Compression force effect on characteristics of loratadinesuccinic acid cocrystal prepared by slurry method

Abstract

Loratadine belongs to second generation antihistamine (H1) drug and is known to form cocrystal withsuccinic acid in stoichiometry of 1:1 using slurry method. This study was conducted to further investigate cocrystalphase behavior upon compression. Sample of cocrystal phase was compressed with various compression forces intotablet form on 10 mm diameter punch. Then, the tablet was characterized for the mechanical properties and physicalcharacterization was conducted using Differential Thermal Analysis (DTA), X-ray Powder Diffraction (XRPD), andScanning Electron Microscope (SEM). According to tensile strength profile, cocrystal phase showed better mechanicalproperty as it possessed higher tensile strength value compared to loratadine alone. DTA thermograms exhibitedsuccinic acid characteristic peak alongside with endothermic peak of cocrystal phase which were compressed on higherforce. It suggests that cocrystal undergoes partial dissociation to the starting components under compression. Powderdiffractograms showed reduced intensity of tableted cocrystal compared to powder one for all compression force. SEMphotomicrograph observed a loss of particle boundaries of cocrystal upon compression, as sintering phenomenaoccurred. It is predicted that compression force can influence physical characteristics of cocrystal of loratadine-succinicacid by driving dissociation and sintering phenomena.