Modulation of anti in flammatory action and ulcerogenically of piroxicam via hydrotropic and complexing solubilization

ABSTRACT

Solubilized systems of piroxicam with the aid of certain hydrotropic and complexing agents viz., nicotinamide, sodium gentisate, sodium benzoate, sodium salicylate, and gentisic acid ethanolamide were prepared. Both nicotinamide and gentisic acid ethanolamide in 10-40% solubilized the therapeutic dose of piroxicam per 5 ml volumes. The spectral analysis as well as thin-layer chromatography revealed that both nicotinamide and sodium benzoate solubilized piroxicam via hydrotropy, while each of sodium salicylate, sodium gentisate, and gentisic acid ethanolamide solubilized the drug through complex formation. The continuous variation [Job's method] applied to determine the stoichiometric ratio of the reached complexes indicated 1 2, 2 1 and 3 2 ratios for piroxicam and each of gentisic acid ethanolamide, sodium gentisate, and sodium salicylate, respectively. The pharmacological screening revealed that solubilized systems of piroxicam with nicotinamide or gentisic acid ethanolamide improved the anti-inflammatory activity of the drug compared to its commercial product. However, solubilized piroxicam proved to be ulcerogenic