Particles for inhalation having sustained release properties
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IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/12
A61K-009/127
출원번호
US-0202616
(2002-07-23)
발명자
/ 주소
Basu,Sujit K.
Hrkach,Jeffrey
Lipp,Michael
Elbert,Katharina
Edwards,David A.
출원인 / 주소
Advanced Inhalation Research, Inc.
대리인 / 주소
Elmore Patent Law Group, PC
인용정보
피인용 횟수 :
46인용 특허 :
78
초록▼
The invention generally relates to a method for pulmonary delivery of therapeutic, prophylactic and diagnostic agents to a patient wherein the agent is released in a sustained fashion, and to particles suitable for use in the method. In particular, the invention relates to a method for the pulmonary
The invention generally relates to a method for pulmonary delivery of therapeutic, prophylactic and diagnostic agents to a patient wherein the agent is released in a sustained fashion, and to particles suitable for use in the method. In particular, the invention relates to a method for the pulmonary delivery of a therapeutic, prophylactic or diagnostic agent comprising administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising a therapeutic, prophylactic or diagnostic agent or any combination thereof in association with a charged lipid, wherein the charged lipid has an overall net charge which is opposite to that of the agent upon association with the agent. Release of the agent from the administered particles occurs in a sustained fashion.
대표청구항▼
What is claimed is: 1. A method for delivery via the pulmonary system comprising: administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising: a bioactive agent in association with a charged lipid wherein the charged
What is claimed is: 1. A method for delivery via the pulmonary system comprising: administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising: a bioactive agent in association with a charged lipid wherein the charged lipid has an overall net positive charge, the agent has an overall net negative charge upon association, the agent is not a nucleic acid and wherein release of the agent is sustained. 2. The method of claim 1, wherein association of the agent and charged lipid comprises an ionic complexation. 3. The method of claim 2, wherein association of the lipid and agent further comprises hydrogen bonding. 4. The method of claim 1, wherein the charge ratio of lipid to bioactive agent is from about 0.25:1 to about 1:0.25. 5. The method of claim 4, wherein the charge ratio of lipid to bioactive agent is from about 0.5:1 to about 1:0.5. 6. The method of claim 5, wherein the charge ratio of lipid to bioactive agent is about 1:1. 7. The method of claim 1, wherein the bioactive agent is a protein. 8. The method of claim 7, wherein the protein is insulin. 9. The method of claim 8, wherein the sustained release is at least about 6 hours post administration. 10. The method of claim 1, wherein the lipid is a 1,2-diacyl-sn-glycero-3-alkylphosphocholine or a 1,2-diacyl-sn-glycero-3-alkylphosphoalkanolamine. 11. The method of claim 10 wherein the 1,2-diacyl-sn-glycero-3-alkylphosphocholine lipid is represented by Formula III: wherein, R1 and R2 are independently an aliphatic group having from about 3 to about 24 carbons; and R3 is an aliphatic group having from about 1 to about 24 carbons. 12. The method of claim 10, wherein the 1,2-diacyl-sn-glycero-3-alkylphosphocholine is 1,2-dipalmitoyl-sn-glycero-3-ethylphosphocholine (DPePC), 1,2-dimyristoyl-sn-glycero-3-ethylphosphocholine(DMePC), 1,2-distearoyl-sn-glycero-3-ethylphosphocholine(DSePC), 1,2-dilauroyl-sn-glycero-3-ethyiphosphocholine (DLePC), 1,2-dioleoyl-sn-glycero-3-ethylphosphocholine(DOePC) or any combination thereof. 13. The method of claim 10, wherein the 1,2-diacyl-sn-glycero-3-alkylphosphoalkanolamine is represented by Formula IV: wherein, R1 and R2 are independently an aliphatic group having from about 3 to about 24 carbons; R3 is an aliphatic group having from about 1 to about 24 carbons; and R4 is independently hydrogen or an aliphatic group having from about 1 to about 6 carbons. 14. The method of claim 10, wherein the 1,2-diacyl-sn-glycero-3-alkylphosphoalkanolamine is 1,2-dipalmitoyl-sn-glycero-3-ethylethanolamine(DPePE), 1,2-dimyristoyl-sn-glycero-3-ethylphosphoethanolamine(DMePE), 1,2-distearoyl-sn-glycero-3-ethylphosphoethanolamine(DSePE), 1,2-dilauroyl-sn-glycero-3-ethylphosphoethanolamine (DLePE), 1,2-dioleoyl-sn-glycero-3-ethylphosphoethanolamine(DOePE) or any combination thereof. 15. The method of claim 1 wherein the particles have a tap density less than about 0.4 g/cm3. 16. The method of claim 15, wherein the particles have a tap density less than about 0.1 g/cm3. 17. The method of claim 1, wherein the particles have a median geometric diameter of from about 5 micrometers and about 30 micrometers. 18. The method of claim 1, wherein the particles have an aerodynamic diameter of from about 1 to about 5 microns. 19. The method of claim 18, wherein the particles have an aerodynamic diameter of from about 1 to about 3 microns. 20. The method of claim 18, wherein the particles have an aerodynamic diameter of from about 3 to about 5 microns. 21. The method of claim 1, wherein delivery to the pulmonary system includes delivery to the deep lung. 22. The method of claim 1, wherein delivery to the pulmonary system includes delivery to the central airways. 23. The method of claim 1, wherein delivery to the pulmonary system includes delivery to the upper airways. 24. The method of claim 1, wherein the particles further comprise a lipid having no overall net charge. 25. The method of claim 1 wherein the particles further comprise a carboxylic acid or salt thereof. 26. The method of claim 25, wherein the carboxylic acid includes at least two carboxyl groups. 27. The method of claim 1, wherein the particles further comprise a multivalent metal salt or ionic components thereof. 28. The method of claim 27, wherein the multivalent salt is a salt of an alkaline earth metal. 29. The method of claim 1, wherein the particles further comprise an amino acid. 30. The method of claim 29, wherein the amino acid is hydrophobic. 31. The method of claim 30, wherein the hydrophobic amino acid is leucine, isoleucine, alanine, valine, phenylalanine or any combination thereof. 32. A method for delivery via the pulmonary system comprising: administering to the respiratory tract of a patient in need of treatment an effective amount of particles comprising: insulin in association with a charged lipid wherein the charged lipid has an overall net positive charge which is opposite to the overall net negative charge of the insulin upon association and wherein release of the insulin is sustained. 33. The method of claim 32, wherein the lipid is a 1,2-diacyl-sn-glycero-3-alkylphosphocholine or a 1,2-diacyl-sn-glycero-3-alkylphosphoalkanolamine. 34. The method of claim 33, wherein the 1,2-diacyl-sn-glycero-3-alkylphosphocholine is 1,2-dipalmitoyl-sn-glycero-3-ethylphosphocholine(DPePC), 1,2-dimyristoyl-sn-glycero-3-ethylphosphocholine(DMePC), 1,2-distearoyl-sn-glycero-3-ethylphosphocholine(DSePC), 1,2-dilauroyl-sn-glycero-3-ethylphosphocholine (DLePC), 1,2-dioleoyl-sn-glycero-3-ethylphosphocholine(DOePC) or any combination thereof. 35. The method of claim 33, wherein the 1,2-diacyl-sn-glycero-3-alkylphosphoalkanolamine is 1,2-dipalmitoyl-sn-glycero-3-ethylethanolamine(DPePE), 1,2-dimyristoyl-sn-glycero-3-ethylphosphoethanolamine(DMePE), 1,2-distearoyl-sn-glycero-3-ethylphosphoethanolamine(DSePE), 1,2-dilauroyl-sn-glycero-3-ethylphosphoethanolamine (DLePE), 1,2-dioleoyl-sn-glycero-3-ethylphosphoethanolamine(DOePE) or any combination thereof. 36. The method of claim 32, wherein association of the agent and charged lipid comprises an ionic complexation. 37. The method of claim 36, wherein association of the lipid and agent further comprises hydrogen bonding. 38. The method of claim 32, wherein the charge ratio of lipid to bioactive agent is from about 0.25:1 to about 1:0.25. 39. The method of claim 38, wherein the charge ratio of lipid to bioactive agent is from about 0.5:1 to about 1:0.5. 40. The method of claim 39, wherein the charge ratio of lipid to bioactive agent is about 1:1. 41. The method of claim 32, wherein the particles further comprise a carboxylic acid. 42. The method of claim 32, wherein the particles further comprise an amino acid. 43. The method of claim 32, wherein the particles further comprise a lipid with no overall net charge. 44. The method of claim 32, wherein the particles further comprise a multivalent metal salt or ionic components thereof. 45. The method of claim 32, wherein delivery to the pulmonary system includes delivery to the deep lung. 46. The method of claim 32, wherein delivery to the pulmonary system includes delivery to the central airways. 47. The method of claim 32, wherein delivery to the pulmonary system includes delivery to the upper airways.
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