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Details for Patent: 6,852,729

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Details for Patent: 6,852,729

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 (Ettingen, CH)
Assignee: Novartis AG (Basel, CH)
Filing Date:Mar 21, 2003
Application Number:10/393,795
Claims:1. A process for stabilizing rapamycin or 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 comprising: a. dissolving the pure rapamycin or rapamycin derivative in an inert solvent; b. adding an antioxidant to the resulting solution in amount of up to 1% based on the rapamycin or rapamycin derivative weight; and c. isolating the resulting mixture of the rapamycin or rapamycin derivative and the antioxidant.

2. The process according to claim 1 wherein the antioxidant is added in an amount of from 0.01 to 0.5% based on the weight of the rapamycin or rapamycin derivative.

3. The process according to claim 2 wherein the antioxidant is added in an amount of 0.2% based on the weight of the rapamycin or rapamycin derivative.

4. The process of claim 1 in which the antioxidant is selected from the group consisting of 2,6-di-tert.butyl-4-methylphenol, vitamin E, vitamin C, and combinations thereof.

5. The process according to claim 4 wherein the antioxidant is 2,6-di -tert.butyl-4-methylphenol.

6. The process according to claim 1 wherein the rapamycin derivative is 40-O-(2-hydroxy)ethyl-rapamycin.

7. The process according to claim 1 wherein the rapamycin is in crystalline form.

8. The process according to claim 1 wherein the resulting mixture is isolated in the form of a solid mixture.

9. The process according to claim 1 wherein the rapamycin or rapamycin derivative is processed into a pharmaceutical composition.

10. A mixture in solid form comprising rapamycin or 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, and an antioxidant wherein the antioxidant is present in an amount of up to 1% based on the rapamycin or rapamycin derivative weight.

11. The mixture according to claim 10 wherein the antioxidant is present in an amount of from 0.01to 0.5% based on the weight of the rapamycin or rapamycin derivative.

12. The mixture according to claim 10 wherein the antioxidant is present in an amount of 0.2% based on the weight of the rapamycin or rapamycin derivative.

13. The mixture of claim 10 in which the antioxidant is selected from the group consisting of 2,6-di-tert.butyl-4-methylphenol, vitamin E, vitamin C, and combinations thereof.

14. The mixture according to claim 13 wherein the antioxidant is 2,6-di-tert.butyl-4-methylphenol.

15. The mixture according to claim 10 wherein the rapamycin derivative is 40-O-(2-hydroxy)ethyl-rapamycin.

16. The mixture according to claim 15 wherein the 40-O-(2-hydroxy)ethyl-rapamycin is in amorphous form.

17. The mixture according to claim 15 wherein the 40-O-(2-hydroxy-ethyl)-rapamycin is in crystalline form.

18. The mixture according to claim 17 wherein the 40-O-(2-hydroxy-ethyl)-rapamycin is in crystalline non-solvate form.

19. The mixture according to claim 17 wherein the 40-O-(2-hydroxy-ethyl)-rapamycin has a crystal lattice as follows: a=14.37 .ANG., b=11.24.ANG., c=18.31 .ANG., the volume being 2805 .ANG..sup.3.

20. A mixture in solid form comprising a rapamycin or 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, and an antioxidant wherein the antioxidant is present in an amount of up to 1% based on the rapamycin or rapamycin derivative weight, wherein the rapamycin or a rapamycin derivative is prepared by a process comprising: a. dissolving the pure rapamycin or rapamycin derivative in an inert solvent; b. adding an antioxidant to the resulting solution in amount of up to 1% based on the rapamycin or rapamycin derivative weight; and c. isolating the resulting mixture of the rapamycin or rapamycin derivative and the antioxidant.

21. A process for preparing 40-O-(2-hydroxy-ethyl)-rapamycin in substantially pure form, comprising crystallizing 40-O-(2-hydroxy-ethyl)-rapamycin from a crystal bearing medium and recovering the crystals thus obtained.

22. The compound 40-O-(2-hydroxy-ethyl)-rapamycin according to claim 21 which is in crystalline non-solvate form.

23. The compound 40-O-(2-hydroxy-ethyl)-rapamycin according to claim 21 having a crystal lattice as follows: a=14.37 .ANG., b=11.24.ANG., c=18.31 .ANG., the volume being 2805 .ANG..sup.3.
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