Sustained-release formulation for injection

Abstract

The present invention relates to a composition comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1′R,2′S,3′R,4′S)-2,3-bicyclo[2,2,1]heptanedicarboximide or a pharmaceutically acceptable acid addition salt thereof. In detail, the composition relates to a sustained release formulation for injection which maintains an effective blood level of the above-mentioned compound.

1 - 35 . (canceled) 
     
     
         36 . A crystal of N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1′R,2′S,3′R,4′S)-2,3-bicyclo[2,2,1]heptanedicarboximide whose mean particle size is about 4 μm-about 55 μm, about 4 μm-about 26 μm, about 4 μm-about 20 μm, about 4 μm-about 18 μm, about 4 μm-about 16 μm, about 5 μm-about 55 μm, about 5 μm-about 26 μm, about 5 μm-about 20 μm, about 5 μm-about 18 μm, about 5 μm-about 16 μm, about 8 μm-about 55 μm, about 8 μm-about 20 μm, about 10 μm-about 55 μm, about 10 μm-about 26 μm, about 10 μm-about 20 μm, about 10 μm-about 18 μm, or about 10 μm-about 16 μm. 
     
     
         37 . The crystal of  claim 36  which is a cubic crystal wherein the ratio between length and width of the cubic crystal is about 1:0.8 to about 1:1.2, and the ratio between length and height thereof is about 1:0.1 to about 1:3. 
     
     
         38 . A depot formulation for injection comprising the crystal of  claim 36  or  37 . 
     
     
         39 . The depot formulation for injection of  claim 38  wherein the crystal is suspended in a medium of the formulation. 
     
     
         40 . The depot formulation for injection of  claim 39  wherein the medium is water. 
     
     
         41 . The depot formulation for injection of  claim 38  which further comprises a surfactant, a buffer and an isotonic agent. 
     
     
         42 . A package containing a container which contains the sustained release formulation for injection comprising the crystal of  claim 36 . 
     
     
         43 - 46 . (canceled)