Sustained release aminopyridine composition

• US 8,663,685 B2
• Filed: 07/20/2011
• Issued: 03/04/2014
• Est. Priority Date: 12/11/2003
• Status: Active Grant

• Current Assignee: Acorda Therapeutics Incorporated
• Original Assignee: Acorda Therapeutics Incorporated
• Inventors: Blight, Andrew R., Cohen, Ron
• Primary Examiner(s): RAO, SAVITHA M
• Application Number:
  US13/187,158
• Publication Number:
  US 20120041034A1
• Time in Patent Office: 958 Days
• Field of Search: 514/352, 514/903, 514/965, 424/468
• US Class Current: 424/468
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61K 31/4409 only substituted in position 4, e.g. isoniazid, iproniazid
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/20 Pills, tablets, discs, rods A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61P 19/00 Drugs for skeletal disorders
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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

1. A method of improving walking in a human multiple sclerosis patient in need thereof comprising orally administering to said patient a sustained release composition of 10 milligrams of 4-aminopyridine twice daily for a time period of at least two weeks, wherein the sustained release composition further comprises one or more pharmaceutically acceptable excipients.

2. The method of claim 1 wherein said sustained release composition provides a mean T_max in a range of about 2 to about 6 hours after administration of the sustained release composition to the patient.

3. The method of claim 2 wherein the sustained release composition is capable of providing, upon administration to the patient, a release profile of the 4-aminopyridine extending over at least 6 hours.

4. The method of claim 3 wherein the sustained release composition is capable of providing, upon administration to the patient, a release profile of the 4-aminopyridine extending over at least about 12 hours.

5. The method of claim 1 wherein the sustained release composition provides an average plasma concentration at steady state in humans in the range of about 15 ng/ml to about 35 ng/ml.

6. The method of claim 1 wherein the 4-aminopyridine is dispersed in a rate of release controlling polymer.

7. The method of claim 1 wherein the sustained release composition comprises a matrix in which the 4-aminopyridine is homogeneously dispersed that is suitable for controlling the release rate of the 4-aminopyridine.

8. The method of claim 1 wherein the step of administering comprises b.i.d. administering or administering at 12 hour intervals.