Porous particles comprising excipients for deep lung delivery
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/00
A61K-009/12
A61K-009/14
A61K-038/00
A61K-033/00
A61K-031/00
A61K-031/70
A61K-031/7052
A61K-031/7042
출원번호
US-0818902
(2004-04-06)
등록번호
US-7435408
(2008-10-14)
발명자
/ 주소
Edwards,David A.
Caponetti,Giovanni
Hrkach,Jeffrey S.
Lotan,Noah
Hanes,Justin
Langer,Robert S.
Ben Jebria,Abdellaziz
출원인 / 주소
Massachusetts Institute of Technology
The Penn State Research Foundation
대리인 / 주소
Elmore Patent Law Group, PC
인용정보
피인용 횟수 :
4인용 특허 :
42
초록▼
Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. The particles may be formed of bio
Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of a functionalized polyester graft copolymer consisting of a linear a-hydroxy-acid polyester backbone having at least one amino acid group incorporated therein and at least one poly(amino acid) side chain extending from an amino acid group in the polyester backbone. In one embodiment, porous particles having a relatively large mean diameter, for example greater than 5 μm, can be used for enhanced delivery of a therapeutic agent to the alveolar region of the lung. The porous particles incorporating a therapeutic agent may be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of wide variety of therapeutic agents.
대표청구항▼
What is claimed is: 1. Therapeutic particles suitable for aerosolization in a dry powder inhaler (DPI) comprising, a therapeutic agent and a pharmaceutically acceptable carrier, wherein the particles are porous, have a tap density less than about 0.4 g/cm3 and wherein upon aerosolization, about 80%
What is claimed is: 1. Therapeutic particles suitable for aerosolization in a dry powder inhaler (DPI) comprising, a therapeutic agent and a pharmaceutically acceptable carrier, wherein the particles are porous, have a tap density less than about 0.4 g/cm3 and wherein upon aerosolization, about 80% of the particles exit the DPI and at least 55% of the particles exiting the DPI have an aerodynamic diameter of less than about 4.7 μm as measured by a cascade impactor for 30 seconds at 28.3 l/min flow rate. 2. The particles of claim 1, wherein the particles have a tap density less than about 0.1 g/cm3. 3. The particles of claim 1, wherein the particles have a mass mean diameter between 5 μm and 30 μm. 4. The particles of claim 1, wherein the pharmaceutically acceptable carrier comprises a pore forming material. 5. The particles of claim 1, wherein the pharmaceutically acceptable carrier is a surfactant. 6. The particles of claim 1, wherein the agent is selected from the group consisting of proteins, peptides, polysaccharides, lipids, nucleic acids and combinations thereof. 7. The particles of claim 1, wherein the agent is selected from the group consisting of antibodies, antigens, antibiotics, antivirals, hormones, vasoactive agents, neuroactive agents, anticoagulants, immunomodulating agents, cytotoxic agents, ribozymes, antisense agents and genes. 8. The particles of claim 1, for use in local inhalation therapy. 9. The particles of claim 8, wherein the agent is an agent for the treatment of asthma, emphysema, or cystic fibrosis. 10. The particles of claim 1, for use in systemic inhalation therapy. 11. The particles of claim 10, wherein the agent is insulin. 12. A method of enhancing the aerosolization efficiency of therapeutic particles administered to a patient by a dry powder inhaler comprising the steps of: a) providing particles suitable for aerosolization in a dry powder inhaler (DPI) wherein the particles are porous, have a tap density less than about 0.4 g/cm3 and comprise a therapeutic agent and a pharmaceutically acceptable carrier, and wherein upon aerosolization, about 80% of the particles exit the DPI and at least 55% of the particles exiting the DPI have an aerodynamic diameter of less than about 4.7 μm as measured by a cascade impactor for 30 seconds at 28.3 l/min flow rate; and b) aerosolizing the particles by activating the DPI such that the particles exit the DPI and are administered to the patient. 13. The method of claim 12, wherein the particles have a tap density less than about 0.1 g/cm3. 14. The method of claim 12, wherein the particles have a mass mean diameter between 5 μm and 30 μm. 15. The method of claim 12, wherein the pharmaceutically acceptable carrier comprises a pore forming material. 16. The method of claim 12, wherein the pharmaceutically acceptable carrier is a surfactant. 17. The method of claim 12, wherein the agent is selected from the group consisting of proteins, peptides, polysaccharides, lipids, nucleic acids and combinations thereof. 18. The method of claim 12, wherein the agent is selected from the group consisting of antibodies, antigens, antibiotics, antivirals, hormones, vasoactive agents, neuroactive agents, anticoagulants, immunomodulating agents, cytotoxic agents, ribozymes, antisense agents and genes. 19. The method of claim 12, for use in local inhalation therapy. 20. The method of claim 19, wherein the agent is an agent for the treatment of asthma, emphysema, or cystic fibrosis. 21. The method of claim 12, for use in systemic inhalation therapy. 22. The method of claim 21, wherein the agent is insulin.
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이 특허에 인용된 특허 (42)
Edwards David A. ; Caponetti Giovanni,ITX ; Hrkach Jeffrey S. ; Lotan Noah,ILX ; Hanes Justin ; Ben-Jebria Abdell Aziz ; Langer Robert S., Aerodynamically light particles for pulmonary drug delivery.
Platz Robert M. ; Patton John S. ; Foster Linda C. ; Eljamal Mohammed,LBX, Dispersible antibody compositions and methods for their preparation and use.
Illum Lisbeth (Nottingham GBX), Enhanced uptake drug delivery system having microspheres containing an active drug and a bioavailability improving mater.
Wise Donald L. (Belmont MA) Trantolo Debra J. (Princeton MA) Gresser Joseph D. (Brookline MA), Method for making a bioerodible material for the sustained release of a medicament and the material made from the method.
Boyes Robert N. (St. Albans AL GB2) Tice Thomas R. (Birmingham AL) Gilley Richard M. (Birmingham AL) Pledger Kenneth L. (Huntsville AL), Pharmaceutical formulations comprising microcapsules.
DeLuca Patrick P. (Lexington KY) Kanke Motoko (Fukuyama JPX) Sato Toyomi (Tokyo CA JPX) Schroeder Hans G. (Encinitas CA), Porous microspheres for drug delivery and methods for making same.
David A. Edwards ; Giovanni Caponetti ; Jeffrey S. Hrkach ; Noah Lotan IL; Justin Hanes ; Robert S. Langer ; Abdellaziz Ben-Jebria, Porous particles comprising excipients for deep lung delivery.
Edwards David A. ; Caponetti Giovanni ; Hrkach Jeffrey S. ; Lotan Noah,ILX ; Hanes Justin ; Langer Robert S. ; Ben-Jebria Abdellaziz, Porous particles for deep lung delivery.
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Phadke Deepak S. (Indianapolis IN) Neddermeyer Melissa P. (Indianapolis IN), Superior tasting pharmaceutical composition having porous particles and the process of preparing such pharmaceutical com.
Liversidge Gary G. (West Chester PA) Cundy Kenneth C. (Pottstown PA) Bishop John F. (Rochester NY) Czekai David A. (Honeoye Falls NY), Surface modified drug nanoparticles.
Leong Helen (Atherton CA) Katz Martin (Menlo Park CA) Delk Ann (Kensington CA) Nacht Sergio (Los Altos CA) Berliner David (Atherton CA), Synthetic melanin aggregates.
Andersson Jan (Sodra Sandby SEX) Jagfeldt Hans (Lund SEX) Trofast Eva (Lund SEX) Wetterlin Kjell (Sodra Sandby SEX), System for dispensing pharmaceutically active compounds.
Backstrom Kjell Goran Erik,SEX ; Dahlback Carl Magnus Olof,SEX ; Edman Peter,SEX ; Johansson Ann Charlotte Birgit,SEX, Systemic administration of a therapeutic preparation.
Bckstrm Kjell G. E. (Lund SEX) Dahlbck Carl M. O. (Lund SEX) Edman Peter (Bjrred SEX) Johansson Ann C. B. (Lund SEX), Systemic administration of a therapeutic preparation.
Bckstrm Kjell G. E. (Lund SEX) Dahlbck Carl M. O. (Lund SEX) Edman Peter (Bjrred SEX) Johansson Ann C. B. (Lund SEX), Therapeutic preparation for inhalation.
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