The effect of compression on solid-state properties of desloratadine and multicomponent crystal

Abstract

Tablet pharmaceuticals manufacturing process involves several processes i.e. granulation, drying, milling, and compression. This study was conducted to determine the effect of compression of desloratadine (DES) and multicomponent crystal (MCC), which is a salt from DES, on their solid-state properties. A compression method for tablet formation was conducted using a hydraulic pressure machine with punch diameter of 13 mm. Both DES and MCC were made into tablets with the same tensile strength, which is 1.36 MPa. DES and MCC powder and tablet were each evaluated for their physicochemical properties, including analysis of powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and tablet dissolution. PXRD diffractogram analysis results on DES and MCC showed that the degree of crystallinity decreased after the compression process. There were no polymorphic transformation in DES and MCC after compression. DSC analysis showed a decrease of enthalpy after DES and MCC are compressed. FTIR showed the same spectra pattern for DES and MCC powder and tablet. The SEM scans showed a tendency for interparticle attachment in DES tablets and none in MCC tablets. Meanwhile, dissolution, as indicated by dissolution efficiency, is only slightly decreased due to the compression process. DES and MCC analysis, all characteristics indicated changes of physicochemical properties after compression pressure, but those changes did not affect their dissolution results.