Romanian Society of Pharmaceutical Sciences
 

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TERNARY SOLID DISPERSIONS OF OXICAMS: DISSOLUTION AND PERMEABILITY STUDY

IBOLYA FÜLÖP1, ÁRPÁD GYÉRESI2, MÁRIA A. DELI4, LÓRÁND KISS4, MIRCEA DUMITRU CROITORU1*, PIROSKA SZABÓ-RÉVÉSZ3, ZOLTÁN AIGNER3

1.University of Medicine and Pharmacy, Târgu Mureş, Faculty of Pharmacy, Department of Toxicology and Biopharmacy, Gheorghe Marinescu 38, 540139, Târgu Mureş, Romania
2.University of Medicine and Pharmacy, Târgu Mureş, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Gheorghe Marinescu 38, 540139, Târgu Mureş, Romania
3.University of Szeged, Faculty of Pharmacy, Department of Pharmaceutical Technology, Eötvös 6, 6720, Szeged, Hungary
4.Laboratory of Molecular Neurobiology, Institute of Biophysics, Biological Research Centre, Temesvári krt. 62, 6726, Szeged, Hungary

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Solid dispersions are efficient means for improving the dissolution rate of hydrophobic drugs. In this study ternary solid dispersions were made by melting method using PEG 6000, three types of sugar esters and three enolic acid derivates used as non-steroidal anti-inflammatory drugs piroxicam, meloxicam and tenoxicam. The prepared solid dispersions were characterized by X-ray diffraction. Dissolution studies, kinetic calculations, and in the case of tenoxicam permeability and toxicity studies on Caco-2 human intestinal epithelial cells were also performed. X-ray diffraction studies showed a significant decrease in the degree of crystallinity due to amorphisation of the active ingredient or formation of a solid solution. The highest amount of drug dissolution in artificial gastric juice was obtained in the presence of 5% sugar esters. In the case of piroxicam and meloxicam the kinetics of dissolution were modified by the studied excipients. PEG 6000 did not change the toxicity of tenoxicam, while stearate and palmitate sucrose esters increased the damage to cultured Caco-2 cells. Laurate sucrose ester was the least toxic. The excipients did not modify the permeability of the lipid soluble tenoxicam across epithelial cells. Sucrose esters significantly increased the dissolution of model drugs, and may reduce the interindividual differences observed in the absorption rate of these drugs, due to their poor solubility.