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US 2008/0176937 A1Published application
Novel crystalline mycophenolate sodium polymorph and processes to manufacture same
AssigneeApotex Fermentation Inc.
InventorsChad Glass, Rudolf Kubela
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Abstract
The present invention includes the discovery of a novel polymorphic form of sodium mycophenolate (MPS) and processes for its formation. Furthermore, the present invention also includes a process to efficiently and cleanly convert the novel polymorphic form to known Form M2.
Claims9
A crystalline mycophenolate sodium salt (Form CG1) characterized by at least one of the following:
- i) a powder XRD pattern with peaks at 4.6, 5.2, 6.1, 7.2, 10.5, 12.4, 14.4, 17.1, 22.9, 24.4, 25.2, 26.6, 26.9±0.2 degrees 2 theta;
- ii) a FT-IR pattern with peaks at 2924, 2854, 1719, 1563, 1461, 1377, 1266, 1135, 1078, 1034 wavenumbers;
- iii) a DSC as shown in FIG. 3.
A process for preparing crystalline mycophenolate sodium salt (Form CG1) comprising the steps of:
- (a) preparing a suspension of mycophenolic acid in water;
- (b) addition of an aqueous solution of a sodium inorganic base to obtain an aqueous mycophenolate sodium salt solution;
- (c) addition of an organic solvent that forms an azeotrope with water to the aqueous mycophenolate sodium salt solution;
- (d) azeotropic removal of water by heating to reflux resulting in the crystalline Form CG1;
- and
- (e) recovering the crystalline form wherein Form CG1 is characterized by at least one of the following:
- i) a powder XRD pattern with peaks at 4.6, 5.2, 6.1, 7.2, 10.5, 12.4, 14.4, 17.1, 22.9, 24.4, 25.2, 26.6, 26.9±0.2 degrees 2 theta;
- ii) a FT-IR pattern with peaks at 2924, 2854, 1719, 1563, 1461, 1377, 1266, 1135, 1078, 1034 wavenumbers;
- or
- iii) a DSC as shown in FIG. 3.
7 more elements
A process for preparing crystalline mycophenolate sodium salt (Form M2) comprising the steps of:
- (a) preparing a suspension of crystalline mycophenolate sodium salt (Form CG1) in toluene;
- (b) heating said suspension at reflux;
- (c) crystallizing the crystalline form;
- and
- (d) recovering the crystalline Form M2.
2 more elements
Dependencies are inferred from the claim text.