Oral and/or buccal composition in the form of a thin film of a weakly soluble active ingredient, method of preparing same and use of same

摘要

The present invention relates to an oral and/or buccal composition in the form of a thin film of a pharmaceutically active ingredient weakly soluble in water and gastro-intestinal tract fluids, comprising particles of said active ingredient dispersed in a film-forming polymer, at least 50% by weight of the total weight of the active ingredient having a particle size distribution such that at least 90% of said particles have a size below 1000 nm, preferably less than 800 nm, and even more preferably less than 600 nm, and to the method of preparing that composition and the use thereof.

主权项

1. A process for preparing an oral and/or buccal composition in the form of a thin film of a pharmaceutically active ingredient which has low solubility in water and gastrointestinal tract fluids and which belongs to classes II and IV of the BCS classification, according to which, successively:
the active ingredient is suspended in a solvent in which it is not soluble, the suspension thus obtained is milled in a wet-process ball nano-mill until 90% of the particles of the active ingredient (D(90)) have a size of less than 1000 nm, the nanosuspension thus obtained is uniformly mixed with at least one film-forming polymer, the composition thus obtained is converted into a thin film, said composition thus prepared having particles of said active ingredient dispersed in said film-forming polymer and having a final water content of from 1% to 5% (w/w).