COCRYSTALLIZATION ACYCLOVIR-SUCCINIC ACID USING SOLVENT EVAPORATION METHODS

• Main Authors: WINANTARI, AGNES NUNIEK, SETYAWAN, DWI, SISWODIHARDJO, SISWANDONO, SOEWANDHI, SUNDONO NURONO
• 格式: Article PeerReviewed
• 語言: English; English
• 出版: Innovare Academic Science 2017
• 主題: RS Pharmacy and materia medica; RS1-441 Pharmacy and materia medica; RS200-201 Pharmaceutical dosage forms
• 在線閱讀: http://repository.unair.ac.id/75757/1/C-15%20Artikel.pdf; http://repository.unair.ac.id/75757/2/C-15%20Validasi%20dan%20Peer%20Reviewer.pdf; http://repository.unair.ac.id/75757/

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 were prepared using solvent evaporation method. The cocrystals were characterized by polarization microscope, scanning electron microscopy (SEM), differential scanning calorimetry, powder X-ray diffraction (PXRD), and Fourier transform infrared spectroscopy. Results: Physical characterization using polarization microscope and SEM showed the AS cocrystals have unique crystal habit and morphology. Phase diagram at a molar ratio of 50:50% (acyclovir:succinic acid) showed a decrease in the melting temperature, i.e., 176.23°C in comparison with the melting point of the constituent materials (acyclovir 253.53°C and succinic acid 187.29°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 AS acid in ethanol and glacial acetic acid were successfully formed using solvent evaporation methods.