Formation of Paliperidone Cocrystals as Multi-Component Systems for the Functionality Enhancement

The aim of the present investigation was to prepare paliperidone-PHBA PAL-PHBA paliperidone-saccharin sodium PAL-SS cocrystals for improved physico-mechanical properties. The paliperidone cocrystals prepared by solvent evaporation technique were fully characterized by employing melting point aqueous solubility dissolution Fourier Transform Infrared spectroscopy FTIR Differential Scanning CalorimetryDSC Powder X-Ray Diffraction PXRD and Scanning Electron Microscopy SEM techniques.Six formulations of orodispersible tablets of selected paliperidone cocrystals were prepared using Croscarmellose Sodium CCS Sodium Starch Glycolate SSG and Crospovidone CP as superdisintegrants. The prepared batches were evaluated for hardness friability weight uniformity content uniformity in vitro dispersion timeandin vitro drug release.Based on the results formation of cocrystals was confirmed. Pharmaceutical behaviors in terms of solubility dissolution and tabletability suggested superior functionality of cocrystals. The formulations F-III and F-VI containing CP were identified as better formulations among the formulations developed by PAL-SS and PAL-PHBA cocrystals respectively. Further it could be reasonably expected that the obtained formulationmayresult in an increase in its bioavailability with the possibility of reducing drug dosage and side effects.The concept of cocrystallizationwas successfulfor preparing paliperidone cocrystals with improved physico-mechanical properties.