Composition comprising salbutamol sulphate

Patent metadata

Field	Value
Publication number	US-10959965-B2
Application number	US-201414784798-A
Country	US
Kind code	B2
Filing date	Apr 17, 2014
Priority date	Apr 17, 2013
Publication date	Mar 30, 2021
Grant date	Mar 30, 2021

Abstract

A pharmaceutical composition is described that is suitable for delivery from a pressurised container. The composition is preferably free of polar excipients and comprises: (a) a propellant component that consists essentially of 1,1-difluoroethane (R-152a); (b) a surfactant component that comprises at least one surfactant compound other than oleic acid; and (c) a drug component that consists of salbutamol sulphate. The pharmaceutical composition can be delivered using a metered dose inhaler (MDI).

First claim

What is claimed is:

1. A pharmaceutical composition that is free of polar excipients, said composition comprising:
(a) a propellant component consisting essentially of 1,1-difluoroethane (R-152a) propellant,
(b) a surfactant component consisting essentially of polyvinylpyrrolidone surfactant; and
(c) a drug component consisting of solid drug particles of salbutamol sulphate,
wherein the 1,1-difluoroethane propellant and polyvinylpyrrolidone surfactant provide a propellant/surfactant mixture in which the solid drug particles of salbutamol sulphate are suspended, and
wherein the salbutamol sulphate and the polyvinylpyrrolidone are included in the mixture with the propellant as separate components.

2. The pharmaceutical composition of claim 1 which consists essentially of components (a), (b) and (c).

3. A pharmaceutical composition for delivery from a pressurised container, said composition consisting essentially of:
(a) a propellant component consisting essentially of 1,1-difluoroethane (R-152a) propellant,
(b) a surfactant component consisting essentially of polyvinylpyrrolidone surfactant; and
(c) a drug component consisting of solid drug particles of salbutamol sulphate,
wherein the 1,1-difluoroethane propellant and polyvinylpyrrolidone surfactant provide a propellant/surfactant mixture in which the solid drug particles of salbutamol sulphate are suspended, and

wherein the salbutamol sulphate and the polyvinylpyrrolidone are included in the mixture with the propellant as separate components.

4. The pharmaceutical composition of claim 1 which consists entirely of components (a), (b) and (c).

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

6. A sealed container that contains a pharmaceutical composition as claimed in claim 1 .

7. The sealed container of claim 6 which is a pressurized container for use with a metered dose inhaler (MDI).

8. A metered dose inhaler (MDI) fitted with a pressurized container as claimed in claim 7 .

9. A method for treating a patient suffering or likely to suffer from a respiratory disorder which comprises administering to the patient a therapeutically or prophylactically effective amount of a pharmaceutical composition as claimed in claim 1 .

10. The method of claim 9 , wherein the respiratory disorder is asthma.

11. The method of claim 9 , wherein the pharmaceutical composition is delivered to the patient using a metered dose inhaler (MDI).

12. The pharmaceutical composition of claim 3 which consists entirely of components (a), (b) and (c).

13. The pharmaceutical composition of claim 12 , wherein the propellant component consists entirely of 1,1-difluoroethane (R-152a).

14. The pharmaceutical composition of claim 2 , wherein the propellant component consists entirely of 1,1-difluoroethane (R-152a).

15. The pharmaceutical composition of claim 3 , wherein the propellant component consists entirely of 1,1-difluoroethane (R-152a).

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

17. The pharmaceutical composition of claim 1 comprising from 0.01 to 1.0 weight % of the drug component, from 96.5 to 99.94 weight % of the propellant component and from 0.05 to 2.5 weight % of the surfactant component.

18. The pharmaceutical composition of claim 2 consisting essentially of from 0.01 to 1.0 weight % of the drug component, from 96.5 to 99.94 weight % of the propellant component and from 0.05 to 2.5 weight % of the surfactant component.

19. The pharmaceutical composition of claim 3 consisting essentially of from 0.01 to 1.0 weight % of the drug component, from 96.5 to 99.94 weight % of the propellant component and from 0.05 to 2.5 weight % of the surfactant component.

20. The pharmaceutical composition of claim 4 consisting of from 0.01 to 1.0 weight % of the drug component, from 96.5 to 99.94 weight % of the propellant component and from 0.05 to 2.5 weight % of the surfactant component.

21. The pharmaceutical composition of claim 5 comprising from 0.01 to 1.0 weight % of the drug component, from 96.5 to 99.94 weight % of the propellant component and from 0.05 to 2.5 weight % of the surfactant component.

22. The pharmaceutical composition of claim 1 further comprising a valve lubricant.

23. The pharmaceutical composition of claim 1 which has been prepared: (i) by mixing the propellant component, the surfactant component, and the salbutamol sulphate together in the required proportions in a suitable mixing vessel, or (ii) by introducing a weighed amount of the salbutamol sulphate into an open container, fitting a valve device onto the container, introducing the propellant component, in liquid form, through the valve into the container under pressure and introducing the surfactant component, either alone or as a premix with the propellant, through the valve into the container under pressure, or (iii) by introducing a weighed amount of the salbutamol sulphate into an open container, introducing the surfactant component into the container, fitting a valve device onto the container, and introducing the propellant component, in liquid form, through the valve into the container under pressure.

24. The pharmaceutical composition of claim 3 which has been prepared: (i) by mixing the propellant component, the surfactant component, and the salbutamol sulphate together in the required proportions in a suitable mixing vessel, or (ii) by introducing a weighed amount of the salbutamol sulphate into an open container, fitting a valve device onto the container, introducing the propellant component, in liquid form, through the valve into the container under pressure and introducing the surfactant component, either alone or as a premix with the propellant, through the valve into the container under pressure, or (iii) by introducing a weighed amount of the salbutamol sulphate into an open container, introducing the surfactant component into the container, fitting a valve device onto the container, and introducing the propellant component, in liquid form, through the valve into the container under pressure.

Assignees

• Mexichem Amanco Holding Sa

Inventors

• Corr Stuart
• Noakes Timothy James

Classifications

• A61P11/06

  Antiasthmatics · CPC title

• A61K9/008

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

• A61K9/124

  characterised by the propellant · CPC title

• A61P11/00

  Drugs for disorders of the respiratory system · CPC title

• A61K31/137 Primary

  Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone} · CPC title