Process for the purification of cyclosporin

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 7/64 (2006.01) C07K 1/16 (2006.01)

Patent

CA 2096892

A process is disclosed for the solution chromatographic purification of cyclosporin A from a starling mixture containing one or more of cyclosporin A, B, C, other cyclosporin components that are more polar or more apolar than cyclosporin A, and other like contaminants, by heating the starting mixture or an evaporation residue thereof to a temperature from about 80°C to about 115°C, melting the heated starting mixture, and carrying out solution chromatography of the melted material, suitably first in a 48 : 50 : 2 mixture of chloroform, methylene chloride, and ethanol, and then in a mixture of like proportions, of the solvents chloroform, ethyl acetate, and ethanol.

L'invention porte sur la purification chromatographique en solution de la cyclosporine A à partir d'un mélange de départ renfermant une ou plusieurs cyclosporines A, B, C, d'autres constituants de type cyclosporine, qui sont plus polaires ou plus apolaires que la cyclosporine A, et d'autres contaminants analogues, par chauffage du mélange de départ ou d'un résidu d'évaporation de ce mélange à une température d'environ 80 à 115 degrés C, fusion du mélange de départ ainsi chauffé et chromatographie en solution du produit fondu, d'abord dans un mélange 48 : 50 : 2 de chloroforme, de chlorure de méthylène et d'éthanol, puis dans un mélange en proportions comparables de chloroforme, d'acétate d'éthyle et d'éthanol.

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