POLYMORPHIC FORMS OF RAMELTEON AND PROCESSES FOR PREPARATION THEREOF

摘要

An amorphous form of ramelteon is provided, as well as mixtures of amorphous and crystalline ramelteon. Also provided are methods of preparing amorphous ramelteon and mixtures of amorphous and crystalline ramelteon, pharmaceutical compositions comprising amorphous ramelteon and mixtures of amorphous and crystalline ramelteon, and methods of treatment of insomnia using the compositions of the invention. (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionainide, whose international nonproprietary name is ramelteon, has the following chemical structure Formula (I). Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 and MT2 receptors and selectivity over the MT3 receptor.