|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|
|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.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.