COCRYSTALLIZATION ACYCLOVIR-SUCCINIC ACID USING SOLVENT EVAPORATION METHODS

摘要

Objective : The aim of this research is to prepare and characterize cocrystals of acyclovir through cocrystallization of acyclovir – succinic acid (AS) to improve the physical properties of the drug. Methods : AS cocrystals was prepared using solvent evaporation method. The cocrystals were characterized by Polarization Microscope, Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD), and Fourier Transform Infrared Spectroscopy (FTIR). Results : Physical characterization using polarization microscope and SEM showed the AS cocrystals have unique crystal habit and morphology. Phase diagram at molar ratio of 50% : 50% (acyclovir : succinic acid) showed a decrease in the melting temperature i.e 176.23 o C in comparison with the melting point of the constituent materials (acyclovir 253.53 o C and succinic acid 187.29 o C). The PXRD pattern of AS cocrystals (ethanol) exhibited new diffraction peaks at 2θ = 5.91; 9.16; and 13.40. Besides, cocrystals of AS (glacial acetic acid) indicated new peaks at 2θ = 5.98; 9.19; and 13.43. Furthermore, there was a shift in the N-H, O-H and C=O. Conclusion : Cocrystallization of acyclovir-succinic acid (AS) in ethanol and glacial acetic acid were succesfully formed using solvent evaporation methods.