Co-micronisation product comprising ulipristal acetate

Abstract

The subject of the present invention is a co-micronization product comprising an active ingredient selected from the group consisting of ulipristal acetate, a ulipristal acetate metabolite and mixtures thereof, and a pharmaceutically acceptable solid surfactant. The invention also relates to a pharmaceutical composition comprising said co-micronization product and to the therapeutic uses thereof.

1 . A co-micronization product comprising:
 an active ingredient selected from the group consisting of ulipristal acetate, a metabolite of ulipristal acetate and mixtures thereof, and   a pharmaceutically acceptable solid surfactant.   
     
     
         2 . The co-micronization product of  claim 1 , wherein the weight ratio of the active ingredient to the surfactant ranges from 0.1 to 10. 
     
     
         3 . The co-micronization product of  claim 1 , wherein the surfactant is selected from C 8 -C 20  alkyl sulphate salts and mixtures thereof. 
     
     
         4 . The co-micronization product of  claim 1 , wherein the active ingredient is selected from the group consisting of ulipristal acetate, 17α-acetoxy-11β-(4-N-methylaminophenyl)-19-norpregna-4,9-diene-3,20-dione, 17α-acetoxy-11β-(4-aminophenyl)-19-norpregna-4,9-diene-3,20-dione and mixtures thereof. 
     
     
         5 . The co-micronization product of  claim 1 , wherein:
 the surfactant is sodium dodecyl sulphate, and   the active ingredient is ulipristal acetate.   
     
     
         6 . The co-micronization product of  claim 1 , having
 a d50 of less than 20 μm, and/or   a d90 of less than 50 μm.   
     
     
         7 . A method for preparing the co-micronization product of  claim 1 , comprising the steps of:
 a) providing an active ingredient selected from the group consisting of ulipristal acetate, a ulipristal acetate metabolite and mixtures thereof,   b) mixing the active ingredient of step a) with the surfactant to form a mixture, and   c) co-micronizing the mixture obtained in step b).   
     
     
         8 . The method for preparing a co-micronization product of  claim 7 , wherein in step a), the active ingredient is provided in a non-micronized form or a micronized form. 
     
     
         9 . A pharmaceutical composition comprising the co-micronization product of  claim 1  and a pharmaceutically acceptable excipient. 
     
     
         10 . The pharmaceutical composition of  claim 9 , wherein the pharmaceutically acceptable excipient is selected from the group consisting of a diluent, a binder, a flow agent, a lubricant, a disintegrant and mixtures thereof. 
     
     
         11 . The pharmaceutical composition of  claim 9 , comprising:
 from 0.5% to 80% of co-micronization product,   from 0% to 10% of disintegrant,   from 15% to 95% of diluent, and   from 0% to 5% of lubricant,   
       the percentages being expressed by weight relative to the total weight of the composition. 
     
     
         12 . The pharmaceutical composition of  claim 9 , which comprises from 1 mg to 100 mg of active ingredient per dose unit. 
     
     
         13 . The pharmaceutical composition of  claim 9 , suitable for oral administration. 
     
     
         14 . The pharmaceutical composition of  claim 9 , in the form of a powder, a granule, a coated tablet, uncoated tablet, or a capsule. 
     
     
         15 . A method for providing contraception to a subject comprising administering to said subject the co-micronization product of  claim 1  or a pharmaceutical composition thereof. 
     
     
         16 . A method for treating or preventing a gynaecological disorder in a subject comprising administering to said subject the co-micronization product of  claim 1  or a pharmaceutical composition thereof.