Process for the preparation of amorphous rosuvastatin calcium
OwnerYatendra Kumar, Mohammad Rafeeq +2inventors
InventorsYatendra Kumar, Mohammad Rafeeq, Shantanu De, Swargam Sathyanarayana
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Abstract
The invention relates to processes for the preparation of amorphous rosuvastatin calcium. More particularly, it relates to the preparation of pure amorphous rosuvastain calcium and pharmaceutical compositions that include the pure amorphous rosuvastatin calcium. The invention also relates to use of said compositions for treating hyperlipidemia, hypercholesterolemia, and atherosclerosis. Formula (I).
Claims54
Amorphous rosuvastatin calcium of Formula I having a purity of more than 99% with diastereomeric impurity less than 0.5% by HPLC.
A pharmaceutical composition comprising:
- a therapeutically effective amount of an amorphous form of rosuvastatin calcium having purity greater than 99% with diastereomeric impurity less than 0.5% by HPLC;
- and one or more pharmaceutically acceptable carriers, excipients or diluents.
Amorphous rosuvastatin calcium having a purity of more than 99.5% with diastereomeric impurity less than 0.25% by HPLC.
A process for the preparation of pure amorphous form of rosuvastatin calcium, the process comprising:
- obtaining a solution of rosuvastatin calcium in one or more solvents;
- and
- recovering the rosuvastatin calcium in the amorphous form from the solution thereof by the removal of the solvent.
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A process for the preparation of pure amorphous form of rosuvastatin calcium, the process comprising:
- subjecting crystalline rosuvastatin calcium to milling until said crystalline form is converted to the amorphous form.
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A process for the preparation of pure amorphous form of rosuvastatin calcium, the process comprising:
- obtaining a solution of rosuvastatin calcium in one or more solvents;
- and
- recovering the rosuvastatin calcium in the amorphous form from the solution thereof by freeze drying or lyophilizing.
A process for the preparation of pure amorphous form of rosuvastatin calcium, the process comprising:
- a) lactonizing rosuvastatin methyl ammonium salt of Formula II,
- to obtain rosuvastatin lactone of Formula III,
- b) reacting the rosuvastatin lactone with a base and a calcium salt, and
- c) recovering the amorphous form of rosuvastatin calcium.
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A process for the preparation of pure amorphous form of rosuvastatin calcium, the process comprising:
- treating rosuvastatin methyl ammonium salt with a base and a calcium salt;
- and
- recovering the amorphous form of rosuvastatin calcium.
A process for the preparation of pure amorphous form of rosuvastatin calcium, the process comprising:
- a) lactonizing rosuvastatin methyl ammonium salt of Formula II,
- to obtain rosuvastatin lactone of Formula III,
- b) reacting the lactone form of rosuvastatin with a base and a calcium salt,
- c) removing water from reaction mass by azeotropic distillation to obtain a solution containing rosuvastatin calcium, and
- d) recovering the amorphous form of rosuvastatin calcium by removing solvent from the resultant solution.
A process of the preparation of pure amorphous form of rosuvastatin calcium, the process comprising:
- a) treating rosuvastatin calcium with an acid to obtain rosuvastatin of
- Formula IV, and
- b) converting the rosuvastatin to the amorphous form of rosuvastatin calcium by treatment with a base and a calcium salt.
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A method of treating hyperlipidemia, hypercholesterolemia, and atherosclerosis in a warm-blooded animal comprising administering a pharmaceutical composition that includes the pure amorphous form of rosuvastatin calcium having a purity of more than 99% with diastereomeric impurity less than 0.5% by HPLC.
Dependencies are inferred from the claim text.