Use of R-enantiomer of N-propargyl-1-aminoindan, salts, compositions and uses thereof

Abstract

The subject invention provides methods of treating a subject afflicted with Parkinson's disease, memory disorder, depression, hyperactive syndrome, Attention Deficit Disorder, dementia, brain ischemia, stroke, head trauma injury, spinal trauma injury, neurotrauma, neurodegenerative disease, neurotoxic injury, multiple sclerosis, nerve damage, affective illness, schizophrenia or symptoms of withdrawal from an addictive substance, using the mesylate salt of R(+)-N-propargyl-1-aminoindan.

1 . An oral pharmaceutical dosage form comprising rasagiline and adapted to retard or inhibit the release of rasagiline in the stomach.  
   
   
       2 . The oral pharmaceutical dosage form of  claim 1  that is a tablet, a capsule, or a core sheathed in an annular body.  
   
   
       3 . The pharmaceutical dosage form of  claim 2  that is a tablet.  
   
   
       4 . The pharmaceutical dosage form of  claim 2  comprising an enteric coating.  
   
   
       5 . The pharmaceutical dosage form of  claim 2  that is a core sheathed in an annular body.  
   
   
       6 . The pharmaceutical dosage form of  claim 5 , wherein the core is a tablet.  
   
   
       7 . The pharmaceutical dosage form of any of  claim 5 , wherein the annular body is an annular sheath.  
   
   
       8 . The pharmaceutical dosage form of any of  claim 6 , wherein the core has an enteric coating.  
   
   
       9 . The pharmaceutical dosage form of  claim 2  that is a capsule.  
   
   
       10 . The pharmaceutical dosage form of  claim 9  comprising solid inactive particles.  
   
   
       11 . The pharmaceutical dosage form of  claim 10  wherein the particles are spheres, microparticles, nanoparticles or pellets made by spheronization, or a mixture thereof.  
   
   
       12 . The pharmaceutical dosage form of  claim 11  wherein the particles are spheres.  
   
   
       13 . The pharmaceutical dosage form of  claim 10 , wherein the particles are comprised of sugars, alcohols, polyols or celluloses, or mixtures thereof.  
   
   
       14 . The pharmaceutical dosage form of  claim 13  wherein the particles are comprised of sugars.  
   
   
       15 . The pharmaceutical dosage form of afy  claim 10 , wherein the solid inactive particles comprise rasagiline.  
   
   
       16 . The pharmaceutical dosage form of  claim 15 , wherein the particles are coated with rasagiline.  
   
   
       17 . The pharmaceutical dosage form of  claim 10 , wherein the particles comprise an enteric coating.  
   
   
       18 . The pharmaceutical dosage form of  claim 4 , wherein the enteric coating comprises polymeric methacrylate.  
   
   
       19 . The pharmaceutical dosage form of  claim 18 , wherein the polymeric methacrylate is methacrylic acid-ethyl acrylate copolymer (1:1) dispersion 30 percent.  
   
   
       20 . The pharmaceutical dosage form of  claim 4 , wherein the enteric coating further comprises a plasticizer.  
   
   
       21 . The pharmaceutical dosage form of  claim 20  wherein the plasticizer is triethyl citrate.  
   
   
       22 . The oral pharmaceutical dosage form of  claim 1 , wherein, upon administration to a patient, the rasagiline is released substantially in the intestinal tract.  
   
   
       23 . The oral pharmaceutical dosage form of  claim 22 , wherein the rasagiline is released substantially in the small intestine.  
   
   
       24 . The pharmaceutical dosage form of  claim 1  having a rasagiline release profile in a United States Pharmacopoeia Apparatus II of less than 10% dissolution in 500 ml 0.1N HCl at 37° C. and 50 rpm after 3 hours, and more than 90% dissolution in phosphate buffer at a pH of 6.8 after an additional 2 hours.  
   
   
       25 . A method of treating a patient suffering from Parkinson's disease, brain ischemia, head trauma injury, spinal trauma injury, neurotrauma, neurodegenerative disease, neurotoxic injury, nerve damage, dementia, Alzheimer's type dementia, senile dementia, depression, memory disorders, hyperactive syndrome, attention deficit disorder, multiple sclerosis, schizophrenia, or an affective illness, comprising administering to the patient the oral dosage form of  claim 1 .  
   
   
       26 . The method of  claim 25  for treating a patient suffering from Parkinson's disease.  
   
   
       27 . The method of  claim 26 , wherein the patient presents impaired gastric motility.  
   
   
       28 - 33 . (canceled)