IMPROVED SOLUBILITY AND DISSOLUTION OF ETORICOXIB VIA MULTICOMPONENT CRYSTALLIZATION WITH MEGLUMINE

Etoricoxib, a non-steroidal anti-inflammatory drug known for its poor water solubility, faces significant challenges in achieving adequate bioavailability due to its slow dissolution rate. This study aimed to improve the solubility and dissolution rate of etoricoxib through the formation of multicomponent crystals with N-methyl-D-glucamine (meglumine) as a coformer. Multicomponent crystals were synthesized via solvent drop grinding in a 1:1 molar proportion and then analyzed for their solid-state characteristics using Differential Scanning Calorimetry, Powder Xray Diffraction, Fourier Transform Infrared Spectroscopy, and Scanning Electron Microscopy. Thermal and diffraction analyses confirmed the formation of new crystalline phases, indicative of successful multicomponent crystal formation. Morphological studies revealed smaller and more uniform particles in the multicomponent crystals compared to the Intact etoricoxib. The multicomponent crystal exhibited a 3.2-fold increase in solubility and a 2.8- fold faster dissolution rate within 60 minutes compared to intact etoricoxib. These improvements are attributed to the reduction in crystal lattice energy, facilitated by the formation of molecular interactions between etoricoxib and the coformer. This strategy offers a promising approach to enhancing the biopharmaceutical performance of a poorly soluble drug.

Authors

Publication Details

Journal
RASAYAN Journal of Chemistry
Published
2025-01-01
DOI
https://doi.org/10.31788/rjc.2025.1839233
Primary Topic
Crystallization and Solubility Studies
Type
article
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article

IMPROVED SOLUBILITY AND DISSOLUTION OF ETORICOXIB VIA MULTICOMPONENT CRYSTALLIZATION WITH MEGLUMINE

Syofyan Syofyan, Rahmadevi Rahmadevi, Yori Yuliandra, Erizal Zaini et al.
RASAYAN Journal of Chemistry
Crystallization and Solubility Studies
article

IMPROVED SOLUBILITY AND DISSOLUTION OF ETORICOXIB VIA MULTICOMPONENT CRYSTALLIZATION WITH MEGLUMINE

Syofyan Syofyan, Rahmadevi Rahmadevi, Yori Yuliandra, Erizal Zaini, Muhammad Nasrul Siregar
article en

Abstract

Etoricoxib, a non-steroidal anti-inflammatory drug known for its poor water solubility, faces significant challenges in achieving adequate bioavailability due to its slow dissolution rate. This study aimed to improve the solubility and dissolution rate of etoricoxib through the formation of multicomponent crystals with N-methyl-D-glucamine (meglumine) as a coformer. Multicomponent crystals were synthesized via solvent drop grinding in a 1:1 molar proportion and then analyzed for their solid-state characteristics using Differential Scanning Calorimetry, Powder Xray Diffraction, Fourier Transform Infrared Spectroscopy, and Scanning Electron Microscopy. Thermal and diffraction analyses confirmed the formation of new crystalline phases, indicative of successful multicomponent crystal formation. Morphological studies revealed smaller and more uniform particles in the multicomponent crystals compared to the Intact etoricoxib. The multicomponent crystal exhibited a 3.2-fold increase in solubility and a 2.8- fold faster dissolution rate within 60 minutes compared to intact etoricoxib. These improvements are attributed to the reduction in crystal lattice energy, facilitated by the formation of molecular interactions between etoricoxib and the coformer. This strategy offers a promising approach to enhancing the biopharmaceutical performance of a poorly soluble drug.

RASAYAN Journal of ChemistryVol. 18(03)
Openalex Percentile: Top 90%
Crystallization and Solubility Studies
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