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
Inventors
Herry, Catherine • Billoet, Vincent • Oury, Pascal
Assignees
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Publication Number
US-9603797-B2
Publication Date
2017-03-28
Expiration Date
Abstract
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.
Core Innovation
The invention relates to an oral and/or buccal composition in the form of a thin film of a pharmaceutically active ingredient having low solubility in water and gastrointestinal tract fluids and belonging to classes II and IV of the BCS classification. The problem addressed is the low solubility of such active ingredients in water and gastrointestinal tract fluids, which complicates effective formulation for oral and/or buccal delivery.
The approach suspends the active ingredient in a solvent in which it is not soluble, and subjects the suspension to wet-process ball nano-milling until 90% of the particles have a size with D(90) of less than 1000 nm. The milled active ingredient forms a nanosuspension that is uniformly mixed with at least one film-forming polymer.
The resulting composition is converted into a thin film with particles of the active ingredient dispersed in the film-forming polymer, and the composition is characterized by a final water content of from 1% to 5% (w/w). This combination of nanometric particle dispersion within a film-forming polymer and controlled final water content is used to prepare the oral and/or buccal thin-film composition for BCS II and IV low-solubility actives.
Claims Coverage
The document contains one independent claim. It defines a successively performed process for preparing an oral and/or buccal thin film, with inventive features centered on (i) nanosuspension formation by wet-process ball nano-milling to a defined D(90) particle size and (ii) thin-film conversion with particles dispersed in a film-forming polymer while maintaining a final water content of 1% to 5% (w/w).
Wet-process ball nano-milling to nanosuspension for BCS II/IV low-solubility thin film
The process suspends the active ingredient in a solvent in which it is not soluble and mils the suspension in a wet-process ball nano-mill until 90% of the particles of the active ingredient have a size with D(90) of less than 1000 nm.
Uniform mixing with film-forming polymer and conversion to thin film with controlled water content
The nanosuspension is uniformly mixed with at least one film-forming polymer and the composition is converted into a thin film having particles of the active ingredient dispersed in the film-forming polymer and having a final water content of from 1% to 5% (w/w).
Across the independent claim, the main inventive coverage is the sequential preparation of a nanosuspension by wet-process ball nano-milling to a D(90) below 1000 nm, followed by uniform mixing with film-forming polymer and conversion into a thin film with a final water content between 1% and 5% (w/w).
Stated Advantages
Documented Applications
No documented applications found
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