone propionate (FP);
(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).

Assignees

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

Inventors

• Corr Stuart
• Noakes Timothy James

Classifications

• A61K31/573

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

• A61K9/124 Primary

  characterised by the propellant · CPC title

• A61K47/10 Primary

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title

• A61K9/008

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

• A61K31/56

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