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Claims for Patent: 9,308,195

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Claims for Patent: 9,308,195

Title:Non-aqueous taxane formulations and methods of using the same
Abstract: Non-aqueous, ethanol-free taxane formulations are provided. Formulations of embodiments of the invention include a taxane, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid component, wherein the organic acid component is soluble in the non-aqueous solvent and the amount by weight of non-ionic surfactant is equal to or greater than the amount by weight of non-aqueous solvent. Also provided are methods of using the formulations, as well as kits that include the formulations. Non-aqueous, ethanol-free docetaxel formulations are provided. Formulations of embodiments of the invention include docetaxel, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid which is soluble in the non-aqueous solvent and is substantially free of any conjugate base. Also provided are methods of using the formulations, as well as kits that include the formulations.
Inventor(s): Nabeta; Kiichiro (Tokyo, JP)
Assignee: Teikoku Pharma USA, Inc. (San Jose, CA)
Application Number:14/564,384
Patent Claims: 1. A non-aqueous, ethanol-free taxane liquid formulation comprising: a taxane; an oil; a non-ionic surfactant; a non-aqueous solvent; and an organic acid component; wherein the organic acid component is soluble in the non-aqueous solvent and the amount by weight of non-ionic surfactant is equal to or greater than the amount by weight of non-aqueous solvent.

2. The formulation according to claim 1, wherein the taxane is present in an amount ranging from about 0.5 to about 5 wt %.

3. The formulation according to claim 1, wherein the taxane is present in about 2 wt %.

4. The formulation according to claim 1, wherein the taxane is paclitaxel.

5. The formulation according to claim 1, wherein the taxane is docetaxel.

6. The formulation according to claim 3, wherein the taxane is anhydrous docetaxel.

7. The formulation according to claim 3, wherein the taxane is docetaxel trihydrate.

8. The formulation according to claim 1, wherein the oil is selected from the group consisting of synthetic oils, vegetable oils, tocopherols and combinations thereof.

9. The formulation according to claim 8, wherein the oil is selected from the group consisting of soybean oil, olive oil, sesame oil, corn oil, a medium chain triglyceride, a tocopherol or derivative thereof and combinations thereof.

10. The formulation according to claim 1, wherein the oil is present in an amount ranging from about 1 to about 20 wt %.

11. The formulation according to claim 10, wherein the oil is soybean oil.

12. The formulation according to claim 11, wherein the soybean oil is present in an amount ranging from about 1 to about 5 wt %.

13. The formulation according to claim 10, wherein the oil is a medium chain triglyceride.

14. The formulation according to claim 13, wherein the medium chain triglyceride is present in an amount ranging from about 1 to about 5 wt %.

15. The formulation according to claim 1, wherein the non-ionic surfactant is present in an amount ranging from about 40 to about 75 wt %.

16. The formulation according to claim 15, wherein the non-ionic surfactant is present in an amount ranging from about 50 to about 60 wt %.

17. The formulation according to claim 1, wherein the non-ionic surfactant is polysorbate 80.

18. The formulation according to claim 1, wherein the non-aqueous solvent is present in an amount ranging from about 20 to about 60 wt %.

19. The formulation according to claim 18, wherein the non-aqueous solvent is present in an amount ranging from about 35 to about 45 wt %.

20. The formulation according to claim 1, wherein the non-aqueous solvent is polyethylene glycol.

21. The formulation according to claim 20, wherein the polyethylene glycol has a melting point of less than 0.degree. C.

22. The formulation according to claim 1, wherein the organic acid component is present in an amount ranging from 0.3 to 3 wt %.

23. The formulation according to claim 22, wherein the organic acid component is present in an amount ranging from 0.5 to 1 wt %.

24. The formulation according to claim 1, wherein the organic acid component is an organic acid.

25. The formulation according to claim 24, wherein the organic acid is selected from the group consisting of lactic acid and acetic acid.

26. The formulation according to claim 25, wherein the organic acid is lactic acid.

27. The formulation according to claim 26, wherein the lactic acid is present in about 0.8 wt %.

28. The formulation according to claim 1, wherein the organic acid component is an organic acid buffer.

29. The formulation according to claim 28, wherein the organic acid buffer is lactic acid buffer.

30. The formulation according to claim 29, wherein the lactic acid buffer is present in about 1 wt %.

31. The formulation according to claim 1, wherein the amount by weight of oil is equal to or less than about 2.5 times the amount of taxane.

32. The formulation according to claim 1, wherein the ratio by weight of taxane to oil is from about 1:0.5 to about 1:2.5.

33. A non-aqueous, ethanol-free docetaxel liquid formulation comprising: docetaxel; soybean oil in an amount ranging from about 1 to about 5 wt %; polysorbate 80 in an amount ranging from about 50 to about 60 wt %; polyethylene glycol in an amount ranging from about 35 to about 45 wt %; and lactic acid or lactic acid buffer in an amount ranging from 0.3 to 1 wt %; wherein the amount by weight of non-ionic surfactant is about equal to or greater than the amount by weight of non-aqueous solvent.

34. A non-aqueous, ethanol-free docetaxel liquid formulation comprising: docetaxel; a medium chain triglyceride in an amount ranging from about 1 to about 5 wt %; polysorbate 80 in an amount ranging from about 50 to about 60 wt %; polyethylene glycol in an amount ranging from about 35 to about 45 wt %; and lactic acid or lactic acid buffer in an amount ranging from 0.3 to 1 wt %; wherein the amount by weight of non-ionic surfactant is about equal to or greater than the amount by weight of non-aqueous solvent.

35. The formulation according to claim 33, wherein the docetaxel is anhydrous docetaxel.

36. The formulation according to claim 33, wherein the docetaxel is docetaxel trihydrate.

37. The formulation according to claim 33, wherein the docetaxel is present in an amount ranging from about 0.5 to about 5 wt %.

38. The formulation according to claim 37, wherein the docetaxel is present in about 2 wt %.

39. The formulation according to claim 33, wherein the polyethylene glycol has a melting point of less than 0.degree. C.

40. The formulation according to claim 33, wherein the ratio by weight of docetaxel to oil is from 1:0.5 to 1:2.5.

41. The formulation according to claim 1, wherein the ethanol-free taxane liquid formulation has a pH of less than about 3.5.

42. The formulation according to claim 1, wherein the formulation is stable for more than 6 months at 40.degree. C.

43. The formulation according to claim 1, wherein the formulation exhibits a taxane recovery rate of greater than 95% after 6 months at 40.degree. C.

44. The formulation according to claim 1, wherein the formulation forms particles of less than about 20 nm when combined with an aqueous medium.

45. A method of administering an ethanol-free taxane liquid formulation to a subject, the method comprising: (a) combining the ethanol-free taxane formulation according to claim 1 with an aqueous medium to provide an ethanol-free taxane diluted solution; and (b) administering the ethanol-free taxane diluted solution to the subject.

46. A kit comprising: (a) a vial containing the ethanol-free taxane formulation according to claim 1; and (b) instructions for using the ethanol-free taxane formulation.

47. The kit according to claim 46, further comprising (c) an aqueous medium.

48. The formulation according to claim 19, wherein the non-aqueous solvent is polyethylene glycol having an average molecular weight of 1000 or less.

49. The non-aqueous, ethanol-free taxanc liquid formulation of claim 1, wherein the taxane is anhydrous docctaxcl or a hydrate thereof; the oil is soybean oil in an amount ranging from about 1 to about 5 wt%; the non-ionic surfactant is polysorbate 80 in an amount ranging from about 50 to about 60 wt%; and the non-aqueous solvent is polyethylene glycol having an average molecular weight of 1000 or less, and in an amount ranging from about 35 to about 45 wt%.

50. A method of administering an ethanol-free taxane liquid formulation to a subject, the method comprising: (a) combining the ethanol-free taxane formulation according to claim 49 with an aqueous medium to provide an ethanol-free taxane diluted solution; and (b) administering the ethanol-free taxane diluted solution to the subject.

51. The formulation according to claim 49, wherein the formulation forms particles of less than about 20 nm when combined with an aqueous medium.
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