Process for the preparation of crystalline nano-particle...

Details Process for the preparation of crystalline nano-particle... Process for the preparation of crystalline nano-particle...

A - Human Necessities

61

K

A61K 9/10 (2006.01) A61K 9/14 (2006.01) A61K 9/51 (2006.01)

Patent

CA 2492709

A process for the preparation of a dispersion of crystalline nano-particles in an aqueous medium comprising combining (i) a first solution comprising a substantially water-insoluble substance in a water-miscible organic solvent with; (ii) an aqueous phase comprising water and optionally a stabiliser, to form a dispersion of amorphous particles; and (iii) sonicating the dispersion of amorphous particles for a sufficient period to form crystalline nano- particles of the substantially water-insoluble substance. The process provides nano-crystals with a mean hydrodynamic diameter of less than 1 micron, particularly less than 300 nm and is particularly useful for the preparation of nano-crystalline dispersions of pharmaceutical substances.

L'invention a trait à un procédé de préparation d'une dispersion de nanoparticules cristallines dans un milieu aqueux. Ledit procédé consiste : à combiner (i) une première solution contenant une substance sensiblement insoluble dans l'eau dans un solvant organique miscible dans l'eau, avec (ii) une phase aqueuse contenant de l'eau et éventuellement un stabilisant, afin de former une dispersion de particules amorphes ; et (iii) à procéder à la sonification de la dispersion de particules amorphes, pendant un temps suffisant pour que se forment des nanoparticules cristallines de la substance sensiblement insoluble dans l'eau. Le procédé permet d'obtenir des nanocristaux présentant un diamètre hydrodynamique moyen inférieur à 1 micron, en particulier inférieur à 300 nm. Ledit procédé est notamment utile à la préparation de dispersions nanocristallines de substances pharmaceutiques.

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