Isostructural cocrystals of metaxalone with improved dissolution characteristics

Abstract

Metaxalone forms isostructural cocrystals with nicotinamide and salicylamide that offer a solubility advantage compared to the native drug. A drug–drug homosynthon is retained in all the cocrystal structures.

Polymorphs and isostructural cocrystals of dexamethasone: towards the improvement of aqueous solubility

“…Recently, we have reported isostructural cocrystals of metaxalone with salicylamide and nicotinamide. 4 The crystal lattice parameters of DEX-CAT and DEX-RES cocrystals are very similar (see Table 2). Similar hydrogen bonding features in DEX-CAT/RES cocrystals further confirm their isostructurility (see Fig.…”

“…exchange of H/F, Cl/Br, Cl/CH 3 , S/O, CH/N, and NH/O, which are defined as isostructural cocrystals. [4][5][6] Often isomers may provide an isostructural packing, as there is no change in elements except the position of atoms/functional groups. Recently, we have reported isostructural cocrystals of metaxalone with salicylamide and nicotinamide.…”

“…3 Cocrystals with a similar molecular arrangement in the crystal lattices are defined as isostructural cocrystals. 4,5 The design of isostructural cocrystals involves either the incorporation of structural homologues or the exchange of atoms/functional groups with equivalent van der Waals radii/volume. The main advantage of isostructural cocrystals is by putting a minor change in the constituents, one can tune the drug properties without altering the overall crystal packing of the cocrystals.…”

Exploiting Supramolecular Synthons in Cocrystals of Two Racetams with 4-Hydroxybenzoic Acid and 4-Hydroxybenzamide Coformers

“…As coformers for PPA and PPAH, we used compounds with molecular structures similar to those which were successfully used for formation of PA cocrystals [10,11], such as 4-hydroxybenzoic acid (HBA) and 4-hydroxybenzamide (HBD). The HBA in particular has performed well in cocrystal design with APIs [11,[23][24][25][26]. Structural, and computational studies were carried out for the following pure and cocrystalline materials: PPA, PPA•HBA, PPA•2HBA, PPAH, and PPAH•HBD•(acetone solvate).…”

A Review of Coformer Utilization in Multicomponent Crystal Formation

“…The solvent evaporation technique has been successfully used to form multicomponent crystals and has succeeded in increasing the solubility of pharmaceutically active substances [15][16][17][18][19][20][21][22][23][24]28].…”