Claims
- 1. Amorphous celecoxib.
- 2. A celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, as amorphous celecoxib.
- 3. The drug substance of claim 2 wherein the amorphous celecoxib is present in an amount of about 10% to about 100% by weight of the celecoxib.
- 4. The drug substance of claim 2 that comprises substantially phase pure amorphous celecoxib.
- 5. A celecoxib-crystallization inhibitor composite comprising particles of amorphous celecoxib in intimate association with one or more crystallization inhibitor(s) in an amount effective to reduce transformation of amorphous celecoxib to crystalline celecoxib.
- 6. The composite of claim 5 wherein the crystallization inhibitor is a polymer.
- 7. The composite of claim 6 wherein the polymer is selected from polyvinylpyrrolidone and hydroxypropylmethylcellulose.
- 8. The composite of claim 6 wherein the polymer is polyvinylpyrrolidone.
- 9. The composite of claim 5 wherein the crystallization inhibitor(s) are present in a total amount of about 10% to about 80% by weight of the composite.
- 10. A celecoxib-crystallization inhibitor composite comprising particles of a celecoxib drug substance of claim 2 in intimate association with one or more crystallization inhibitor(s) in an amount effective to reduce transformation of amorphous celecoxib to crystalline celecoxib.
- 11. The composite of claim 10 wherein the crystallization inhibitor is a polymer.
- 12. The composite of claim 11 wherein the polymer is selected from polyvinylpyrrolidone and hydroxypropylmethylcellulose.
- 13. The composite of claim 11 wherein the polymer is polyvinylpyrrolidone.
- 14. The composite of claim 10 wherein the crystallization inhibitor(s) are present in a total amount of about 10% to about 80% by weight of the composite.
- 15. A pharmaceutical composition comprising amorphous celecoxib in a total celecoxib dosage amount of about 10 mg to about 1000 mg, and one or more pharmaceutically acceptable excipients.
- 16. A pharmaceutical composition comprising a celecoxib drug substance of claim 2 in a total celecoxib dosage amount of about 10 mg to about 1000 mg, and one or more pharmaceutically acceptable excipients.
- 17. A pharmaceutical composition comprising a celecoxib-crystallization inhibitor composite of claim 5, in a total celecoxib dosage amount of about 10 mg to about 1000 mg, and one or more pharmaceutically acceptable excipients
- 18. A pharmaceutical composition comprising a celecoxib-crystallization inhibitor composite of claim 10, in a total celecoxib dosage amount of about 10 mg to about 1000 mg, and one or more pharmaceutically acceptable excipients.
- 19. A process for preparing a celecoxib drug substance, the process comprising
(a) melting celecoxib; (b) rapidly cooling the resulting melted celecoxib to form a celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, in amorphous form; and optionally (c) grinding the celecoxib drug substance to form a celecoxib drug substance powder.
- 20. A process for preparing a celecoxib-crystallization inhibitor composite, the process comprising
(a) dissolving celecoxib and one or more crystallization inhibitors in a solvent liquid to form a solution; (b) drying the solution to form a celecoxib-crystallization inhibitor composite wherein the celecoxib is present, at least in a detectable amount, in amorphous form; and optionally (c) grinding the celecoxib drug substance to form a celecoxib-crystallization inhibitor composite powder.
- 21. The process of claim 20 wherein drying step (b) is performed by spray drying.
- 22. The process of claim 20 wherein the solvent liquid comprises isopropanol.
- 23. A process for preparing a pharmaceutical composition, the process comprising
(a) blending amorphous celecoxib, or a celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, as amorphous celecoxib, with one or more excipients to form a blend; and (b) tableting or encapsulating the blend to form celecoxib tablets or capsules respectively.
- 24. The process of claim 23, further comprising granulating the blend to form a granulate prior to tableting or encapsulating.
- 25. The process of claim 24 wherein granulating is performed by wet granulation to form a wet granulate, and wherein the wet granulate is dried prior to tableting or encapsulating.
- 26. A process for preparing a pharmaceutical composition, the process comprising
(a) blending a celecoxib-crystallization inhibitor composite of claim 5 with one or more excipients to form a blend; and (b) tableting or encapsulating the blend to form celecoxib tablets or capsules respectively.
- 27. The process of claim 26, further comprising granulating the blend to form a granulate prior to tableting or encapsulating.
- 28. The process of claim 27 wherein granulating is performed by wet granulation to form a wet granulate, and wherein the wet granulate is dried prior to tableting or encapsulating.
- 29. A process for preparing a pharmaceutical composition, the process comprising
(a) blending a celecoxib-crystallization inhibitor composite of claim 10 with one or more excipients to form a blend; and (b) tableting or encapsulating the blend to form celecoxib tablets or capsules respectively.
- 30. The process of claim 29, further comprising granulating the blend to form a granulate prior to tableting or encapsulating.
- 31. The process of claim 30 wherein granulating is performed by wet granulation to form a wet granulate, and wherein the wet granulate is dried prior to tableting or encapsulating.
- 32. A method of treating a medical condition or disorder in a subject where treatment with a cyclooxygenase-2 inhibitor is indicated, comprising orally administering one or more dose units of a composition of claim 15 once or twice a day.
- 33. A method of treating a medical condition or disorder in a subject where treatment with a cyclooxygenase-2 inhibitor is indicated, comprising orally administering one or more dose units of a composition of claim 16 once or twice a day.
- 34. A method of treating a medical condition or disorder in a subject where treatment with a cyclooxygenase-2 inhibitor is indicated, comprising orally administering one or more dose units of a composition of claim 17 once or twice a day.
- 35. A method of treating a medical condition or disorder in a subject where treatment with a cyclooxygenase-2 inhibitor is indicated, comprising orally administering one or more dose units of a composition of claim 18 once or twice a day.
Parent Case Info
[0001] This application is a continuation-in-part of a U.S. application (identified as docket no. C-3411, Ser. No. not yet known) filed on Dec. 1, 2000, and also claims priority of U.S. provisional application Ser. No. 60/169,856 filed on Dec. 9, 1999.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60169856 |
Dec 1999 |
US |