Details for Patent: 7,572,804

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; Francois (Bruebach, FR), Petit; Samuel (Mont Saint-Aignan, FR), Stone; Guy (Crosshaven Co. Cork, IE)
Assignee:	Novartis AG (Basel, CH)
Filing Date:	Oct 11, 2007
Application Number:	11/973,927
Claims:	1. A pharmaceutical composition comprising a crystalline form of 40-O-(2-hydroxy)ethyl-rapamycin having a crystal lattice a=14.37 .ANG., b=11.24 .ANG., c=18.31 .ANG., the volume being 2805 .ANG..sup.3, together with one or more pharmaceutically acceptable diluents or carriers. 2. The pharmaceutical composition according to claim 1 for oral administration. 3. A method for preventing or treating acute or chronic allo- or xeno-transplant rejection in a subject in need of such treatment, comprising administering to said subject a therapeutically affective amount of the pharmaceutical composition according to claim 1. 4. A process for preparation of a crystalline form of 40-O-(2-hydroxy)ethyl-rapamycin having a crystal lattice a=14.37 .ANG., b=11.24 .ANG., c=18.31 .ANG., the volume being 2805 .ANG..sup.3, comprising dissolving amorphous 40-O-(2-hydroxy)ethyl-rapamycin in ethyl acetate and adding an aliphatic hydrocarbon CnH2n+2, wherein n=5, 6 or 7, and recovering the crystals thus obtained. 5. A process for purifying a crystalline form of 40-O-(2-hydroxy)ethyl-rapamycin having a crystal lattice a=14.37 .ANG., b=11.24 .ANG., c=18.31 .ANG., the volume being 2805 .ANG..sup.3, comprising crystallizing 40-O-(2-hydroxy)ethyl-rapamycin from a crystal bearing medium comprising ethyl acetate and an aliphatic hydrocarbon, and recovering the crystals thus obtained. 6. The process according to claim 5, wherein the crystal bearing medium comprises 2 parts ethyl acetate and 5 parts aliphatic hydrocarbon C.sub.nH.sub.2n+2, wherein n=5, 6 or 7.