Details for Patent: 6,605,613

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.