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 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.