Olanzapinium Salts, Isostructural Solvates, and Their Physicochemical Properties

Solubility and dissolution play a
crucial role in the activity
and efficacy of an oral drug. Olanzapine is an antipsychotic drug
of the Biopharmaceutics Classification System (BCS) class II category.
Several solvates, cocrystals, salts, and amorphous forms of olanzapine
have been prepared to study materials properties and its X-ray crystal
structures were classified. We report herein a few salts, solvates,
and solvate polymorphs of olanzapine to improve the physicochemical
properties and study novel structural motifs. Olanzapinium dimaleate
monofumaric acid is the first case of a ternary cocrystal of an active
pharmaceutical ingredients (API) in the CSD database with maleate
ion and fumaric acid coformers. The olanzapine disalts, olanzapinium
dipicrate, dimaleate, and dimaleate monofumaric acid, contain a novel
structural motif, different from the dimer motif characteristic of
the four structural categories reported in the literature.