PREPARATION OF ACYCLOVIR-ISONICOTINAMIDE COCRYSTAL BY SOLVENT EVAPORATION METHOD WITH METHANOL AND ISOPROPANOL
Keywords:
Acyclovir, Cocrystal, Isonicotinamide, Solvent EvaporationAbstract
Acyclovir is a nucleoside synthetic analog antiviral group used in the treatment of Herpes simplex virus (HSV-1 & HSV-2) and Varicella zoster virus (VZV). Acyclovir has low water solubility, so it needs to be modified in the form of cocrystal with isonicotinamide. This study aims to obtain the physical characteristics produced by acyclovir-isonicotinamide cocrystal (1:1) made through the solvent evaporation method with methanol and isopropanol. The crystalline formed is characterized by DSC, PXRD, FT-IR and SEM. The characterization results showed the presence of new crystals that formed between acyclovir-isonicotinamide in methanol and isopropanol solvents. Thermograms showed sharp exothermic peaks at 183.31°C and 186.24°C. The diffractogram showed a new peak at 2θ = 5.19 and 5.82. The spectrum showed a shift in wavelength in the cocrystal formed. The cocrystal has a different morphology compared with parent drug and coformer on analysis using SEM. This research shows that acyclovir can form cocrystal with isonicotinamide by solvent evaporation method with methanol and isopropanol.
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References
W. E. Benitz, “Infectious Disease and Pharmacology: Neonatology Questions and Controversies”, Elsevier Heal. Sci.
K. Robert, M and B. Stanton, Nelson Textbook of Pediatrics volume 2. Elsevier Health Sciences., 2016.
R. Cortesi, L. Ravani, E. Menegatti, M. Dreschsler, and E. Esposito, “Colloidal Dispersions for the Delivery of Acyclovir: A Comparative Study”, Indian J. Pharm. Sci., vol. 73, no. 6, pp. 687–93, 2011.
American Hospital Formulary, AHFS Drug Information. 2008.
B. Gill, T. Kaur, S. Kumar, and G. D. Gupta, “Formulation and evaluation of glimepiride solid dispersion tablets”, Asian J. Pharm., vol. 4, no. 3, pp. 212–218, 2010.
S. Yadav, prakash chandra Gupta, N. Sharma, and J. Kumara, “Cocrystals/ : An Alternative Approach to Modify Physicochemical Properties of Drugs”, Int. J. Pharm. Chem. Biol. Sci., vol. 4, no. March, 2015.
Y. Wicaksono, D. Setyawan, and Siswandono, “Formation of ketoprofen-malonic acid cocrystal by solvent evaporation method”, Indones. J. Chem., vol. 17, no. 2, pp. 161–166, 2017.
A. N. Allam, V. F. Naggar, and S. S. El Gamal, “Formulation and physicochemical characterization of chitosan/Acyclovir cocrystals”, Pharm. Dev. Technol., vol. 18, no. 4, pp. 856–865, 2013.
Y. Kang, J. Gu, and X. Hu, “Syntheses, structure characterization and dissolution of two novel cocrystals of febuxostat”, J. Mol. Struct., vol. 1130, pp. 480–486, 2017.
J. Li et al., “Improving the solubility of dexlansoprazole by cocrystallization with isonicotinamide”, Eur. J. Pharm. Sci., vol. 85, pp. 47–52, 2016.
P.J. Sinko, Martin, N. Alfred, Martin’s Physical Pharmacy and Pharmaceutical Sciences: Physical Chemical and Biopharmaceutical Principles in the Pharmaceutical Sciences. Lippicott Williams & Wilkins, 2011.
A. N. Winantari, D. Setyawan, S. Siswodihardjo, and S. N. Soewandhi, “Cocrystallization acyclovirsuccinic acid using solvent evaporation methods”, Asian J. Pharm. Clin. Res., vol. 10, no. 6, pp. 91– 94, 2017.
Dodd, W. James, Tonge, and H. Kenneth, Thermal Methods. Wiley India PVT., 2008.
F. Alatas, H. Ratih, and S. N. Soewandhi, “Enhancement of solubility and dissolution rate of telmisartan by telmisartan-oxalic acid co-crystal formation”, Int. J. Pharm. Pharm. Sci., vol. 7, no. 3, pp. 423–426, 2015.
H. Yamashita, Y. Hirakura, M. Yuda, T. Teramura, and K. Terada, “Detection of cocrystal formation based on binary phase diagrams using thermal analysis.”, Pharm. Res., vol. 30, no. 1, pp. 70–80, 2013.
N. I. Hilya, W. Agnes Nuniek, D. Setyawan, and E. Hendradi, “Improvement of dissolution properties through acyclovir - Succinic acid cocrystal using solvent evaporation technique”, Int. J. Drug Deliv. Technol., vol. 7, no. 4, pp. 304–309, 2017.
F. Rahman, A. N. Winantari, D. Setyawan, and Siswandono, “Comparison study of grinding and slurry method on physicochemical characteristic of acyclovir – Succinic acid cocrystal”, Asian J. Pharm. Clin. Res., vol. 10, no. 3, pp. 153–158, 2017.
K. Ma, Y. Zhang, H. Kan, L. Cheng, L. Luo, Q. SU, J. Gao, Y. Gao, J. Zhang, “Thermodynamic and Kinetic Investigation on the Crucial Factors Affecting Adefovir Dipivoxil-Saccharin Cocrystallization”, Pharmaceutical Research, vol. 31, pp. 1766-1778, 2014.
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