Claims for Patent: 11,033,626

Summary for Patent: 11,033,626

Title:	Progesterone formulations having a desirable pk profile
Abstract:	This disclosure provides progesterone formulations, methods of using these formulations, and their related pharmacokinetic parameters. In particular embodiments, the formulations disclosed herein allow for a reduction in the amount of progesterone administered to a patient in need thereof, while still providing the benefits of a larger dosage amount.
Inventor(s):	Cacace; Janice (St. Petersburg, FL), Persicaner; Peter H. R. (Boca Raton, FL), Thorsteinsson; Thorsteinn (West Palm Beach, FL), Sancilio; Frederick (Palm Beach Gardens, FL), Amadio; Julia (Boca Raton, FL), Bernick; Brian (Boca Raton, FL), Irani; Neda (Palm Beach Gardens, FL)
Assignee:	TherapeuticsMD, Inc. (Boca Raton, FL)
Application Number:	16/578,148
Patent Claims:	1. A pharmaceutical composition for orally administering progesterone to a subject in need thereof, the composition comprising: progesterone; a solubilizing agent; and lauroyl polyoxyl-32 glycerides; wherein the solubilizing agent comprises predominantly caprylic fatty acid (C8) and capric fatty acid (C10) tri-esters of glycerol; and 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 solubilizing agent further comprises a C.sub.6-C.sub.12 fatty acid mono-ester of glycerol. 3. The pharmaceutical composition of claim 2, wherein the solubilizing agent further comprises a C.sub.6-C.sub.12 fatty acid di-ester of glycerol. 4. The pharmaceutical composition of claim 1, wherein the amount of progesterone is from 25 mg to 200 mg. 5. The pharmaceutical composition of claim 1, wherein the amount of progesterone is 75 mg or 150 mg. 6. The pharmaceutical composition of claim 1, wherein the progesterone includes solubilized progesterone and suspended progesterone. 7. The pharmaceutical composition of claim 1, wherein the composition is provided in a gelatin capsule. 8. The pharmaceutical composition of claim 1, wherein the composition has a total mass of less than 500 mg. 9. The pharmaceutical composition of claim 1, wherein the amount of progesterone comprises about 33% by weight of the composition; the solubilizing agent comprises about 65% by weight of the composition, the non-ionic surfactant comprises about 1.7% by weight of the composition. 10. The pharmaceutical composition of claim 1, wherein the amount of progesterone comprises about 33.33% by weight of the composition; the solubilizing agent comprises about 64.93% by weight of the composition, the non-ionic surfactant comprises about 1.67% by weight of the composition. 11. The pharmaceutical composition of claim 9, further comprising an antioxidant. 12. The pharmaceutical composition of claim 11, wherein the antioxidant is butylated hydroxyl toluene. 13. The pharmaceutical composition of claim 12, wherein the amount of progesterone is 200 mg. 14. The pharmaceutical composition of claim 12, wherein the amount of progesterone is 150 mg. 15. The pharmaceutical composition of claim 12, wherein the progesterone is ultra-micronized and has an X50 of less than or equal to 15 microns. 16. The pharmaceutical composition of claim 1, wherein the progesterone is ultra-micronized and has an X90 of less than or equal to 25 microns. 17. The pharmaceutical composition of claim 1, wherein the progesterone is the sole active ingredient in the composition. 18. A pharmaceutical composition for orally administering progesterone to a subject in need thereof, the composition comprising: progesterone; a solubilizing agent; and lauroyl polyoxyl-32 glycerides; wherein the solubilizing agent comprises predominantly caprylic fatty acid (C8) and capric fatty acid (C10) tri-esters of glycerol; and wherein the progesterone is present from about 20 to about 50 weight percent of the composition and wherein less than 6 percent of the progesterone is soluble in the solubilizing agent. 19. The pharmaceutical composition of claim 18, wherein more than 5 percent of the progesterone is soluble in the solubilizing agent. 20. A method of treating a progesterone-deficient state in a subject in need thereof, the method comprising administering to a subject in need thereof an effective amount of the pharmaceutical composition of claim 1. 21. The method of claim 20, wherein the progesterone-deficient state is endometrial hyperplasia, secondary amenorrhea, preterm birth, shortened cervix, or another disease states or condition treated with supplemental progesterone. 22. The method of claim 21, wherein the progesterone-deficient state is secondary amenorrhea. 23. A method of treating a progesterone-deficient state in a subject in need thereof, the method comprising administering to a subject in need thereof an effective amount of the pharmaceutical composition of claim 18. 24. The method of claim 23, wherein the progesterone-deficient state is endometrial hyperplasia, secondary amenorrhea, preterm birth, shortened cervix, or another disease states or condition treated with supplemental progesterone. 25. The method of claim 24, wherein the progesterone-deficient state is secondary amenorrhea.