Extended release formulations of erythromycin derivatives

Abstract

Disclosed is a pharmaceutical composition for extended release of an erythromycin derivative in the gastrointestinal environment. The composition comprises an erythromycin derivative and a pharmaceutically acceptable polymer so that, when ingested orally, the composition induces statistically significantly lower C max in the plasma than an immediate release composition of the erythromycin derivative while maintaining bioavailability and minimum concentration substantially equivalent to that of the immediate release composition of the erythromycin derivative upon multiple dosing. The compositions of the invention have an improved taste profile and reduced gastrointestinal side effects as compared to those for the immediate release composition.

1 - 20 . (canceled)  
     
     
         21 . A method of reducing gastrointestinal adverse events associated with clarithromycin therapy comprising: administering an extended release composition comprising clarithromycin wherein upon administration, the composition provides 
 a) a lower mean C max  than the immediate release composition having an equal amount of clarithromycin, and    b) a lower mean C max  than the controlled release formulation having an equal amount of clarithromycin, a water soluble alginate salt, a complex salt of alginic acid and an organic carboxylic acid.    
     
     
         22 . A method of reducing gastrointestinal adverse events associated with clarithromycin therapy comprising: administering an extended release composition comprising clarithromycin wherein upon administration, the composition provides 
 a) a lower mean degree of flucuation than the immediate release composition having an equal amount of clarithromycin, and    b) a lower mean degree of fluctuation than the controlled release formulation having an equal amount of clarithromycin, a water soluble alginate salt, a complex salt of alginic acid and an organic carboxylic acid.    
     
     
         23 . A method of reducing taste perversion associated with clarithromycin therapy comprising: administering an extended release composition comprising clarithromycin wherein upon administration, the composition provides 
 a) a lower mean C max  than the immediate release composition having an equal amount of clarithromycin, and    b) a lower mean C max  than the controlled release formulation having an equal amount of clarithromycin, a water soluble alginate salt, a complex salt of alginic acid and an organic carboxylic acid.    
     
     
         24 . A method of reducing taste perversion associated with clarithromycin therapy comprising: administering an extended release composition comprising clarithromycin wherein upon administration, the composition provides 
 a) a lower mean degree of flucuation than the immediate release composition having an equal amount of clarithromycin, and    b) a lower mean degree of fluctuation than the controlled release formulation having an equal amount of clarithromycin, a water soluble alginate salt, a complex salt of alginic acid and an organic carboxylic acid.    
     
     
         25 . A method of increasing compliance with clarithromycin therapy comprising: providing a pharmaceutical composition for extended release of clarithromycin having 
 a) a lower mean C max  than the immediate release composition having an equal amount of clarithromycin, and    b) a lower mean C max  than the controlled release formulation having an equal amount of clarithromycin, a water soluble alginate salt, a complex salt of alginic acid and an organic carboxylic acid.    
     
     
         26 . A method of increasing compliance with clarithromycin therapy comprising: providing a pharmaceutical composition for extended release of clarithromycin having 
 a) a lower mean degree of flucuation than the immediate release composition having an equal amount of clarithromycin, and    b) a lower mean degree of fluctuation than the controlled release formulation having an equal amount of clarithromycin, a water soluble alginate salt, a complex salt of alginic acid and an organic carboxylic acid.    
     
     
         27 . A method of increasing incidence of completion of a prescribed antibiotic therapy comprising providing a pharmaceutical compositon for extended release of clarithromycin having 
 a) a lower mean C max  than the immediate release composition having an equal amount of clarithromycin, and    b) a lower mean C max  than the controlled release formulation having an equal amount of clarithromycin, a water soluble alginate salt, a complex salt of alginic acid and an organic carboxylic acid.    
     
     
         28 . A method of increasing incidence of completion of a prescribed antiobiotic therapy comprising providing a pharmaceutical compositon for extended release of clarithromycin having 
 a) a lower mean degree of flucuation than the immediate release composition having an equal amount of clarithromycin, and    b) a lower mean degree of fluctuation than the controlled release formulation having an equal amount of clarithromycin, a water soluble alginate salt, a complex salt of alginic acid and an organic carboxylic acid.