Process for the preparation of accelerated release...

A - Human Necessities – 61 – K

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A61K 9/14 (2006.01) A61K 9/16 (2006.01)

Patent

CA 2403343

The following description refers to a process for the impregnation of cross- linked polymers with an active ingredient. The process is based on the used of compressed fluids, in particular C02, with antisolvent effect, and involves the steps of impregnating the polymer with an active ingredient solution, adding a compressed fluid until precipitation of the active ingredient caused by the compressed fluid antisolvent effect, removing the solvent and the compressed fluid. The process allows to obtain accelerated release pharmaceutical formulations that, compared with the formulations already known, contain larger quantities of amorphous or nanocrystalline active ingredient.

La présente invention concerne un procédé qui permet d'imprégner des polymères réticulés avec un ingrédient actif. Le procédé est fondé sur l'utilisation de fluides comprimés, plus particulièrement du CO¿2?, ayant un effet anti-solvant et comprend les étapes suivantes : on imprègne le polymère avec une solution d'ingrédient actif, on ajoute un fluide comprimé jusqu'à ce que ce produise la précipitation de l'ingrédient actif provoquée par l'effet anti-solvant du fluide comprimé, puis on élimine le solvant et le fluide comprimé. Ce procédé permet de produire des formulations pharmaceutiques à libération accélérée qui, comparativement aux formulations connues actuellement, contiennent de plus grandes quantités d'ingrédient actif amorphe ou nanocristallin. .

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