Film dosage forms containing amorphous active agents
AssigneeIntelgenx Corp.
InventorsNadine Paiement, Rodolphe Obeid, Billal Tir
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Abstract
Oral thin film dosage form of a stable dispersion of non-solubilized amorphous or partially amorphous active agent(s), having a mean particle size diameter D50 equal or lower than 250 μm, that remains uniformly distributed within a film matrix and contains at least one film former polymer, and optional pharmaceutically-acceptable excipients, such as diluents, plasticizers, surfactants, sweeteners, and taste-masking agent(s). The oral thin film dosage exhibits increased solubility or rate of dissolution and enhanced bioavailability compared to a crystalline form of the active agent(s). The oral dosage form also exhibits long term stability confirmed by no changes in the dissolution profile over time.
Claims25
An oral film dosage form of a stable dispersion of non-solubilized amorphous or partially amorphous active agent(s), having a mean particle size diameter D50 equal or lower than 250 μm, that remains uniformly distributed within a film matrix and contains at least one film former polymer, and one or more optional pharmaceutically-acceptable excipients selected from diluents, plasticizers, surfactants, sweeteners, and taste-masking agent(s).
A process for preparing an oral film dosage form containing an active agent in an amorphous form, comprising:
- providing the active agent in an amorphous particle form having a mean particle size diameter D50 equal or lower than 250 μm;
- providing a liquid film-forming formulation including at least one film-forming polymer and a solvent system including at least one solvent, and optionally including one or more pharmaceutically acceptable excipients selected from diluents, plasticizers, surfactants, sweeteners and taste-masking agents;
- suspending the active agent in the amorphous particle form in the liquid film-forming formulation without dissolving the active agent;
- and
- removing the solvent system to form a film containing the active agent in the amorphous form and retaining a mean particle size diameter D50 equal or lower than 250 μm.
An oral dosage form of amorphous or partially amorphous active agent(s) uniformly distributed in a polymer film, the dosage form maintaining phase stability of the active agent(s) as characterized by a dissolution profile after exposure to adverse conditions of a temperature of 40° C. and a relative humidity of 75% for a period of six months that is within 10% of a dissolution profile determined before the exposure to the adverse conditions.
Dependencies are inferred from the claim text.