Pharmaceutical composition for the sublingual administration of progesterone, and method for its preparation

Abstract

A pharmaceutical composition is described for the sublingual administration of progesterone in the form of a rapidly-disintegrating tablet, which is capable of promoting a greater bioavailability of the progesterone; a method for preparing said pharmaceutical composition is also described.

1 - 23 . (canceled) 
     
     
         24 . A method to significantly increase the sublingual bioavailability of a progesterone fast disintegrating tablet without significantly modifying the tablet disintegration time, characterized by including in said tablet: (a) progesterone combined with a cyclodextrin, and (b) citric acid and sodium bicarbonate, each present in an amount between 5 and 20% of the total weight of the tablet composition. 
     
     
         25 . The method according to  claim 24 , characterized in that said tablet comprises citric acid amounting to 10% w/w of the total weight of the composition. 
     
     
         26 . The method according to  claim 24 , characterized in that said tablet comprises bicarbonate amounting to 12% w/w of the total weight of the composition. 
     
     
         27 . The method according to  claim 24 , characterized in that said cyclodextrin is chosen from either β-cyclodextrin or 2-hydroxypropyl-β-cyclodextrin. 
     
     
         28 . The method according to  claim 24 , characterized in that the molar ratio of said progesterone to said cyclodextrin is between 1 and 2. 
     
     
         29 . The method according to  claim 24 , characterized in that the content of cyclodextrin is between 27 and 40% w/w of the total weight of the composition. 
     
     
         30 . The method according to  claim 24 , characterized in that when placed under the tongue, said tablet disintegrates completely within a time approximately between 60 and 120 seconds. 
     
     
         31 . A method to significantly increase the sublingual bioavailability of a progesterone fast disintegrating tablet without significantly modifying the tablet hardness, characterized by including in said tablet: (a) progesterone combined with a cyclodextrin, and (b) citric acid and sodium bicarbonate, each present in an amount between 5 and 20% of the total weight of the tablet composition. 
     
     
         32 . The method according to  claim 31 , characterized in that said tablet comprises citric acid amounting to 10% w/w of the total weight of the composition. 
     
     
         33 . The method according to  claim 31 , characterized in that said tablet comprises bicarbonate amounting to 12% w/w of the total weight of the composition. 
     
     
         34 . The method according to  claim 31 , characterized in that said cyclodextrin is chosen from either β-cyclodextrin or 2-hydroxypropyl-β-cyclodextrin. 
     
     
         35 . The method according to  claim 31 , characterized in that the molar ratio of said progesterone to said cyclodextrin is between 1 and 2. 
     
     
         36 . The method according to  claim 31 , characterized in that the content of cyclodextrin is between 27 and 40% w/w of the total weight of the composition. 
     
     
         37 . The method according to  claim 31 , characterized in that when placed under the tongue, said tablet disintegrates completely within a time approximately between 60 and 120 seconds.