PENGARUH PENGGILINGAN TERHADAP KARAKTERISTIK PADATAN DIDANOSIN

Abstract

Application of mechanical energy in a solid crystalline can cause damage to the crystal and will affect the physicochemical properties of these solids. The purpose of this study is to investigate the effect of milling on the characteristics of solids didanosin (2',3'-dideoxyinosine or DDI). The milling of DDI was performed using Retsch mortar grinder RM 100 for 15 and 30 minutes. Characterization was carried out using X-Ray Powder Diffraction, Differential Scanning Calorimeter (DSC), Scanning Electron Microscope (SEM), and Fourier Transform-Infra Red (FT-IR) methods. The relative crystallinity index was determined by X-ray powder diffraction method. Solvent solubility test was performed in water to observe the effects of mechanical milling on the physicochemical properties. Diffractogram of DDI shows several major peaks and the maximum intensity is observed at the 2θ angle of 6.0 o and was used to calculate the relative crystallinity index. Milling of the DDI does not change the positions of the 2θ reflection angles, but has reduced the peak intensity at those particular angles by a factor of up to 40.8% and 30.4%, respectively. DSC thermogram of DDI shows the appearance of two endothermic peaks at 179.5 o C, which is the melting point of the DDI, and at 285.0 o C, as well as the appearance of one exothermic peak at 183 oC. The melting point of the DDI is slightly shifted to 180.2 o C and 176.9 o C after milling for 15 minutes and 30 minutes respectively. SEM photomicrographs shows that the size of DDI decreases with milling time. FTIR spectrum shows no shift in wave number of the clusters in DDI after milling. The solubility of the DDI increases after 15 and 30 minutes of milling, from 24.83 ± 0.73 to 30.25 ± 0 : 18 and 0 : 33 ± 33.76 mg/mL, respectively. Therefore milling, in addition to causing an increase in the surface area, has also caused some crystals to become amorphous, thus increases the DDI’s solubility in water.