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:
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 progesterone are uniformly dispersed;
wherein at least about 90% of the estradiol is solubilized in the solubilizing agent; and
wherein the solubilizing agent comprises an effective amount of a monoglyceride, a diglyceride or a combination thereof containing an ester of a C6-C12 fatty acid.
2. The pharmaceutical composition of claim 1 , further comprising partially solubilized progesterone, wherein the partially solubilized progesterone is solubilized in the solubilizing agent.
3. The pharmaceutical composition of claim 1 , wherein the formulation is formulated as a gelatin capsule.
4. The pharmaceutical composition of claim 1 , wherein said estradiol has a dosage strength of at least about 0.125 mg and wherein said progesterone has a dosage strength of at least about 25 mg.
5. The pharmaceutical composition 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.
6. The pharmaceutical composition of claim 1 , wherein the estradiol does not precipitate for at least 14 days.
7. A 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 progesterone are uniformly dispersed;
wherein at least about 90% of the estradiol is solubilized in the solubilizing agent; and
wherein the solubilizing agent comprises an effective amount of a monoglyceride thereof containing an ester of a C6-C12 fatty acid.
8. The pharmaceutical composition of claim 7 , further comprising partially solubilized progesterone, wherein the partially solubilized progesterone is solubilized in the solubilizing agent.
9. The pharmaceutical composition of claim 7 , wherein the composition is formulated as a gelatin capsule.
10. The pharmaceutical composition of claim 7 , 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.
11. The pharmaceutical composition of claim 7 , 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.
12. The pharmaceutical composition of claim 7 , wherein the estradiol does not precipitate for at least 14 days.
13. A 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 progesterone are uniformly dispersed;
wherein at least about 90% of the estradiol is solubilized in the solubilizing agent; and
wherein the solubilizing agent comprising an effective amount of a diglyceride containing an ester of a C6-C12 fatty acid.
14. The pharmaceutical composition of claim 13 , further comprising partially solubilized progesterone, wherein the partially solubilized progesterone is solubilized in the solubilizing agent.
15. The pharmaceutical composition of claim 13 , wherein the composition is formulated in a gelatin capsule.
16. The pharmaceutical composition of claim 13 , 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.
17. The pharmaceutical composition of claim 13 , 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.
18. The pharmaceutical composition of claim 13 , wherein the estradiol does not precipitate for at least 14 days.