Anti-first-pass effect compounds

Abstract

Safe, effective first-pass inhibiting compounds and citrus-derived substances are provided. Formulations containing the compounds are also provided as are methods for their preparation and for inhibiting the first pass effect

We claim:  
     
         1 . A method of inhibiting the first-pass effect of a material taken orally by a patient which is subject to the first-pass effect, comprising the step of co-administering to said patient said material and a compound comprising one of the following cores:  
       
         
           
           
               
               
           
         
       
     
     
         2 . In a method of designing an inhibitor of an enzyme or polypeptide, the improvement comprising providing, as a compound to be altered, a compound comprising one of the following cores:  
       
         
           
           
               
               
           
         
       
     
     
         3 . A method for preparing a grapefruit juice-derived solids preparation comprising: 
 a) passing grapefruit juice through an initial filter having a filter size equal or greater than 200 μm to produce an initial filtrate;    passing the initial filtrate through a filter having a filter size of from 25-75 μm and thereby trapping said grapefruit juice-derived solids preparation on said 25-75 μm filter; or    b) centrifuging grapefruit juice at about 1000 G for about 10 minutes to produce a supernatant and a pellet, optionally suspending said pellet in water and re-centrifuging to produce a washed pellet,    wherein said pellet or washed pellet is said grapefruit juice-derived solids preparation.    
     
     
         4 . The method as claimed in  claim 3 , wherein said grapefruit juice-derived solids preparation is dried, optionally extracted with alcohol, and the extract is optionally purified.