Pharmaceutical compositions comprising cyclosporin for oral...

A - Human Necessities – 61 – K

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Details

A61K 38/13 (2006.01) A61K 9/00 (2006.01) A61K 9/08 (2006.01) A61K 9/107 (2006.01) A61K 9/48 (2006.01) A61K 47/10 (2006.01) A61K 47/14 (2006.01)

Patent

CA 2494762

The application discloses 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 triglycerol monoester of a fatty acid having from 6 to 30 carbon atoms or mixtures thereof, (c) polyethylene glycol, (d) a non ionic surfactant having a hydrophilic lipophilic balance (HLB) greater than 10, and (e) optionally, a viscosity reducing agent, the composition being substantially free from ethanol. The preferred carrier medium is triglycerol monooleate. Examples of the viscosity reducing agent are glycerol monocaprylate and glycerol monooleate.

L'invention concerne une composition pharmaceutique appropriée à l'administration orale se présentant sous forme d'une solution homogène qui suite à une exposition à l'eau ou aux fluides gastro-intestinaux constitue une émulsion dotée d'une taille particulaire inférieure à 5 microns. Cette solution contient (a) une quantité efficace pharmaceutiquement d'une cyclosporine, notamment, une cyclosporine A, (b) un milieu porteur renfermant un monoester de triglycérol d'un acide gras possédant de 6 à 30 atomes de carbones ou des mélanges correspondants, (c) un glycol de polyéthylène, (d) un agent de surface non ionique possédant un équilibre hydrophile lipophile supérieur à 10, et (e) facultativement un agent de diminution de la viscosité, ladite composition étant pratiquement exempte d'éthanol. Le milieu porteur préféré est un monooléate de triglycérol. Des exemples de l'agent de diminution de la viscosité sont le monocaprylate de glycérol et le monooléate de glycérol.

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