TY - JOUR
T1 - Development of Mefenamic Acid-Soluplus ® amorphous dispersions via hot melt extrusion and in silico prediction of oral absorption
AU - Chavero, Estrella
AU - Kurowska, Aleksandra
AU - Lewis, Shaila A.
N1 - Publisher Copyright:
© 2023, Istanbul Medipol University. All rights reserved.
PY - 2023
Y1 - 2023
N2 - The objective of this study was to increase the solubility of Mefenamic Acid (MA), a BCS class II drug by formulating amorphous solid dispersions via Holt-Melt Extru-sion. The extrudates were prepared at different drug to polymer ratios and charac-terised by standard analytical techniques. Dissolution studies were performed in Phosphate buffer saline (PBS) pH 7.4 medium. Stability of the different ratios of MA: Soluplus (1:1, 1:4 and 4:1) was studied at room temperature for 12 months. Computer simulation using GastroPlus™ was run to depict the gastrointestinal absorption of MA in humans. DSC thermograms and the diffractograms of the solid dispersions confirmed amorphous nature. Dissolution studies showed enhanced dissolution rate of MA from the solid dispersions. Stability studies indicated 1:4 (MA: Soluplus®) dispersion as the most stable dispersion. GastroPlus™ simulation using in vitro data showed improvement in the PK parameters of the solid disper-sión in comparison with pure MA.
AB - The objective of this study was to increase the solubility of Mefenamic Acid (MA), a BCS class II drug by formulating amorphous solid dispersions via Holt-Melt Extru-sion. The extrudates were prepared at different drug to polymer ratios and charac-terised by standard analytical techniques. Dissolution studies were performed in Phosphate buffer saline (PBS) pH 7.4 medium. Stability of the different ratios of MA: Soluplus (1:1, 1:4 and 4:1) was studied at room temperature for 12 months. Computer simulation using GastroPlus™ was run to depict the gastrointestinal absorption of MA in humans. DSC thermograms and the diffractograms of the solid dispersions confirmed amorphous nature. Dissolution studies showed enhanced dissolution rate of MA from the solid dispersions. Stability studies indicated 1:4 (MA: Soluplus®) dispersion as the most stable dispersion. GastroPlus™ simulation using in vitro data showed improvement in the PK parameters of the solid disper-sión in comparison with pure MA.
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U2 - 10.23893/1307-2080.APS6101
DO - 10.23893/1307-2080.APS6101
M3 - Article
AN - SCOPUS:85149197027
SN - 1307-2080
VL - 61
SP - 1
EP - 17
JO - Acta Pharmaceutica Sciencia
JF - Acta Pharmaceutica Sciencia
IS - 1
ER -