SUSTAINED RELEASE AMINOPYRIDINE COMPOSITION

• US 20120041034A1
• Filed: 07/20/2011
• Published: 02/16/2012
• 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
• Granted Patent: US 8,663,685 B2
• Time in Patent Office: Days
• US Class Current: 514/352
• 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

1-23. -23. (canceled)

24. 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.

25. The method of claim 24 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.

26. The method of claim 25 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.

27. The method of claim 26 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.

28. The method of claim 24 wherein the sustained release composition provides an average maximum plasma concentration in humans in the range of about 15 ng/ml to about 35 ng/ml.

29. The method of claim 24 wherein the 4-aminopyridine is dispersed in a rate of release controlling polymer.

30. The method of claim 24 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.

31. The method of claim 24 wherein the step of administering comprises b.i.d. administering or administering at 12 hour intervals.

32. A method of improving walking in a multiple sclerosis patient in need thereof comprising orally administering to said patient a sustained release oral dosage formulation comprising a therapeutically effective amount of 4-aminopyridine dispersed in a matrix that provides a therapeutically effective blood plasma level of 4-aminopyridine in the patient extending over about 24 hours.

33. A method of improving walking in a multiple sclerosis patient in need thereof comprising orally administering to said patient a compressed tablet formulation that provides a release profile of 4-aminopyridine that permits establishment of a therapeutically effective concentration of the 4-aminopyridine in the patient with once daily dosing of the compressed tablet formulation.