Author/Authors :
Jukka Lepp?nen، نويسنده , , Juhani Huuskonen، نويسنده , , Jouko Savolainen، نويسنده , , Tapio Nevalainen، نويسنده , , Hannu Taipale، نويسنده , , Jouko Veps?l?inen، نويسنده , , Jukka Gynther، نويسنده , , Tomi J?rvinen، نويسنده ,
Abstract :
Entacapone was reacted with phosphorous oxychloride in dry pyridine to yield a phosphate ester. The phosphate promoiety increased aqueous solubility of the parent drug by more than 1700- and 20-fold at pH 1.2 and 7.4, respectively. The phosphate ester provides adequate stability (t1/2=2227 h; pH 7.4) towards chemical hydrolysis, and allowed for release of the parent drug via enzymatic hydrolysis in liver homogenate.
