Microparticulate pharmaceutical forms resistant to immediate...

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/48 (2006.01) A61K 9/16 (2006.01) A61K 9/50 (2006.01) A61K 9/26 (2006.01) A61K 9/32 (2006.01) A61K 9/52 (2006.01)

Patent

CA 2649265

The invention aims at minimizing the risks of release of the dose associated with the concurrent consumption of alcohol and certain pharmaceutical or dietary forms with modified release. The invention concerns an oral form comprising reservoir-type microparticles, with modified release of at least one active principle. The invention is characterized in that it is resistant to the immediate release of the dose of active principle in the presence of alcohol. In particular, the inventive oral form is characterized in that the releasing time of 50% of the active principle, in an alcohol-containing solution is not reduced by more than 3 times compared to the releasing time of 50% of the active principle in an alcohol-free aqueous medium. The form comprises an agent D which is a pharmaceutically acceptable compound of which the hydrating or solvating speed and capacity is higher in an alcohol-free aqueous medium than in an alcohol-containing solution.

L'objectif de la présente invention est de minimiser les risques de décharge de la dose associée à la consommation concomitante d'alcool et de certaines formes pharmaceutiques ou diététiques à libération modifiée. L'invention vise une forme orale comprenant des microparticules de type réservoir, à libération modifiée d'au moins un principe actif (PA), caractérisée en ce qu'elle résiste à la décharge immédiate de la dose de PA en présence d'alcool. En particulier, la forme orale selon l'invent ion est caractérisée en ce que le temps de libération de 50 % du PA, dans une solution alcoolique n'est pas diminué de plus de 3 fois par rapport au temps de libération de 50 % du PA mesuré en milieu aqueux exempt d'alcool. La forme comprend un agent D qui est un composé pharmaceutiquement acceptable dont la vitesse ou la capacité à s'hydrater ou à se solvater est supérieure en milieu aqueux exempt d'alcool qu'en solution alcoolique.

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