HILYA NUR IMTIHANI, NIM.: 051415153016 (2016) PEMBENTUKAN KOKRISTAL ASIKLOVIR DENGAN MENGGUNAKAN KOFORMER ASAM SUKSINAT YANG DIBUAT DENGAN METODE PENGUAPAN PELARUT (Menggunakan Tiga Jenis Pelarut yang Berbeda yaitu Etanol, Asam Asetat Glasial, dan HCl 0,1 N). Thesis thesis, Airlangga University.

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Abstract

Acyclovir is one of the most important antiviral drug used today that have several problems with its physical properties. The aim of this study is to prepared cocrystal of acyclovir with succinic acid as coformer to improve the physical properties of the drug especially its dissolution rate. Screening for formation of cocrystals was conducted with various solvent with the used of the solvent evaporation-crystallization method that is ethanol, acetic acid glacial and HCl 0,1 N. The potential cocrystalline phase were characterized by PXRD, DSC, FTIR and SEM. The dissolution test was conducted using Spectrophotometry UV method with λ =252.04 nm. The screening indicated that acyclovir formed novel cocrystals with succinic acid in the three different solvents. PXRD profile show that there is three puncaks in ethanol cocrystal in angle 2θ 5.9134o (int = 79.35%) ; 9.1645o (int = 16.81%) and 13.4044o (int = 13.99 %). For acetic acid glacial and HCl 0,1 N cocrystal there is one puncak in angle 2θ 5.9263o (int = 10.18%) and 2θ 9.6011o (int = 28.26%). In analysis diffractogram DSC formed ethanol cocrystal with melting point 175.84oC (Δ H = -1.86 Jg^-1). The melting point of acetic acid glacial cocrystal is 178.41oC (Δ H = -0.14 Jg^-1) and HCl 0,1 N cocrystal is 156.75oC (Δ H = -23.53 Jg^-1). The dissolution rate of the cocrystals measured by the effisiency disolution (ED45) that considerable faster than that pure acyclovir and the physical mixtures (ACV-SA). On the result of FTIR analysis there is changes of the wavenumber that indicated that there is cocrystal formed. And for SEM analysis, morphology of cocrystals was different than the original materials. In dissolution test, ethanol and acetic acid glacial cocrystals have better efficiency dissolution (ED45) (92.96 %) than the acyclovir ED45 (84.48 %). But HCl 0,1 N cocrystal has lower ED45 than acyclovir that is 48.19 %. We successfully improved the physical properties and dissolution rate of acyclovir by cocrystallization using ethanol and acetic acid glacial solvents.

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