SUSTAINED RELEASE AMINOPYRIDINE COMPOSITION
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 .