Formulating delayed release rasagiline. process for making rasagiline citrate

2010 
CLAIMS 1. A form of stable oral dosage characterized by comprising a core having rasagiline base form, which is the result of a production process, and at least one pharmaceutically acceptable excipient, and a coating resistant to pharmaceutically acceptable acid, wherein the production process comprising a) preparing the core by admixing rasagiline base form, citric acid and / or malic acid, and a pharmaceutically acceptable excipient; b) coating the core with resistant coating pharmaceutically acceptable acid. Claim 10: The dosage form of any of claims 1-9, wherein the core is a tablet. Claim 14: The dosage form of any of claims 1-13, wherein, in step b), the core is coated with a methacrylic-acrylic acid acetate (1: 1) and a plasticizer. Claim 17: The dosage form of any of claims 14-16, wherein, in step b), the plasticizer is triethyl citrate. Claim 18: The dosage form of any of claims 1-17, wherein, in step b), the acid resistant coating comprises two coating layers. Claim 21: A form of stable oral dosage characterized by comprising a core having rasagiline base form, the rasagiline citrate malate rasagiline, or a mixture of at least two of the following: rasagiline base form, the rasagiline citrate rasagiline malate, and at least one pharmaceutically acceptable excipient, and a coating resistant to pharmaceutically acceptable acid. Claim 64: A method for treating a patient suffering from Parkinson's disease, comprising administering to the patient the dosage form of any of claims 21-63. Claim 65: The method of claim 64, wherein the patient suffers from delayed gastric emptying. Claim 81: The composition of any of claims 72-7 8, characterized in that takes the form of a transdermal patch.
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