Improved nanoparticulate compositions of poorly soluble...

A - Human Necessities – 61 – K

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A61K 9/50 (2006.01) A61K 9/51 (2006.01) A61K 31/00 (2006.01)

Patent

CA 2739499

The present invention relates to a method for the production of a nanoparticulate pharmaceutical composition. The method comprises the steps of a) suspending in water a poorly soluble active ingredient without the presence of a detergent, b) mechanically treating said suspension to obtain particles comprising the active ingredient with an effective average size of less than about 5000 nm, c) contacting said active ingredient or suspension with a first polyelectrolyte during and/or before mechanically treating, d) optionally contacting said suspension with a one or more second or further polyelectrolytes during, before and/or after mechanically treating, e) optionally drying said suspension. The invention also pertains to the pharmaceutical compositions obtained by the method of the invention.

La présente invention concerne un procédé de production dune composition pharmaceutique nanoparticulaire. Le procédé comprend les étapes consistant à a) suspendre dans leau un ingrédient actif faiblement soluble sans la présence dun détergent, b) traiter mécaniquement ladite suspension afin dobtenir des particules comprenant lingrédient actif ayant une taille moyenne effective inférieure à environ 5 000 nm, c) mettre en contact ledit ingrédient actif ou sa suspension avec un premier polyélectrolyte pendant et/ou avant le traitement mécanique, d) éventuellement mettre en contact ladite suspension avec un ou plusieurs second ou plusieurs polyélectrolytes pendant, avant et/ou après le traitement mécanique, e) éventuellement sécher ladite suspension. Linvention concerne également les compositions pharmaceutiques obtenues par le procédé de linvention.

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