Effect of coamorphization on meloxicam/saccharine: Intermolecular interaction investigations using chemometrics

Yuta Otsuka

Published 2025 in Bio-medical materials and engineering

ABSTRACT

Background: Aqueous solubility of pharmaceuticals is a factor as it is directly associated with bioavailability; accordingly, strategies to enhance solubility have been well investigated. Objectives: The purpose of this study was to determine the effects of coamorphization on meloxicam (MX) and saccharine (SA) mixtures. Methods: An equimolar mixture of MX and SA was ground for 4 h at 300 rpm. The obtained samples were evaluated using Fourier-transform mid-infrared spectroscopy, Fourier transform near-infrared spectroscopy, powder X-ray diffraction (PXRD), and thermal analysis. No molecular interactions were observed in the physical mixture sample. The ground samples showed broad peaks in the PXRD patterns and an exothermic peak at an early temperature. Results: The results suggested that the grinding process transformed MX and SA into a coamorphous phase. The attenuated total reflection - IR spectra exhibited new peaks at 1719 cm−1 and 1398 cm−1, and the NH peak disappeared with grinding time. Measurement data of MX and SA ground sample suggested they constructed coamorphous phase. Conclusion: It was indicated by multivariate analysis that the formation of the MX/SA coamorphous system occurred in a two-step process.

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