Sustained release aminopyridine composition

Abstract

A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.

1 - 23 . (canceled) 
     
     
         24 . A process for preparing a sustained release 4-aminopyridine composition comprising the steps of:
 (a) dry blending said 4-aminopyridine with a rate-controlling polymer to form a blend comprising 4-aminopyridine dispersed in said rate-controlling polymer; and   (b) compressing the blend formed in step (a) to form one or more tablets, wherein the 4-aminopyridine content of each of the one or more tablets is 10 mg of 4-aminopyridine.   
     
     
         25 . The process of  claim 24  further comprising the step of milling the 4-aminopyridine to produce a particle size distribution such that 90% of the 4-aminopyridine particles are smaller than 1.5 mm, 50% of the 4-aminopyridine particles are smaller than 1 mm, and 10% of the 4-aminopyridine particles are smaller than 500 μm. 
     
     
         26 . The process of  claim 25 , wherein the milling step is carried out prior to dispersing the 4-aminopyridine in the rate-controlling polymer. 
     
     
         27 . The process of  claim 24 , wherein one or more excipients are added to the blend during the dry blending step. 
     
     
         28 . The process of  claim 27 , wherein a diluent, a glidant and/or a lubricant are added to the blend during the dry blending step. 
     
     
         29 . The process of  claim 24  further comprising the step of: (c) coating one or more tablets formed in step (b) with a film coating. 
     
     
         30 . The process of  claim 29 , wherein the film coating is a light-protective and/or cosmetic film coating. 
     
     
         31 . The process of  claim 28 , wherein the blend is formed using 4-aminopyridine in an amount from about 0.5 to about 6.25% w/w, the rate-controlling polymer in an amount from about 20 to about 96% w/w, and the diluent in an amount from about 10 to about 80% w/w of the sustained release composition. 
     
     
         32 . The process of  claim 28 , wherein the blend is formed using 4-aminopyridine in an amount less than 4.75% w/w, the rate-controlling polymer in an amount from 20 to 70% w/w, and the diluent in an amount from 20 to 50% w/w of the sustained release composition. 
     
     
         33 . The process of  claim 32 , wherein the rate-controlling polymer is hydroxypropyl methylcellulose and the diluent is microcrystalline cellulose. 
     
     
         34 . A sustained release 4-aminopyridine composition that is the product of the process of  claim 24 ,  25 ,  32 , or  33 .