Progesterone formulations having a desirable PK profile
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.
1. A pharmaceutical composition for orally administering progesterone to a subject in need thereof, the composition comprising:
progesterone;
a solubilizing agent; and
a nonionic surfactant;
wherein the solubilizing agent comprises predominantly C 6 -C 12 fatty acid tri-esters of glycerol;
wherein the progesterone is present from about 20 to about 50 weight percent of the composition; and
wherein the nonionic surfactant is lauroyl polyoxyl-32 glycerides.
2. The pharmaceutical composition of claim 1 , wherein the solubilizing agent further comprises a C 6 -C 12 fatty acid mono-ester of glycerol.
3. The pharmaceutical composition of claim 2 , wherein the solubilizing agent further comprises a C 6 -C 12 fatty acid di-ester of glycerol.
4. The pharmaceutical composition of claim 1 , wherein the tri-ester of glycerol comprises predominantly esters of caprylic fatty acid (C 8 ) and capric fatty acid (C 10 ).
5. The pharmaceutical composition of claim 1 , wherein the amount of progesterone is from 25 mg to 200 mg.
6. The pharmaceutical composition of claim 1 , wherein the amount of progesterone is 75 mg or 150 mg.
7. The pharmaceutical composition of claim 1 , wherein the progesterone includes solubilized progesterone and suspended progesterone.
8. The pharmaceutical composition of claim 1 , wherein the composition is provided in a gelatin capsule.
9. The pharmaceutical composition of claim 1 , wherein the composition has a total mass of less than 500 mg.
10. 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, and the non-ionic surfactant comprises about 1.7% by weight of the composition.
11. 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, and the non-ionic surfactant comprises about 1.67% by weight of the composition.
12. The pharmaceutical composition of claim 10 , further comprising an antioxidant.
13. The pharmaceutical composition of claim 12 , wherein the antioxidant is butylated hydroxy toluene.
14. The pharmaceutical composition of claim 13 , wherein the solubilizing agent is medium chain triglycerides of caprylic fatty acid (C8) and capric fatty acid (C10).