Ulipristal Acetate Tablets

Abstract

The invention relates to a pharmaceutical tablet for oral administration comprising ulipristal acetate together with the following excipients: at least one diluent in an amount of 50 to 98.5 wt %, at least one binding agent in an amount of 0 to 10 wt %, at least one disintegrating agent in an amount of 0.5 to 10 wt %, and at least one lubricant in an amount of 0 to 10 wt %.

1 . An oral pharmaceutical tablet comprising ulipristal acetate in an amount ranging from 1 mg to 50 mg, a diluent, a disintegrating agent, and a lubricant, wherein at least 80% of ulipristal acetate present in the tablet is dissolved within about 20 minutes when said tablet is subjected to an in vitro dissolution assay in a paddle apparatus at 37° C.±0.5° C., and at pH=1. 
     
     
         2 . The tablet of  claim 1 , wherein at least 90% of ulipristal acetate present in the tablet is dissolved within about 20 minutes when the said tablet is subjected to an in vitro dissolution assay in a paddle apparatus at 37° C.±0.5° C., a rotation speed of 50 rpm, and at pH=1. 
     
     
         3 . The tablet of  claim 1 , wherein the disintegrating agent is sodium croscarmellose. 
     
     
         4 . The tablet of  claim 1 , which further comprises a binder. 
     
     
         5 . The tablet of  claim 4 , wherein the binder is a synthetic or natural polymer. 
     
     
         6 . The tablet of  claim 5  wherein the binder is povidone and/or hydroxypropyl methyl cellulose. 
     
     
         7 . The tablet of  claim 1 , wherein the diluent is selected from the group consisting of monosaccharides, disaccharides, calcium phosphate, sodium phosphate, calcium carbonate, sodium carbonate, cellulose, microcrystalline cellulose, combinations and hydrates thereof. 
     
     
         8 . The tablet of  claim 7 , wherein the diluent is selected from the group consisting of mannitol, lactose, microcrystalline cellulose, hydrates thereof and combinations thereof. 
     
     
         9 . The tablet of  claim 1 , wherein the lubricant is selected from the group consisting of steraic acid, talc, magnesium stearate and combinations thereof. 
     
     
         10 . The tablet of  claim 1 , which comprises:
 from 1% to 18% by weight of ulipristal acetate,   from 50% to 98.5% by weight of a diluent,   from 0.5% to 10% by weight of a disintegrating agent, and   from 0% to 10% of a lubricant.   
     
     
         11 . The diluent of  claim 10  wherein the diluent is in an amount of 65 to 92 wt %. 
     
     
         12 . The tablet of  claim 10 , wherein the binding agent is in an amount of 1.5 to 8.5 wt %. 
     
     
         13 . The tablet of  claim 10 , wherein the disintegrating agent is in an amount of 1.5 to 8.5 wt %. 
     
     
         14 . The tablet of  claim 10 , wherein the lubricant is in an amount of 0.5 to 5 wt %. 
     
     
         15 . The tablet of  claim 10 , comprising from 5 to 30 mg of ulipristal acetate. 
     
     
         16 . The tablet of  claim 1 , which is uncoated. 
     
     
         17 . The tablet of  claim 1 , wherein ulipristal acetate is micronized. 
     
     
         18 . A method of manufacturing an oral ulipristal acetate tablet of  claim 1 , the method comprising the step of mixing the ingredients and ulipristal acetate and forming a tablet, preferably by wet granulation or by direct compression.