Natural combination hormone replacement formulations and therapies
View Patent ↗Estrogen and progesterone replacement therapies are provided herein. Among others, the following formulations are provided herein: solubilized estradiol without progesterone; micronized progesterone without estradiol; micronized progesterone with partially solubilized progesterone; solubilized estradiol with micronized progesterone; solubilized estradiol with micronized progesterone in combination with partially solubilized progesterone; and solubilized estradiol with solubilized progesterone.
1. A pharmaceutical composition comprising:
a solubilizing agent, the solubilizing agent comprising an effective amount of a C6-C12 oil;
1.0 mg estradiol or 1.03 mg estradiol hemihydrate, the estradiol or estradiol hemihydrate being at least about 90% solubilized in the solubilizing agent; and
100 mg progesterone;
wherein the estradiol or the estradiol hemihydrate, and the progesterone are uniformly dispersed in the solubilizing agent.
2. The pharmaceutical composition of claim 1 , wherein the solubilizing agent is selected from at least one of monoglycerides, diglycerides, triglycerides, and combinations thereof, wherein the monoglycerides, diglycerides, and triglycerides are predominantly of C6-C12 fatty acid chain lengths.
3. The pharmaceutical composition of claim 2 , wherein the monoglycerides, diglycerides, and triglycerides are >50% C6-C12 fatty acid chain lengths.
4. A pharmaceutical composition comprising:
about 100 mg progesterone;
about 1.0 mg estradiol or 1.03 mg estradiol hemihydrate, the estradiol or estradiol hemihydrate being at least about 90% solubilized;
about 195.97 mg of monoglycerides and diglycerides of caprylic acid and capric acid (CAPMUL MCM); and
about 3.0 mg of at least one of lauroyl macrogol-32 glycerides EP, lauroyl polyoxyl-32 glycerides NF, or lauroyl polyoxylglycerides (GELUCIRE 44/14);
wherein the estradiol or the estradiol hemihydrate, and the progesterone are uniformly dispersed in the solubilizing agent.
5. A method of treating a menopause-related symptom in a woman comprising administering an effective amount of pharmaceutical composition to a subject in need thereof, the pharmaceutical composition comprising:
about 100 mg progesterone;
about 1.0 mg estradiol or 1.03 mg estradiol hemihydrate, the estradiol or estradiol hemihydrate being at least about 90% solubilized;
about 195.97 mg of monoglycerides and diglycerides of caprylic acid and capric acid (CAPMUL MCM); and
about 3.0 mg of at least one of lauroyl macrogol-32 glycerides EP, lauroyl polyoxyl-32 glycerides NF, or lauroyl polyoxylglycerides (GELUCIRE 44/14);
wherein the estradiol or the estradiol hemihydrate, and the progesterone are uniformly dispersed in the solubilizing agent.
6. The method of claim 5 , wherein the pharmaceutical composition is administered as a continuous-combined therapy regimen.
7. The method of claim 5 , wherein the pharmaceutical composition is administered a sequentially-combined therapy regimen.
8. A method of treating a vasomotor symptom in a woman comprising administering an effective amount of a pharmaceutical composition comprising:
1.0 mg estradiol or 1.03 mg estradiol hemihydrate, the estradiol or estradiol hemihydrate being at least about 90% solubilized in the solubilizing agent;
100 mg progesterone; and
a solubilizing agent, the solubilizing agent comprising an effective amount of a C6-C12 oil;
wherein the estradiol or the estradiol hemihydrate, and the progesterone are uniformly dispersed in the solubilizing agent; and
wherein the pharmaceutical composition is administered once daily for the treatment of symptoms associated with menopause.
9. The method of claim 8 , wherein the pharmaceutical composition is administered as a continuous-combined therapy regimen.
10. The method of claim 8 , wherein the pharmaceutical composition is administered as a sequentially-combined therapy regimen.
11. The method of claim 8 , wherein the solubilizing agent is selected from at least one of monoglycerides, diglycerides, triglycerides, and combinations thereof, wherein the monoglycerides, diglycerides, and triglycerides are predominantly of C6-C12 fatty acid chain lengths.
12. The method of claim 11 , wherein the monoglycerides, diglycerides, and triglycerides are >50% C6-C12 fatty acid chain lengths.