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A New 1:1 Cocrystal of Lamotrigine and 1,2,3,6-4hydrophthalimide:Discovery,Characterization, and Construction of Ternary Phase Diagrams

Abstract

ABSTRACT 1:1 cocrystal of lamotrigine (LAM) with 1,2,3,6-4 hydrophthalimide (HTHP) was first successfully synthesized and was characterized by XRD (power and single-crystal X-ray diffraction), FT-IR, DSC TG. Molecular Hirshfeld surfaces and the corresponding two-dimensional (2D) fingerprint plots have been evaluated and hirshfeld surface analysis indicated that hydrogen bonding N···H and O···H mainly constitutes the connection between cocrystal molecules.Ternary phase diagrams (TPDs) of LAM-HPHT in isobutanol was constructed at 293.15 K and 313.15K. The result indicated that pure cocrystal preparation or stability region became larger as temperature increasing without changing the TPDS shape. And meanwhile, the solubility of LAM-HPHT in isobutanol was measured, the solubility product (Ksp) and solution complexation constants (K11) were proposed to illustrate the solubility of LAM-HPHT. The result indicated that Ksp gradually increases while K11 decreases with the cocrystal solubility increasing. Dissolution results indicated LAM-HPHT was found to exhibit improved aqueous solubility when compared to pure LAM. Stability study demonstrated that LAM-HPHT were much more stable than original LAM crystal under the condition of 98% RH (25℃) or 85% RH (25℃).

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Supplementary files

Article information


Submitted
06 Feb 2020
Accepted
01 Mar 2020
First published
02 Mar 2020

CrystEngComm, 2020, Accepted Manuscript
Article type
Paper

A New 1:1 Cocrystal of Lamotrigine and 1,2,3,6-4hydrophthalimide:Discovery,Characterization, and Construction of Ternary Phase Diagrams

W. Kuang, S. Ji, Y. Wei , J. Zhang and P. Lan, CrystEngComm, 2020, Accepted Manuscript , DOI: 10.1039/D0CE00178C

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