<abstract xmlns="http://www.w3.org/1999/xhtml"><p> Mefenamic acid (MA) is a widely used non-steroidal antiinflammatory (NSAID) drug. The adverse effects typical of NSAIDs are also present in the case of MA, partly due to its low water solubility. The aim of this study was to increase the water solubility of MA in order to influence its absorption and bioavailability. Solid dispersions of MA were prepared by the melting method using polyethylene glycol 6000 and different types (laurate, D-1216; palmitate, P-1670; stearate, S-1670) and amounts of sucrose esters as carriers. The X-ray diffraction results show that MA crystals were not present in the products. Dissolution tests carried out in artificial intestinal juice showed that the product containing 10 % D-1216 increased water solubility about 3 times. The apparent permeability coefficient of MA across human Caco-2 intestinal epithelial cell layers was high and, despite the difference in solubility, there was no further increase in drug penetration in the presence of the applied additives.</p></abstract>

Mefenamic acid (MA) is a widely used non-steroidal antiinflammatory (NSAID) drug. The adverse effects typical of NSAIDs are also present in the case of MA, partly due to its low water solubility. The aim of this study was to increase the water solubility of MA in order to influence its absorption and bioavailability. Solid dispersions of MA were prepared by the melting method using polyethylene glycol 6000 and different types (laurate, D-1216; palmitate, P-1670; stearate, S-1670) and amounts of sucrose esters as carriers. The X-ray diffraction results show that MA crystals were not present in the products. Dissolution tests carried out in artificial intestinal juice showed that the product containing 10 % D-1216 increased water solubility about 3 times. The apparent permeability coefficient of MA across human Caco-2 intestinal epithelial cell layers was high and, despite the difference in solubility, there was no further increase in drug penetration in the presence of the applied additives.

Preparation and investigation of mefenamic acid – polyethylene glycol – sucrose ester solid dispersions

University of Medicine and Pharmacy Tîrgu Mureş, Faculty of Pharmacy 540139, Tîrgu Mureş, Romania

Institute of Biophysics Biological Research Centre Hungarian Academy of Sciences 6726, Szeged, Hungary

University of Szeged Faculty of Pharmacy Department of Pharmaceutical Technology 6720, Szeged, Hungary

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Mefenamic acid (MA) is a widely used non-steroidal antiinflammatory (NSAID) drug. The adverse effects typical of NSAIDs are also present in the case of MA,...

Preparation and investigation of mefenamic acid – polyethylene glycol – sucrose ester solid dispersions

Published Online: Dec 17, 2015

Page range: 453 - 462

Accepted: Jul 14, 2015

DOI: https://doi.org/10.1515/acph-2015-0035

Keywords
mefenamic acid, sucrose esters, PEG 6000, solid dispersion, Caco-2 cells

© by Mircea Dumitru Croitoru

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Preparation and investigation of mefenamic acid – polyethylene glycol – sucrose ester solid dispersions

Published Online: Dec 17, 2015

Page range: 453 - 462

Accepted: Jul 14, 2015

DOI: https://doi.org/10.1515/acph-2015-0035

Keywordsmefenamic acid, sucrose esters, PEG 6000, solid dispersion, Caco-2 cells

© by Mircea Dumitru Croitoru

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Keywords
mefenamic acid, sucrose esters, PEG 6000, solid dispersion, Caco-2 cells