Claims for Patent: 7,297,703
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Summary 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 Litigation and PTAB cases: | See patent lawsuits and PTAB cases for patent 7,297,703 |
| 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. |
