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1. WO2012064306 - EFFERVESCENT FORMULATIONS OF ROSUVASTATIN

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[ EN ]

CLAIMS

1. An effervescent formulation comprising rosuvastatin and/or a pharmaceutically acceptable salt thereof as active agent characterized in that said formulations comprise at least one organic salt in which the cation is divalent.

2. The effervescent formulation according to claim 1 characterized in that the organic salt with divalent cation is calcium carbonate or magnesium carbonate.

3. The effervescent formulation according to claim 2 characterized in that the organic salt comprised in said formulations is calcium carbonate.

4. The effervescent formulation according to any preceding claims characterized in that the amount of the organic salt used in the formulations is in the range of 1% to 10% by weight.

5. The effervescent formulation according to claim 4 characterized in that the amount of the organic salt used in the formulations is in the range of 1% to 5% by weight.

6. The effervescent formulation according to any preceding claims characterized in that rosuvastatin used in the formulations is in calcium salt form.

7. The effervescent formulation according to claim 6 characterized in that the amount of rosuvastatin calcium used in the formulations is in the range of 0.1% to 5% by weight.

8. The effervescent formulation according to claim 7 characterized in that the amount of rosuvastatin calcium used in the formulations is in the range of 0.1% to 2% by weight.

9. The effervescent formulation according to claim 1 characterized in that said formulation comprises other pharmaceutically acceptable components such as additives and excipients selected from disintegrants, viscosity enhancing agents, filling agents, drying agents, stabilizing agents, lubricants, diluents, binders, glidants, anti-foam agents, wetting agents, effervescent mixtures, sweeteners and flavoring agents.

10. The effervescent formulation according to claim 9 characterized in that the effervescent mixture in the formulations is composed of at least one effervescent acid and at least one effervescent base.

11. The effervescent mixture according to claim 10 characterized in that the effervescent base in the mixture is selected from a group excluding calcium carbonate.

12. The effervescent mixture according to claim 11 characterized in that the effervescent base in the mixture is selected from a group comprising sodium carbonate, sodium bicarbonate, potassium carbonate, potassium bicarbonate.

13. The effervescent base according to claim 12, wherein said effervescent base is preferably sodium hydrogen carbonate.

14. The effervescent mixture according to claim 10 characterized in that the effervescent acid in the mixture is a mixture of at least two effervescent acids which are chemically different.

15. The effervescent mixture according to claim 14 characterized in that the effervescent acid in the mixture is selected from a group comprising citric acid, monosodium citrate, tartaric acid, fumaric acid, malic acid and/or their pharmaceutically acceptable salts, hydrates, anhydrates or preferably a combination thereof.

16. The effervescent mixture according to claim 15 characterized in that the effervescent acid in the mixture preferably comprises malic acid and citric acid anhydrate.

17. The effervescent formulation according to claim 9 characterized in that the lubricant in said formulations is selected from a group comprising magnesium stearate, calcium stearate, aluminium stearate, sodium stearyl fumarate, stearic acid, fatty alcohols, glyceryl behenate, mineral oil, paraffins, hydrogenated vegetable oils, leucine, polyethylene glycols (PEG), sodium lauryl sulphate, magnesium lauryl sulphate, sodium chloride, sodium benzoate, sodium acetate and talc and/or hydrates thereof.

18. The effervescent formulation according to claim 1 characterized in that said formulation comprises at least one sterol absorption inhibitor as a second active agent.

19. The sterol absorption inhibitor according to claim 18, wherein said sterol absorption inhibitor is preferably ezetimibe and/or its pharmaceutically acceptable salts, hydrates, enantiomers, racemates, organic salts, inorganic salts, esters, polymorphs, crystalline forms and amorphous forms and/or combinations thereof.

20. The effervescent formulation according to any preceding claims characterized in that said formulation is used in prophylaxis and/or treatment of atherosclerosis, hypercholesterolemia, hyperlipoproteinemia, hypertriglyceridemia, myocardial infarction, stroke.