Progesterone containing oral dosage forms and kits

Abstract

The present invention provides for progesterone containing pharmaceutical oral dosage forms, pharmaceutical kits, and related methods. In one embodiment, an oral dosage form formulated for on-going administration is provided. The oral dosage form includes an amount of progesterone and a pharmaceutically acceptable carrier. The oral dosage form is formulated such that upon single dose administration to a non-pregnant woman in follicular phase, the oral dosage form provides a serum progesterone C 24h of at least 0.20 ng/mL.

What is claimed is: 
     
         1 . An oral dosage form, for ongoing administration comprising:
 an amount of progesterone; and   a pharmaceutically acceptable carrier;   wherein upon single dose administration to a non-pregnant woman in follicular phase the oral dosage form provides a serum progesterone C 24h  of at least 0.20 ng/mL.   
     
     
         2 . The oral dosage form of  claim 1 , wherein upon single dose administration to a subject the oral dosage form provides a serum total pregnane C max  of no greater than 40 ng/mL. 
     
     
         3 . The oral dosage form of  claim 1 , wherein upon single dose administration to a subject the oral dosage form provides a serum progesterone C max  of no greater than 10 ng/mL. 
     
     
         4 . The oral dosage form of  claim 1 , wherein upon single dose administration to a subject the oral dosage form provides a serum progesterone C 24h  of 1.5 ng/mL or less. 
     
     
         5 . The oral dosage form of  claim 1 , wherein the oral dosage form has an in vitro release rate such that, when measured using a USP Type-1 dissolution apparatus in 900 mL of de-ionized water with 2.0% (w/v) of sodium lauryl sulfate at 100 rpm, about 10 wt % or less of the progesterone in the oral dosage form is released in the first 60 minutes and at least 70 wt % of the progesterone is released from the oral dosage form within 12 hours. 
     
     
         6 . The oral dosage form of  claim 1 , wherein the progesterone is present in the oral dosage form in an amount of about 200 mg to about 600 mg. 
     
     
         7 . The oral dosage form of  claim 1 , wherein the progesterone is present in the oral dosage form in an amount of about 400 mg. 
     
     
         8 . The oral dosage form of  claim 1 , wherein the progesterone comprises about 15 wt % to about 45 wt % of the oral dosage form. 
     
     
         9 . The oral dosage form of  claim 1 , wherein upon single dose administration to a subject the oral dosage form provides a serum progesterone AUC 12-24h  (ng*h/mL) to administered progesterone dose (mg) ratio of at least 0.005 (ng*h/ml)/mg. 
     
     
         10 . The oral dosage form of  claim 1 , wherein upon single dose administration to a subject the oral dosage form provides a ratio of administered progesterone dose (mg) to serum progesterone C 24h  (ng/mL) of about 100 mg/(ng/mL) to about 1000 mg/(ng/mL). 
     
     
         11 . The oral dosage form of  claim 1 , wherein the oral dosage form further includes a pharmaceutical hydrophilic release rate modulator present in an amount of from about 20 wt % to about 80 wt % of the dosage form. 
     
     
         12 . The oral dosage form of  claim 1 , wherein the oral dosage form further includes a lipophilic release modulator present in an amount of about 8 wt % to about 50 wt % of the oral dosage form. 
     
     
         13 . The oral dosage form of  claim 12 , wherein the lipophilic release modulator is non-lipidic release modulator and is present in an amount of about 8 wt % to about 35 wt % of the oral dosage form. 
     
     
         14 . The oral dosage form of  claim 12 , wherein the lipophilic release modulator is a lipidic release modulator present in the amount of about 10 wt % to about 50 wt % of the oral dosage form. 
     
     
         15 . The oral dosage form of  claim 1 , wherein the oral dosage form further includes hydrophilic release modulator in an amount of about 10 wt % to about 65 wt % and a lipophilic release modulator present in the amount of about 5 wt % to about 30 wt % of the oral dosage form. 
     
     
         16 . The oral dosage form of  claim 1 , wherein the oral dosage form is formulated for administration to a subject to provide contraception. 
     
     
         17 . The oral dose form of  claim 1 , wherein the amount of the pharmaceutical acceptable carrier comprises from about 55 wt % to about 85 wt % of the oral dosage form. 
     
     
         18 . The oral dosage form of  claim 1 , further comprising an estrogenic agent. 
     
     
         19 . The oral dosage form of  claim 18 , wherein the estrogenic agent is selected from the group consisting of estradiol, conjugated estradiol, conjugated equine estrogens, and esterified estradiol. 
     
     
         20 . The oral dosage form of  claim 18 , wherein the estrogenic agent is estradiol and is present in the oral dosage form in an amount of about 0.5 mg to about 2.5 mg.