EP4691460A1 — Ramelteon sublingual film and preparation method therefor

USPTO Abstract

A ramelteon sublingual film and a preparation method therefor. The sublingual film at least comprises ramelteon, a film forming material, and one or more of a plasticizer, a disintegrating agent, a flavoring agent or a sweetener, and a stabilizer, wherein the ramelteon is in an amorphous state. The ramelteon is developed into a sublingual film, such that the ramelteon can be administrated through sublingual mucosa. The ramelteon is present in an amorphous state and is thus easier to absorb; the particle size of the ramelteon in the film is molecular-level dispersion, such that the ramelteon can be absorbed better, drugs are not easy to gather and recrystallize, the stability is better, and the solubility is good; the ramelteon can be completely dissolved in water within 1 min and rapidly absorbed by oral mucosa, thereby achieving the objective of rapid onset of action; absolute bioavailability is greater than 30%, and the ramelteon sublingual film has obviously higher bioavailability than that of an original tablet and a common film, and has more rapid onset of action, no food effect, low costs, and less side effects.