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Details for Patent: 8,168,223

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Details for Patent: 8,168,223

Title:Engineered particles and methods of use
Abstract: Engineered particles are provided may be used for the delivery of a bioactive agent to the respiratory tract of a patient. The particles may be used in the form of dry powders or in the form of stabilized dispersions comprising a nonaqueous continuous phase. In particularly preferred embodiments the particles may be used in conjunction with an inhalation device such as a dry powder inhaler, metered dose inhaler or a nebulizer.
Inventor(s): Tarara; Thomas E. (San Diego, CA), Weers; Jeffry G. (San Diego, CA), Kabalnov; Alexey (Corvallis, OR), Schutt; Ernest G. (San Diego, CA), Dellamary; Luis A. (San Marcos, CA)
Assignee: Novartis Pharma AG (Basel, CH)
Filing Date:Jun 21, 2001
Application Number:09/886,296
Claims:1. An inhaleable powder composition comprising a plurality of particulate microstructures, the particulate microstructures comprising: (a) a structural matrix comprising phospholipid and calcium, wherein the particulate microstructures comprise greater than about 50% phospholipid; (b) an active agent; (c) a mean geometric diameter of 1-30 microns; (d) a mean aerodynamic diameter of less than 5 microns; and (e) a bulk density of less than about 0.5 g/cm.sup.3.

2. The composition of claim 1 wherein the particulate microstructures are porous and have a mean porosity of 0.5-80%.

3. The composition of claim 2 wherein the particulate microstructures have a mean porosity of 2-40%.

4. The composition of claim 3 wherein the particulate microstructures have a mean pore size of 20-200 nm.

5. The composition of claim 1 wherein the fine particle fraction of the particulate microstructures in the composition is greater than 20% w/w.

6. The composition of claim 5 wherein the fine particle fraction of the particulate microstructures in the composition is from about 30% to 70% w/w.

7. The composition of claim 1 wherein the particulate microstructures comprise a bulk density of less than 0.1 g/cm.sup.3.

8. The composition of claim 7 wherein the particulate microstructures comprise a bulk density of less than 0.05 g/cm.sup.3.

9. The composition of claim 1 wherein the particulate microstructures comprise perforated microstructures.

10. The composition of claim 1 wherein said particulate microstructures comprise hollow microspheres.

11. The composition of claim 1 wherein the particulate microspheres comprise a shell with a thickness of 0.1-0.5 .mu.m.

12. The composition of claim 1 wherein the particulate microstructures comprise a mean aerodynamic diameter of between 0.5 .mu.m and 5 .mu.m.

13. The composition of claim 1 wherein the particulate microstructures comprise a mean geometric diameter of less than 10 microns.

14. The composition of claim 13 wherein the particulate microstructures comprise mean geometric diameter is less than 5 microns.

15. The composition of claim 1 wherein the phospholipid comprises a gel to liquid crystal transition temperature of greater than 40.degree. C.

16. The composition of claim 1 wherein the phospholipid comprises a zwitterionic phospholipid.

17. The composition of claim 1 wherein the phospholipid comprises at least one of dilauroylphosphatidylcholine, dioleoylphosphatidylcholine, dipalmitoylphosphatidylcholine, disteroylphosphatidylcholine dibehenoylphosphatidylcholine, diarachidoylphosphatidylcholine and combinations thereof.

18. The composition of claim 1 wherein the active agent is a bioactive agent.

19. The composition of claim 18 wherein the bioactive agent comprises at least one of antiallergics, bronchodilators, pulmonary lung surfactants, analgesics, antibiotics, antiinfectives, leukotriene inhibitors or antagonists, antihistamines, antiinflammatories, antineoplastics, anticholinergics, anesthetics. antituberculars, antivirals, fungicides, immunoactive agents, vaccines, immunosuppressive agents, imaging agents, cardiovascular agents, enzymes, steroids, DNA, RNA, viral vectors, antisense agents, proteins, peptides and combinations thereof.

20. The composition of claim 18 wherein the bioactive agent comprises at least one of fentanyl, morphine, lung surfactant, leuprolide, interferon, insulin, budesonide, formoterol, goserelin, and growth hormones.

21. The composition of claim 18 wherein the bioactive agent is an aminoglycoside antibiotic.

22. The composition of claim 18 wherein the bioactive agent is a fungicide.

23. A composition comprising a plurality of particulate microstructures, the particulate microstructures comprising: (a) a structural matrix comprising phospholipid and calcium, the phospholipid comprising a gel to liquid crystal transition temperature of greater than 40.degree. C., wherein greater than about 50% of the particulate microstructures comprise phospholipid; (b) an active agent; (c) a mean geometric diameter of 1-30 microns; (d) a mean aerodynamic diameter of less than 5 microns; and (e) a bulk density of less than about 0.5 g/cm.sup.3.

24. The composition of claim 23 wherein the particulate microstructures are porous and have a mean porosity of 0.5-80%.

25. The composition of claim 24 wherein the particulate microstructures have a mean porosity of 2-40%.

26. The composition of claim 24 wherein the particulate microstructures have a mean pore size of 20-200 nm.

27. The composition of claim 23 wherein the fine particle fraction of the particulate microstructures in the composition is greater than 20% w/w.

28. The composition of claim 27 wherein the fine particle fraction of the particulate microstructures in the composition is from about 30% to 70% w/w.

29. The composition of claim 23 wherein the particulate microstructures comprise a bulk density of less than 0.1 g/cm.sup.3.

30. The composition of claim 29 wherein the particulate microstructures comprise a bulk density of less than 0.05 g/cm.sup.3.

31. The composition of claim 23 wherein the particulate microstructures comprise perforated microstructures.

32. The composition of claim 23 wherein said particulate microstructures comprise hollow microspheres.

33. The composition of claim 23 wherein the particulate microspheres comprise a shell with a thickness of 0.1-0.5 .mu.m.

34. The composition of claim 23 wherein the particulate microstructures comprise a mean aerodynamic diameter of between 0.5 .mu.m and 5 .mu.m.

35. The composition of claim 23 wherein the particulate microstructures comprise a mean geometric diameter of less than 10 microns.

36. The composition of claim 35 wherein the particulate microstructures comprise mean geometric diameter is less than 5 microns.

37. The composition of claim 23 wherein the phospholipid comprises a gel to liquid crystal transition temperature of greater than 40.degree. C.

38. The composition of claim 23 wherein the phospholipid comprises a zwitterionic phospholipid.

39. The composition of claim 23 wherein the phospholipid comprises at least one of dilauroylphosphatidylcholine, dioleoylphosphatidylcholine, dipalmitoylphosphatidylcholine, disteroylphosphatidylcholine dibehenoylphosphatidylcholine, diarachidoylphosphatidylcholine and combinations thereof.

40. The composition of claim 23 wherein the active agent is a bioactive agent.

41. The composition of claim 40 wherein the bioactive agent comprises at least one of antiallergics, bronchodilators, pulmonary lung surfactants, analgesics, antibiotics, antiinfectives, leukotriene inhibitors or antagonists, antihistamines, antiinflammatories, antineoplastics, anticholinergics, anesthetics. antituberculars, antivirals, fungicides, immunoactive agents, vaccines, immunosuppressive agents, imaging agents, cardiovascular agents, enzymes, steroids, DNA, RNA, viral vectors, antisense agents, proteins, peptides and combinations thereof.

42. The composition of claim 40 wherein the bioactive agent comprises at least one of fentanyl, morphine, lung surfactant, leuprolide, interferon, insulin, budesonide, formoterol, goserelin, and growth hormones.

43. The composition of claim 40 wherein the bioactive agent is an aminoglycoside antibiotic.

44. The composition of claim 40 wherein the bioactive agent is a fungicide.
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