Nanoparticle compositions of water-soluble drugs for oral...

A - Human Necessities – 61 – K

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A61K 47/44 (2006.01) A61K 9/14 (2006.01)

Patent

CA 2549383

The present invention relates to an orally administrable composition containing nanoparticles with the particle size of 500 nm or less, comprising 0.130 weight% of a complex of a water-soluble drug and a counter-ion substance in which -the charged water-soluble drug is bonded with the counter-ion substance, 0.5-80 weight% of a lipid, 0.5-80 weight% of a polymer, and 1-80 weight% of an emulsifier, wherein the weight ratio of said lipid and said polymer is in the range of 1:0.053, and a preparation method thereof. The composition of the present invention has high gastrointestinal absorption rate upon oral administration, and has high drug entrapping rate in the nanoparticle, and is also stable against lipases.

La présente invention concerne une composition pouvant être administrée par voie orale contenant des nanoparticules avec une dimension de particule de 500 nm ou moins, comprenant 0,1~30 % en pois d'un complexe d'un médicament soluble dans l'eau et une substance à contre-ions à laquelle est lié le médicament chargé soluble dans l'eau, 0,5~80 % en poids d'un lipide, 0,5~80 % en poids d'un polymère, 1~80 % en poids d'un émulsifiant, le rapport de pondération dudit lipide et dudit polymère étant de 1:0,05~3, et une méthode de préparation de ladite composition. La composition de la présente invention présente un taux d'absorption gastro-intestinale élevé lors d'une administration orale et un taux de piégeage de médicament élevé dans la nanoparticule, et est également stable par rapport aux lipases.

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