Method for converting sparingly water-soluble medical...

A - Human Necessities – 61 – K

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A61K 9/14 (2006.01) A61J 3/00 (2006.01) A61K 9/10 (2006.01)

Patent

CA 2228907

A process for preparing a solid dispersion of a hardly soluble medicine which comprises heating the hardly soluble medicine, an amorphism-inducing agent and an amorphism stabilizer or mechanochemically treating the same; and a process for producing a solid dispersion of a hardly soluble medicine which comprises high-frequency heating the hardly soluble medicine and an amorphism stabilizer. These processes make it possible to make hardly soluble medicines amorphous at a temperature lower than those employed in the conventional methods. The solid dispersions of the amorphous hardly soluble medicines thus obtained have an improved mucosal or rectal adsorption rate, which makes it possible to elevate their bioavailability.

Cette invention concerne un procédé de préparation d'une dispersion solide d'un médicament peu soluble, lequel procédé consiste à chauffer le médicament peu soluble, un agent inducteur d'état amorphe et un stabilisateur d'état amorphe, ou encore à effectuer un traitement mécanique et chimique de ces derniers. Cette invention concerne également un procédé de production d'une dispersion solide d'un médicament peu soluble, lequel procédé consiste à chauffer à haute fréquence le médicament peu soluble et un stabilisateur d'état amorphe. Ces procédés permettent de rendre amorphes des médicaments peu solubles à des températures inférieures à celles auxquelles on a recours dans les procédés traditionnels. Les dispersions solides de médicaments peu solubles et amorphes ainsi obtenues ont un meilleur taux d'adsorption rectal et dans les muqueuses, ce qui permet d'accroître leur biodisponibilité.

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