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Kafe 바로가기국가/구분 | United States(US) Patent 등록 |
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국제특허분류(IPC7판) |
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출원번호 | US-0971785 (2015-12-16) |
등록번호 | US-10130581 (2018-11-20) |
발명자 / 주소 |
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출원인 / 주소 |
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대리인 / 주소 |
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인용정보 | 피인용 횟수 : 0 인용 특허 : 887 |
Methods are provided for drying a particle. Specifically, there is provided a spray-dried diketopiperazine-insulin particle formulation having improved aerodynamic performance and in which the active agent is more stabile and efficiently delivered as compared to that of the lyophilized diketopiperaz
Methods are provided for drying a particle. Specifically, there is provided a spray-dried diketopiperazine-insulin particle formulation having improved aerodynamic performance and in which the active agent is more stabile and efficiently delivered as compared to that of the lyophilized diketopiperazine-insulin formulation. The dry powders have utility as pharmaceutical formulations for pulmonary delivery.
1. A method for forming a dry powder medicament with an improved pharmaceutic property, comprising a) a step for forming microparticles comprising a diketopiperazine with acidic or basic side chains, resulting in a suspension of microparticles of the diketopiperazine with acidic or basic side chains
1. A method for forming a dry powder medicament with an improved pharmaceutic property, comprising a) a step for forming microparticles comprising a diketopiperazine with acidic or basic side chains, resulting in a suspension of microparticles of the diketopiperazine with acidic or basic side chains in an appropriate solvent, and optionally a step for loading said microparticles with an active agent, then b) removing solvent by spray drying to obtain a dry powder, wherein the dry powder has an improved pharmaceutic property as compared to a dry powder obtained by removing solvent by lyophilization, and wherein the improved pharmaceutic property is increased density of the powder, and wherein said dry powder has a bulk density from 0.15 to 0.20 g/cc. 2. The method of claim 1, wherein said diketopiperazine is a diketopiperazine having the formula 3,6-di(4-X-aminobutyl)-2,5-diketopiperazine, wherein X is succinyl, glutaryl, maleyl, or fumaryl. 3. The method of claim 2, wherein X is fumaryl diketopiperazine. 4. The method of claim 1, wherein the method comprises a step for loading the microparticle with an active agent prior to the solvent removal step. 5. The method of claim 4, wherein said loading step comprises: providing a solution or a suspension of the active agent; and adding said solution or suspension of active agent to the suspension of microparticles of the diketopiperazine with acidic or basic side chains. 6. The method of claim 4, wherein the active agent is insulin, calcitonin, parathyroid hormone 1-34, bioactive fragment of parathyroid hormone, octreotide, leuprolide, RSV peptide, felbamate, cannabinoid antagonists and/or agonists, muscurinic antagon and/or agonists, heparin, low molecular weight heparin, cromolyn, sildenafil, vardenafil, tadalafil, growth hormone, AZT, DDI, GCSF, lamotrigine, chorionic gonadotropin releasing factor, luteinizing release hormone, .beta.-galactosidase, GLP-1, exendins 1-4, or ghrelin. 7. The method of claim 4, wherein the active agent is a peptide or protein. 8. The method of claim 6, wherein the active agent is insulin or an analogue thereof. 9. The method of claim 8, wherein the active agent is human insulin. 10. The method of claim 9, wherein the insulin content of the microparticle is about 3% to about 50% by weight of the dry powder formulation. 11. The method of claim 10, wherein the insulin content of the microparticle is about 7% to about 25% by weight of the dry powder formulation. 12. The method of claim 11, wherein the insulin content of the microparticle is about 11% by weight of the dry powder formulation. 13. A method for delivering an active agent to a patient in need thereof, comprising administering by inhalation to the patient an effective amount of the dry powder made by the method of claim 4. 14. The method of claim 1, wherein the step for forming microparticles comprises adjusting the pH of a solution comprising a diketopiperazine with acidic or basic side chains.
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