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Claims for Patent: 8,026,276

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Claims for Patent: 8,026,276

Title:Parenteral CCI-779 formulations containing cosolvents, an antioxidant, and a surfactant
Abstract: Parenteral formulations of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl) -2-methylpropionic acid (CCI-779) are provided. One parenteral formulation contains CCI-779, an alcoholic co-solvent, and an antioxidant. Another parenteral formulation contains CCI-779, an alcoholic solvent, an antioxidant, a diluent solvent, and a surfactant. Processes for preparing parenteral CCI-779 formulations using a co-solvent concentrate are also provided.
Inventor(s): Rubino; Joseph T. (Towaco, NJ), Siskavich; Victoria (Lyon Mountain, NY), Harrison; Maureen M. (Sugar Loaf, NY), Gandhi; Pooja (Highland Mills, NY)
Assignee: Wyeth LLC (Madison, NJ)
Application Number:10/626,943
Patent Claims: 1. A parenteral composition comprising: (i) a first mixture of about 1 to about 25 mg/mL of CCI-779, about 15 to about 60% w/v of dehydrated ethanol, about 0.01 to about 0.1% w/v of d,1-.alpha.-tocopherol, about 0.001 to about 0.005% w/v of citric acid, and about 15 to about 60% w/v of propylene glycol, and (ii) a second mixture of about 15 to about 60% w/v of polysorbate 80, 15 to 60% w/v of polyethylene glycol 400, and about 15 to about 60% w/v of dehydrated ethanol.

2. The parenteral composition according to claim 1, wherein (i) and (ii) are present in a ratio of about 1:1.5 to 1:2.

3. The parenteral composition according to claim 1, comprising about 10 mg/mL of CCI-779.

4. The parenteral composition according to claim 1, comprising about 0.0025 to about 0.005% w/v of citric acid.

5. The parenteral composition according to claim 1, comprising: (i) a first mixture of about 25 mg/mL CCI-779, about 40% w/v of dehydrated ethanol, about 0.075% w/v of d,1-a-tocopherol, about 0.0025% w/v of citric acid, and 35% w/v propylene glycol, and (ii) a second mixture of about 20% w/v of dehydrated ethanol, about 40% w/v of polysorbate 80, and about 40% w/v of polyethylene glycol 400.

6. The parenteral composition according to claim 5, wherein (i) and (ii) are present in a ratio of about 1:1.5.

7. The parenteral composition according to claim 1, comprising: (i) a first mixture of about 1 to about 25 mg/mL of CCI-779, about 40% w/v of dehydrated ethanol, about 0.075% w/v of d,1-.alpha.-tocopherol, about 0.0025% w/v of citric acid, and q.s. of propylene glycol, and (ii) a second mixture of about 40% w/v of polysorbate 80, about 20% w/v of polyethylene glycol 400, and about 40% w/v of dehydrated ethanol.

8. A parenteral composition comprising: (i) a first mixture of about 1 to about 25 mg/mL of CCI-779, about 15 to about 60% w/v of dehydrated ethanol, about 0.01 to about 0.1% w/v of d,1-.alpha.-tocopherol, and about 15 to about 60% w/v of propylene glycol, and (ii) a second mixture of about 15 to about 60% w/v of polysorbate 80, 15 to 60% w/v of polyethylene glycol 400, and about 15 to about 60% w/v of dehydrated ethanol.

9. A parenteral composition consisting of: (i) a concentrate of about 1 to about 25 mg/mL of CCI-779, about 0.01 to 0.1% w/v of d,1-.alpha.-tocopherol, about 0.001 to about 0.005% w/v of citric acid, and about 15 to about 60% w/v of dehydrated ethanol and propylene glycol, and (ii) a diluent of about 15 to about 60% w/v of polysorbate 80, 15 to 60% w/v of polyethylene glycol 400, and about 15 to about 60% w/v of dehydrated ethanol.

10. The parenteral composition according to claim 9, wherein (i) and (ii) are present in a ratio of about 1:1.5 to 1:2 of concentrate to diluent.

11. The parenteral composition according to claim 9, consisting of about 10 mg/mL of CCI-779.

12. A parenteral composition consisting of (i) a concentrate of about 1 to about 25 mg/mL of CCI-779, about 0.01 to 0.1% w/v of d,1-.alpha.-tocopherol, and about 15 to about 60% w/v of dehydrated ethanol and propylene glycol, and (ii) a diluent of about 15 to about 60% w/v of polysorbate 80, 15 to 60% w/v of polyethylene glycol 400, and about 15 to about 60% w/v of dehydrated ethanol.

13. A parenteral composition comprising: (i) about 1 to about 25 mg/mL of CCI-779, (ii) about 0.01 to 0.1% w/v of d,1-.alpha.-tocopherol, (iii) about 0.001 to about 0.005% w/v of citric acid, (iv) about 15 to about 60% w/v of a combination of dehydrated ethanol and propylene glycol, and (v) about 15 to about 60% w/v of a combination of polysorbate 80 and polyethylene glycol 400.

14. The parenteral composition according to claim 13, wherein the ratio of polysorbate 80 to polyethylene glycol 400 is about 1:1.

15. The parenteral composition according to claim 13, wherein the ratio of dehydrated ethanol to propylene glycol in (iv) is about 1.4:1.

16. The parenteral composition according to claim 13, wherein the ratio of component (iv) to (i) is about 50:1.

17. The parenteral composition according to claim 13, wherein the ratio of component (v) to (i) is about 50:1.

18. A parenteral composition comprising: (i) about 1 to about 25 mg/mL of CCI-779, (ii) about 0.01 to 0.1% w/v of d,1-.alpha.-tocopherol, (iii) about 0.001 to about 0.005% w/v of citric acid, (iv) about 15 to about 60% w/v of a combination of dehydrated ethanol and propylene glycol, wherein the ratio of dehydrated ethanol to propylene glycol is about 1.4:1, and (v) about 15 to about 60% w/v of a combination of polysorbate 80 and polyethylene glycol 400, wherein the ratio of polysorbate 80 to polyethylene glycol 400 is about 1:1; wherein: the ratio of mixture (iv) to (i) is about 50:1; and the ratio of mixture (v) to (i) is about 50:1.

19. A parenteral composition comprising: (i) about 1 to about 25 mg/mL of CCI-779, (ii) about 0.01 to 0.1% w/v of d,1-.alpha.-tocopherol, (iii) about 15 to about 60% w/v of a combination of dehydrated ethanol and propylene glycol, wherein the ratio of dehydrated ethanol to propylene glycol is about 1.4:1, and (iv) about 15 to about 60% w/v of a combination of polysorbate 80 and polyethylene glycol 400, wherein the ratio of polysorbate 80 to polyethylene glycol 400 is about 1:1; wherein: the ratio of mixture (iii) to (i) is about 50:1; and the ratio of mixture (iv) to (i) is about 50:1.

20. A parenteral composition comprising: (i) about 2.5% w/v of CCI-779, about 0.075% w/v of d,1-.alpha.-tocopherol, about 0.0025% w/v of citric acid, about 40% w/v of dehydrated ethanol, and about 50% w/v of propylene glycol, and (ii) about 40% w/v of polysorbate 80, about 20% w/v of dehydrated ethanol, and about 43% w/v of polyethylene glycol 400.

21. The parenteral composition according to claim 20, wherein (i) and (ii) are present in a ratio of about 1:1.5 to 1:2.

22. A parenteral composition comprising: (i) about 1% w/v of CCI-779, (ii) about 0.03% w/v of d,1-.alpha.-tocopherol, (iii) about 0.001% w/v of citric acid, (iv) about 28% w/v of dehydrated ethanol, (v) about 20% w/v propylene glycol, (vi) about 24% w/v of polysorbate 80 and (vii) about 26% w/v of polyethylene glycol 400.

23. A process for preparing a parenteral composition of claim 1, said process comprising combining mixtures (i) and (ii).

24. The process according to claim 23, further comprising combining mixtures (i) and (ii) with water.
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