Preparation and In-vitro Evaluation of Piroxicam Dispersible Tablets Prepared by Direct Compression and Sublimation Techniques for Enhanced Dissolution

Abstract

ABSTRACTPiroxicam is a Non-Steroidal Anti-Inflammatory Drug (NSAID) that belongs to theBiopharmaceutical Classification System (BCS) Class II. It has low aqueous solubility, whichcould be a significant factor in the dissolution-limited oral absorption.[1,2] The presentinvestigation was undertaken to develop piroxicam dispersible tablets using differentsuperdisintegrants and manufacturing techniques with the aim of enhancing drug dissolutionand improving the suitability of the dosage form for oral administration. Rapidlydisintegrating oral dosage forms are prepared to disintegrate or dissolve quickly in thepresence of saliva and can aid in the administration to patients for whom swallowing ofconventional tablets may be difficult.[3] Twelve formulations (PXM1–PXM12) wereprepared by direct compression and sublimation techniques using crospovidone,croscarmellose sodium and sodium starch glycolate at different concentrations. The precompression properties of the prepared powder blends were evaluated and the compressedtablets were characterized for weight variation, hardness, friability, drug content, wettingtime, water absorption ratio, disintegration time and in-vitro dissolution behavior. Allformulations showed acceptable pharmaceutical characteristics and were in compliance withthe relevant pharmacopeial specifications. Tablets prepared by the sublimation techniqueshowed improved wetting, faster disintegration and enhanced dissolution performance ascompared to the directly compressed formulations, which agrees with the known role ofsublimation in generating tablet porosity and facilitating water penetration.[4,5] Of all theformulations, PXM8 exhibited the most desirable performance with wetting time of 24 ± 0.8 s, disintegration time of 30 ± 0.9 s, water absorption ratio of 89.4 ± 2.0%, and cumulativedrug release of 99.9 ± 0.5% within 60 min. Figures 3–6 illustrate the comparativeperformance of the formulations. Drug release kinetic analysis showed that the optimizedformulation followed first order kinetics. Accelerated stability study did not reveal anysignificant change in the quality attributes of the tablet or dissolution profile during 90 daysof storage under the specified conditions. The stability profile and drug-release kinetics. Theresults as a whole suggested that the sublimation method together with crospovidoneenhanced the dissolution properties of piroxicam dispersible tablets and may be a promisingformulation method to enhance the in-vitro dissolution performance of poorly soluble drugsin water.