Pharmaceutical formulation comprising cyclosporin, propylene...

A - Human Necessities – 61 – K

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A61K 9/48 (2006.01) A61K 9/00 (2006.01) A61K 9/107 (2006.01) A61K 38/13 (2006.01) A61K 47/14 (2006.01)

Patent

CA 2494796

The application discloses a pharmaceutical composition suitable for oral administration in the form of a homogeneous solution which on exposure to water or gastrointestinal fluids forms an emulsion having a particle size of less than 5 microns, the solution comprising: (a) a pharmaceutically effective amount of a cyclosporin, in particular Cyclosporin A, (b) a carrier medium comprising a mixture of mono-and diesters of propylene glycol with fatty acids having from 8 to 10 carbon atoms or with mixtures of such fatty acids, wherein the monoester makes up less than 60mol% of the mixture, and (c) a non-ionic surfactant having a hydrophilic lipophilic balance (HLB) greater than 10.

L'invention concerne une composition pharmaceutique destinée à être administrée par voie orale sous forme d'une solution homogène qui, lorsqu'elle est exposée à de l'eau ou à des fluides gastro-intestinaux, forme une émulsion qui présente une taille particulaire inférieure à 5 microns. Cette solution comprend: (a) une dose pharmaceutiquement efficace d'une cyclosporine, en particulier la cyclosporine A; (b) un support qui comporte un mélange de mono- et de diesters du propylène glycol avec des acides gras qui possèdent entre 8 et 10 atomes de carbone ou avec des mélanges de ces acides gras, le monoester représentant moins de 60 % molaire du mélange; et (c) un tensioactif non ionique présentant un rapport hydro-lipophile (HLB) supérieur à 10.

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