Sustained release aminopyridine composition
AssigneeAcorda Therapeutics, Inc.
InventorsAndrew R. Blight, Ron Cohen
Life of this patent
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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.
Claims41
A method for maintaining a therapeutically effective concentration of 4-aminopyridine in order to improve walking in a human with multiple sclerosis in need thereof, said method comprising:
- orally administering to the human a sustained release composition of 10 milligrams of 4-aminopyridine twice daily for a day;
- and thereafter,
- maintaining administration of 4-aminopyridine by orally administering to said human a sustained release composition of 10 milligrams of 4-aminopyridine twice daily for a time period of at least two weeks, whereby an in vivo 4-aminopyridine CmaxSS:CminSS ratio of 1.0 to 3.5 and a CavSS of 15 ng/ml to 35 ng/ml are obtained in the human.
A dosing regimen method for providing a 4-aminopyridine at a therapeutically effective concentration in order to improve walking in a human with multiple sclerosis in need thereof, said method comprising:
- initiating administration of 4-aminopyridine by orally administering to said human a sustained release composition of 10 milligrams of 4-aminopyridine twice daily for a day without a prior period of 4-aminopyridine titration, and then,
- maintaining administration of 4-aminopyridine by orally administering to said human a sustained release composition of 10 milligrams of 4-aminopyridine twice daily;
- without a subsequent period of 4-aminopyridine titration,
- whereby an in vivo CmaxSS:CminSS ratio of 1.0 to 3.5 and a CavSS of 15 ng/ml to 35 ng/ml are maintained in the human.
A method for maintaining a therapeutically effective concentration of 4-aminopyridine in a human with multiple sclerosis in need of an improvement in walking, in order to improve walking in the human, said method comprising:
- orally administering twice daily to the human a sustained release composition comprising a pharmaceutically acceptable excipient and 4-aminopyridine, the 4-aminopyridine consisting of 10 milligrams of 4-aminopyridine, for one day;
- and thereafter,
- maintaining twice daily administration for a time period of greater than two weeks of a sustained release composition comprising a pharmaceutically acceptable excipient and 4-aminopyridine, the 4-aminopyridine consisting of 10 milligrams of 4-aminopyridine;
- whereby an in vivo 4-aminopyridine CmaxSS:CminSS ratio of 1.0 to 3.5 and a CavSS of 15 ng/ml to 35 ng/ml are obtained in the human.
A method to improve walking by a human with multiple sclerosis in need thereof, said method comprising:
- orally administering twice daily for one day to the human a sustained release composition of 10 milligrams of 4-aminopyridine and an agent selected from the group consisting of one or more additional active ingredients, one or more pharmaceutically acceptable excipients and a combination thereof;
- and thereafter,
- maintaining twice daily administration of 4-aminopyridine by orally administering twice daily to said human a sustained release composition of 10 milligrams of 4-aminopyridine and an agent selected from the group consisting of one or more additional active ingredients, one or more pharmaceutically acceptable excipients and a combination thereof for a time period of greater than two weeks;
- whereby an in vivo 4-aminopyridine CmaxSS:CminSS ratio of 1.0 to 3.5 and a CavSS of 15 ng/ml to 35 ng/ml are obtained and there is an improvement in walking by the human.
A method of increasing walking speed 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 greater than two weeks, wherein said sustained release composition provides a mean Tmax in a range of about 1 to about 6 hours after administration of the sustained release composition to the patient.
A method to improve walking in a patient with multiple sclerosis in need thereof by use of a sustained release composition of 4-aminopyridine, where sustained indicates that the composition achieves an in vivo 4-aminopyridine CmaxSS:CminSS ratio of 1.0 to 3.5 and a CavSS of 15 ng/ml to 35 ng/ml in a human, said method comprising:
- orally administering twice daily for one day to the patient an amount of the sustained release composition having only 10 milligrams of 4-aminopyridine;
- and thereafter,
- maintaining twice daily administration of 4-aminopyridine by orally administering to said patient an amount of the sustained release composition having only 10 milligrams of 4-aminopyridine for a time period of at least two weeks.
A method of increasing walking speed 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 greater than two weeks, wherein said sustained release composition provides a mean Tmax in a range of about 2 to about 5.2 hours after administration of the sustained release composition to the patient.
Dependencies are inferred from the claim text.