US2023218636A1PendingUtilityA1

Natural Combination Hormone Replacement Formulations and Therapies

87
Assignee: THERAPEUTICSMD INCPriority: Jun 18, 2012Filed: Nov 7, 2022Published: Jul 13, 2023
Est. expiryJun 18, 2032(~5.9 yrs left)· nominal 20-yr term from priority
Inventors:Brian A. BernickJanice Louise CacacePeter H. R. PersicanerNeda IraniJulia M. AmadioFrederick D. Sancilio
A61K 31/57A61K 31/565A61K 9/4858A61K 47/10A61K 47/14A61K 9/1075A61K 9/48A61P 15/00A61P 15/12A61P 43/00A61P 5/24A61K 9/0034A61K 9/02A61K 9/4866A61K 47/44A61K 9/2013A61K 2300/00
87
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Claims

Abstract

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.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         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 distributed 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 distributed in the solubilizing agent.   
     
     
         5 . A method of treating a menopause-related symptom in a woman in need thereof, the method comprising administering an effective amount of a pharmaceutical composition to the woman, 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 distributed 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 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 55 to about 75 weight percent of monoglycerides and diglycerides of caprylic acid and capric acid (CAPMUL MCM); and   about 0.5 to about 10 weight percent 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 distributed in the solubilizing agent.   
     
     
         9 . The pharmaceutical composition according to  claim 8 , wherein the monoglycerides and diglycerides of caprylic acid and capric acid (CAPMUL MCM) are present at about 65 weight percent. 
     
     
         10 . The pharmaceutical composition according to  claim 8 , wherein the lauroyl macrogol-32 glycerides EP, lauroyl polyoxyl-32 glycerides NF, or lauroyl polyoxylglycerides (GELUCIRE 44/14) is present at about 1 weight percent. 
     
     
         11 . A method of treating a menopause-related symptom in a woman in need thereof, the method comprising administering an effective amount of a pharmaceutical composition to the woman, 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 55 to about 75 weight percent of monoglycerides and diglycerides of caprylic acid and capric acid (CAPMUL MCM); and   about 0.5 to about 10 weight percent 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 distributed in the solubilizing agent. 
     
     
         12 . The method of  claim 11 , wherein the pharmaceutical composition is administered as a continuous-combined therapy regimen. 
     
     
         13 . The method of  claim 11 , wherein the pharmaceutical composition is administered a sequentially-combined therapy regimen. 
     
     
         14 . The method of  claim 11 , wherein the monoglycerides and diglycerides of caprylic acid and capric acid (CAPMUL MCM) are present at about 65 weight percent. 
     
     
         15 . The method of  claim 11 , wherein the lauroyl macrogol-32 glycerides EP, lauroyl polyoxyl-32 glycerides NF, or lauroyl polyoxylglycerides (GELUCIRE 44/14) is present at about 1 weight percent. 
     
     
         16 . 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 55 to about 75 weight percent of monoglycerides and diglycerides of caprylic acid and capric acid (CAPMUL MCM); and   about 0.5 to about 10 weight percent of a surfactant;   wherein the estradiol or the estradiol hemihydrate, and the progesterone are uniformly distributed in the solubilizing agent.   
     
     
         17 . The pharmaceutical composition according to  claim 16 , wherein the monoglycerides and diglycerides of caprylic acid and capric acid (CAPMUL MCM) are present at about 65 weight percent. 
     
     
         18 . The pharmaceutical composition according to  claim 16 , wherein surfactant comprises fatty acid mono- and di-esters of polyethylene glycol. 
     
     
         19 . The pharmaceutical composition according to  claim 18 , wherein the fatty acid mono- and di-esters of polyethylene glycol are present at about 1 weight percent of the pharmaceutical composition. 
     
     
         20 . A method of treating a menopause-related symptom in a woman in need thereof, the method comprising administering an effective amount of a pharmaceutical composition to the woman, 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 55 to about 75 weight percent of monoglycerides and diglycerides of caprylic acid and capric acid (CAPMUL MCM); and   about 0.5 to about 10 weight percent of fatty acid mono- and di-esters of polyethylene glycol; 
 wherein the estradiol or the estradiol hemihydrate, and the progesterone are uniformly distributed in the solubilizing agent. 
     
     
         21 . The method of  claim 20 , wherein the pharmaceutical composition is administered as a continuous-combined therapy regimen. 
     
     
         22 . The method of  claim 20 , wherein the pharmaceutical composition is administered a sequentially-combined therapy regimen. 
     
     
         23 . The method of  claim 20 , wherein the monoglycerides and diglycerides of caprylic acid and capric acid (CAPMUL MCM) are present at about 65 weight percent. 
     
     
         24 . The method of  claim 20 , wherein the fatty acid mono- and di-esters of polyethylene glycol are present at about 1 weight percent.

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