Vapor Sorption and Halogen-Bond-Induced Solid-Form Rearrangement of a Porous Pharmaceutical

Cryst Growth Des. 2023 Feb 28;23(4):2628-2633. doi: 10.1021/acs.cgd.2c01464. eCollection 2023 Apr 5.

Abstract

A porous, nonsolvated polymorph of the voltage-gated sodium channel blocker mexiletine hydrochloride absorbs iodine vapor to give a pharmaceutical cocrystal incorporating an I2Cl- anion that forms a halogen-π interaction with the mexiletine cations. The most thermodynamically stable form of the compound does not absorb iodine. This example shows that vapor sorption is a potentially useful and underused tool for bringing about changes in pharmaceutical solid form as part of a solid form screening protocol.