초록 ▼

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.

대표청구항 ▼

1. A dry powder therapeutic composition comprising: a biologically active agent; anda pharmaceutically acceptable anion of a heterocyclic compound according to Formula 1: wherein R1 or R2 are independently selected from succinate-4-aminobutyl, glutarate-4-aminobutyl, maleate-4-aminobutyl, citraconat

1. A dry powder therapeutic composition comprising: a biologically active agent; anda pharmaceutically acceptable anion of a heterocyclic compound 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 NH; andwherein the salt further comprises at least one cation. 2. The dry powder of claim 1, wherein the at least one carboxylate functional group is a terminal carboxylate functional group. 3. The dry powder of claim 1, wherein the powder is formed by the removal of a solvent from a solution containing the biologically active agent, the pharmaceutically acceptable anion of the heterocyclic compound, and the at least one cation. 4. The dry powder of claim 3, wherein removal of the solvent is achieved by spray drying. 5. The dry powder of claim 3, wherein removal of the solvent is achieved by distillation. 6. The dry powder of claim 3, wherein removal of the solvent is achieved by evaporation. 7. The dry powder of claim 3, wherein removal of the solvent is achieved by lyophilization. 8. The dry powder of claim 1, wherein the at least one cation is selected from the group consisting of sodium, potassium, calcium, magnesium, lithium, triethylamine, butylamine, diethanolamine, and triethanolamine. 9. The dry powder of claim 1, wherein the at least one cation is sodium. 10. The dry powder of claim 1, wherein the 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. 11. The dry powder of claim 1, wherein the dry powder is prepared by a method that includes micronizing a solid to form the dry powder. 12. The dry powder of claim 11, wherein the particles of the dry powder are suitable for pulmonary delivery. 13. The dry powder of claim 11, wherein the particles of the dry powder have a rugosity of less than 2. 14. The dry powder of claim 1, wherein the dry powder comprises microparticles. 15. The dry powder of claim 14, wherein at least 50% of the microparticles have a diameter less than 5 μm. 16. The dry powder of claim 14, wherein at least 70% of the microparticles have a diameter less than 5 μm. 17. The dry powder of claim 14, wherein the microparticles have a rugosity of less than 2. 18. The dry powder of claim 14, wherein the microparticles are suitable for pulmonary delivery. 19. The dry powder of claim 1, wherein the dry powder is formulated into a solid dosage form.