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Kafe 바로가기국가/구분 | United States(US) Patent 등록 |
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국제특허분류(IPC7판) |
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출원번호 | US-0127158 (2012-06-18) |
등록번호 | US-9364436 (2016-06-14) |
국제출원번호 | PCT/US2012/042998 (2012-06-18) |
§371/§102 date | 20131231 (20131231) |
국제공개번호 | WO2012/174556 (2012-12-20) |
발명자 / 주소 |
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출원인 / 주소 |
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대리인 / 주소 |
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인용정보 | 피인용 횟수 : 1 인용 특허 : 867 |
Disclosed herein are diketopiperazine microparticles having high capacity for adsorbing a drug or active agent. In particular, the diketopiperazine microparticle are formed using fumaryl diketopiperazine and can comprise a drug in large doses for the treatment of disease or disorders by pulmonary de
Disclosed herein are diketopiperazine microparticles having high capacity for adsorbing a drug or active agent. In particular, the diketopiperazine microparticle are formed using fumaryl diketopiperazine and can comprise a drug in large doses for the treatment of disease or disorders by pulmonary delivery via oral inhalation.
1. A composition comprising a plurality of diketopiperazine microparticles and a drug or an active agent; wherein each of the diketopiperazine microparticles comprises a plurality of structural domains, each structural domain comprising a nucleus surrounded by layers of a porous crystalline material
1. A composition comprising a plurality of diketopiperazine microparticles and a drug or an active agent; wherein each of the diketopiperazine microparticles comprises a plurality of structural domains, each structural domain comprising a nucleus surrounded by layers of a porous crystalline material, and said diketopiperazine microparticles have a mass-weighted average particle size of about 33,000 to about 216,000 voxels measured by X-ray tomography for particle size measuring about 0.5 μm to about 4 μm in geometric diameter. 2. The composition of claim 1, wherein the diketopiperazine microparticles comprise structural domains ranging in number-weighted size from about 250 voxels to about 1,400 voxels. 3. The composition of claim 1, wherein the diketopiperazine microparticles comprise structural domains ranging in voxel-weighted size from about 500 voxels to about 2,000 voxels. 4. The composition of claim 1, wherein each of the diketopiperazine microparticles have a specific surface area greater than 35 m2/g. 5. The composition of claim 1, wherein each of the diketopiperazine microparticles have a specific surface area greater than 70 m2/g. 6. The composition of claim 1, wherein the plurality of structural domains have an average size from about 300 nm to about 450 nm as measured by radius of gyration. 7. The composition of claim 1, wherein said drug or active agent is a small organic molecule, peptide or protein, or a nucleic acid molecule or combinations thereof. 8. The composition of claim 7, wherein said peptide is an endocrine hormone. 9. The composition of claim 7, wherein said peptide or protein is insulin, parathyroid hormone, calcitonin, glucagon, glucagon-like peptide 1, oxyntomodulin, oxytocin, CCK-8, PYY3-36, ghrelin, vasoactive intestinal peptide, leuprolide, growth hormone, RGD (Arg-Gly-Asp) peptide, growth hormone releasing peptide, DDAVP (desamino-Cys-1, D-arg8) vasopressin peptide, cyclosporine, detirelex, somatostatin, interferon-a, granulocyte colony stimulating factor, IgG, or an analog or active fragment thereof. 10. The composition of claim 7, wherein the small organic molecule is a neurotransmitter agonist, a neurotransmitter antagonist, a pain inhibitory agent, a vaccine, an anti-inflammatory agent, an anti-cancer agent, a cell receptor agonist molecule, a cell receptor antagonist molecule, an immunosuppressant, a statin, or an anti-infective agent. 11. The composition of claim 1, wherein said diketopiperazine is fumaryl diketopiperazine (3,6-bis(N-fumaryl-4-aminobutyl)-2,5-diketopiperazine; or salt thereof. 12. The composition of claim 1 in the form of a dry powder. 13. The composition of claim 12, further comprising insulin in an amount greater than 4 units per milligram of the dry powder. 14. The composition of claim 13, wherein the amount of insulin is 6 units per milligram of dry powder. 15. The composition of claim 14, wherein the dry powder comprises an insulin dose comprising 60 units or more of insulin for delivering to a patient in a single inhalation using a dry powder inhaler. 16. A method of synthesizing fumaryl diketopiperazine microparticles, the method comprising: feeding equal masses of a first solution comprising about 11 wt % to about 12 wt % acetic acid and a second solution comprising about 2.75 wt % fumaryl diketopiperazine solutions and containing a surfactant at a concentration of 0.05 wt % at a temperature of about 17° C. to about 22° C. through a high shear mixer, andcollecting the fumaryl diketopiperazine microparticles. 17. The method according to claim 16, wherein said surfactant is polysorbate 80. 18. The method according to claim 17, further comprising the step of washing the suspension with deionized water to remove excess acid. 19. The method according to claim 17, further comprising the step of adding a solution comprising an active agent to said suspension and adjusting the pH of the solution to pH 4.5 with an aqueous ammonia solution. 20. A method of delivering insulin to a patient in need thereof comprising administering to a subject the composition dry powder composition of claim 1 to the deep lung by inhalation of said dry powder formulation by said patient. 21. A diketopiperazine microparticle comprising a plurality of structural domains, each structural domain comprising a nucleus surrounded by layers of a porous crystalline material, and having a mass-weighted average particle size of about 33,000 to about 216,000 voxels measured by X-ray tomography for a particle size measuring about 0.5 μm to about 4 μm in geometric size.
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