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Claims for Patent: 5,714,512

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Claims for Patent: 5,714,512

Title: Compositions containing taxane derivatives
Abstract:This invention relates to compositions containing taxane derivatives, consisting of a solution of such derivatives in a surfactant. These compositions can be used to prepare perfusion solutions.
Inventor(s): Bastart; Jean-Pierre (Lesigny, FR), Dupechez; Thierry (Villemoisson Sur Orge, FR), Fabre; Jean-Louis (Paris, FR)
Assignee: Rhone-Poulenc Rorer, S.A. (Antony Cedex, FR)
Application Number:08/568,760
Patent Claims: 1. A composition comprising a compound of the formula (I)

in which Ar is unsubstituted phenyl, R.sub.7 is phenyl or t.butoxy, R.sub.6 is hydrogen, R.sub.5 is acetyloxy or hydroxy, R.sub.3 and R.sub.4 taken together form an oxo radical, R.sub.1 is hydroxy and R.sub.2 is hydrogen, said composition being dissolved in a surfactant selected from polysorbate, polyoxyethylated vegetable oil, and polyethoxylated castor oil, said composition being essentially free or free of ethanol.

2. The composition of claim 1, wherein R.sub.5 is acetyloxy and R.sub.7 is phenyl.

3. The composition of claim 2, wherein said surfactant is polysorbate.

4. The composition of claim 2, wherein said surfactant is polyoxyethylated vegetable oil.

5. The composition of claim 2, wherein said surfactant is polyethoxylated castor oil.

6. The composition of claim 1, wherein R.sub.5 is hydroxy and R.sub.7 is t.butoxy.

7. The composition of claim 6, wherein said surfactant is polysorbate.

8. The composition of claim 6, wherein said surfactant is polyoxyethylated vegetable oil.

9. The composition of claim 6, wherein said surfactant is polyethoxylated castor oil.

10. The composition of claim 1, said composition being a stock solution containing less than 5 volume % ethanol.

11. The composition of claim 10, said composition containing less than 2 volume % ethanol.

12. The composition of claim 10, said composition containing from 1 to 2 volume % ethanol.

13. The composition of claim 1, said composition containing up to 200 mg/ml of the compound of formula (I).

14. The composition of claim 13, said composition containing from 10 to 80 mg/ml of the compound of formula (I).

15. The composition of claim 14, said composition containing from 20 to 80 mg/ml of the compound of formula (I).

16. The composition of claim 13, said composition containing from 6 to 20 mg/ml of the compound of formula (I).

17. The composition of claim 13, said composition containing up to 80 mg/ml of the compound of formula (I).

18. The composition of claim 1, said composition being a perfusion containing less than 0.5 mg/ml of said compound of formula (I), less than 1 ml/l of said ethanol, and less than 15 ml/l of said surfactant.

19. The composition of claim 1, said composition being a perfusion containing less than 1 mg/ml of said compound of formula (I), and less than 1 ml/l of said ethanol.

20. The composition of claim 2, said composition being a perfusion containing 0.1 to 0.3 mg/ml of said compound of formula (I).

21. A method for preparing a composition according to claim 1, which comprises dissolving said compound of formula (I) in ethanol, adding said surfactant and removing said ethanol.

22. The method of claim 21, wherein said ethanol is removed by evaporation.

23. A method for preparing a composition according to claim 1, which comprises slowly adding said compound of formula (I) to a solution of the surfactant containing 1 to 2 volume % ethanol.

24. A stock solution comprising a compound of the formula (I) ##STR4## in which Ar is unsubstituted phenyl, R.sub.7 is phenyl or t.butoxy, R.sub.6 is hydrogen, R.sub.5 is acetyloxy or hydroxy, R.sub.3 and R.sub.4 taken together form an oxo radical, R.sub.1 is hydroxy and R.sub.2 is hydrogen, said compound being dissolved in a surfactant selected from polysorbate, polyoxyethylated vegetable oil, and polyethoxylated castor oil, wherein said stock solution contains from 10 to 200 mg/ml of said compound of formula (I).

25. The stock solution of claim 24, wherein said stock solution contains from 10 to 80 mg/ml of said compound of formula (I).

26. The stock solution of claim 25, wherein said stock solution contains from 12 to 80 mg/ml of said compound of formula (I).

27. The stock solution of claim 26, wherein said stock solution contains from 20 to 80 mg/ml of said compound of formula (I).

28. The stock solution of claim 24, wherein R.sub.5 is acetyloxy and R.sub.7 is phenyl.

29. The stock solution of claim 28, wherein said surfactant is polysorbate.

30. The stock solution of claim 28, wherein said surfactant is polyoxyethylated vegetable oil.

31. The stock solution of claim 28, wherein said surfactant is polyethoxylated castor oil.

32. The stock solution of claim 24, wherein R.sub.5 is hydroxy and R.sub.7 is t.butoxy.

33. The stock solution of claim 32, wherein said surfactant is polysorbate.

34. The stock solution of claim 32, wherein said surfactant is polyoxyethylated vegetable oil.

35. The stock solution of claim 32, wherein said surfactant is polyethoxylated castor oil.
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