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Claims for Patent: 7,297,703

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Claims for Patent: 7,297,703

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)
Application Number:11/020,860
Patent Claims: 1. A solid mixture comprising a poly-ene macrolide and an antioxidant wherein the poly-ene macrolide is selected from the group consisting of rapamycin, a 16-O-substituted rapamycin, and a 40-O-substituted rapamycin and wherein the antioxidant is present in a catalytic amount.

2. A mixture according to claim 1, wherein the antioxidant is present in an amount of up to 1% based on the poly-ene macrolide weight.

3. A mixture according to claim 1 or 2, wherein the antioxidant is present in an amount of 0.01 to 0.5% based on the macrolide weight.

4. A mixture according to claim 3, wherein the antioxidant is selected from the group consisting of vitamin B, vitamin C, 2,6-di-tert-butyl-4-methylphenol (BHT), and combinations thereof.

5. A mixture according to claim 3, wherein the antioxidant is present in an amount of 0.2% based on the macrolide weight.

6. A pharmaceutical composition comprising as active ingredient, a mixture according to claim 1 or 2, admixed with one or more pharmaceutically acceptable carriers or diluents.

7. A pharmaceutical composition according to claim 6 for oral administration.

8. A process for stabilizing a poly-ene macrolide selected from the group consisting of rapamycin, a 16-O-substituted rapamycin, and a 40-O-substituted rapamycin, said process comprising: (a) dissolving pure rapamycin, pure 16-O or pure 40-O-substituted rapamycin in an inert solvent; (b) adding an antioxidant to the resulting solution in an amount up to 1% based on the rapamycin or 16-O or 40-O-substituted rapamycin, weight, and (c) isolating the resulting mixture of the rapamycin or 16-O or 40-O-substituted rapamycin and the antioxidant.

9. The process of claim 8 wherein the antioxidant is selected from the group consisting of vitamin E, vitamin C, 2,6-di-tert.-butyl-4-methylphenol (BHT) and combinations thereof.

10. The process of claim 8 wherein the antioxidant is present in an amount of up to 1% based on the macrolide weight.

11. The process of claim 8 wherein the antioxidant is present in an amount of from 0.01 to 0.5% based on the macrolide weight.

12. The process of claim 8 wherein the antioxidant is present in an amount of 0.2% based on the macrolide weight.
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