US2003105360A1PendingUtilityA1

Form a of fluoxetine hydrochloride

Priority: Jan 31, 2001Filed: Aug 20, 2002Published: Jun 5, 2003
Est. expiryJan 31, 2021(expired)· nominal 20-yr term from priority
A61K 31/138C07C 217/48
60
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Claims

Abstract

The present invention relates to novel polymorphic Form A of fluoxetine hydrochloride.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . Form A of fluoxetine hydrochloride in pure form.  
     
     
         2 . Form A of fluoxetine hydrochloride in pure form characterized by having an x-ray powder diffraction pattern consistent with fluoxetine hydrochloride, and further having a single endotherm as determined by differential scanning calorimetry run at a maximum rate of 1° C. per minute.  
     
     
         3 . Form A of fluoxetine hydrochloride according to  claim 2  wherein said single DSC endotherm occurs in the temperature range from about 155° C. to about 160° C.  
     
     
         4 . Form A of fluoxetine hydrochloride according to  claim 2  wherein said single DSC endotherm occurs in the temperature range from about 157° C. to about 159° C.  
     
     
         5 . Form A of fluoxetine hydrochloride in pure form characterized by the following single crystallographic parameters:  
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                     
                 
                     
                   crystal class 
                   orthorhombic 
                 
                     
                   space group 
                   Pbca (#61) 
                 
                     
                   a (Å) 
                   10.3754 (4) 
                 
                     
                   b (Å) 
                   10.4603 (2) 
                 
                     
                   c (Å) 
                   32.3412 (12) 
                 
                     
                   V (Å 3 ) 
                   3510.0 (3) 
                 
                     
                   d calc (g/cm 3 ) 
                   1.31 
                 
                     
                   R, R W   
                   0.038, 0.038. 
                 
                     
                     
                 
                     
                     
                 
             
                
                
               
               
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         6 . Form A of fluoxetine hydrochloride according to  claim 5  further characterized by having an x-ray powder diffraction pattern consistent with fluoxetine hydrochloride, and further characterized by having a single endotherm as determined by differential scanning calorimetry run at a maximum rate of 1° C. per minute.  
     
     
         7 . Form A of fluoxetine hydrochloride according to  claim 6  wherein said single DSC endotherm occurs in the temperature range from about 155° C. to about 160° C.  
     
     
         8 . Form A of fluoxetine hydrochloride according to  claim 6  wherein said DSC single endotherm occurs in the temperature range from about 157° C. to about 159° C.  
     
     
         9 . Form A of fluoxetine hydrochloride in essentially pure form.  
     
     
         10 . Form A of fluoxetine hydrochloride characterized by having an x-ray powder diffraction pattern consistent with fluoxetine hydrochloride, and further characterized by having at least two endotherms as determined by differential scanning calorimetry run at a maximum rate of 1° C. per minute, provided that the amount of fluoxetine hydrochloride polymorphs other than Form A does not exceed an amount greater than about ten percent (w/w).  
     
     
         11 . Form A of fluoxetine hydrochloride according to  claim 10  wherein the peak of said DSC endotherms occurs in the temperature range from about 155° C. to about 160° C.  
     
     
         12 . Form A of fluoxetine hydrochloride according to  claim 10  wherein said Form A is further characterized by the following crystallographic parameters:  
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                     
                 
                     
                   crystal class 
                   orthorhombic 
                 
                     
                   space group 
                   Pbca (#6 1) 
                 
                     
                   a (Å) 
                   10.3754 (4) 
                 
                     
                   b (Å) 
                   10.4603 (2) 
                 
                     
                   c (Å) 
                   32.3412 (12) 
                 
                     
                   V (Å 3 ) 
                   3510.0 (3) 
                 
                     
                   d calc (g/cm 3 ) 
                   1.31 
                 
                     
                   R, R W   
                   0.038, 0.038. 
                 
                     
                     
                 
                     
                     
                 
             
                
                
               
               
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         13 . Form A of fluoxetine hydrochloride according to  claim 12  wherein the peak of said DSC endotherms occurs in the temperature range from about 155° C. to about 160° C.  
     
     
         14 . Form A of fluoxetine hydrochloride form characterized by having an x-ray powder diffraction pattern consistent with fluoxetine hydrochloride, and further characterized by having at least two endotherms as determined by differential scanning calorimetry run at a maximum rate of 1° C. per minute, provided that the amount of fluoxetine hydrochloride polymorphs other than Form A does not exceed an amount greater than about five percent (w/w).  
     
     
         15 . Form A of fluoxetine hydrochloride according to  claim 14  wherein the peak of said DSC endotherms occurs in the temperature range from about 155° C. to about 160° C.  
     
     
         16 . Form A of fluoxetine hydrochloride according to  claim 14  wherein said Form A is further characterized by the following crystallographic parameters:  
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                     
                 
                     
                   crystal class 
                   orthorhombic 
                 
                     
                   space group 
                   Pbca (#61) 
                 
                     
                   a (Å) 
                   10.3754 (4) 
                 
                     
                   b (Å) 
                   10.4603 (2) 
                 
                     
                   c (Å) 
                   32.3412 (12) 
                 
                     
                   V (Å 3 ) 
                   3510.0 (3) 
                 
                     
                   d calc (g/cm 3 ) 
                   1.31 
                 
                     
                   R, R w   
                   0.038, 0.038. 
                 
                     
                     
                 
                     
                     
                 
             
                
                
               
               
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         17 . Form A of fluoxetine hydrochloride according to  claim 16  wherein the peak of said DSC endotherms occurs in the temperature range from about 155° C. to about 160° C.  
     
     
         18 . A method for inhibiting serotonin uptake in mammals comprising administering to a mammal requiring increased neurotransmission of serotonin an effective amount of fluoxetine hydrochloride as claimed in any one of claims  1  through  17 .

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