Pharmaceutical composition

Patent metadata

Field	Value
Publication number	US-11559506-B2
Application number	US-201916575069-A
Country	US
Kind code	B2
Filing date	Sep 18, 2019
Priority date	Dec 4, 2015
Publication date	Jan 24, 2023
Grant date	Jan 24, 2023

Abstract

A pharmaceutical composition is described. The composition comprises: (i) at least one formoterol compound selected from formoterol, pharmaceutically acceptable salts of formoterol, prodrugs of formoterol, solvates of formoterol, solvates of pharmaceutically acceptable salts of formoterol and solvates of prodrugs of formoterol; (ii) at least one corticosteroid; (iii) a surfactant component comprising at least one surfactant compound; and (iv) a propellant component comprising 1,1-difluoroethane (R-152a).

First claim

What is claimed is:

1. A pharmaceutical composition comprising:
(i) formoterol fumarate dihydrate;
(ii) budesonide;
(iii) a surfactant; and
(iv) a propellant component comprising at least 90 weight % 1,1-difluoromethane (R-152a);
wherein the pharmaceutical composition is in the form of a suspension.

2. The pharmaceutical composition of claim 1 further comprising ethanol.

3. The pharmaceutical composition of claim 1 which is free of ethanol.

4. The pharmaceutical composition of claim 1 , wherein at least 95 weight % of the pharmaceutical composition consists of the four components (i), (ii), (iii), and (iv).

5. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition consists entirely of the four components (i), (ii), (iii) and (iv).

6. The pharmaceutical composition of claim 1 , wherein at least 95 weight % of the propellant component is 1,1-difluoroethane (R-152a).

7. The pharmaceutical composition of claim 6 , wherein the propellant component comprises from 0.5 to 10 ppm of unsaturated impurities.

8. The pharmaceutical composition of claim 1 , wherein the surfactant is selected from the group consisting of polyvinylpyrrolidone, a polyethylene glycol surfactant and a mixture thereof.

9. The pharmaceutical composition of claim 1 which after storage in uncoated aluminum containers at 40° C. and 75% relative humidity for 3 months will produce less than 0.7% by weight of impurities from the degradation of the formoterol fumarate dihydrate and the budesonide based on the total weight of the formoterol fumarate dihydrate, the budesonide and the impurities.

10. The pharmaceutical composition of claim 9 which after storage in uncoated aluminum containers at 40° C. and 75% relative humidity for 3 months will produce less than 0.5% by weight of impurities from the degradation of the formoterol fumarate dihydrate and the budesonide based on the total weight of the formoterol fumarate dihydrate, the budesonide and the impurities.

11. The pharmaceutical composition of claim 10 which after storage in uncoated aluminum containers at 40° C. and 75% relative humidity for 3 months will produce less than 0.3% by weight of impurities from the degradation of the formoterol fumarate dihydrate and the budesonide based on the total weight of the formoterol fumarate dihydrate, the budesonide and the impurities.

12. The pharmaceutical composition of claim 1 , wherein at least 99.0% by weight of the formoterol fumarate dihydrate and the budesonide that are contained originally in the pharmaceutical composition immediately following preparation will be present in the composition after storage in uncoated aluminum containers at 40° C. and 75% relative humidity for 3 months.

13. The pharmaceutical composition of claim 12 , wherein at least 99.5% by weight of the formoterol fumarate dihydrate and the budesonide that are contained originally in the pharmaceutical composition immediately following preparation will be present in the composition after storage in uncoated aluminum containers at 40° C. at 75% relative humidity for 3 months.

14. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises less than 500 ppm of water based on the total weight of the pharmaceutical composition.

15. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises less than 1000 ppm of oxygen based on the total weight of the pharmaceutical composition.

16. The pharmaceutical composition of claim 1 , wherein the formoterol fumarate dihydrate and the budesonide are in a micronized form and wherein the pharmaceutical composition is free of perforated microstructures.

17. A sealed container which is a pressurized aerosol container for use with a metered dose inhaler (MDI) that comprises a pharmaceutical composition as claimed in claim 1 .

18. A metered dose inhaler (MDI) fitted with a sealed container as claimed in claim 17 .

19. The pharmaceutical composition of claim 1 , comprising from 0.01 to 1.0 weight % of the formoterol fumarate dihydrate and the budesonide combined.

Assignees

• Mexichem Fluor Sa De Cv

Inventors

• Corr Stuart
• Noakes Timothy James

Classifications

• A61K31/573

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

• A61K9/0073

  Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy; (nasal sprays A61K9/0043; inhalation of vapours of volatile or heated drugs, e.g. essential oils or nicotine, A61K9/007; devices A61M) · 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

• A61K31/167 Primary

  having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol · CPC title