Steroid hormone compositions in medium chain oils

Abstract

This disclosure provides a novel pharmaceutical composition capable of forming micelles upon exposure to the gastric environment. The pharmaceutical composition is suitable for delivering steroid hormones, and progesterone in particular, to a subject in need thereof.

What is claimed is: 
     
         1 . A pharmaceutical composition for providing enhanced oral bioavailability of progesterone, the pharmaceutical composition comprising:
 progesterone, a polysorbate, and a medium chain oil, wherein
 the medium chain oil comprises at least about 50 weight percent of a predominantly medium chain monoglyceride; and 
 the progesterone is fully solubilized. 
   
     
     
         2 . The pharmaceutical composition of  claim 1 , wherein the medium chain oil comprises at least about 70 weight percent of a predominantly medium chain monoglyceride. 
     
     
         3 . The pharmaceutical composition of  claim 2 , wherein the polysorbate is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 65, and polysorbate 80. 
     
     
         4 . The pharmaceutical composition of  claim 1 , wherein the pharmaceutical composition provides an oral bioavailability of at least about 150 percent as measured by an increase in AUC when compared to a reference product. 
     
     
         5 . The pharmaceutical composition of  claim 1 , further comprising at least one of a polyoxyethylene hydrogenated castor oil, a D-α-Tocopherol polyethylene glycol succinate derivative, or a terpene. 
     
     
         6 . The pharmaceutical composition of  claim 1 , wherein the predominantly medium chain monoglyceride and the progesterone can be present at a weight ratio of about 10:1 to about 15:1. 
     
     
         7 . The pharmaceutical composition of  claim 6 , wherein the predominantly medium chain monoglyceride comprises at least about 90 weight percent of the medium chain oil. 
     
     
         8 . The pharmaceutical composition of  claim 7 , wherein the polysorbate is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 65, and polysorbate 80. 
     
     
         9 . The pharmaceutical composition of  claim 6 , wherein the pharmaceutical composition provides an oral bioavailability of at least about 150 percent as measured by an increase in AUC when compared to a reference product. 
     
     
         10 . The pharmaceutical composition of  claim 6 , further comprising at least one of a polyoxyethylene hydrogenated castor oil, d-α-tocopherol polyethylene glycol succinate derivative, or a terpene. 
     
     
         11 . An oral, fully-solubilized progesterone pharmaceutical composition comprising:
 progesterone and a polysorbate in a weight ratio of from about 1:2 to about 2:1; and   a medium chain oil comprising a mixture of medium chain mono- and diglycerides, the medium chain oil not containing more than about 10 weight percent triglycerides.   
     
     
         12 . The pharmaceutical composition of  claim 11 , wherein the polysorbate is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 65, and polysorbate 80. 
     
     
         13 . The pharmaceutical composition of  claim 11 , wherein the pharmaceutical composition provides an oral bioavailability of at least about 150 percent as measured by an increase in AUC when compared to a reference product. 
     
     
         14 . The pharmaceutical composition of  claim 11 , further comprising at least one of a polyoxyethylene hydrogenated castor oil, a d-α-tocopherol polyethylene glycol succinate derivative, or a terpene. 
     
     
         15 . A pharmaceutical composition for providing enhanced oral bioavailability of progesterone, the pharmaceutical composition comprising:
 progesterone, a polysorbate, and a medium chain oil, wherein
 the medium chain oil comprises at least about 50 weight percent of a first medium chain oil component; and 
 the progesterone is fully solubilized. 
   
     
     
         16 . The pharmaceutical composition of  claim 15 , wherein the medium chain oil further comprises a second medium chain oil component and wherein the first medium chain oil component is a predominantly medium chain monoglyceride and wherein the second medium chain oil component is a predominantly medium chain diglyceride. 
     
     
         17 . The pharmaceutical composition of  claim 16 , wherein the predominantly medium chain diglyceride is a mixed or complex diglyceride.