Pharmaceutical aerosol formulation containing a particulate medicament, a propellant and substantially free of a surfactant

• US 6,251,368 B1
• Filed: 06/17/1997
• Issued: 06/26/2001
• Est. Priority Date: 12/12/1991
• Status: Expired due to Fees

• Current Assignee: Glaxo Group Limited (GSK plc)
• Original Assignee: Glaxo Group Limited (GSK plc)
• Inventors: Wyatt, David Andrew, Taylor, Anthony James, Akehurst, Rachel Ann
• Primary Examiner(s): Bawa, Raj
• Application Number:
  US08/877,198
• Time in Patent Office: 1,470 Days
• Field of Search: 424/45, 424/46, 514/937
• US Class Current: 424/45
• 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

A pharmaceutical aerosol formulation which comprises particulate medicament selected from the group consisting of salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate and physiologically acceptable salts and solvates thereof and a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant, which formulation is substantially free of surfactant is disclosed. Also disclosed is a method of treating respiratory disorders which comprises administration by inhalation of an effective amount of the, pharmaceutical aerosol formulation which may be contained in a canister.

Claims

1. A pharmaceutical aerosol formulation which comprises particulate medicament selected from the group consisting of salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate and physiologically acceptable salts and solvates 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 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.

2. A formulation as claimed in claim 1 wherein the medicament is salmeterol xinafoate.

3. A formulation as claimed in claim 1 wherein the medicament is salbutamol sulphate.

4. A formulation as claimed in claim 1 wherein the medicament is fluticasone propionate.

5. A formulation as claimed in claim 1 wherein the medicament is beclomethasone dipropionate or a physiologically acceptable solvate thereof.

6. A formulation as claimed in any one of claims 1 or 2 to 5 wherein the medicament is present in an amount of 0.005 to 10% w/w based on the total weight of the formulation.

7. A formulation as claimed in any one of claims 1, 2 to 5 or 6 which contains two or more particulate medicaments.

8. A formulation as claimed in claim 7 which contains salbutamol or salmeterol or a physiologically acceptable salt thereof in combination with an anti-inflammatory steroid or an anti-allergic.

9. A formulation as claimed in claim 8 which contains salmeterol or salbutamol or a physiologically acceptable salt thereof in combination with fluticasone propionate or beclomethasone dipropionate or a physiologically acceptable solvate thereof.

10. A formulation as claimed in claim 9 which contains salmeterol xinafoate and fluticasone propionate.

11. A formulation as claimed in claim 9 which contains salbutamol and beclomethasone dipropionate.

12. A formulation as claimed in any one of claims 1, 2 to 5 or 7 to 11 which has a respirable fraction of 20% or more by weight of the medicament.

13. A formulation as claimed in any one of claims 1, 2 to 5 or 8-12 wherein said particulate medicament is surface-modified.