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Original scientific paper

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

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

IBOLYA FÜLÖP ; University of Medicine and Pharmacy, Tîrgu Mureş, Faculty of Pharmacy, Department of Toxicology and Biopharmacy, 540139, Tîrgu Mureş, Romania
ÁRPÁD GYÉRESI ; University of Medicine and Pharmacy, Tîrgu Mureş, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 540139, Tîrgu Mureş, Romania
LÓRÁND KISS ; Institute of Biophysics, Biological Research Centre, Hungarian Academy of Sciences, 6726, Szeged, Hungary
MÁRIA A. DELI ; Institute of Biophysics, Biological Research Centre, Hungarian Academy of Sciences, 6726, Szeged, Hungary
MIRCEA DUMITRU CROITORU ; University of Medicine and Pharmacy, Tîrgu Mureş, Faculty of Pharmacy, Department of Toxicology and Biopharmacy, 540139, Tîrgu Mureş, Romania
PIROSKA SZABÓ-RÉVÉSZ ; University of Szeged, Faculty of Pharmacy, Department of Pharmaceutical Technology, 6720, Szeged, Hungary
ZOLTÁN AIGNER ; University of Szeged, Faculty of Pharmacy, Department of Pharmaceutical Technology, 6720, Szeged, Hungary


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Abstract

Mefenamic acid (MA) is a widely used non-steroidal anti-inflammatory (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.

Keywords

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

Hrčak ID:

144153

URI

https://hrcak.srce.hr/144153

Publication date:

31.12.2015.

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