Granted Patent B2

US 8,426,472 · App. 13/284,630 · Granted Apr 23, 2013

Abstract

Claims (18)

1. A method of administering memantine to a human subject in need thereof, comprising:

orally administering to the subject once per day over multiple days a sustained release oral dosage form comprising memantine or a pharmaceutically acceptable salt thereof and a component that sustains release of the memantine or the salt thereof;

wherein a daily dose of 12.5 to 40 mg of memantine or pharmaceutically acceptable salt thereof is administered from the initiation of therapy without prior dose escalation of memantine;

wherein such administration results in the subject achieving a therapeutically effective steady state memantine plasma concentration within 20 days after initiation of therapy with said dosage form; and

wherein the subject has a condition selected from the group consisting of Alzheimer's disease, dementia, Parkinson's disease and neuropathic pain.

2. The method of claim 1 , wherein said sustained release memantine provides a change in plasma concentration as a function of time (dC/dT) in a defined time period of 0 to 6 hours after administration as measured in a single dose human PK study, that is less than about 50% of the dC/dT provided by the same quantity of an immediate release form of memantine in said defined time period.

3. The method of claim 1 , wherein said sustained release memantine provides a change in plasma concentration as a function of time (dC/dT) that is less than about 50% of the dC/dT provided by the same quantity of an immediate release form of memantine, wherein the dC/dT is measured in a single dose human PK study between the time period of 0 to Tmax of the immediate release form of memantine.

4. The method of claim 1 , wherein the dosage form has a memantine in vitro dissolution profile ranging between 0.1-20% in one hour, 5-30% in two hours, 40-80% in six hours, and 50 to 90% in 10 hours, wherein the dissolution profile is determined using a USP type 2 (paddle) dissolution system at 50 rpm, at a temperature of 37±0.5° C., in 500 ml water.

5. The method of claim 1 , wherein said subject has not been administered memantine or a pharmaceutically acceptable salt thereof within one week prior to the initiation of therapy with said sustained release oral dosage form.

6. A method of administering memantine to a human subject in need thereof, comprising:

orally administering to the subject once per day over multiple days a sustained release oral dosage form comprising memantine or a pharmaceutically acceptable salt thereof and a component that sustains release of the memantine or the salt thereof;

wherein 12.5 to 40 mg of memantine or pharmaceutically acceptable salt thereof is administered daily from the initiation of therapy without prior dose escalation of memantine;

wherein daily administration of 12.5 to 40 mg of memantine or pharmaceutically acceptable salt thereof results in the subject achieving a therapeutically effective steady state memantine plasma concentration within 20 days after initiation of therapy with said dosage form; and

wherein the subject has a condition selected from the group consisting of Alzheimer's disease, dementia, Parkinson's disease and neuropathic pain.

7. The method of claim 6 , wherein said sustained release memantine provides a change in plasma concentration as a function of time (dC/dT) in a defined time period of 0 to 6 hours after administration as measured in a single dose human PK study, that is less than about 50% of the dC/dT provided by the same quantity of an immediate release form of memantine in said defined time period.

8. The method of claim 6 , wherein said sustained release memantine provides a change in plasma concentration as a function of time (dC/dT) that is less than about 50% of the dC/dT provided by the same quantity of an immediate release form of memantine, wherein the dC/dT is measured in a single dose human PK study between the time period of 0 to Tmax of the immediate release form of memantine.

9. The method of claim 6 , wherein the dosage form has a memantine in vitro dissolution profile ranging between 0.1-20% in one hour, 5-30% in two hours, 40-80% in six hours, and 50 to 90% in 10 hours, wherein the dissolution profile is determined using a USP type 2 (paddle) dissolution system at 50 rpm, at a temperature of 37±0.5° C., in 500 ml water.

10. The method of claim 6 , wherein said subject has not been administered memantine or a pharmaceutically acceptable salt thereof within one week prior to the initiation of therapy with said sustained release oral dosage form.

Assignments (8)