Directly compressible formulations of azithromycin

Abstract

The present invention relates to a dry blend, used for forming azithromycin tablets by direct compression, comprising non-dihydrate azithromycin and at least one pharmaceutically acceptable excipient. This invention also relates to an azithromycin tablet comprising non-dihydrate azithromycin and at least one pharmaceutically acceptable excipient. Preferably, the azithromycin tablet is formed by directly compressing the dry blend, of the present invention, to form said azithromycin tablet. Preferably, the azithromycin tablet, of the present invention, contains a dosage of 250 mgA, 500 mgA or 600 mgA of azithromycin. This invention further relates to an azithromycin tablet which is produced by forming a dry blend of a non-granulated azithromycin form A and at least one pharmaceutically acceptable excipient. The azithromycin tablet is then formed by directly compressing the dry blend.

1 - 55 . (canceled)  
   
   
       56 . A method of forming an azithromycin tablet, comprising: 
 (a) mixing particles of a non-dihydrate azithromycin and at least one pharmaceutically acceptable excipient to form a dry blend; and    (b) directly compressing said dry blend to form the azithromycin tablet;    wherein said non-dihydrate azithromycin is selected from the group consisting of azithromycin monohydrate hemi-ethanol solvate, azithromycin monohydrate hemi-isopropanol solvate, azithromycin monohydrate hemi-n-propanol solvate and azithromycin sesquihydrate.    
   
   
       57 . he method of  claim 56  wherein the non-dihydrate azithromycin is non-granulated.  
   
   
       58 . he method of  claim 57  further comprising the step of removing azithromycin fines from the non-dihydrate azithromycin.  
   
   
       59 . (canceled)  
   
   
       60 . The method of  claim 57  further comprising the step of precompressing the dry blend.  
   
   
       61 . The method of  claim 57  further comprising the step of force feeding the dry blend into a tableting means.  
   
   
       62 - 65 . (canceled)  
   
   
       66 . The method of  claim 57  wherein the dry blend has an internal angle of friction of less than about 34°.  
   
   
       67 . The method of  claim 57  wherein the dry blend has an internal angle of friction of less than about 31°.  
   
   
       68 . The method of  claim 57  wherein less than about 6% of the total azithromycin particles, by volume as measured by the Malvern method, in the dry blend have a diameter of 16 μm or less.  
   
   
       69 . The method of  claim 57  wherein less than about 20% of the total azithromycin particles, by volume as measured by the Malvern method, in the dry blend have a diameter of 44 μm or less.  
   
   
       70 . The method of  claim 69  wherein less than about 14% of the total azithromycin particles, by volume as measured by the Malvern method, in the dry blend have a diameter of 44 μm or less.  
   
   
       71 . The method of  claim 69  wherein less than about 60% of the total azithromycin particles, by volume as measured by the Malvern method, in the dry blend have a diameter of 105 μm or less.  
   
   
       72 . The method of  claim 71  wherein less than about 50% of the total azithromycin particles, by volume as measured by the Malvern method, in the dry blend have a diameter of 105 μm or less.  
   
   
       73 . The method of  claim 69  wherein less than about 27% of the total azithromycin particles, by volume as measured by the Malvern method, in the dry blend have a diameter of 74 μm or less.  
   
   
       74 . The method of  claim 69  wherein less than about 6% of the total azithromycin particles, by volume as measured by the Malvern method, have a diameter of 16 μm or less.  
   
   
       75 . The method of  claim 57  wherein, by volume as measured by the Malvern method, in the dry blend 
 (a) less than about 6% of the azithromycin particles have a diameter of about 16 μm or less; and    (b) less than about 20% of the azithromycin particles have a diameter of about 44 μm or less.    
   
   
       76 . The method of  claim 75  wherein less than about 14% of the total azithromycin particles, by volume as measured by the Malvern method, in the dry blend have a diameter of 44 μm or less.  
   
   
       77 . The method of  claim 57  wherein, by volume as measured by the Malvern method, in the dry blend 
 (a) less than about 6% of the azithromycin particles have a diameter of about 16 μm or less;    (b) less than about 20% of the azithromycin particles have a diameter of about 44 μm or less; and    (c) less than about 27% of the azithromycin particles have a diameter of about 74 μm or less.    
   
   
       78 . The method of  claim 77  wherein less than about 14% of the total azithromycin particles, by volume as measured by the Malvern method, in the dry blend have a diameter of 44 μm or less.  
   
   
       79 . The method of  claim 57  wherein, by volume as measured by the Malvern method, in the dry blend 
 (a) less than about 6% of the azithromycin particles have a diameter of about 16 μm or less;    (b) less than about 20% of the azithromycin particles have a diameter of about 44 μm or less;    (c) less than about 27% of the azithromycin particles have a diameter of about 74 μm or less; and    (d) less than about 60% of the azithromycin particles have a diameter of about 105 μm or less.    
   
   
       80 . The method of  claim 79  wherein less than about 14% of the total azithromycin particles, by volume as measured by the Malvern method, in thr dry blend have a diameter of 44 μm or less.  
   
   
       81 . The method of  claim 57  wherein, by volume as measured by the Malvern method, in the dry blend 
 (a) less than about 14% of the azithromycin particles have a diameter of 44 μm or less; and    (b) less than about 50% of the azithromycin particles have a diameter of 105 μm or less.    
   
   
       82 - 83 . (canceled)