Medicaments

• US 7,498,020 B2
• Filed: 11/23/2004
• Issued: 03/03/2009
• 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): Richter; Johann R
• Assistant Examiner(s): ALSTRUM ACEVEDO, JAMES HENRY
• Application Number:
  US10/994,318
• Publication Number:
  US 20050089477A1
• Time in Patent Office: 1,561 Days
• Field of Search: 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 31/4741 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 process for preparing a filled pharmaceutical aerosol canister which comprises:

(a) preparing a pharmaceutical aerosol formulation for use for the administration of medicaments by inhalation wherein the formulation comprises particulate fluticasone propionate as medicament and 1,1,1,2-tetrafluoroethane as propellant, which formulation is free of surfactant and chlorofluorcarbons; and

(b) filling the formulation into a canister.

2. A process according to claim 1 wherein the formulation of step (a) is substantially free of alcohols.

3. A process according to claim 1 wherein the formulation of step (a) consists essentially of particulate fluticasone propionate as medicament and 1,1,1,2-tetrafluoroethane as propellant.

4. A process according to claim 1 wherein the formulation of step (a) consists of particulate fluticasone propionate as medicament and 1,1,1,2-tetrafluoroethane as propellant.

5. A process according to claim 1 wherein the formulation of step (a) contains particulate salmeterol or a physiologically acceptable salt thereof in combination with particulate fluticasone propionate as medicament.

6. A process according to claim 5 wherein the formulation of step (a) contains salmeterol xinafoate in combination with fluticasone propionate as medicament.

7. A process according to claim 1 wherein the formulation of step (a) consists essentially of particulate salmeterol or a physiologically acceptable salt thereof in combination with particulate fluticasone propionate as medicament and 1,1,1,2-tetrafluoroethane as propellant.

8. A process according to claim 1 wherein the formulation of step (a) consists of particulate salmeterol or a physiologically acceptable salt thereof in combination with particulate fluticasone propionate as medicament and 1,1,1,2-tetrafluoroethane as propellant.

9. A process according to claim 7 wherein salmeterol is present as its xinafoate salt.

10. A process according to claim 8 wherein salmeterol is present as its xinafoate salt.

11. A process according to claim 1 wherein in the formulation of step (a) the medicament is present in an amount of 0.005-5% w/w relative to the total weight of the formulation.

12. A process according to claim 11 wherein in the formulation of step (a) the medicament is present in an amount of 0.01-1% w/w relative to the total weight of the formulation.

13. A process according to claim 1 wherein in step (a) the formulation is prepared by dispersing the medicament in the propellant.

14. A process according to claim 1 wherein the canister is an aluminium can which is closed with a metering valve.

15. A process according to claim 14 wherein in step (b) an aliquot of the formulation is filled through the metering valve into the canister.

16. A process according to claim 1 which comprises:

(a) adding particulate medicament to a charge vessel and pressure filling the liquefied propellant through the charge vessel into a manufacturing vessel to form a drug suspension;

(b) mixing the drug suspension before recirculation to a filling machine; and

(c) filling an aliquot of the drug suspension through the metering valve into a canister, said canister being formed of an aluminium can to which a metering valve has been crimped.