Details for Patent: 6,392,036

Title:	Dry heat sterilization of a glucocorticosteroid
Abstract:	The invention provides a process for the sterilization of a powdered form of a glucocorticosteroid, sterile glucocorticosteroids, sterile formulations containing glucocorticosteroids and use thereof in the treatment of an allergic and/or inflammatory condition of the nose or lungs.
Inventor(s):	Karlsson; Ann-Kristin (Staffanstorp, SE), Larrivee-Elkins; Cheryl (Framingham, MA), Molin; Ove (Huddinge, SE)
Assignee:	AstraZeneca AB (CH)
Filing Date:	Jan 29, 1999
Application Number:	09/230,781
Claims:	1. A process for the sterilization of a powder comprising a glucocorticosteroid or ester, acetal, or salt thereof, said process comprising heat treating the powder at a temperature of from 100.degree. C. to 130.degree. C., wherein the glucocorticosteroid or ester, acetal, or salt thereof contains an asymmetric acetal structure comprising 16.alpha.,17.alpha.-butylidenedioxy. 2. The process according to claim 1, wherein the glucocorticosteroid is an anti-inflammatory glucocorticosteroid. 3. The process according to claim 1, wherein the glucocorticosteroid or ester, acetal, or salt thereof is selected from the group consisting of budesonide, rofleponide and rofleponide palmitate. 4. The process according to claim 1, wherein the glucocorticosteroid is heat treated at a temperature of from 110 to 120.degree. C. 5. The process according to claim 1, wherein the glucocorticosteroid is heat treated for no more than 10 hours. 6. The process according to claim 1, wherein the glucocorticosteroid is heat treated at a temperature of from about 110.degree. C. to 130.degree. C. for no more than 8 hours. 7. The process according to claim 6, wherein the glucocorticosteroid is heat treated at a temperature of about 120.degree. C. for no more than 4 hours. 8. The process according to claim 6, wherein the glucocorticosteroid is heat treated at a temperature of about 120.degree. C. for no more than 2 hours. 9. The process according to claim 1, wherein the glucocorticosteroid contains less than about 1% (w/w) of water before the heat treatment. 10. The process according to claim 1, wherein the glucocorticosteroid powder has a mass median diameter (MMD) of less than 10 .mu.m. 11. The process according to claim 1, said process being carried out under an inert gas atmosphere. 12. The process according to claim 1, wherein the amount of heat resistant spores in the powder is reduced by more than log 6 by the heat treatment. 13. The process according to claim 1, wherein the time required to reduce by 90% a population of spores in the powder is less than about 240 minutes at a temperature of from 100.degree. C. to 130.degree. C. 14. The process according to claim 1, wherein the glucocorticosteroid is heat treated at a temperature of from about 110.degree. C. to about 130.degree. C. for no more than 4 hours. 15. The process according to claim 1, wherein the glucocorticosteroid contains less than about 0.5% (w/w) of water before the heat treatment. 16. The process according to claim 1, wherein the glucocorticosteroid powder has a mass median diameter (MMD) of less than 5 .mu.m. 17. The process according to claim 1, wherein the amount of heat resistant spores in the powder is reduced by more than log 7 by the heat treatment. 18. The process according to claim 1, wherein the time required to reduce by 90% a population of spores in the powder is less than 90 minutes at a temperature of from 100.degree. C. to 130.degree. C.