Progesterone formulations
View Patent ↗Various pharmaceutical formulations are disclosed herein. For example, a pharmaceutical formulation is disclosed comprising ultra-micronized progesterone.
1. A pharmaceutical composition comprising:
progesterone;
a medium chain oil; and a non-ionic surfactant;
wherein the progesterone is present from about 20 to about 50 weight percent of the composition.
2. The pharmaceutical composition of claim 1 , wherein the progesterone is ultra-micronized and has an X50 less than or equal to 15 microns.
3. The pharmaceutical composition of claim 2 , wherein the ultra-micronized progesterone has an X90 of less than about 25 microns.
4. The pharmaceutical composition of claim 1 , wherein a portion of the progesterone is solubilized and a portion of the progesterone is suspended.
5. The pharmaceutical composition of claim 1 , wherein the non-ionic surfactant is selected from the group consisting of lauroyl macrogol-32 glycerides EP, lauroyl polyoxyl-32 glycerides, and caprylocaproyl macrogol-8 glycerides EP.
6. The pharmaceutical composition of claim 1 , wherein the composition is provided in a gelatin capsule.
7. The pharmaceutical composition of claim 1 , wherein the composition provides increased bioavailability compared to a micronized progesterone suspended in peanut oil.
8. The pharmaceutical composition of claim 1 , wherein progesterone is the sole active ingredient.
9. The pharmaceutical composition of claim 1 , wherein the medium chain oil comprises at least one C 6 -C 14 fatty acid mono-, di-, or tri-ester of glycerol or mono- or di-ester of a glycol.
10. The pharmaceutical composition of claim 9 , wherein the at least one C 6 -C 14 fatty acid mono-, di-, or tri-ester of glycerol is a C 8 fatty acid mono-, di-, or tri-ester of glycerol.
11. The pharmaceutical composition of claim 10 , further comprising a second C 6 -C 14 fatty acid mono-, di-, or tri-ester of glycerol.
12. The pharmaceutical composition of claim 11 , wherein the second C 6 -C 14 fatty acid mono-, di-, or tri-ester of glycerol is a C 10 fatty acid mono-, di-, or tri-ester of glycerol.
13. The pharmaceutical composition of claim 12 , wherein the medium chain oil is MIGLYOL 812.
14. A pharmaceutical composition comprising:
75 mg of progesterone;
a medium chain oil; and
a non-ionic surfactant;
wherein the progesterone is present at from about 20 to about 50 weight percent of the composition.
15. The pharmaceutical composition of claim 14 , wherein the progesterone is ultra-micronized and has an X50 less than or equal to 15 microns.
16. The pharmaceutical composition of claim 15 , wherein the ultra-micronized progesterone has an X90 of less than about 25 microns.
17. The pharmaceutical composition of claim 14 , wherein a portion of the progesterone is solubilized and a portion of the progesterone is suspended.
18. The pharmaceutical composition of claim 14 , wherein the non-ionic surfactant is selected from the group consisting of lauroyl macrogol-32 glycerides EP, lauroyl polyoxyl-32 glycerides, and caprylocaproyl macrogol-8 glycerides EP.
19. The pharmaceutical composition of claim 14 , wherein the composition is provided in a gelatin capsule.
20. The pharmaceutical composition of claim 14 , wherein the composition provides increased bioavailability compared to a micronized progesterone suspended in peanut oil.
21. The pharmaceutical composition of claim 14 , wherein progesterone is the sole active ingredient.
22. The pharmaceutical composition of claim 14 , wherein the medium chain oil comprises at least one C 6 -C 14 fatty acid mono-, di-, or tri-ester of glycerol or mono- or di-ester of a glycol.
23. The pharmaceutical composition of claim 22 , wherein the at least one C 6 -C 14 fatty acid mono-, di-, or tri-ester of glycerol is a C 8 fatty acid mono-, di-, or tri-ester of glycerol.
24. The pharmaceutical composition of claim 23 , further comprising a second C 6 -C 14 fatty acid mono-, di-, or tri-ester of glycerol.
25. The pharmaceutical composition of claim 24 , wherein the second C 6 -C 14 fatty acid mono-, di-, or tri-ester of glycerol is a C 10 fatty acid mono-, di-, or tri-ester of glycerol.
26. The pharmaceutical composition of claim 25 , wherein the medium chain oil is MIGLYOL 812.
27. A pharmaceutical composition comprising:
150 mg progesterone;
a medium chain oil; and
a non-ionic surfactant;
wherein the progesterone is present at from about 20 to about 50 weight percent of the composition.
28. The pharmaceutical composition of claim 27 , wherein the progesterone is ultra-micronized and has an X50 less than or equal to 15 microns.
29. The pharmaceutical composition of claim 28 , wherein the ultra-micronized progesterone has an X90 of less than about 25 microns.
30. The pharmaceutical composition of claim 27 , wherein a portion of the progesterone is solubilized and a portion of the progesterone is suspended.
31. The pharmaceutical composition of claim 27 , wherein the non-ionic surfactant is selected from the group consisting of lauroyl macrogol-32 glycerides EP, lauroyl polyoxyl-32 glycerides, and caprylocaproyl macrogol-8 glycerides EP.
32. The pharmaceutical composition of claim 27 , wherein the composition is provided in a gelatin capsule.
33. The pharmaceutical composition of claim 27 , wherein the composition provides increased bioavailability compared to a micronized progesterone suspended in peanut oil.
34. The pharmaceutical composition of claim 27 , wherein progesterone is the sole active ingredient.
35. The pharmaceutical composition of claim 27 , wherein the medium chain oil comprises at least one C 6 -C 14 fatty acid mono-, di-, or tri-ester of glycerol or mono- or di-ester of a glycol.
36. The pharmaceutical composition of claim 35 , wherein the at least one C 6 -C 14 fatty acid mono-, di-, or tri-ester of glycerol is a C 8 fatty acid mono-, di-, or tri-ester of glycerol.
37. The pharmaceutical composition of claim 36 , further comprising a second C 6 -C 14 fatty acid mono-, di-, or tri-ester of glycerol.
38. The pharmaceutical composition of claim 37 , wherein the second C 6 -C 14 fatty acid mono-, di-, or tri-ester of glycerol is a C 10 fatty acid mono-, di-, or tri-ester of glycerol.
39. The pharmaceutical composition of claim 38 , wherein the medium chain oil is MIGLYOL 812.
40. The pharmaceutical composition of claim 27 , wherein the medium chain oil is MIGLYOL 812, the non-ionic surfactant is lauroyl polyoxyl-32-glycerides, and wherein the pharmaceutical formulation provides increased progesterone bioavailability compared to a formulation comprising an equivalent amount of micronized progesterone suspended in peanut oil.