2010 Volume 25 Issue 4 Pages 384-391
It is known that a gradual increase in pH is observed on passing through the small intestine. We designed enteric-coated dosage forms that start to disintegrate when they reach the middle-to-lower region of the small intestine, with the aim of circumventing food-drug interactions that reduce the bioavailability of drugs taken after a meal(negative food effects). The low absorption of a drug with the negative food effect in fed dogs was improved when the drug was administered orally as dosage forms enteric-coated with hypromellose acetate succinate(HPMCAS)that dissolves at pH above 7, which corresponds to pH at the ileum. Data indicated that food-drug interactions were avoided by separating the main absorption site of drugs from that of food components.