Polymorphs of pitavastatin calcium
AssigneeHetero Research Foundation
InventorsBandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Samala Malla Reddy, Bandi Vamsi Krishna
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Abstract
The present invention provides a solid of pitavastatin tert-butyl ester and process for its preparation. The present invention also provides a novel crystalline form of pitavastatin calcium, process for its preparation and pharmaceutical compositions comprising it.
Claims28
A process for the preparation of solid of pitavastatin tert-butyl ester, which comprises:
- a. reacting R-(-)-camphor sulfonic acid with tert-butyl-(3R,5S,6Z)-7-{2-cyclopropyl-4-(4-fluorophenyl)quinoline-3-yl}-3,5-isopropylidenedioxy-6-heptenoate in a nitrile solvent and water;
- b. adding a mixture of water and a solvent selected from an ester solvent, a chlorinated solvent, an ether solvent or mixture thereof;
- c. concentrating the reaction mass;
- d. adding hydrocarbon solvent to the residual mass obtained in step (c);
- and
- e. isolating solid pitavastatin tert-butyl ester.
A pitavastatin calcium crystalline form H1, characterized by peaks in the powder x-ray diffraction spectrum having 2θ angle positions at about 4.9, 6.9, 10.9, 14.8, 15.3, 16.6, 17.7, 19.1, 19.5, 19.9, 20.3, 21.0 and 21.8±0.2 degrees.
A pitavastatin calcium crystalline form H1, characterized by an x-ray powder diffractogram as shown in FIG. 2.
A pharmaceutical composition that comprises crystalline form H1 of pitavastatin calcium and pharmaceutically acceptable excipients.
Dependencies are inferred from the claim text.