Novel crude and crystalline forms of lercanidipine hydrochloride

Abstract

The invention describes novel lercanidipine crude Forms (A) and (B), novel lercanidipine hydrochloride crystalline Forms (I) and (II) obtained from said crude Forms, pharmaceutical, antihypertensive compositions containing as active agent at least one of the lercanidipine hydrochloride crystalline Forms (I) and (II) and methods of use thereof.

1 - 84 . (canceled)  
     
     
         85 . A crystalline lercanidipine hydrochloride Form I having at least one significant X-ray powder diffraction pattern peak at a 2θ value selected from the group consisting of 5.4, 14.2, 18.6, 21.7, 21.9, and 22.8.  
     
     
         86 . The crystalline lercanidipine hydrchloride Form I of  claim 85  having at least three significant X-ray powder diffraction pattern peaks at 20 values selected from the group consisting of 5.4, 14.2, 18.6, 21.7, 21.9, and 22.8.  
     
     
         87 . The crystalline lercanidipine hydrochloride Form I of  claim 86  having significant X-ray powder diffraction pattern peaks at 20 values of 5.4, 14.2, 18.6, 21.7, 21.9, and 22.8.  
     
     
         88 . The crystalline lercanidipine hydrochloride Form I of  claim 85  having a melting point of about 197-201° C. as determined by DSC.  
     
     
         89 . The crystalline lercanidipine hydrochloride Form I of  claim 85 , said crystalline lercanidipine hydrochloride Form I being substantially free of crystalline lercanidipine hydrochloride Form II having at least one significant X-ray powder diffraction peak at a 2θ value selected from the group consisting of 9.5, 14.7, 16.1, 19.1, 20.8, 23.4, 23.6, 24.8 and 25.2.  
     
     
         90 . An antihypertensive composition comprising the crystalline lercanidipine hydrochloride Form I of  claim 85  and amorphous lercanidipine hydrochloride.  
     
     
         91 . The antihypertensive composition of  claim 90  wherein the composition is substantially free of crystalline lercanidipine hydrochloride Form II having at least one significant X-ray powder diffraction peak at a 2θ value selected from the group consisting of 9.5, 14.7, 16.1, 19.1, 20.8, 23.4, 23.6, 24.8 and 25.2.  
     
     
         92 . The antihypertensive composition of  claim 90  further comprising a pharmaceutically acceptable excipient.  
     
     
         93 . An antihypertensive composition comprising the crystalline lercanidipine hydrochloride Form I of  claim 86  and amorphous lercanidipine hydrochloride.  
     
     
         94 . The antihypertensive composition of  claim 93  wherein the composition is substantially free of crystalline lercanidipine hydrochloride Form II having at least one significant X-ray powder diffraction peak at a 2θ value selected from the group consisting of 9.5, 14.7, 16.1, 19.1, 20.8, 23.4, 23.6, 24.8 and 25.2.  
     
     
         95 . The antihypertensive composition of  claim 93  further comprising a pharmaceutically acceptable excipient.  
     
     
         96 . An antihypertensive composition comprising the crystalline lercanidipine hydrochloride Form I of  claim 87  and amorphous lercanidipine hydrochloride.  
     
     
         97 . The antihypertensive composition of  claim 96  wherein the composition is substantially free of crystalline lercanidipine hydrochloride Form II having at least one significant X-ray powder diffraction peak at a 2θ value selected from the group consisting of 9.5, 14.7, 16.1, 19.1, 20.8, 23.4, 23.6, 24.8 and 25.2.  
     
     
         98 . The antihypertensive composition of  claim 96  further comprising a pharmaceutically acceptable excipient.  
     
     
         99 . A lercanidipine hydrochloride preparation comprising a crystalline lercanidipine hydrochloride Form I having at least one significant X-ray powder diffraction pattern peak at a 2θ value selected from the group consisting of 5.4, 14.2, 18.6, 21.7, 21.9, and 22.8 subjected to micronization.  
     
     
         100 . The lercanidipine hydrochloride preparation of  claim 99  comprising a crystalline lercanidipine hydrochloride Form I having at least three significant X-ray powder diffraction pattern peaks at 2θ values selected from the group consisting of 5.4, 14.2, 18.6, 21.7, 21.9, and 22.8 subjected to micronization.  
     
     
         101 . The lercanidipine hydrochloride preparation of  claim 100  comprising a crystalline lercanidipine hydrochloride Form I having significant X-ray powder diffraction pattern peaks at 2θ values of 5.4, 14.2, 18.6, 21.7, 21.9, and 22.8 subjected to micronization.