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Kafe 바로가기국가/구분 | United States(US) Patent 등록 |
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국제특허분류(IPC7판) |
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출원번호 | US-0991777 (2016-01-08) |
등록번호 | US-9675674 (2017-06-13) |
발명자 / 주소 |
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출원인 / 주소 |
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대리인 / 주소 |
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인용정보 | 피인용 횟수 : 0 인용 특허 : 874 |
Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provide
Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.
1. A method of preparing a solid composition for drug delivery comprising: preparing a solution containing a biologically active agent and a pharmaceutically-acceptable salt of a heterocyclic compound in a solvent;and a step for removing said solvent;wherein said pharmaceutically acceptable salt of
1. A method of preparing a solid composition for drug delivery comprising: preparing a solution containing a biologically active agent and a pharmaceutically-acceptable salt of a heterocyclic compound in a solvent;and a step for removing said solvent;wherein said pharmaceutically acceptable salt of a heterocyclic compound has the structure according to Formula 1: wherein R1 or R2 are independently selected from succinate-4-aminobutyl, glutarate-4-aminobutyl, maleate-4-aminobutyl, citraconate-4-aminobutyl, malonate-4-aminobutyl, oxalate-4-aminobutyl, and fumarate-4-aminobutyl;E1 and E2 are NH2; andsaid salt further comprises at least one cation. 2. The method of claim 1, wherein said step for removing said solvent comprises distillation. 3. The method of claim 1, wherein said step for removing said solvent comprises evaporation. 4. The method of claim 1, wherein said step for removing said solvent comprises spray drying. 5. The method of claim 1, wherein said step for removing said solvent comprises lyophilization. 6. The method of claim 1, wherein said at least one cation is selected from the group consisting of sodium, potassium, calcium, magnesium, lithium, triethylamine, butylamine, diethanolamine, and triethanolamine. 7. The method of claim 1, wherein said at least one cation is sodium. 8. The method of claim 1, wherein said biologically active agent is selected from the group consisting of hormones, anticoagulants, immunomodulating agents, cytotoxic agents, antibiotics, antivirals, antisense, anti-inflammatories, vasoactive agents, neuroactive agents, cannabinoids, antigens, antibodies and active fragments and analogues thereof. 9. The method of claim 1 further comprising the step of micronizing said solid to form a dry powder. 10. The method of claim 9, wherein the particles of said dry powder are suitable for pulmonary delivery. 11. The method of claim 9, wherein the particles of said dry powder have a rugosity of less than 2. 12. The method of claim 1, wherein said solid composition comprises microparticles. 13. The method of claim 12, wherein at least 50% of said particles have a diameter less than 5 μm. 14. The method of claim 12, wherein at least 70% of said particles have a diameter less than 5 μm. 15. diameter The method of claim 12, wherein said microparticles have a rugosity of less than 2. 16. The method of claim 12, wherein said microparticles comprise a dry powder. 17. The method of claim 12, wherein said microparticles are suitable for pulmonary delivery. 18. The method of claim 1, wherein said solid composition is a precipitate. 19. The method of claim 1, wherein said solid composition is formulated into a solid dosage form. 20. The method of claim 19, wherein said solid dosage form is selected from the group consisting of tablets and capsules.
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