Ternary solid dispersions of oxicams: Dissolution and permeability study

Ibolya Fülöp, Árpád Gyéresi, Mária A. Deli, Lóránd Kiss, Mircea Dumitru Croitoru, Piroska Szabó-Révész, Zoltán Aigner

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)286-295
Number of pages10
JournalFarmacia
Volume63
Issue number2
Publication statusPublished - Jan 1 2015

Keywords

  • Macrogol
  • Oxicam
  • Solid dispersion
  • Sugar ester

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)

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