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Injection-Molded Coamorphous Tablets: Analysis of Intermolecular Interaction and Crystallization Propensity
Ryoma Tanaka1, Sae Ishihara2, Tetsuo Sasaki3
1Graduate School of Pharmaceutical Sciences, Musashino University, 1-1-20 Shin-machi, Nishi-Tokyo, Tokyo 202-8585, Japan.
Journal of Pharmaceutical Sciences
|June 20, 2021
Summary
This study developed a single-step method for creating coamorphous tablets using injection molding (IM). The resulting loratadine coamorphous tablets showed enhanced dissolution and improved physical stability, linked to drug-acid interactions.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Coamorphous systems offer enhanced drug solubility and dissolution.
- Traditional tablet manufacturing can lead to coamorphous system recrystallization and dissociation.
- Injection molding (IM) presents a novel approach for coamorphous tablet production.
Purpose of the Study:
- To develop a single-step preparation of coamorphous tablets via injection molding.
- To mechanistically characterize loratadine-organic acid coamorphous formulations.
- To investigate the impact of drug-acid interactions on coamorphous tablet stability and dissolution.
Main Methods:
- Coamorphous tablets of loratadine and organic acids (citric, succinic, tartaric, malic) were prepared using injection molding.
- Dissolution testing was performed on coamorphous tablets and pure amorphous loratadine.
- Fourier Transform Infrared (FT-IR) and terahertz spectroscopies were used for interaction analysis.
- Physical stability was assessed by storing tablets at 40°C/75%RH and analyzing X-ray diffraction (XRD) patterns over time.
Main Results:
- Loratadine coamorphous tablets exhibited enhanced dissolution compared to pure amorphous loratadine.
- Ionic interactions between loratadine and organic acids were confirmed via FT-IR and terahertz spectroscopy.
- Tablet physical stability correlated positively with the strength of loratadine-acid interactions.
- Terahertz spectroscopy revealed molecular mobility's role in coamorphous system crystallization propensity.
Conclusions:
- Injection molding provides a robust, single-step method for producing stable coamorphous tablets.
- Understanding drug-acid interaction strength is crucial for designing stable coamorphous formulations.
- Molecular mobility, detectable by terahertz spectroscopy, influences crystallization behavior in coamorphous systems.
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