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US 2006/0142299 A1Published application
Crystalline aripiprazole solvates
AssigneeSynthon BV
InventorsGerrit Ettema, Raymond Westheim, Faysal Kalmoua
Life of this patent
Estimating the term…
Abstract
Alcoholates of aripiprazole are useful as pharmaceuticals and/or as intermediates in making aripiprazole Form A or Form B.
Claims15
An alcoholate of aripiprazole selected from aripiprazole hemi-ethanolate and aripiprazole methanolate.
A process for making aripiprazole hemi-ethanolate, which comprises:
- providing a solution of aripiprazole in ethanol;
- crystallizing aripiprazole from said solution;
- and
- drying said crystals to have a bound solvent content within the range of about 0.4 to 0.6 moles per mole of aripiprazole.
1 more element
A process for making an aripiprazole methanolate, which comprises providing a solution of aripiprazole in methanol;
- and
- crystallizing aripiprazole to form crystalline aripiprazole methanolate.
A process for making a pharmaceutical granulate, which comprises:
- granulating a mixture of a granulateable binder, an aripiprazole alcoholate selected from hemi-ethanolate and methanolate, and optionally a granulating liquid, to form granules;
- and
- drying said granules.
Dependencies are inferred from the claim text.