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Generated: January 23, 2018

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Title: Macrolides
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
Application Number:09/866,977
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.
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