KAJIAN PUSTAKA PSEUDOPOLIMORF OBAT ANTIVIRAL SERTA ANALISIS TRANSFORMASI HIDRAT ANTIVIRAL LAMIVUDIN DAN ASIKLOVIR

• Main Author: Hanifah Ismi Putri, Syimah
• Format: Final Project
• Language: Indonesia
• Online Access: https://digilib.itb.ac.id/gdl/view/56600
• Institution: Institut Teknologi Bandung

Antivirals as solid pharmaceutical ingredients can be found in their pseudopolymorphs, namely hydrates and solvates. Pseudopolymorphs affect antiviral physicochemical properties and sometimes undergo transformation because of solvents or manufacturing processes. This final project reviewed articles about antiviral pseudopolymorphy with stability, solubility, and dissolution rate. Several antivirals were reported in hydrates and solvates forms, that can transform to the most stable form, have various solubility, and various dissolution rates. Further experiments were carried out on lamivudine and acyclovir. This experiment was conducted to observ their pseudopolymorphs in various solvent compositions and their transformations due to thermal and mechanical processes. Lamivudin was reported as anhydrates, 1/5 hydrate, and hemihydrate forms. While acyclovir was reported as 2/3 hydrate, dihydrate, and two stable anhydrates forms. Each antiviral was recrystallized in various methanol-water compositions, then the starting material was crushed and heated at 100o C. Characterization was carried out using electrothermal, DSC, TG/DTA, FTIR, and PXRD. In this study, the starting material of lamivudine was anhydrates, its water recrystallite is 1/5 hydrate, and its methanol-water recrystallite is hemihydrate. Both recrystallites are needle-shaped. Meanwhile the starting material of acyclovir was 2/3 hydrate, its methanol recrystallite is square-shaped crystals, and its water recrystallite is needle-shaped dihydrate, with transition solvent of these two forms is 40% methanol. Crushing the two antivirals did not give significant effect on their pseudopolymorphs, meanwhile heating of acyclovir caused transformation from 2/3 hydrate to form I anhydrates. Therefore, it is necessary to pay attention during acyclovir manufacturing which gives temperature changes.