Azithromycin dosage forms with reduced side effects

Abstract

The present invention is related to an oral dosage form comprising an effective amount of an alkalizing agent and an azithromycin multiparticulate wherein said multiparticulate comprises azithromycin, a glyceride which comprises glyceryl monobehenate, glyceryl dibehenate, glyceryl tribehenate, or a mixture thereof and a poloxamer. Typically, the oral dosage form includes any suitable oral dosing means such as a powder for oral suspension, a unit dose packet or sachet, a tablet or a capsule.

1 - 114 . (canceled)  
   
   
       115 . An oral dosage form of azithromycin, comprising: 
 (a) an effective amount of an alkalizing agent; and    (b) multiparticulates having having a mean diameter of from about 100 to about 300 mm; wherein said multiparticulates comprise (i) about 20% to about 75% azithromycin, and (ii) about 25% to about 80% of a carrier having a melting point of less than about 113° C.    
   
   
       116 . The oral dosage form of  claim 115  wherein said alkalizing agent comprises an aluminum salt, a magnesium salt, a calcium salt, a bicarbonate, a phosphate, a metal hydroxide, a metal oxide, N-methyl glucamine, arginine, an arginine salt, an amine, or a combination thereof.  
   
   
       117 . The oral dosage form of  claim 116  wherein said alkalizing agent comprises a bicarbonate, a phosphate, a metal hydroxide, a metal oxide or a combination thereof.  
   
   
       118 . The oral dosage form of  claim 117  wherein said phosphate is monobasic calcium phosphate, dibasic calcium phosphate, dibasic sodium phosphate, tribasic sodium phosphate, dibasic potassium phosphate, tribasic potassium phosphate or a mixture thereof.  
   
   
       119 . The oral dosage form of  claim 117  wherein said bicarbonate is calcium bicarbonate, sodium bicarbonate or a mixture thereof.  
   
   
       120 . The oral dosage form of  claim 117  wherein said metal oxide is magnesium oxide.  
   
   
       121 . The oral dosage form of  claim 115  wherein said alkalizing agent comprises tribasic sodium phosphate and magnesium hydroxide.  
   
   
       122 . A method for reducing the frequency of gastrointestinal side effects, associated with administering azithromycin to a mammal, comprising contiguously administering oral dosage form of  claim 115  to said mammal wherein the frequency of gastrointestinal side effects is reduced as compared to the frequency experienced when administering an equal dose of azithromycin without said alkalizing agent.  
   
   
       123 . The method of  claim 122  wherein said mammal is human.  
   
   
       124 . The method of  claim 122  wherein said azithromycin is administered in a single dose.  
   
   
       125 . The method of  claim 122  wherein said azithromycin comprises an immediate release form of azithromycin.  
   
   
       126 . The method of  claim 122  wherein said azithromycin comprises a sustained release form of azithromycin.  
   
   
       127 . The oral dosage form of  claim 115  wherein the alkalizing agent comprises tribasic sodium phosphate.  
   
   
       128 . The oral dosage form of  claim 125  wherein the alkalizing agent further comprises magnesium hydroxide.