Zaini Erizal, Wahyu Deni, Octavia Maria Dona, Fitriani Lili
Department of Pharmaceutics, Faculty of Pharmacy, Andalas University, Padang, Indonesia.
Department of Pharmaceutical Technology, Sekolah Tinggi Ilmu Farmasi, Padang, Indonesia.
J Pharm Bioallied Sci. 2017 Jan-Mar;9(1):22-25. doi: 10.4103/0975-7406.206218.
The aim of this study was to investigate the influence of the milling process on the solubility of efavirenz.
Milling process was done using Nanomilling for 30, 60, and 180 min. Intact and milled efavirenz were characterized by powder X-ray diffraction, scanning electron microscopy (SEM), spectroscopy infrared (IR), differential scanning calorimetry (DSC), and solubility test.
The X-ray diffractogram showed a decline on peak intensity of milled efavirenz compared to intact efavirenz. The SEM graph depicted the change from crystalline to amorphous habit after milling process. The IR spectrum showed there was no difference between intact and milled efavirenz. Thermal analysis which performed by DSC showed a reduction on endothermic peak after milling process which related to decreasing of crystallinity. Solubility test of intact and milled efavirenz was conducted in distilled water free CO with 0.25% sodium lauryl sulfate media and measured using high-performance liquid chromatography method with acetonitrile: distilled water (80:20) as mobile phases. The solubility was significantly increased ( < 0.05) after milling processes, which the intact efavirenz was 27.12 ± 2.05, while the milled efavirenz for 30, 60, and 180 min were 75.53 ± 1.59, 82.34 ± 1.23, and 104.75 ± 0.96 μg/mL, respectively.
Based on the results, the solubility of efavirenz improved after milling process.
本研究的目的是调查研磨过程对依非韦伦溶解度的影响。
使用纳米研磨进行研磨过程，时间分别为30、60和180分钟。通过粉末X射线衍射、扫描电子显微镜（SEM）、红外光谱（IR）、差示扫描量热法（DSC）和溶解度测试对完整和研磨后的依非韦伦进行表征。
X射线衍射图显示，与完整的依非韦伦相比，研磨后的依非韦伦峰强度下降。SEM图描绘了研磨过程后从结晶习性到无定形习性的变化。IR光谱显示完整和研磨后的依非韦伦之间没有差异。DSC进行的热分析表明，研磨过程后吸热峰降低，这与结晶度降低有关。在含有0.25%十二烷基硫酸钠介质的无CO蒸馏水（原文有误，应为无二氧化碳蒸馏水）中对完整和研磨后的依非韦伦进行溶解度测试，并使用以乙腈：蒸馏水（80:20）作为流动相的高效液相色谱法进行测量。研磨过程后溶解度显著增加（P<0.05），完整的依非韦伦溶解度为27.12±2.05，而研磨30、60和180分钟后的依非韦伦溶解度分别为75.53±1.59、82.34±1.23和104.75±0.96μg/mL。
基于结果，研磨过程后依非韦伦的溶解度提高。
