Compositions comprising microparticles of water-insoluble...

A - Human Necessities – 61 – K

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A61K 9/16 (2006.01) A61K 9/14 (2006.01) A61K 9/51 (2006.01)

Patent

CA 2263102

Submicron size particles of pharmaceutical or other water-insoluble or poorly water-insoluble substances are prepared using a combination of one or more surface modifiers/surfactants such as polaxomers, poloxamines, polyoxyethylene sorbitan fatty acid esters and the like together with natural or synthetic phospholipids. Particles so produced have a volume weighted mean particle size at least one-half smaller than obtainable using a phospolipid alone. Compositions so prepared are resistant to particle size growth on storage.

On prépare des particules, de taille inférieure au micron, de substances pharmaceutiques ou d'autres substances insolubles dans l'eau ou à faible pouvoir d'insolubilité dans l'eau, en utilisant une combinaison d'un ou de plusieurs modificateurs de surface/tensioactifs tels que des polaxomères, poloxamines, esters d'acides gras à base de polyoxyéthylène sorbitane et analogues, à laquelle on ajoute des phospholipides naturels ou synthétiques. Des particules ainsi produites présentent une dimension de particule moyenne, pondérée en fonction du volume, qui est au moins moitié plus petite que celle pouvant être obtenue à l'aide d'un phospholipide seul. Des compositions ainsi préparées résistent à la croissance particulaire lors du stockage.

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