Bupropion hydrobromide polymorphs

Abstract

Polymorphous and amorphous forms of bupropion hydrobromide are described.

What is claimed is: 
     
         1 . Bupropion hydrobromide in crystalline form, characterized by at least one of the following properties:
 PXRD as in  FIG. 39 ,   DSC as in  FIG. 40 ,   TGA as in  FIG. 41 ,   IR as in  FIG. 42 .   
     
     
         2 . Bupropion hydrobromide in crystalline form, characterized by at least one of the following properties:
 PXRD as in  FIG. 43 ,   DSC as in  FIG. 44 ,   TGA as in  FIG. 45 ,   IR as in  FIG. 46 .   
     
     
         3 . Bupropion hydrobromide in amorphous form, characterized by a PXRD as in  FIG. 47 . 
     
     
         4 . Bupropion hydrobromide in amorphous form, characterized by a PXRD as in  FIG. 48 . 
     
     
         5 . A composition comprising the bupropion hydrobromide according to  claim 1 ,  2 ,  3 , or  4  and a pharmaceutically acceptable carrier or excipient. 
     
     
         6 . The composition according to  claim 5 , further comprising at least one other drug other than bupropion hydrobromide selected from the group consisting of anti-depressants, anti-anxiety agents, steroidal inflammatories, non-steroidal inflammatories, SSRIs, antimigraine agents, anti-emetics, drugs for treating abuse, appetite modulators, anti-virals, vasodilators, anti-pain agents, and combinations thereof. 
     
     
         7 . The composition according to  claim 5  further comprising at least one other drug other than bupropion hydro bromide selected from the group consisting of a monoamine oxidase (MAO) inhibitor, a tricyclic antidepressant, a serotonin reuptake inhibitor, a selective norepinephrine reuptake inhibitor (SNRIs), amino ketones, serotonin antagonists, dopamine reuptake inhibitors, dual reuptake inhibitors, norepinephrine enhancers, serotonin activity enhancers, dopamine activity enhancers, and combinations thereof. 
     
     
         8 . The composition of  claim 5 , in the form of a microparticle comprising a solid core, said core comprising the bupropion hydrobromide and the at least one pharmaceutically acceptable excipient, said core of said microparticle being at least partially surrounded by a controlled release coat which permits entry of an aqueous liquid into the core and delivery of the bupropion hydrobromide from the core to the exterior of the microparticle through the controlled release coat. 
     
     
         9 . The composition of  claim 5 , in the form of a tablet comprising a core comprising the bupropion hydrobromide and a controlled release coating at least partially surrounding said core, the coating comprising at least one water-soluble polymer, at least one water-insoluble polymer, and optionally a plasticizer. 
     
     
         10 . A method of treating depression, seasonal effective disorder, obesity, anxiety, obsessive compulsive disorder, post-traumatic stress disorder (PTSD), panic disorder, disorders requiring a stimulant effect, attention deficit hyperactivity disorder (ADHD), narcolepsy, hypersomnia, female sexual dysfunction, male sexual dysfunction, premenstrual syndrome, premenstrual dysphoric disorder, neuropathic pain, fibromyalgia, diabetic neuropathy, viral infection, sleep apnea, sleep disorders or migraines comprising administering an effective amount of the bupropion hydrobromide of  claim 1 ,  2 ,  3 , or  4  to treat depression, seasonal effective disorder, obesity, anxiety, obsessive compulsive disorder, post-traumatic stress disorder (PTSD), panic disorder, disorders requiring a stimulant effect, attention deficit/hyperactivity disorder (ADHD), narcolepsy, hypersomnia, female sexual dysfunction, male sexual dysfunction, premenstrual syndrome, premenstrual dysphoric disorder, neuropathic pain, fibromyalgia, diabetic neuropathy, viral infection, sleep apnea, sleep disorders or migraines to a subject in need thereof. 
     
     
         11 . A composition comprising two or more of the following forms of bupropion hydrobromide:
 i. a crystalline form having the following properties PXRD as in  FIG. 39 , DSC as in  FIG. 40 , TGA as in  FIG. 41 , IR as in  FIG. 42 ;   ii. a crystalline form having the following properties PXRD as in  FIG. 43 , DSC as in  FIG. 44 , TGA as in  FIG. 45 , IR as in  FIG. 46 ;   iii. an amorphous form having the following property PXRD as in  FIG. 47 ; and   iv. an amorphous form having the following property PXRD as in  FIG. 48 .