Water soluble nanoparticles comprising inclusion complexes

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) A01N 25/04 (2006.01) A01N 43/653 (2006.01) A61P 5/32 (2006.01) A61P 25/28 (2006.01) A61P 31/04 (2006.01) A61P 31/10 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2540104

Nano-dispersions of water-soluble and stable nano-sized particlesare provided comprising hydrophilic inclusion complexes of an active compound in a non- crystalline state surrounded by and entrapped within an amphiphilic polymer. The inclusion complex is stabilized by non-valent interactions between the active compound and the polymer. The following pairs of active compound/amphiphilic polymers are provided: (i) azithromycin/ a polysaccharide or polyvinyl alcohol, or clarithromycin/alginate or chitosan; (ii) donepezil hydrochloride/ a polysaccharide; (iii) an azole compound/a polysaccharide, polyacrylic acid, a copolymer of polyacrylic acid, polymethacrylic acid and a copolymer of polymethacrylic acid; and (iv) a taxane/gelatin.

La présente invention a trait à des nanodispersions de particules hydrosolubles de taille nanométrique comportant des complexes d'inclusions hydrophiles d'un composé actif dans un état non cristallin enrobés et retenus au sein d'un polymère amphiphile. Le complexe d'inclusions est stabilisé par des interactions non covalentes entre le composé actif et le polymère. L'invention a trait aux paires suivantes de composé actif/polymères amphiphiles : (i) azithromycine/un polysaccharide ou alcool polyvinylique, ou clarithromycine/alginate ou chitosane ; (ii) chlorhydrate de donepezile/un polysaccharide ; (iii) un composé azole/un polysaccharide, l'acide polyacrylique, un copolymère d'acide polyacrylique, l'acide polyméthacrylique et un copolymère d'acide polyméthacrylique ; et (iv) un taxane/gélatine.

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