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 method of treating a menopause-related symptom in a woman comprising:
administering to the woman an effective amount of a pharmaceutical composition, the pharmaceutical composition comprising solubilized estradiol, suspended progesterone, and a solubilizing agent;
wherein each of the estradiol and the suspended progesterone are present in the solubilizing agent and the estradiol and the suspended progesterone are uniformly dispersed;
wherein the solubilizing agent contains an effective amount of C6-C12 oil; and
wherein at least about 90% of the estradiol is solubilized in the solubilizing agent.
2. The method of claim 1 , further comprising partially solubilized progesterone, the partially solubilized progesterone being solubilized in the solubilizing agent.
3. The method of claim 1 , wherein the composition is formulated as a gelatin capsule.
4. The method of claim 1 , wherein the C6-C12 oil is selected from at least one of mono-, di-, and triglycerides and combinations thereof.
5. The method of claim 1 , wherein the estradiol has a dosage strength of at least about 0.125 mg and wherein the progesterone has a dosage strength of at least about 25 mg.
6. The method of claim 1 , wherein the ratio of progesterone to estradiol is about 24:1, about 25:1, about 96:1, about 100:1, about 192:1, or about 200:1.
7. The method of claim 1 , wherein the composition is bioequivalent to a 200 mg progesterone soft gel capsule and to a 2 mg estradiol tablet.
8. A method of treating a menopause symptom in a woman comprising administering a pharmaceutical composition to the woman, the pharmaceutical composition comprising:
solubilized estradiol;
suspended progesterone; and
a solubilizing agent, the solubilizing agent containing an effective amount of a C6-C12 oil;
wherein the estradiol and the suspended progesterone are present in the solubilizing agent, the estradiol and the suspended progesterone are uniformly dispersed and at least about 90% of the estradiol is solubilized in the solubilizing agent; and
wherein the estradiol does not precipitate for at least 14 days.
9. The method of claim 8 , further comprising partially solubilized progesterone, the partially solubilized progesterone being solubilized in the solubilizing agent.
10. The method of claim 8 , wherein the composition is formulated as a gelatin capsule.
11. The method of claim 8 , wherein the C6-C12 oil is selected from at least one of mono-, di-, and triglycerides and combinations thereof.
12. The method of claim 8 , wherein the estradiol has a dosage strength of at least about 0.125 mg and wherein the progesterone has a dosage strength of at least about 25 mg.
13. The method of claim 8 , wherein the ratio of progesterone to estradiol is about 24:1, about 25:1, about 96:1, about 100:1, about 192:1, or about 200:1.
14. The method of claim 8 , wherein the composition is bioequivalent to a 200 mg progesterone soft gel capsule and to a 2 mg estradiol tablet.
15. A method of treating a menopause symptom comprising:
administering an effective amount of a pharmaceutical composition to a woman, the pharmaceutical composition comprising solubilized estradiol, suspended progesterone, and a solubilizing agent, the estradiol being stable in the solubilizing agent for at least 14 days;
wherein each of the estradiol and the suspended progesterone are present in the solubilizing agent and the estradiol and the suspended progesterone are uniformly dispersed;
wherein at least about 90% of the estradiol is solubilized in the solubilizing agnent, and wherein the solubilizing agent contains an effective amount of a C6-C12 oil.
16. The method of claim 15 , further comprising partially solubilized progesterone, the partially solubilized progesterone being solubilized in the solubilizing agent.
17. The method of claim 15 , wherein the composition is formulated as a gelatin capsule.
18. The method of claim 15 , wherein the C6-C12 oil is selected from at least one of mono-, di-, and triglycerides and combinations thereof.
19. The method of claim 15 , wherein the estradiol has a dosage strength of at least about 0.125 mg and wherein the progesterone has a dosage strength of at least about 25 mg.
20. The method of claim 15 , wherein the ratio of progesterone to estradiol is about 24:1, about 25:1, about 96:1, about 100:1, about 192:1, or about 200:1.