Solid Forms Of An N-(Phenylmethyl)Propanamide Derivative And Processes Of Preparation
AssigneeMedichem, S.A.
InventorsErnesto Durán López, Monica Benito Velez, Jordi Bosch i Lladó
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Abstract
The invention relates to solid forms of the anti-epileptic agent lacosamide (I). The invention also relates to mixtures of solid forms of lacosamide. The invention further relates to mixtures of lacosamide enantiomers crystallized in a conglomerate Form and the use thereof in providing enantiomerically enriched lacosamide, preferably lacosamide enriched with the (R)-enantiomer of lacosamide.
Claims27
Lacosamide crystalline Form III characterized by an XRD pattern comprising peaks (2θ) at 6.5, 8.3, 10.3, 12.9, 15.6, 16.5, 17.5, 19.5, 21.2, 22.5, 24.2, 24.9, 27.0, and 28.5 degrees (±0.2 degrees).
Lacosamide crystalline Form III characterized by a melting point with an onset temperature of about 143.4° C. and a peak temperature of about 145.0° C. as measured by DSC.
A mixture of lacosamide enantiomers crystallized in a conglomerate Form.
A process for preparing enantiomerically enriched lacosamide, comprising providing a supersaturated solution of lacosamide, seeding the supersaturated solution of lacosamide with enantiomerically enriched lacosamide and recovering enantiomerically enriched lacosamide as a conglomerate.
A process for preparing enantiomerically enriched lacosamide, comprising providing a supersaturated solution of lacosamide comprising an epimerization agent, seeding the supersaturated solution of lacosamide with enantiomerically enriched lacosamide and recovering enantiomerically enriched lacosamide as a conglomerate.
A process for increasing the enantiomeric excess of an enantiomerically enriched lacosamide, comprising providing a solution of enantiomerically enriched lacosamide, conducting at least one direct crystallization of the solution comprising the enantiomerically enriched lacosamide and recovering enantiomerically enriched lacosamide as a conglomerate.
A mixture of lacosamide enantiomers crystallized in a conglomerate Form obtained by crystallization from ethyl acetate.
Dependencies are inferred from the claim text.