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Abstract

The present invention relates to the stabilization of a pharmaceutically active oxidation sensitive ingredient, for example a polyene macrolide, preferably a polyene macrolide having immunosuppressive properties, particularly rapamycins and a particular macrolide obtained in crystalline form. A procedure for stabilizing a polyene macrolide comprising: a. dissolve the pure macrolide in an inert solvent; b. adding an antioxidant to the resulting solution; and c. Isolate the resulting mixture of the polyene macrolide and the antioxidant. A process according to Claim 1, characterized in that the antioxidant is added in an amount of up to 1% based on the weight of the macrolide. A method according to Claim 2, characterized in that the antioxidant is added in an amount of from 0.01 to 0.5% based on the weight of the macrolide. A process according to Claim 3, characterized in that the antioxidant is added in an amount of 0.2% based on the weight of the macrolide. A process according to any one of Claims 1 to 4, characterized in that the antioxidant is 2,6-di-tert-butyl-4-methylphenol. A process according to any one of Claims 1 to 5, characterized in that the polyene macrolide is rapamycin or 40-O- (2-hydroxy) ethyl-rapamycin. A process according to Claim 6, characterized in that the macrolide used in step a) is 40-0- (2-hydroxy) ethyl-rapamycin or rapamycin in crystalline form. A method according to any one of Claims 1 to 7, characterized in that the resulting mixture is isolated in the form of a solid mixture.

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First Claim

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