Medicaments

• US 20030143163A1
• Filed: 03/11/2003
• Published: 07/31/2003
• Est. Priority Date: 12/12/1991
• Status: Abandoned Application

• Current Assignee: Glaxo Group Limited (Glaxosmithkline Holdings Ltd.)
• Original Assignee: Glaxo Group Limited (Glaxosmithkline Holdings Ltd.)
• Inventors: Wyatt, David Andrew, Taylor, Anthony James, Akehurst, Rachel Ann
• Application Number:
  US10/384,568
• Publication Number:
  US 20030143163A1
• Time in Patent Office: Days
• US Class Current: 424/46
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/138 Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/352 condensed with carbocyclic rings, e.g. methantheline cannabinoids A61K31/658
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61K 31/4402 only substituted in position 2, e.g. pheniramine, bisacodyl
• CPC Class Codes: A61K 31/4458 only substituted in position 2, e.g. methylphenidate
• CPC Class Codes: A61K 31/4535 containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
• CPC Class Codes: A61K 31/4741 condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
• CPC Class Codes: A61K 31/48 Ergoline derivatives, e.g. lysergic acid, ergotamine
• CPC Class Codes: A61K 31/522 having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/0073 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 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 11/00 : Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/02 : Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 11/06 : Antiasthmatics
• CPC Class Codes: A61P 11/08 : Bronchodilators

Abstract

This invention relates to aerosol formulations of use for the administration of medicaments by inhalation, in particular a pharmaceutical aerosol formulation which comprises particulate salbutamol and physiologically acceptable salts and solvates thereof and a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant, which formulation is substantially free of surfactant. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as defined is also described.

Claims

1. A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, with the proviso that when said formulation consists essentially of salbutamol or salbutamol sulphate and 1,1,1,2-tetrafluoroethane the weight to weight ratio of medicament to propellant is other than 69:

7900 (0.866%).

9. A formulation as claimed in any one of claims 1 to 8 wherein the medicament is salbutamol sulphate.

10. A formulation as claimed in any one of claims 1 to 8 which contains salbutamol or a physiologically acceptable salt or solvate thereof in combination with an anti-inflammatory steroid or an anti-allergic.

11. A formulation as claimed in any one of claims 1 to 8 which contains salbutamol or a physiologically acceptable salt or solvate thereof in combination with fluticasone propionate or beclomethasone dipropionate or a physiologically acceptable solvate thereof.

12. A formulation as claimed in any one of claims 1 to 8 which contains salbutamol and beclomethasone dipropionate.

13. A formulation as claimed in any one of claims 1 to 8 which has a respirable fraction of 20% or more by weight of the salbutamol or a physiologically acceptable salt or solvate thereof.

2. A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, with the provisos that when said formulation consists essentially of salbutamol and 1,1,1,2-tetrafluoroethane in a weight ratio of 0.05:

18, said salbutamol is present in the form of a physiologically acceptable salt and when said formulation consists essentially of salbutamol or salbutamol sulphate and 1,1,1,2-tetrafluoroethane the weight to weight ratio of medicament to propellant is other than 69;

7900 (0.866%).

3. A pharmaceutical aerosol formulation consisting essentially of a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, with the proviso that when said formulation consists essentially of salbutamol or salbutamol sulphate and 1,1,1,2-tetrafluoroethane the weight to weight ratio of medicament to propellant is other than 69:

7900 (0.866%).

4. A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, and wherein the salbutamol or a physiologically acceptable salt or solvate thereof is present in an amount of less than 0.866% w/w based on the total weight of the formulation.

5. A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, and wherein the salbutamol or a physiologically acceptable salt or solvate thereof is present in an amount of 0.005 to 0.594% w/w based on the total weight of the formulation.

6. A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, and wherein the salbutamol or a physiologically acceptable salt or solvate thereof is present in an amount of 0.005 to 0.264% w/w based on the total weight of the formulation.

7. A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, and wherein the salbutamol or a physiologically acceptable salt or solvate thereof is present in an amount of 0.005 to 0.174% w/w based on the total weight of the formulation.

8. A pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant, and wherein the weight ratio of salbutamol or a pharmaceutically acceptable salt or solvate thereof to propellant is less than 0.05:

18.

14. A canister suitable for delivering a pharmaceutical aerosol formulation which comprises a container capable of withstanding the vapour pressure of the propellant used, which container is closed with a metering valve and contains a pharmaceutical aerosol formulation which comprises a physiologically effective amount of particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant and with the proviso that when said formulation consists essentially of salbutamol or salbutamol sulphate and 1,1,1,2-tetrafluoroethane the weight to weight ratio of medicament to propellant is other than 69:

7900 (0.866%).

15. A canister as claimed in claim 14 wherein the container is a metal can.

16. A metered dose inhaler which comprises a canister as claimed in claim 14 fitted into a suitable channelling device.

17. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation which comprises particulate salbutamol or a physiologically acceptable salt or solvate thereof and 1,1,1,2-tetrafluoroethane as propellant, which formulation is substantially free of surfactant.