Methods and Compositions for the Treatment of CNS-Related Conditions
First Claim
Patent Images
1. A pharmaceutical composition comprising:
- (a) an NMDAr antagonist;
(b) an acetylcholinesterase inhibitor (ACheI), wherein at least one of said NMDAr antagonist or said second agent is provided in an extended release dosage form and wherein the agent in said extended release dosage form has an in vitro dissolution profile less than 70% in one hour, less than 90% in two hours, greater than 40% in six hours, and greater than 85% in 12 hours as measured using a USP type 2 (paddle) dissolution system at 50 rpm, at a temperature of 37±
0.5°
with water as a dissolution medium.
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Abstract
The present invention provides novel methods and compositions for the treatment and prevention of CNS-related conditions. One of the CNS-related conditions treated by the methods and compositions of the invention is Alzheimer'"'"'s disease.
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Citations
49 Claims
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1. A pharmaceutical composition comprising:
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(a) an NMDAr antagonist; (b) an acetylcholinesterase inhibitor (ACheI), wherein at least one of said NMDAr antagonist or said second agent is provided in an extended release dosage form and wherein the agent in said extended release dosage form has an in vitro dissolution profile less than 70% in one hour, less than 90% in two hours, greater than 40% in six hours, and greater than 85% in 12 hours as measured using a USP type 2 (paddle) dissolution system at 50 rpm, at a temperature of 37±
0.5°
with water as a dissolution medium. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 44, 45, 46)
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12. A method of preventing or treating a CNS-related condition comprising administering to a subject in need thereof a therapeutically effective amount of:
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(a) an NMDAr antagonist; and (b) an acetylcholinesterase inhibitor, wherein at least one of said NMDAr antagonist or said second agent is provided in an extended release dosage form and wherein the agent in said extended release dosage form has an in vitro dissolution profile less than 70% in one hour, less than 90% in two hours, greater than 40% in six hours, and greater than 85% in 12 hours as measured using a USP type 2 (paddle) dissolution system at 50 rpm, at a temperature of 37±
0.5°
with water as a dissolution medium. - View Dependent Claims (13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29)
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30. A method of treating, preventing or reducing a condition associated with a deregulation in NMDAr activity comprising administering to a subject at risk of suffering or suffering from said condition a composition comprising an NMDAr antagonist provided in an extended release dosage form and a second agent, wherein said second agent ACheI selected from the group consisting of donepezil, rivastigmine, tacrine, metrifonate, Huperzine-A;
- wherein said composition is administered at a substantially identical daily dose.
- View Dependent Claims (31, 32, 33, 34, 35)
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36. Use of an NMDAr antagonist and an acetylcholinesterase inhibitor in the manufacture of a combined preparation for preventing or treating a CNS-related condition wherein at least one of said NMDAr antagonist or said acetylcholinesterase inhibitor has an in vitro dissolution profile less than 70% in one hour, less than 90% in two hours, greater than 40% in six hours, and greater than 85% in 12 hours as measured using a USP type 2 (paddle) dissolution system at 50 rpm, at a temperature of 37±
- 0.5°
with water as a dissolution medium. - View Dependent Claims (37, 38, 39)
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40. Use of an NMDAr antagonist in the manufacture of a medicament for preventing or treating a CNS-related condition in a subject in need thereof by combination therapy wherein said combination therapy comprises administration of said NMDAr antagonist and an acetylcholinesterase inhibitor to the subject, and wherein at least one of said NMDAr antagonist or said ACheI has an in vitro dissolution profile less than 70% in one hour, less than 90% in two hours, greater than 40% in six hours, and greater than 85% in 12 hours as measured using a USP type 2 (paddle) dissolution system at 50 rpm, at a temperature of 37±
- 0.5°
with water as a dissolution medium.
- 0.5°
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41. Use of an ACheI in the manufacture of a medicament for preventing or treating a CNS-related condition in a subject in need thereof by combination therapy wherein said combination therapy comprises administration of said ACheI and an NMDAr antagonist to the subject, and wherein at least one of said NMDAr antagonist or said ACheI has an in vitro dissolution profile less than 70% in one hour, less than 90% in two hours, greater than 40% in six hours, and greater than 85% in 12 hours as measured using a USP type 2 (paddle) dissolution system at 50 rpm, at a temperature of 37±
- 0.5°
with water as a dissolution medium.
- 0.5°
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42. A kit comprising:
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(a) an NMDAr antagonist; (b) an acetylcholinesterase inhibitor selected from the group consisting of donepezil, rivastigmine, tacrine, metrifonate, Huperzine-A; and (c) instructions for treating or preventing CNS related conditions such as Alzheimer'"'"'s disease, and wherein at least one of said NMDAr antagonist or said ACheI has an in vitro dissolution profile less than 70% in one hour, less than 90% in two hours, greater than 40% in six hours, and greater than 85% in 12 hours as measured using a USP type 2 (paddle) dissolution system at 50 rpm, at a temperature of 37±
0.5°
with water as a dissolution medium. - View Dependent Claims (43)
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47. A pharmaceutical composition comprising:
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(a) memantine in a dose ranging between 20 and 30 mg; and (b) donepezil in a dose ranging between 2 and 5 mg; wherein memantine and donezepil are both provided in an extended release dosage form, said extended release dosage form having an in vitro dissolution profile less than 70% in one hour, less than 90% in two hours, greater than 40% in six hours, and greater than 85% in 12 hours as measured using a USP type 2 (paddle) dissolution system at 50 rpm, at a temperature of 37±
0.5°
with water as a dissolution medium; - View Dependent Claims (48, 49)
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Specification