The present invention relates to active substances in particulate form, to methods for preparing them and to their uses. The present invention provides particulate powders, such as might be of use for delivery using a dry powder inhaler (DPI) or similar delivery device, having properties which may b
The present invention relates to active substances in particulate form, to methods for preparing them and to their uses. The present invention provides particulate powders, such as might be of use for delivery using a dry powder inhaler (DPI) or similar delivery device, having properties which may be beneficial to the DPI delivery process.
대표청구항▼
1. An active substance in particulate form suitable for administration via a dry powder inhaler, the particulates comprising: a volume mean aerodynamic diameter of less than 7 microns;a bulk powder density within a range from about 0.1 g/cm3 to about 0.5 g/cm3; anda surface-to-volume ratio of at lea
1. An active substance in particulate form suitable for administration via a dry powder inhaler, the particulates comprising: a volume mean aerodynamic diameter of less than 7 microns;a bulk powder density within a range from about 0.1 g/cm3 to about 0.5 g/cm3; anda surface-to-volume ratio of at least 2.5 times that of spherical particles of a corresponding volume diameter, wherein the particulates are solid, non-hollow, non-porous particles and the active substance is selected from the group consisting of insulin, pro-insulin, mono-acylated insulin, insulinotropin, and insulin-like growth factor. 2. The active substance of claim 1, further comprising a shape factor of at least 2. 3. The active substance of claim 1, further comprising a shape coefficient of greater than 10. 4. The active substance of claim 1, further comprising an aerodynamic shape factor of at least 1.4. 5. The active substance of claim 1, further comprising a specific surface area of at least 10 m2/g. 6. The active substance of claim 5, wherein the specific surface area is at least 15 m2/g. 7. The active substance of claim 6, wherein the specific surface area is at least 20 m2/g. 8. The active substance of claim 7, wherein the specific surface area is at least 25 m2/g. 9. The active substance of claim 1, further comprising a volume mean diameter of less than 6 microns. 10. The active substance of claim 1, further comprising a specific surface energy of less than 100 mJ/m2. 11. The active substance of claim 10, wherein the specific surface energy is less than 70 mJ/m2. 12. The active substance of claim 1, wherein the active substance is insulin. 13. The active substance of claim 1, wherein the active substance is pro-insulin. 14. The active substance of claim 1, wherein the active substance is mono-acylated insulin. 15. The active substance of claim 1, wherein the active substance is insulinotropin. 16. The active substance of claim 1, wherein the active substance is insulin-like growth factor. 17. The active substance of claim 1, further comprising a RMS roughness, measured using AFM, of 0.5 nm or less. 18. The active substance of claim 1, further comprising a particle size distribution (X90) within a range from about 0.5 μm to about 10 μm. 19. The active substance of claim 1, further comprising an amorphous phase content of less than 1% w/w. 20. The active substance of claim 1, wherein the bulk powder density is about 0.2 g/cm3 or less. 21. The active substance of claim 1, further comprising a shape factor of at least 3.5. 22. The active substance of claim 1, further comprising a RMS roughness, measured using atomic force microscopy, of about 0.2 nm or less. 23. The active substance of claim 1, which when delivered using a passive dry powder inhaler yields a fine particle fraction in an emitted dose of about 20% or greater. 24. The active substance of claim 23, wherein the fine particle fraction is about 31% or greater. 25. The active substance of claim 24, wherein the fine particle fraction is about 55% or greater. 26. An active substance in particulate form suitable for administration via a dry powder inhaler, the particulates comprising: a volume mean aerodynamic diameter of less than 7 microns;a bulk powder density within a range from about 0.1 g/cm3 to about 0.5 g/cm3; anda surface-to-volume ratio of at least 2.5 times that of spherical particles of a corresponding volume diameter, wherein the particulates are solid, non-hollow, non-porous particles and the active substance is selected from the group consisting of amphotericin-B, parathyroid hormone, glucagon-like peptide, and an anti-infective agent. 27. The active substance of claim 26, wherein the active substance is the amphotericin-B. 28. The active substance of claim 26, wherein the active substance is the parathyroid hormone. 29. The active substance of claim 26, wherein the active substance is the glucagon-like peptide. 30. The active substance of claim 26, wherein the active substance is the anti-infective agent. 31. The active substance of claim 30, wherein the anti-infective agent comprises an aminoglycoside. 32. The active substance of claim 30, wherein the anti-infective agent comprises tobramycin. 33. The active substance of claim 30, wherein the anti-infective agent comprises a fluoroquinolone. 34. The active substance of claim 30, wherein the anti-infective agent comprises ciprofloxacin. 35. The active substance of claim 26, further comprising a specific surface area of at least 10 m2/g. 36. The active substance of claim 35, wherein the specific surface area is at least 20 m2/g. 37. The active substance of claim 36, wherein the specific surface area is at least 25 m2/g. 38. An active substance in particulate form suitable for administration via a dry powder inhaler, the particulates comprising: a volume mean aerodynamic diameter of less than 7 microns;a bulk powder density within a range from about 0.1 g/cm3 to about 0.5 g/cm3; anda surface-to-volume ratio of at least 2.5 times that of spherical particles of a corresponding volume diameter, wherein the particulates are solid, non-hollow, non-porous particles and the active substance is selected from the group consisting of salbutamol, terbutalene, salmeterol, fenoterol, and bromocriptine. 39. The active substance of claim 38, wherein the active substance is salbutamol. 40. The active substance of claim 38, wherein the active substance is bromocriptine. 41. The active substance of claim 38, wherein the active substance is terbutalene, salmeterol, or fenoterol. 42. The active substance of claim 38, further comprising a specific surface area of at least 10 m2/g. 43. The active substance of claim 42, wherein the specific surface area is at least 20 m2/g. 44. The active substance of claim 43, wherein the specific surface area is at least 25 m2/g.
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Lee Ping I. (Berwyn PA), Active agent containing hydrogel devices wherein the active agent concentration profile contains a sigmoidal concentrati.
Edwards David A. ; Caponetti Giovanni,ITX ; Hrkach Jeffrey S. ; Lotan Noah,ILX ; Hanes Justin ; Ben-Jebria Abdell Aziz ; Langer Robert S., Aerodynamically light particles for pulmonary drug delivery.
Evans Richard M. (Westwood MA) Farr Stephen J. (Llandaf GB7), Aerosol formulations including proteins and peptides solubilized in reverse micelles and process for making the aerosol.
Ehrenberg Scott G. (Fishkill NY) Paul Alan (Kingston NY) Wohlford Elizabeth J. (Kingston NY), Apparatus and method for applying a stream of atomized fluid.
Wang Yu-chang J. (Los Altos CA) Lee William A. (Los Altos CA) Narog Blair (Palo Alto CA), Composition and method for administration of pharmaceutically active substances.
Van Bommel Elvira M. G. (Weesp NLX) Fokkens Jasper G. (Weesp NLX), Compositions with controlled zero-order delivery rate and method of preparing these compositions.
Andersson Jan A. R. (S. Sandby SEX) Nilsson Nils G. (Lund SEX) Fagerstrm Per-Olof S. (Bjrred SEX) Wendel Thomas M. (Genarp SEX), Device in connection with an inhaler.
Newell Robert E. (Pinner GB2) Rand Paul K. (Nitchin GB2) Fitzsimmons Robert A. (Barnard Castle GB2), Devices for administering medicaments to patients.
Prestrelski Steven J. (1971 W. Middlefield Rd. ; Unit #5 Mountain View CA 94043) Zhang Mei Z. (444 Via Colinas Thousand Oaks CA 91362), Formulation of a reconstituted protein, and method and kit for the production thereof.
Chien Yie W. (North Brunswick NJ) Kong-Jiann Li John (Plainsboro NJ) Liu Jue-Chen (East Brunswick NJ) Shi Wei-Min (Piscataway NJ) Siddiqui Ovais (Piscataway NJ) Sun Ying (King of Prussia PA), Iontotherapeutic device and process and iontotherapeutic unit dose.
Zoltan Bart J. (Old Tappan NJ) Laube Beth L. (Baltimore MD) Adams ; III George K. (Baltimore MD) Bow Clark F. (Newton NJ) Devito Ralph J. (Stanhope NJ) Harrington Walter (Flanders NJ) Hoffman Louis S, Medication delivery system phase two.
Borchert Ralph,DEX ; Willert-Porada Monika,DEX, Metal-ceramic gradient material, product made from a metal-ceramic gradient material and process for producing a metal-ceramic gradient material.
Fischer Wilfried (Burscheid DEX) Mller Bernd W. (Flintbek DEX), Method and apparatus for the manufacture of a product having a substance embedded in a carrier.
Nielsen Kenneth Andrew ; Argyropoulos John Nicholas ; Wagner Burkhard Eric, Method for producing coating powders catalysts and drier water-borne coatings by spraying compositions with compressed f.
Rouanet Stephane Fabrice ; McGovern William Edward ; Cao Wanging ; Moses John M. ; Carrillo Angel L. ; Klotz Irving M., Method of forming particles using a supercritical fluid, aerogel particles formed thereby, and antiperspirants contain.
Bruno Joseph A. (Blue Bell PA) Doty Brian D. (Phoenixville PA) Gustow Evan (Ardmore PA) Illig Kathleen J. (Phoenixville PA) Rajagopalan Nats (Phoenixville PA) Sarpotdar Pramod (Malvern PA), Method of grinding pharmaceutical substances.
Gorissen Elke (Offenburg DEX) Biskup Heike (Langenfeld DEX) Schneider Hannelore (Dusseldorf DEX), Method of producing microscopic particles made of hydrolytically decomposable polymers and containing active substances.
Subramaniam Bala ; Saim Said ; Rajewski Roger A. ; Stella Valentino, Methods for particle micronization and nanonization by recrystallization from organic solutions sprayed into a compresse.
Boyes Robert N. (St. Albans AL GB2) Tice Thomas R. (Birmingham AL) Gilley Richard M. (Birmingham AL) Pledger Kenneth L. (Huntsville AL), Pharmaceutical formulations comprising microcapsules.
Kodas Toivo T. ; Hampden-Smith Mark J. ; Caruso James ; Powell Quint H. ; Skamser Daniel J., Powder batch of pharmaceutically-active particles and methods for making same.
Sutton Andrew D. (Ruddington GB2) Johnson Richard A. (West Bridgford GB2) Senior Peter J. (Near Melbourne GB2) Heath David (The Park GB2), Preparation of diagnostic agents.
Osborne Nicholas,GBX ; Sutton Andrew Derek,GBX ; Johnson Richard Alan,GBX, Preparation of hollow microcapsules by spray-drying an aqueous solution of a wall-forming material and a water-miscible.
Nouri, Noureddine; Zuccarelli, Jean-Marc; Chauveau, Charles; Bruna, Etienne, Process for manufacturing coated granules with masked taste and immediate release of the active principle.
Bosch H. William (Bryn Mawr PA) Marcera Donna M. (Collegeville PA) Mueller Ronald L. (Downingtown PA) Swanson Jon R. (Macungie PA) Mishra Dinesh S. (Harleysville PA), Process for preparing therapeutic compositions containing nanoparticles.
Kilbride ; Jr. Terence K. (Bloomfield Hills MI) Lisa Rudolph E. (Grosse Ile MI), Process for spray drying riboflavin to produce a granulate product having low binder content.
Lindner Christian (Cologne DEX) Roth Edwin (Bergisch-Gladbach DEX) Koch Otto (Cologne DEX) Braese Hans-Eberhard (Cologne DEX) Bamelis Pol (Overath DEX), Process for the preparation of polymer powders by spray drying.
Glatt Werner (Binzen DEX) Grab Erwin (Rummingen DEX), Process of coating of particles, particularly particles of medicinal drugs, and apparatus for implementation of the proc.
Backstrom Kjell Goran Erik,SEX ; Dahlback Carl Magnus Olof,SEX ; Edman Peter,SEX ; Johansson Ann Charlotte Birgit,SEX, Processes for preparing compositions for inhalation.
Oliver Raymond (Cleveland GBX) Fairclough Anthony R. N. (Cleveland GBX) Antonini Alejandro M. (Lancashire GBX) Munro Robert J. (Cleveland GBX) Lipscombe Lynn W. (Hampshire GBX), Production of particulate materials.
Levendis Yiannis A. (Boston MA) Panagiotou Thomai (Brookline MA) Flagan Richard (La Crescenta CA), Production of polymer particles in powder form using an atomization technique.
Takada Shigeyuki (Salt Lake City UT) Uda Yoshiaki (Takarazuka JPX) Ogawa Yasuaki (Kyoto JPX), Prolonged release microparticle preparation and production of the same.
Takada Shigeyuki (Salt Lake City UT) Uda Yoshiaki (Takarazuka JPX) Ogawa Yasuaki (Ohyamazaki-cho JPX), Prolonged release microparticle preparation and production of the same.
Desai Neil P. ; Tao Chunlin ; Yang Andrew ; Louie Leslie ; Zheng Tianli ; Yao Zhiwen ; Soon-Shiong Patrick ; Magdassi Shlomo,ILX, Protein stabilized pharmacologically active agents, methods for the preparation thereof and methods for the use thereof.
Sarin Virender K. (Libertyville IL) Fox Jack L. (Lake Bluff IL) Gupta Shanker L. (Vernon Hills IL) Absolom Darryl R. (Columbus OH), Pulmonary surfactant protein fragments.
Knight Jack V. (Houston TX) Wilson ; Jr. Samuel Z. (Houston TX), Small particle aerosol generator for treatment of respiratory disease including the lungs.
Knight Jack V. (Houston TX) Gilbert Brian E. (Houston TX) Wilson Samuel Z. (Houston TX) Six Howard R. (East Stroudsborg PA) Wyde Philip R. (Houston TX), Small particle aerosol liposome and liposome-drug combinations for medical use.
Dower Steven K. (Redmond WA) March Carl J. (Bainbridge Island WA) Sims John E. (Seattle WA) Urdal David L. (Seattle WA), Soluble human interleukin-1 receptors, compositions and method of use.
Sutton Andrew D.,GBX ; Johnson Richard A.,GBX ; Senior Peter J.,GBX ; Heath David,GBX, Spray-dried microparticles and their use as therapeutic vehicles.
Schmidt Douglass N. (Grosse Ile MI) Finnan Jeffrey L. (Southgate MI) Lisa Rudolph E. (Grosse Ile MI), Spray-dried vitamin powders using hydrophobic silica.
Lee Chinsoo (Charleston WV) Hoy Kenneth L. (St. Albans WV) Donohue Marc D. (Ellicot City MD), Supercritical fluids as diluents in liquid spray application of coatings.
Kogan Patricia W. (Union NJ) Rudnic Edward M. (Boca Raton FL) Sequeira Joel A. (New York NY) Chaudry Imtiaz A. (Denville NJ), Sustained release oral suspensions.
Bckstrm Kjell G. E. (Lund SEX) Dahlbck Carl M. O. (Lund SEX) Edman Peter (Bjrred SEX) Johansson Ann C. B. (Lund SEX), Systemic administration of a therapeutic preparation.
Alkire Todd G. (Crystal MN) Sanftleben Ronald A. (Maple Grove MN) Schuehle Steven S. (Maple Grove MN), Taste masking microparticles for oral dosage forms.
Bckstrm Kjell G. E. (Lund SEX) Dahlbck Carl M. O. (Lund SEX) Edman Peter (Bjrred SEX) Johansson Ann C. B. (Lund SEX), Therapeutic preparation for inhalation.
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