Claims
- 1. A pharmaceutical composition for oral administration comprising a granulation, said granulation comprising CCI-779, a water soluble polymer, a surfactant, an antioxidant, and a pH modifying agent.
- 2. The composition of claim 1, wherein the water soluble polymer is PVP, hydroxypropylmethylcellulose, polyethylene glycol, or cyclodextrin or mixtures thereof.
- 3. The composition of claim 2, wherein the water soluble polymer is PVP.
- 4. The composition of claim 3, wherein the surfactant is polysorbate 80, sodium lauryl sulfate, sodium dodecyl sulfate, a salt of a bile acid, an ethoxylated vegetable oil, a polyoxyethylene-polyoxypropylene block copolymer, or a poloxamer.
- 5. The composition of claim 4, wherein the surfactant is sodium lauryl sulfate or sodium dodecyl sulfate.
- 6. The pharmaceutical composition of claim 5, wherein the pH modifying agent is sodium citrate, citric acid, or dilute hydrochloric acid.
- 7. A process for preparing a CCI-779 oral composition, which comprises
(a) dissolving CCI-779 and an antioxidant in an alcohol to form an alcoholic solution; (b) dissolving PVP, a pH modifying agent, and a surfactant in water to form an aqueous solution; (c) mixing the alcoholic solution and the aqueous solution to form a hydroholic solution. (d) adding the hydroholic solution to a mixer containing one or more intragranular excipients; (e) granulating the mixture; and (f) drying the resulting granulation.
- 8. A process for preparing a CCI-779 oral composition, which comprises
(a) dissolving CCI-779 and an antioxidant in an alcohol to form an alcoholic solution; (b) dissolving PVP, a pH modifying agent, and a surfactant in water to form an aqueous solution; (c) adding the aqueous and alcoholic solutions stepwise, and in one or more portions each, to a mixer containing one or more intragranular excipients; (e) granulating the mixture; and (f) drying the resulting granulation.
- 9. A CCI-779 oral composition prepared by wet granulation.
- 10. A CCI-779 oral composition prepared the process comprising
(a) dissolving CCI-779 and an antioxidant in an alcohol; (b) dissolving PVP, a pH modifying agent, and a surfactant in water; (c) combining the aqueous and alcoholic solutions to provide a hydroholic solution; (d) adding the hydroalcoholic solution to a mixer containing one or more intragranular excipients; (e) granulating the mixture; and (f) drying the resulting granulation.
- 11. The composition of claim 10, wherein the pH modifying agent is selected from the group consisting of citric acid, sodium citrate, hydrochloric acid and mixtures thereof.
- 12. The composition of claim 11, wherein the alcohol is ethanol.
- 13. The composition of claim 12, wherein the antioxidant is butylated hydroxyanisole and butylated hydroxytoluene.
- 14. The composition of claim 13, wherein the surfactant is sodium lauryl sulfate.
- 15. A CCI-779 oral formulation prepared by the process comprising
(a) dissolving CCI-779 and an antioxidant in an alcohol; (b) dissolving PVP, a pH modifying agent, and a surfactant in water; (c) adding the aqueous and alcoholic solutions stepwise, and in one or more portions each, to a mixer containing one or more intragranular excipients; (e) granulating the mixture; and (f) drying the resulting granulation.
- 16. The composition of claim 15, wherein the pH modifying agent is selected from the group consisting of citric acid, sodium citrate, hydrochloric acid and mixtures thereof.
- 17. The composition of claim 16, wherein the alcohol is ethanol.
- 18. The composition of claim 17, wherein the antioxidant is butylated hydroxyanisole and butylated hydroxytoluene.
- 19. The composition of claim 18, wherein the surfactant is sodium lauryl sulfate.
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This is a non-provisional of U.S. Patent Application No. 60/411,264, filed Sep. 17, 2002, and claims the benefit of priority thereof.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60411264 |
Sep 2002 |
US |