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Claims for Patent: 8,940,786

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Claims for Patent: 8,940,786

Title:Non-aqueous taxane nanodispersion formulations and methods of using the same
Abstract: Non-aqueous, ethanol-free taxane nanodispersion formulations are provided. Nanodispersion 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 nanodispersion formulations, as well as kits that include the nanodispersion formulations. Non-aqueous, ethanol-free docetaxel nanodispersion formulations are provided. Nanodispersion 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 nanodispersion formulations, as well as kits that include the nanodispersion formulations.
Inventor(s): Nabeta; Kiichiro (Tokyo, JP)
Assignee: Teikoku Pharma USA, Inc. (San Jose, CA)
Application Number:14/041,675
Patent Claims: 1. A non-aqueous, ethanol-free taxane liquid nanodispersion 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 nanodispersion formulation according to claim 1, wherein the taxane is present in an amount ranging from about 0.5 to about 5 wt %.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

43. The nanodispersion 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 nanodispersion 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 nanodispersion formulation to a subject, the method comprising: (a) combining the ethanol-free taxane nanodispersion formulation according to any one of the above claims 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 nanodispersion formulation according to claim 1; and (b) instructions for using the ethanol-free taxane nanodispersion formulation.

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