US2010272795A1PendingUtilityA1

Sustained release aminopyridine composition

74
Assignee: CUNNINGHAM SEANPriority: Dec 11, 2003Filed: Nov 25, 2009Published: Oct 28, 2010
Est. expiryDec 11, 2023(expired)· nominal 20-yr term from priority
Inventors:Sean CunninghamSeamus MulliganMichael Myers
A61P 43/00A61P 25/00A61P 25/28A61P 19/00A61K 9/2054A61K 47/38A61K 47/12A61K 9/20A61K 47/44A61K 31/44A61K 31/4409A61K 47/14A61K 9/2077
74
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Cited by
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Claims

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.

Claims

exact text as granted — not AI-modified
1 .- 23 . (canceled) 
     
     
         24 . A sustained release composition comprising:
 4-aminopyridine dispersed in a sustained release matrix wherein said composition comprises 4-aminopyridine in an amount from 0.5% by weight of the composition to 4.75% by weight of the composition.   
     
     
         25 . The sustained release composition of  claim 24 , wherein the sustained release matrix exhibits a release profile to obtain a C max :C τ  ratio in vivo of about 1.0 to about 3.5. 
     
     
         26 . The sustained release composition of  claim 25 , wherein the composition further exhibits a release profile to obtain a predetermined C avSS . 
     
     
         27 . The sustained release composition of  claim 24  wherein the composition provides a C avSS  of about 15 ng/ml to about 35 ng/ml. 
     
     
         28 . The sustained release composition of  claim 26 , wherein said predetermined C avSS  is about 21 ng/ml. 
     
     
         29 . The sustained release composition of  claim 26 , wherein said predetermined C avSS  is about 31 ng/ml. 
     
     
         30 . The sustained release composition of  claim 26 , wherein said predetermined C avSS  is about 40 ng/ml. 
     
     
         31 . The sustained release composition of  claim 24 , wherein the 4-aminopyridine is released from said sustained release matrix at a rate to maintain an in vivo C max :C τ  ratio of 1.0 to 3.5 and a C avSS  of about 15 ng/ml to about 35 ng/ml. 
     
     
         32 . The sustained release composition of  claim 31 , wherein said sustained release matrix is hydroxypropylmethylcellulose. 
     
     
         33 . The sustained release composition of  claim 25  or  31 , wherein said C max :C τ  ratio is about 1.5 to about 3.0. 
     
     
         34 . The sustained release composition of  claim 25  or  31 , wherein said C max :C τ  ratio is about 2.0 to about 3.0. 
     
     
         35 . The sustained release composition of  claim 24 , wherein said sustained release matrix is hydroxypropylmethylcellulose. 
     
     
         36 . The sustained release composition of  claim 24 , in tablet form. 
     
     
         37 . The sustained release composition of  claim 36 , wherein the tablet comprises 5 mg of 4-aminopyridine. 
     
     
         38 . The sustained release composition of  claim 36 , wherein the tablet comprises 7.5 mg of 4-aminopyridine. 
     
     
         39 . The sustained release composition of  claim 36 , wherein the tablet comprises 10 mg of 4-aminopyridine. 
     
     
         40 . The sustained release composition of  claim 36 , wherein the tablet comprises 12.5 mg of 4-aminopyridine. 
     
     
         41 . The sustained release composition of  claim 36 , wherein the tablet comprises 15 mg of 4-aminopyridine. 
     
     
         42 . The sustained release composition of  claim 24 , wherein said 4-aminopyridine is present from 0.5 milligrams to 80 milligrams. 
     
     
         43 . The sustained release composition of  claim 24 , wherein said 4-aminopyridine is present from 5 milligrams to 50 milligrams. 
     
     
         44 . The sustained release composition of  claim 24 , further comprising a pharmaceutically acceptable excipient. 
     
     
         45 . The sustained release composition of  claim 24 , further comprising an additional active ingredient. 
     
     
         46 . A sustained release aminopyridine composition comprising:
 a sustained release matrix and 4-aminopyridine,   wherein said 4-aminopyridine is present in said composition in an amount from 0.5% to 6.25% by weight of the composition, and,   the matrix comprises a hydrophilic polymer.   
     
     
         47 . The sustained release composition of  claim 46 , wherein the hydrophilic polymer is hydroxypropylmethylcellulose. 
     
     
         48 . The sustained release composition of  claim 46 , wherein said 4-aminopyridine is dispersed in said sustained release matrix. 
     
     
         49 . The sustained release composition of  claim 46 , wherein said 4-aminopyridine is homogeneously dispersed in said sustained release matrix. 
     
     
         50 . The sustained release composition of  claim 46 , wherein said composition is selected from a tablet, capsule and granule. 
     
     
         51 . The sustained release composition of  claim 46 , in tablet form. 
     
     
         52 . The sustained release composition of  claim 51 , wherein the tablet comprises 5 mg of 4-aminopyridine. 
     
     
         53 . The sustained release composition of  claim 51 , wherein the tablet comprises 7.5 mg of 4-aminopyridine. 
     
     
         54 . The sustained release composition of  claim 51 , wherein the tablet comprises 10 mg of 4-aminopyridine. 
     
     
         55 . The sustained release composition of  claim 51 , wherein the tablet comprises 12.5 mg of 4-aminopyridine. 
     
     
         56 . The sustained release composition of  claim 51 , wherein the tablet comprises 15 mg of 4-aminopyridine. 
     
     
         57 . A sustained release aminopyridine composition comprising:
 a sustained release matrix and 4-aminopyridine,   wherein said 4-aminopyridine is present in said composition in an amount less than 5% by weight of said composition, and,   the matrix comprises a hydrophilic polymer.   
     
     
         58 . The sustained release composition of  claim 46 , wherein said 4-aminopyridine is present in said composition in an amount from 0.5% to 4.75% by weight of said composition. 
     
     
         59 . The sustained release composition of  claim 46 , wherein said 4-aminopyridine is present from 0.5 milligrams to 80 milligrams. 
     
     
         60 . The sustained release composition of  claim 46 , wherein said 4-aminopyridine is present from 5 milligrams to 50 milligrams. 
     
     
         61 . The sustained release composition of  claim 46 , further comprising a pharmaceutically acceptable excipient. 
     
     
         62 . The sustained release composition of  claim 46 , further comprising an additional active ingredient. 
     
     
         63 . A sustained release aminopyridine composition comprising:
 a sustained release matrix and 4-aminopyridine, wherein said 4-aminopyridine is present in said composition in an amount from 0.5% to 6.25% by weight of the composition, and,   the matrix comprises a hydrophobic polymer.   
     
     
         64 . The sustained release composition of  claim 63 , wherein said 4-aminopyridine is dispersed in said sustained release matrix. 
     
     
         65 . The sustained release composition of  claim 63 , wherein said 4-aminopyridine is homogeneously dispersed in said sustained release matrix. 
     
     
         66 . The sustained release composition of  claim 63 , wherein said sustained release matrix further comprises a hydrophilic polymer. 
     
     
         67 . The sustained release composition of  claim 63 , wherein said composition is a tablet, capsule or granule. 
     
     
         68 . The sustained release composition of  claim 63 , in tablet form. 
     
     
         69 . The sustained release composition of  claim 68 , wherein the tablet comprises 5 mg of 4-aminopyridine. 
     
     
         70 . The sustained release composition of  claim 68 , wherein the tablet comprises 7.5 mg of 4-aminopyridine. 
     
     
         71 . The sustained release composition of  claim 68 , wherein the tablet comprises 10 mg of 4-aminopyridine. 
     
     
         72 . The sustained release composition of  claim 68 , wherein the tablet comprises 12.5 mg of 4-aminopyridine. 
     
     
         73 . The sustained release composition of  claim 68 , wherein the tablet comprises 15 mg of 4-aminopyridine. 
     
     
         74 . A sustained release aminopyridine composition comprising:
 a sustained release matrix and 4-aminopyridine, wherein said 4-aminopyridine is present in said composition in an amount less than 5% by weight of said composition, and,   the matrix comprises a hydrophobic polymer.   
     
     
         75 . The sustained release composition of  claim 63 , wherein said 4-aminopyridine is present in said composition in an amount from 0.5% to 4.75% by weight of said composition. 
     
     
         76 . The sustained release composition of  claim 63 , wherein said 4-aminopyridine is present from 0.5 milligrams to 80 milligrams. 
     
     
         77 . The sustained release composition of  claim 63 , wherein said 4-aminopyridine is present from 5 milligrams to 50 milligrams. 
     
     
         78 . The sustained release composition of  claim 63 , further comprising a pharmaceutically acceptable excipient. 
     
     
         79 . The sustained release composition of  claim 63 , further comprising an additional active ingredient.

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