Injection-Molded Coamorphous Tablets: Analysis of Intermolecular Interaction and Crystallization Propensity

The processing steps involved in converting from a powder to a tablet entail numerous operations in a which the coamorphous system is recrystallized and dissociated easily. This research focused on (i) a single-step preparation of a coamorphous tablet during injection molding (IM) from the bulk powder, and (ii) a mechanistic characterization of the coamorphous formulation. We selected several organic acids [citric acid, succinic acid, tartaric acid, and malic acid] in an effort to compound with basic loratadine (a poorly watersoluble drug). Loratadine-acids coamorphous tablets were produced via an IM process, and the dissolution was more enhanced than in the pure loratadine amorphous. The interaction was analyzed by FT-IR and terahertz spectroscopies. Each tablet was stored at 40 degrees C/75%RH, and then XRD patterns were acquired at the desired timepoints. In summary, loratadine exhibited ionic interaction with each acid, and the physical stability of the coamorphous tablet was in proportion to the loratadine-acids interaction strength. Terahertz spectra detected the molecular mobility, which plays an important role in the crystallization propensity of a coamorphous system. This understanding offers a framework for robust coamorphous tablet formulation using the IM methodology. (c) 2021 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.

Automated summary

This research focused on a single-step preparation of coamorphous tablet during injection molding and mechanistic characterization. The results showed that coamorphous tablet had enhanced dissolution compared to pure loratadine amorphous, and the physical stability was correlated with the interaction strength between loratadine and acids. Terahertz spectra played an important role in detecting molecular mobility and crystallization propensity in the coamorphous system.