Patent EA-002562-B1 (EA)
Title: Perforated microparticles and methods of use
Inventor: TARARA THOMAS E
IPC: A61K9/22
Filed: 1998-09-29
Abstract: 1. A powder composition, comprising a plurality of perforated microstructures containing an active agent and at least 20% by weight of a surfactant, and having the geometrical diameter from 1 to 30 (m, the aerodynamic diameter of less than about 5 (m and a bulk density of less than 0,5 g/cm<3>. 2. The composition according to claim 1 further comprising calcium. 3. The composition according to claim 1 wherein the mean porosity of microstructures is 0,5-80%. 4. The composition according to claim 3 wherein the porosity of microstructures is 2-40%. 5. The composition according to claim 4 wherein the mean pore size is 20-200 (m. 6. The composition according to claim 1 wherein the microstructures comprise not more than 20% of the composition. 7. The composition according to claim 6 wherein the microstructures comprise 30-70% of the composition. 8. The composition according to claim 1 wherein the bulk density of the microstructures is less than 0,1 g/cm<3>. 9. The composition according to claim 1 wherein said collected perforated microstructures comprise hollow porous microspheres. 10. The composition according to claim 9 wherein a thickness of the microstructures casing is 0,1-0,5 (m. 11. The composition according to claim 1 wherein the aerodynamic diameter of the microstructures is from 0,5 to 5 (m. 12. The composition according to claim 1 wherein the geometric diameter of the microstructures is less than 5 (m. 13. The composition according to 1 wherein said surfactant is selected from the group consisting of phospholipids, nonionic detergents, nonionic block copolymers, ionic surfactants, biocompatible fluorinated surfactants and combinations thereof. 14. The composition according to claim 13 wherein said phospholipid is selected from the group consisting of dilauroylphosphatidylcholine, dioleylphosphatidylcholine, dipalmitoylphosphatidylcholine, disteroylphosphatidylcholine, dibehenoylphosphatidylcholine, diarachidoylphosphatidylcholine and combinations thereof. 15. The composition according to claim 14 wherein said phospholipid is a gel transforming into a liquid state at a temperature exceeding 40 degree C. 16. The composition according to claim 1 wherein said active agent is a bioactive agent selected from the group consisting of antiallergics, bronchodilators, pulmonary lung surfactants, analgesics, antibiotics, leukotriene inhibitors or antagonists, antihistamines, antiinflammatories, antineoplastics, anticholinergics, anesthetics, anti-tuberculars, imaging agents, cardiovascular agents, enzymes, steroids, genetic material, viral vectors, antisense agents, proteins, peptides and combinations thereof. 17. The composition according to claim 16 wherein said bioactive agent is selected from the group comprising fentanyl, morphine, light surfactant, LHRH, leuprolyde, interferon, goseremine and growth hormones. 18. A powder composition, comprising a plurality of perforated microstructures, having the geometrical diameter from 1 to 30 (m, the aerodynamic diameter of less than about 5 (m and a bulk density of less than 0,5 g/cm<3>, comprising calcium and at least 20% by weight of a phospholipid. 19. A powder composition, comprising a plurality of perforated microstructures, having porosity 0,5-80%, the geometrical diameter from 1 to 30 (m, the aerodynamic diameter of less than about 5 (m and a bulk density of less than 0,5 g/cm<3>. 20. The composition according to claim 19 wherein comprises an active agent. 21. The composition according to claim 20 wherein the porosity is 20-40%. 22. The composition according to claim 21 wherein the pores are 20-200 nm. 23. The composition according to claim 22 wherein the bulk density is less than 0,1 g/cm<3>. 24. The composition according to claim 21 wherein the microstructures are hollow porous microspheres. 25. A powder composition, comprising a plurality of perforated microstructures, having shear index not less than 0,98, the geometrical diameter from 1 to 30 (m, the aerodynamic diameter of less than about 5 (m and a bulk density of less than 0,5 g/cm<3>. 26. The composition according to claim 25 wherein the microstructures comprise an active agent and at least 20% by weight of a phospholipid selected from the group consisting of dilauroylphosphatidylcholine, dioleylphosphatidylcholine, dipalmitoylphosphatidylcholine, disteroylphosphatidylcholine, dibehenoylphosphatidylcholine, diarachidoylphosphatidylcholine and combinations thereof. 27. The composition according to claim 26 wherein said phospholipid is a gel transforming into a liquid state at a temperature exceeding 40 degree C.