# US 7,744,925 B2 · Solid dose delivery vehicle and methods of making same > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 7,744,925 B2 - Document ID: US7744925B2 - Status: Granted - Kind: B2 - Application number: 11/134,573 - Filed: 2005-05-20 - Published: 2005-12-15 - Granted: 2010-06-29 - Earliest claimed: 1994-12-02 - Assignees: Quadrant Drug Delivery Limited - Inventors: Bruce J. Roser; Jaap Kampinga; Camilo Colaco; Julian Blair - Web page: https://patentgrep.com/patent/US7744925B2 ## CPC - A61K 9/1623: {Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules} - A61K 9/0021: {Intradermal administration, e.g. through microneedle arrays or needleless injectors} - A61K 9/145: {with organic compounds} - Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE ## Abstract The present invention encompasses a therapeutic composition in solid dose form that is suitable for pulmonary administration. The therapeutic composition may comprise therapeutic particles in a glassy state. The therapeutic composition preferably comprises a bioactive material such as insulin, and a sugar alcohol. The components are optionally in solid solution. The therapeutic composition can preferably remain in a glassy state when stored at elevated temperatures, and/or extended periods. ## Claims ### Claim 1 A therapeutic composition in solid dose form comprising a bioactive material and a sugar alcohol, wherein a) the bioactive material is insulin, b) the therapeutic composition comprises therapeutic particles containing insulin homogeneously distributed in a solid solution with a sugar alcohol, wherein the therapeutic particles are in a glassy state, c) the therapeutic composition is a powder suitable for pulmonary administration, d) the therapeutic particles containing the insulin in the solid solution with the sugar alcohol remain in the glassy state when stored at elevated temperature for one month, wherein the elevated temperature is 60° C., and e) the therapeutic particles have a mean particle size of 0.5 to 5 μm. ### Claim 2 (depends on 1) The therapeutic composition according to claim 1, wherein the particles have a mean particle size of 1 to 4 μm. ### Claim 3 (depends on 2) The therapeutic composition according to claim 2, said particles further comprising a glass modifier, wherein the glass modifier is not the bioactive material. ### Claim 4 (depends on 3) The therapeutic composition according to claim 3, wherein the glass modifier is a protein. ### Claim 5 (depends on 1) The therapeutic composition according to claim 1, said therapeutic particles further comprising a physiologically acceptable inhibitor of the Maillard reaction. ### Claim 6 (depends on 5) The therapeutic composition according to claim 5, wherein the particles have a mean particle size of 1 to 4 μm. ### Claim 7 (depends on 5) The therapeutic composition according to claim 5, said therapeutic particles further comprising a glass modifier, wherein the glass modifier is not the bioactive material. ### Claim 8 (depends on 7) The therapeutic composition according to claim 7, wherein the glass modifier is a protein. ### Claim 9 (depends on 1) The therapeutic composition according to claim 1, said therapeutic particles further comprising an amino acid that is capable of inhibiting the Maillard reaction. ### Claim 10 (depends on 9) The therapeutic composition according to claim 9, further comprising a glass modifier, wherein the glass modifier is not the bioactive material. ### Claim 11 (depends on 9) The therapeutic composition according to claim 9, wherein the particles have a mean particle size of 1 to 4 μm. ### Claim 12 (depends on 1) The therapeutic composition according to claim 1, wherein the therapeutic composition is suitable for delivering the insulin by transalveolar administration. ### Claim 13 (depends on 1) The therapeutic composition according to claim 1, said therapeutic particles further comprising a glass modifier, wherein the glass modifier is not the bioactive material. ### Claim 14 (depends on 13) The therapeutic composition according to claim 13, wherein the glass modifier is a protein. ### Claim 15 (depends on 1) The therapeutic composition according to claim 1, wherein the therapeutic particles remain in a glassy state when stored for one month at 70° C. ### Claim 16 (depends on 15) The therapeutic composition according to claim 15, wherein said therapeutic particles are spray-dried. ### Claim 17 (depends on 16) The therapeutic composition according to claim 16, said therapeutic particles further comprising an amino acid that is capable of inhibiting the Maillard reaction. ### Claim 18 (depends on 17) The therapeutic composition according to claim 17, said therapeutic particles further comprising a glass modifier, wherein the glass modifier is not the bioactive material. ### Claim 19 (depends on 16) The therapeutic composition according to claim 16, said therapeutic particles further comprising a physiologically acceptable inhibitor of the Maillard reaction. ### Claim 20 (depends on 15) The therapeutic composition according to claim 15, said therapeutic particles further comprising a glass modifier, wherein the glass modifier is not the bioactive material. ### Claim 21 (depends on 15) The therapeutic composition according to claim 15, said therapeutic particles further comprising an amino acid that is capable of inhibiting the Maillard reaction. ### Claim 22 (depends on 1) The therapeutic composition according to claim 1, wherein the therapeutic particles are spray-dried. ### Claim 23 (depends on 22) The therapeutic composition according to claim 22, said therapeutic particles further comprising a glass modifier, wherein the glass modifier is not the bioactive material. ### Claim 24 (depends on 22) The therapeutic composition according to claim 22, said therapeutic particles further comprising an amino acid that is capable of inhibiting the Maillard reaction. ### Claim 25 (depends on 1) The therapeutic composition according to claim 1, wherein said therapeutic particles additionally comprise a physiologically acceptable glass. ### Claim 26 (depends on 25) The therapeutic composition according to claim 25 wherein the physiologically acceptable glass is water soluble. ### Claim 27 (depends on 25) The therapeutic composition according to claim 25 wherein the physiologically acceptable glass in said composition comprises a water soluble physiologically acceptable carboxylate glass. ### Claim 28 (depends on 26, 27) The therapeutic composition according to claim 26 or claim 27 wherein the composition is suitable for transalveolar delivery. ### Claim 29 (depends on 28) The therapeutic composition according to claim 28 wherein the therapeutic particles of said composition are spray-dried. ### Claim 30 (depends on 29) The therapeutic composition according to claim 29 said therapeutic particles additionally comprising an amino acid that is capable of inhibiting the Maillard reaction. ### Claim 31 (depends on 26, 27) The therapeutic composition according to claim 26 or claim 27 wherein the therapeutic particles of said composition remain in a glassy state when stored for one month at 70° C. ### Claim 32 (depends on 28) The therapeutic composition according to claim 28 wherein the therapeutic particles of said composition remain in a glassy state when stored for one month at 70° C. ### Claim 33 (depends on 29) The therapeutic composition according to claim 29 wherein the therapeutic particles of said composition remain in a glassy state when stored for one month at 70° C. ### Claim 34 (depends on 30) The therapeutic composition according to claim 30 wherein the therapeutic particles of said composition remain in a glassy state when stored for one month at 70° C.