Details for Patent: 8,246,934

Title:	Respiratory dispersion for metered dose inhalers comprising perforated microstructures
Abstract:	A respiratory dispersion for pulmonary delivery comprises one or more bioactive agents, a suspension medium, and a plurality of perforated microstructures having a mean aerodynamic diameter of less than 5 .mu.m. The suspension medium comprises at least one propellant and permeates the perforated microstructures.
Inventor(s):	Weers; Jeffry G. (Belmont, CA), Schutt; Ernest G. (San Diego, CA), Dellamary; Luis A. (San Marcos, CA), Tarara; Thomas E. (Burlingame, CA), Kabalnov; Alexey (Corvallis, OR)
Assignee:	Novartis AG (Basel, CH)
Filing Date:	Sep 03, 2010
Application Number:	12/875,966
Claims:	1. A respiratory dispersion for pulmonary delivery, the respiratory dispersion comprising: one or more bioactive agents; a suspension medium; a plurality of perforated microstructures having a mean aerodynamic diameter of less than 5 .mu.m, wherein said suspension medium comprises at least one propellant and permeates said perforated microstructures. 2. The respiratory dispersion of claim 1, wherein said propellant is selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane, perfluoroethane, monochlorodifluoromethane, 1,1-difluoroethane and combinations thereof. 3. The respiratory dispersion of claim 1 wherein said perforated microstructures comprise a surfactant. 4. The respiratory dispersion of claim 3 wherein said surfactant is selected from the group consisting of phospholipids, nonionic detergents, nonionic block copolymers, ionic surfactants, biocompatible fluorinated surfactants and combinations thereof. 5. The respiratory dispersion of claim 3 wherein said surfactant comprises a phospholipid. 6. The respiratory dispersion of claim 5 wherein said phospholipid is selected from the group consisting of dilauroylphosphatidylcholine, dioleylphosphatidylcholine, dipalmitoylphosphatidylcholine, disteroylphosphatidyl-choline behenoylphosphatidylcholine, arachidoylphosphatidylcholine and combinations thereof. 7. The respiratory dispersion of claim 1 wherein the mean geometric diameter of the perforated microstructures is between 1 and 5 .mu.m. 8. The respiratory dispersion of claim 1 wherein said bioactive agent is selected from the group consisting of antiallergics, bronchodilators, pulmonary lung surfactants, analgesics, antibiotics, antiinfectives, leukotriene inhibitors or antagonists, antihistamine, antiinflammatories, antineoplastics, antocholinergics, anesthetics, anti-tuberculars, imaging agents, cardiovascular agents, enzymes, steroids, genetic material, viral vectors, antisense agents, proteins, peptides, and combinations thereof. 9. A respiratory dispersion of claim 1 wherein the bioactive agent comprises a bronchodilator. 10. A respiratory dispersion of claim 9 wherein said bronchodilator is selected from ephedrine, adrenaline, fenoterol, formoterol, isoprenaline, metaproterenol, albuterol, salmeterol, and terbutaline. 11. A respiratory dispersion of claim 1 wherein the bioactive agent comprises an anti-inflammatory agent. 12. A respiratory dispersion of claim 11 wherein the anti-inflammatory agent comprises an anti-inflammatory steroid. 13. A respiratory dispersion of claim 12 wherein the anti-inflammatory agent comprises one or more of fluticasone, beclomethasone, flunisolide, budesonide, tripedane, cortisone, prednisone, prednisolone, dexamethoasone, betamethasone or triamcinalone. 14. A respiratory dispersion of claim 1 comprising beclomethasone. 15. A respiratory dispersion of claim 1 comprising formoterol. 16. A respiratory dispersion of claim 1 comprising beclomethasone diproprionate and formoterol. 17. A respiratory dispersion of claim 1 wherein the bioactive agent comprises an anti-cholinergic agent. 18. A respiratory dispersion of claim 17 where the anti-cholinergic agent comprises one or more of ipratropium, atropine, or oxitropium. 19. A respiratory dispersion of claim 9 wherein said bronchodilator is salbutamol.