Medicaments

• US 6,221,339 B1
• Filed: 05/10/1999
• Issued: 04/24/2001
• Est. Priority Date: 12/12/1991
• Status: Expired due to Fees

• 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
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): WARE, TODD
• Application Number:
  US09/307,552
• Time in Patent Office: 715 Days
• Field of Search: 424/45, 424/46
• 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 31/46 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
• 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 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• CPC Class Codes: A61K 9/008 comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]

Abstract

A pharmaceutical aerosol formulation comprising (i) particulate medicament, (ii) 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3,-heptafluoro-n-propane or a mixture thereof as propellant, and (iii) 0.01 to 5% w/w based upon the propellant of a polar cosolvent, the particulate medicament being present in an amount from 0.005% to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, and which formulation contains less than 0.0001% w/w surfactant based upon the weight of medicament.

Claims

1. A pharmaceutical aerosol formulation consisting essentially of (i) a particulate medicament which is triamcinolone acetonide, (ii) 1,1,1,2-tetrafluoroethane as propellant, and (iii) 0.05 to 5% w/w based upon propellant of a polar cosolvent which is ethanol, the particulate medicament being present in an amount from 0.005 to 5% w/w relative to the total weight of the formulation and having a particle size less than 100 microns, and which formulation contains less than 0.0001% w/w surfactant based upon the weight of medicament.

3. A formulation as claimed in claim 1 wherein the polar cosolvent is present in an amount of 0.05 to 3% w/w based upon the propellant.

4. A formulation as claimed in claim 1 wherein the polar cosolvent is present in an amount of less than 1% w/w based upon the propellant.

5. A formulation as claimed in claim 1 wherein the polar cosolvent is present in an amount of approximately 0.1% w/w based upon the propellant.

6. A formulation as claimed in claim 1 wherein the particulate medicament is present in an amount from 0.01% to 1% w/w relative to the total weight of the formulation.

13. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as claimed in claim 1.

2. A pharmaceutical aerosol formulation consisting of (i) a particulate medicament which is triamcinolone acetonide, (ii) 1,1,1,2-tetrafluoroethane as propellant, and (iii) 0.05 to 5% w/w based upon propellant of a polar cosolvent which is ethanol, the particulate medicament being present in an amount from 0.005 to 5% w/w relative to the total weight of the formulation and having a particle size less than 100 microns.

7. A formulation as claimed in claim 2 wherein the polar cosolvent is present in an amount of 0.05 to 3% w/w based upon the propellant.

8. A formulation as claimed in claim 2 wherein the polar cosolvent is present in an amount of less than 1% w/w based upon the propellant.

9. A formulation as claimed in claim 2 wherein the polar cosolvent is present in an amount of approximately 0.1% w/w based upon the propellant.

10. A formulation as claimed in claim 2 wherein the particulate medicament is present in an amount from 0.01% to 1% w/w relative to the total weight of the formulation.

14. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as claimed in claim 2.

11. A pharmaceutical aerosol formulation consisting essentially of (i) particulate medicament which is triamcinolone acetonide, (ii) 1,1,1,2-tetrafluoroethane as propellant, and (iii) approximately 0.1% w/w based upon propellant of a polar cosolvent which is ethanol, the particulate medicament being present in an amount from 0.01 to 1% w/w relative to the total weight of the formulation and having a particle size less than 100 microns, and which formulation contains less than 0.0001% w/w surfactant based upon the weight of medicament.

15. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as claimed in claim 11.

12. A pharmaceutical aerosol formulation consisting of (i) particulate medicament which is triamcinolone acetonide, (ii) 1,1,1,2-tetrafluoroethane as propellant, and (iii) approximately 0.1% w/w based upon propellant of a polar cosolvent which is ethanol, the particulate medicament being present in an amount from 0.01 to 1% w/w relative to the total weight of the formulation and having a particle size less than 100 microns.

16. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as claimed in claim 12.