Drug formulations having improved pharmacokinetic properties

Abstract

The present application relates to novel drug formulations of vardenafil which dissolve rapidly in the mouth and lead to increased bioavailability and to a plateau-like plasma concentration profile, and to processes for their preparation.

1 . Drug formulation which disintegrates rapidly in the mouth and comprises vardenafil, characterized in that at least 80% of the vardenafil dose in the substance form employed dissolves at 25° C. in 10 ml of physiological saline and, the rate of release from the drug formulation in 900 ml of physiological saline within the first 5 minutes in the USP pedal stirrer apparatus at 50 rotations per minute at 37° C. is at least 70%. 
     
     
         2 . Drug formulation according to  claim 1 , comprising vardenafil in the form of a salt with an acid or vardenafil with an acid. 
     
     
         3 . Drug formulation according to  claim 2 , comprising vardenafil hydrochloride or vardenafil hydrochloride trihydrate. 
     
     
         4 . Drug formulation according to  claim 3 , comprising vardenafil hydrochloride or vardenafil hydrochloride trihydrate in micronized form with a mean particle size of less than 20 pm. 
     
     
         5 . Drug formulation according to  claim 1 , comprising from 40% to 99% of sugar alcohols. 
     
     
         6 . Drug formulation according to  claim 1  in a drug packaging with a note on the information leaflet, label or packaging box that the drug formulation is to be inserted into the oral cavity and, after its disintegration, to be swallowed.