Compositions and methods for treating alzheimer's disease and parkinson's disease

Abstract

The present invention is directed to tablets for oral administration to a subject, comprising a therapeutically effective amount of SYN120 or a pharmaceutically acceptable salt thereof, wherein the tablet is substantially free of lactose. The present invention is also directed to methods for treating diseases or conditions including Alzheimer's disease and/or Parkinson's disease, comprising administering to a patient in need thereof tablets regarding the same.

What is claimed is: 
     
         1 . A tablet comprising a therapeutically effective amount of SYN120 or a pharmaceutically acceptable salt thereof, wherein the tablet is substantially free of lactose. 
     
     
         2 . The tablet of  claim 1 , wherein said tablet is substantially free of isomers of lactose selected from the group consisting of sucrose, trehalose, maltose, isomaltose, maltulose, isomaltulose, turanose, and cellobiose. 
     
     
         3 . The tablet of  claim 1 , wherein said tablet is substantially free of all isomers of lactose. 
     
     
         4 . The tablet of  claim 3 , wherein said tablet is substantially free of reducing sugars selected from the group consisting of galactose, glucose, fructose, ribose, xylose, and isomers thereof. 
     
     
         5 . The tablet of  claim 4 , wherein said tablet is substantially free of any reducing sugar or an isomer thereof. 
     
     
         6 . The tablet of  claim 1 , wherein said tablet comprises about 2.5 mg to about 200 mg of SYN120 or a pharmaceutically acceptable salt thereof. 
     
     
         7 . The tablet of  claim 1 , wherein said tablet comprises about 50 mg to about 100 mg of SYN120 or a pharmaceutically acceptable salt thereof. 
     
     
         8 . The tablet of  claim 1 , wherein said tablet comprises about 5 mg to about 15 mg of SYN120 or a pharmaceutically acceptable salt thereof. 
     
     
         9 . The tablet of  claim 1 , wherein said tablet is an immediate release tablet. 
     
     
         10 . The tablet of  claim 1 , wherein at least about 90% of said SYN120 or a pharmaceutically acceptable salt thereof is released in 60 minutes when tested for dissolution using a USP II paddle apparatus at a speed of 75 rpm in 900 mL of 0.2% w/v Sodium Lauryl Sulfate (SLS) in pH 1.2 Hydrochloric Acid (37% v/v) at 37° C. 
     
     
         11 . The tablet of  claim 1 , wherein at least about 80% of said SYN120 or a pharmaceutically acceptable salt thereof is released in 30 minutes when tested for dissolution using a USP II paddle apparatus at a speed of 75 rpm in 900 mL of 0.2% w/v Sodium Lauryl Sulfate (SLS) in pH 1.2 Hydrochloric Acid (37% v/v) at 37° C. 
     
     
         12 . The tablet of  claim 1 , wherein at least about 70% of said SYN120 or a pharmaceutically acceptable salt thereof is released in 15 minutes when tested for dissolution using a USP II paddle apparatus at a speed of 75 rpm in 900 mL of 0.2% w/v Sodium Lauryl Sulfate (SLS) in pH 1.2 Hydrochloric Acid (37% v/v) at 37° C. 
     
     
         13 . The tablet of  claim 1 , wherein said tablet is substantially free of mannitol. 
     
     
         14 . The tablet of  claim 1 , wherein said tablet is substantially free of all isomers of mannitol. 
     
     
         15 . The tablet of  claim 1 , wherein said tablet is substantially free of the compounds selected from the group consisting of sorbitol, xylitol, erythritol, lactitol, and maltitol. 
     
     
         16 . The tablet of  claim 1 , wherein said tablet has a mean tablet hardness of about 4 kP to about 15 kP. 
     
     
         17 . The tablet of  claim 1 , wherein said tablet additionally comprises microcrystalline cellulose. 
     
     
         18 . The tablet of  claim 17 , wherein said microcrystalline cellulose is a microcrystalline cellulose prepared by partial depolymerization of alpha-cellulose having a nominal particle size of about 20 μm to about 180 μm. 
     
     
         19 . The tablet of  claim 1 , wherein after the administration of a single tablet to a patient, the tablet provides a SYN120 T max  ranging from about 1 hr to about 4 hrs. 
     
     
         20 . The tablet of  claim 1 , wherein after the administration of a single tablet to a patient, the tablet provides a SYN120 mean T max  ranging from about 1.5 hrs to about 5 hours. 
     
     
         21 . The tablet of  claim 1 , wherein after the administration of a single tablet to a patient, the tablet provides a SYN120 mean C max  ranging from about 4 ng/mL to 6.5 ng/mL per mg dosed. 
     
     
         22 . The tablet of  claim 1 , wherein after administration of a single tablet to a patient, the tablet provides a SYN120 mean AUC 0-24  ranging from about 100 ng-hr/mL to about 6,000 ng-hr/mL. 
     
     
         23 . The tablet of  claim 1 , wherein after administration of a single tablet to a patient, the tablet provides a SYN120 mean AUC 0-inf  ranging from about 100 ng-hr/mL to about 7,500 ng-hr/mL. 
     
     
         24 . A method of treating a cognitive condition or disease in a subject, comprising administering to a subject in need thereof the tablet of  claim 1 . 
     
     
         25 . The method of  claim 24 , wherein the subject is suffering from a disease or condition selected from the group consisting of Alzheimer's disease, Parkinson's disease, Huntington's disease, dementia, Lewy Body Dementia, frontotemporal dementia, Down's Syndrome, autism, cognitive impairment associated with schizophrenia, cognitive impairment associated with multiple sclerosis, anxiety, depression, manic depression, psychoses, epilepsy, autism, obsessive compulsive disorders, mood disorders, migraine, sleep disorders, eating disorders, anorexia, bulimia, obesity, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from drug abuse, schizophrenia, neurological disorders associated with spinal trauma, neurological disorders associated with head injury, neurological disorders associated with stroke, neurological disorders associated with cerebral vascular disease, and functional bowel disorder. 
     
     
         26 . A method of improving cognitive function of a subject, comprising administering to a subject in need thereof a tablet of  claim 1 . 
     
     
         27 . The method of  claim 26 , wherein the subject has been diagnosed with Alzheimer's disease. 
     
     
         28 . The method of  claim 26 , wherein the subject has been diagnosed with Parkinson's disease. 
     
     
         29 . The method of  claim 24 , wherein said administering comprises administering a 50 mg tablet of SYN120 once per day for 7 days, then administering a 100 mg tablet of SYN120 once per day for 7 days, and then administering a 100 mg or 200 mg tablet of SYN120 once per day thereafter.