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 with succinic acid in stoichiometry of 1:1 using slurry method. This study was conducted to further investigate cocrystal phase behavior upon compression. Sample of cocrystal phase was compressed with various compression forces into tablet form on 10 mm diameter punch. Then, the tablet was characterized for the mechanical properties and physical characterization was conducted using Differential Thermal Analysis (DTA), X-ray Powder Diffraction (XRPD), and Scanning Electron Microscope (SEM). According to tensile strength profile, cocrystal phase showed better mechanical property as it possessed higher tensile strength value compared to loratadine alone. DTA thermograms exhibited succinic acid characteristic peak alongside with endothermic peak of cocrystal phase which were compressed on higher force. It suggests that cocrystal undergoes partial dissociation to the starting components under compression. Powder diffractograms showed reduced intensity of tableted cocrystal compared to powder one for all compression force. SEM photomicrograph observed a loss of particle boundaries of cocrystal upon compression, as sintering phenomena occurred. It is predicted that compression force can influence physical characteristics of cocrystal of loratadine-succinic acid by driving dissociation and sintering phenomena.

Keywords

• Cocrystal
• compression force
• loratadine
• physical characterization
• succinic acid

References

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