Gastrointestinal Absorption Enhancer Mediated By Proton-Coupled Transporter and Its Preparing Method

Abstract

The present invention provides a pharmaceutical preparation that can improve absorption of a pharmaceutical compound in the gastrointestinal tract and that provides, through oral administration or like method, a blood concentration from which sufficient remedial effects can be expected, and a method for producing such a preparation. The invention is directed to a pharmaceutical preparation exhibiting excellent gastrointestinal absorbability comprising a compound recognized by a proton-coupled transporter and a pH-sensitive polymer in an amount sufficient for the gastrointestinal tract to acquire a pH at which the proton-coupled transporter optimally absorbs the compound into a cell.

1 . A method for formulating a pharmaceutical preparation having excellent gastrointestinal absorbability comprising the steps of:
 (1) determining a pH at which the proton-coupled transporter optimally transports a compound recognized by the proton-coupled transporter into a cell is; and   (2) adding to the compound a pH-sensitive polymer in an amount sufficient to impart the optimum pH for cellular uptake of the compound.   
     
     
         2 . A pharmaceutical preparation formulated according to the method of  claim 1 . 
     
     
         3 . A method for enhancing gastrointestinal absorbability of a compound recognized by a proton-coupled transporter,
 the method comprising conditioning the gastrointestinal tract to a pH at which the proton-coupled transporter optimally transports the compound into a cell.   
     
     
         4 . A method for using a pH-sensitive polymer, to enhance gastrointestinal absorbability of a compound recognized by a proton-coupled transporter, in an amount sufficient to impart to the gastrointestinal tract a pH at which the proton coupled transporter optimally transports the compound into a cell.