Apremilast Cocrystals with Phenolic Coformers
2024

Cocrystals of Apremilast with Phenolic Compounds

publication Evidence: moderate

Author Information

Author(s): Yelizaveta Naumkina, Bohumil Kratochvíl, Elena Korotkova, Jan Čejka

Primary Institution: University of Chemistry and Technology, Prague

Hypothesis

Can cocrystallization of Apremilast with phenolic coformers improve its solubility?

Conclusion

The study found that the cocrystals of Apremilast with phenolic compounds exhibited minimal differences in melting points despite variations in the coformers' hydroxyl groups.

Supporting Evidence

  • Four novel cocrystal forms were synthesized and characterized.
  • The cocrystals crystallized in the same space group P41212.
  • Despite expectations, the number of hydroxyl groups did not significantly affect molecular packing.
  • Thermal analysis indicated the stability of the new solid forms.

Takeaway

Scientists mixed a medicine called Apremilast with some plant-based compounds to see if it would dissolve better, but they found that it didn't change much.

Methodology

Cocrystallization of Apremilast with four phenolic coformers was performed, followed by characterization using X-Ray diffraction and thermal analysis techniques.

Limitations

The variability in molecular packing did not change with the increasing number or variety of hydroxyl groups in the coformers.

Digital Object Identifier (DOI)

10.3390/molecules29246060

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