Novel cyclosporine preparation forms for oral administration...

A - Human Necessities – 61 – K

Patent

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Details

A61K 38/13 (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 2231404

The invention relates to novel preparation forms of cyclosporine of simple composition and high bio-availability for oral administration, containing 0,5 to 2 parts by weight (p/wt) of one or more amorphous cyclosporine(s), preferably cyclosporine A and/or cyclosporine G and 6 to 9 p/wt of one or mone polyethylene glycol ester(s) of saturated C10- C22 hydroxy fatty acids, especially SOLUTOL® HS 15, and 1-3 p/wt of one or more monovalent or multivalent alcohols, preferably ethanol and propylene glycol. The medical form is produced by first dissolving the amorphous cyclosporing in ethanol and adding under agitation propylene glycol and SOLUTOL® until a clear, viscous solution is obtained, which is packed as a drinking solution or capsules in the prior art manner.

L'invention concerne de nouvelles formes de préparations de cyclosporines, de composition simple et haute biodisponibilité, pour l'administration par voie orale, contenant 0,5 à 2 parties en poids d'au moins une cyclosporine amorphe, de préférence la cyclosporine A et/ou la cyclosporine G, et 6 à 9 parties en poids d'au moins un ester de polyéthylène-glycol d'acides gras hydroxy saturés C10-C22, en particulier de SOLUTOL3 HS 15, ainsi que 1 à 3 parties en poids d'au moins un alcool monovalent ou multivalent, de préférence de l'éthanol et du propylène-glycol. On produit la forme médicale d'une telle préparation en faisant d'abord dissoudre la cyclosporine amorphe dans l'éthanol puis en ajoutant, en maintenant la solution sous agitation, le polypropylène-glycol et le SOLUTOL3 jusqu'à obtention d'une solution claire et visqueuse, laquelle est, enfin, conditionnée de manière connue en soi sous forme de solution buvable ou de capsules.

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