Crystalline eltrombopag monoethanolamine salt form d
AssigneeF.I.S. Fabbrica Italiana Sintetici S.p.A.
InventorsNicolas TESSON, Jordi DE MIER VINUE, Paolo STABILE, Pierluigi PADOVAN, Matteo DE POLI, Angelo RESTELLI
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Abstract
Object of the present invention is a better crystalline form of Eltrombopag (ETP) monoethanolamine salt, named Form D, stable, suitable for pharmaceutical purposes, and with the highest solubility in water and excellent non-hygroscopicity, then the related process and intermediates thereof.
Claims17
Crystalline Eltrombopag monoethanolamine salt Form D of formula (I):
- having one of the following characteristic peaks of X-ray powder diffraction pattern expressed in 2-Theta values (2θ) at:
- 7.8, 11.1 and 19.1, each peak±0.2.
A process for the preparation of the crystalline Eltrombopag monoethanolamine salt Form D of formula (I):
- comprising:
- a) salifying Eltrombopag in a solvent with ammonia to give a crystalline Eltrombopag ammonium salt Form C1 or crystalline Eltrombopag ammonium salt Form C2 or mixture thereof,
- b) providing a suspension of the product of the step a) in a solvent and ethanolamine, and
- c) distilling the mixture of the step b) to give crystalline Eltrombopag monoethanolamine salt Form D of formula (I):
Crystalline Eltrombopag ammonium salt Form C1 having characteristic peaks of X-ray powder diffraction pattern expressed in 2-Theta values (2θ) at:
- 12.5 and 22.5, each peak±0.3.
Crystalline Eltrombopag ammonium salt Form C2 having characteristic peaks of X-ray powder diffraction pattern expressed in 2-Theta values (2θ) at:
- 14.6, 15.8 and 17.6, each peak±0.3.
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Dependencies are inferred from the claim text.