Available online at www.sciencedirect.com
ScienceDirect
Materials Today: Proceedings 14 (2019) 504–513 www.materialstoday.com/proceedings
*Corresponding author e-mail: Arthanareeswari@gmail.com
2214-7853 © 2019 Elsevier Ltd. All rights reserved.
Selection and/or Peer-review under responsibility of 2nd International Conference On Recent Advances In Material Chemistry.
ICRAMC2018
Co-crystallisation of Lamotrigine with diprotic acids:
synthesis, single crystal analysis, and in-vitro evaluation
Praveen Chappa
1
, Arthanareeswari Maruthapillai
1
*, M. Tamilselvi
2
,
S. Devikala
1
and Arockia Selvi J
1
1
Department of Chemistry, Faculty of Engineering and Technology, SRM Institute of Science and Technology, Kattankulathur,
Kancheepuram District, Tamil Nadu - 603203, India
2
Department of Chemistry, ThiruKolanjiappar Government Arts College, Virudhachalam, 606001, India
Abstract
The present study investigates the structural and pharmaceutical properties of two novel cocrystalsof lamotrigine
(LTG) forming with maleic acid (MA) and malonic acid (MLA).Preliminary solid-state characterization was done by single
crystal XRD, FT-IR, DSC and powder XRD. LTG-MA crystallized in P-1 space group whereas LTG-MLA crystallized in
P21/c space group. Pseudo–quadruple hydrogen bond with R42(16) motif graph set notation was observed in all two crystal
structures of LTG co-crystals. The FT-IR spectra of the two cocrystalsshowed a red shift in -NH2 stretching vibrations in the in
the region of 3500-3300 cm-1, blue shift in carbonyl groups of MA and MLA in the region of 1650 to 1670cm-1 indicatesthe
formation of an N-H…O=C intermolecular interaction between LTG and carboxylic acids(MA and MLA). Further, these two co-
crystals were subjected to solubility, powder dissolutionstudies in 0.1 N HCl, in comparison with pure LTG base. The solubility
of these compoundsin 0.1 N HCl is significantly enhanced compared with that of the pure base, which can beattributed to the
type of packing motifs present in their crystal structures.
© 2019 Elsevier Ltd. All rights reserved.
Selection and/or Peer-review under responsibility of 2nd International Conference On Recent Advances In Material Chemistry.
Keywords: Lamotrigine, multi-component, dissolution enhancement, solubility improvement
1. Introduction
The quest for novel solid forms like polymorphs, salts, co-amorphous systems and co-crystals etc. is one of the
major areas of research in the pharmaceutical industry for expansion of patent portfolios and lifecycle management
of active pharmaceutical ingredients (API) [1, 2]. Of all the solid forms co-crystals, which are dissociable
multicomponent supramolecular complexes composed of two or more components within the same crystal lattice