Pharmaceutical formulation containing tadalafil

Abstract

Disclosed herein are pharmaceutical compositions comprising Tadalafil, or a salt, or derivatives thereof and pharmaceutical excipients, processes for the preparation thereof, and pharmaceutical compositions containing them. The pharmaceutical compositions have improved physicochemical properties that provide faster onset of action for the treatment of erectile dysfunction.

1 .- 25 . (canceled) 
     
     
         26 . A method of treating erectile dysfunction, benign prostatic hyperplasia, pulmonary arterial hypertension or Duchenne muscular dystrophy in a subject in need thereof, comprising administering to the subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising
 10-40% by weight of tadalafil or a salt thereof;   35-70% by weight of a primary pharmaceutical excipient which is copovidone (copolymer of vinylpyrrolidone and vinyl acetate); and   5-50% by weight of a secondary pharmaceutical excipient which is sodium lauryl sulfate;   wherein said pharmaceutical composition is obtained by a process comprising mixing followed by spray-drying;   wherein said pharmaceutical composition has a controlled particle size in the range between 10 nm and 500 nm; and   wherein said pharmaceutical composition shows X-ray amorphous character in the solid form.   
     
     
         27 . The method as recited in  claim 26 , wherein said pharmaceutical composition is characterized by said Raman spectrum as shown in  FIG. 7 . 
     
     
         28 . The method as recited in  claim 26 , wherein said particle size is between 10 nm and 200 nm. 
     
     
         29 . The method as recited in  claim 26 , wherein said pharmaceutical composition shows a t max  of 0.5-0.75 hours. 
     
     
         30 . The method as recited in  claim 26 , wherein said pharmaceutical composition has a dissolution profile such that about 60% of the pharmaceutical composition is dissolved in simulated gastric fluid over two hours. 
     
     
         31 . The method as recited in  claim 26 , wherein said pharmaceutical composition is suitable for oral administration. 
     
     
         32 . The method as recited in  claim 26 , wherein said pharmaceutical composition is suitable for the preparation of liquid dispersible granules, sachets, liquid dispersible tablets, orodispersible tablets, orally dissolving tablets, chewing tablets and immediate release (IR) tablets. 
     
     
         33 . The method as recited in  claim 32 , wherein the pharmaceutical composition disperses within 10 minutes in liquid or biorelevant media or gastric acid. 
     
     
         34 . The method as recited in  claim 33 , wherein said dispersion time is between 0.1 min and 5 min. 
     
     
         35 . The method as recited in  claim 26 , wherein the pharmaceutical composition has an apparent solubility in water of at least 0.7 mg/mL. 
     
     
         36 . The method as recited in  claim 26 , wherein the pharmaceutical composition has a PAMPA permeability of at least 4×10 −6  cm/s when dispersed in water, FaSSIF or FeSSIF biorelevant media, which does not decrease in time at least for 6 months.