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Inclusion complexes of meloxicam and selected cyclodextrins in solution and in the solid state

Meloxicam (MEL) is a non-steroidal anti- inflammatory drug with low solubility and high permeability, used in the treatment of rheumatoid arthritis and osteoarthritis [1]. Cyclodextrins (CD) are cyclic oligosaccharides containing six (α-CD), seven (β-CD) or eight (γ- CD) glucose subunits, linked with (α-1, 4)- glycosidic bond. Their ability to improve the solubility of drugs by forming inclusion complexes is well known [2]. The influence of β-CD and its hydroxypropyl derivative (HPβCD) on MEL solubility in water and buffered solutions at different pH values has already been studied [1, 3, 4]. Mechanochemical activation by grinding is a fast, efficient, and environmentally friendly method of preparing inclusion complexes in the solid state [5]. A previous study confirmed it as suitable for preparation of MEL/β-CD complex [1]. The aim of this study was to investigate the influence of β- CD and its sulphobutylether derivative (SBEβCD) on the solubility of MEL in water and biorelevant media (simulated gastric, pH 1 ; duodenal, pH 4.5 and intestinal media, pH 6.8) according to the method presented by Higuchi and Connors [6]. Phase solubility diagrams were constructed, and stability constants, complexation efficacies and solubility enhancement were determined. Inclusion complexes in the solid state were then prepared by grinding and characterized by IR spectroscopy.

cyclodextrins ; meloxicam ; phase solubility ; IR spectroscopy

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