Aceclofenac polymorphs: Preparation, characterization and intestinal permeation studies

PurposeAceclofenac (ACE) is one of the most popular anti-inflammatory drugs, frequently used for the pain relief in conditions like osteoarthritis, muscular pain, rheumatoid arthritis, periarthritis, spondylitis, sprain and alkylosing arthritis. However, being important non-steroidal anti-inflammatory agent (NSAID), still the polymorphic attributes of ACE are relatively less explored. Therefore, we aimed to study the polymorphic transitions of ACE employing various solvents and also to correlate with the biological transport of ACE.MethodsThe various polymorphic forms were prepared using rotatory evaporation and solvent drying techniques. The developed polymorphic forms were characterized by melting point, Fourier-transform infrared (FTIR) spectroscopy, Raman spectroscopy, differential scanning calorimetry (DSC), X-ray powder diffraction and were biologically evaluated in rats vis-à-vis the plain ACE.ResultsThe developed forms were found to enhance the drug permeability across GIT in comparison to that of the granular plain drug, indicating the significant dependence of bioavailability of ACE on the packing arrangement of the drug molecules.ConclusionThese findings are encouraging and provide an insight of the relationship between the polymorphic forms of drugs and the respective biological outcomes.

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