Pharmaceutical Cocrystal of Piroxicam: Design, Formulation and Evaluation

Abstract

Purpose: Cocrystallisation of drug with coformers is a promising approach to alter the solid sate properties of drug substances like solubility and dissolution. The objective of the present work was to prepare, formulate and evaluate the piroxicam cocrystal by screening various coformers.Methods: Cocrystals of piroxicam were prepared by dry grinding method. The melting point and solubility of crystalline phase was determined. The potential cocrystal was characterized by DSC, IR, XRPD. Other pharmaceutical properties like solubility and dissolution rate were also evaluated. Orodispersible tablets of piroxicam cocrystal were formulated, optimized and evaluated using 32 factorial design.Results: Cocrystals of piroxicam-sodium acetate revealed the variation in melting points and solubility. The cocrystals were obtained in 1:1 ratio with sodium acetate. The analysis of Infrared explicitly indicated the shifting of characteristic bands of piroxicam. The X-Ray Powder Diffraction pattern denoted the crystallinity of cocrystals and noteworthy difference in 2θ value of intense peaks. Differential scanning calorimetry spectra of cocrystals indicated altered endotherms corresponding to melting point. The pH solubility profile of piroxicam showed sigmoidal curve, which authenticated the pKa-dependent solubility. Piroxicam cocrystals also exhibited a similar pH-solubility profile. The cocrystals exhibited faster dissolution rate owing to cocrystallization as evident from 30% increase in the extent of dissolution. The orodispersible tablets of piroxicam cocrystals were successfully prepared by direct compression method using crosscarmelose sodium as superdisintegrant with improved disintegration time (30 sec) and dissolution rate.Conclusion: The piroxicam cocrystal with modified properties was prepared with sodium acetate and formulated as orodispersible tablets having faster disintegration and greater dissolution rate.

Co-Crystals: A Review

“…Author synthesized Cocrystal of Piroxicam using sodium acetate, saccharine sodium Urea, Nicotinamide, resorcinolas conformer and studied difference in melting point of drug and cocrystals. Melting point of sodium acetate, saccharine sodium coformers were high previously but after forming cocrystal with Piroxicam it get decreased, while melting point of cocrystal of Urea, Nicotinamide, resorcinol was increased 19 .…”

Design and Preparation of Zaltoprofen-Nicotinamide Pharmaceutical Cocrystals via Liquid Assisted Grinding Method

“…The similarity factor test denotes the dissolution of ZFN was dissimilar to the prepared cocrystals (f 2 value 15 and 20 for 1:1 and 1:2 cocrystals respectively). 39 The result was compared by Dunnet test and statistically significant difference in the dissolution of cocrystals and ZFN was obtained (P< 0.05).…”

Crystal Engineering of Antiviral Agent Efavirenz for Solubility Enhancement

“…The active pharmaceutical ingredient-EFV and its corystals with FA was evaluated for various micromeritic flow properties that is bulk density, tapped density, Carr's index, Hausner's ratio and angle of repose 19 .…”

“…The resulting ∆δ value for EFV and FA is 6.11 (MJ/m 3 ) 1/2 which indicates the miscibility of an API with the coformer-FA 16) as ∆δ value <7. It indicates that the components are miscible consequently may result in formation of cocrystal 19,25 .…”