The Effect of Compression Force on Alteration of Desloratadine and its Multicomponent Crystal Crystallinities Using X-Ray Diffraction and ATR-FTIR Techniques

Abstract

This work studied the effect of compression force on the desloratadine (DES) and its multi-component crystal (MCC) formulation and focused on the molecular crystal behavior of DES and MCC after compression. Crystallinity behavior of drugs in a mechanical process is to be interesting manner. In this research, DES and MCC were compressed using hydraulic presser equipped with 13 mm flat-face punch under different compression pressures in a range of 25 – 350 MPa. The solid state of DES and its MCC was evaluated using powder X-ray diffraction (XRD) and attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy. Single XRD was carried out to confirm the molecular structure of crystal lattice. Powder XRD diffractogram under different compression forces was compared to the crystallinity degree, crystallite size and peak broadening. Those parameters were processed using Origin software. Crystallinity degree was calculated using Ruland’s methods, meanwhile, the crystallinity size was calculated using Scherrer’s equation after corrected to the broadening (full width at half maximum; FWHM) and diffraction baseline. As increasing the compression force, degree and size of crystallinity and FWHM were altered. In addition, the degree of crystallinity and crystallite size of DES and MCC decreased, while the FWHM increased. Furthermore, alteration of PXRD in DES was higher than that of MCC which had no alteration as increase as the compression force. FTIR result showed that neither DES nor MCC had no significant alteration after compression. However, the tabletability of MCC was better than DES owing to the potential slip plane of MCC.