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|Abstract:||A mixture comprising a poly-ene macrolide and an antioxidant. Preferably, the poly-ene macrolide is rapamycin and the antioxidant is 2,6-di-tert.-butyl-4-methylphenol. The presence of the antioxidant improves the stability of the poly-ene macrolide to oxidation.|
|Inventor(s):||Navarro; Fran.cedilla.ois (Bruebach, FR), Petit; Samuel (Mont Saint-Aignan, FR), Stone; Guy (Ettingen, CH)|
|Assignee:||Novartis AG (Basel, CH)|
|Filing Date:||May 29, 2001|
|Claims:||1. A composition comprising a rapamycin derivative selected from the group consisting of 40-O-(2-hydroxy)ethyl-rapamycin, 40-O-(3-hydroxy)propyl-rapamycin, and 40-O-[2-(2-hydroxy)ethoxy]ethyl-rapamycin, or rapamycin; and an antioxidant selected from the group consisting of 2,6-di-tert.-butyl-4-methylphenol, vitamin C, and combinations thereof, wherein the rapamycin derivative or rapamycin is in crystalline form. |
2. The composition according to claim 1 wherein the 40-O-(2-hydroxy)ethyl-rapamycin has a crystal lattice a=14.37 .ANG., b=11.24 .ANG., c=18.31 .ANG., the volume being 2805 .ANG..sup.3.
3. The composition according to claim 1 wherein the antioxidant is present in an amount of up to 1 weight percent, based on the weight of the rapamycin derivative or rapamycin.
4. The composition according to claim 3 wherein the antioxidant is present in an amount of 0.2 weight percent.
5. The composition according to claim 1 wherein the antioxidant is 2,6-di-tert.-butyl-4-methylphenol.