The present invention provides a pharmaceuticalpreparation that can improve absorption of a pharmaceuticalcompound in the gastrointestinal tract and that provides, throughoral administration or like method, a blood concentration fromwhich sufficient remedial effects can be expected, and a methodfor producing such a preparation. The invention is directed to apharmaceutical preparation exhibiting excellent gastrointestinalabsorbability comprising a compound recognized by a proton-coupledtransporter and a pH-sensitive polymer in an amountsufficient for the gastrointestinal tract to acquire a pH atwhich the proton-coupled transporter optimally absorbs thecompound into a cell.