微晶纤维素
无定形固体
去玻璃化
溶解试验
材料科学
溶解度
化学
分析化学(期刊)
色谱法
结晶
溶解
色散(光学)
纤维素
结晶学
有机化学
生物制药分类系统
光学
物理
作者
Rania Hamed,Eman M. Mohamed,Khaldia Sediri,Mansoor A. Khan,Ziyaur Rahman
标识
DOI:10.1016/j.ijpharm.2021.120657
摘要
This study aimed to improve the dissolution of the poorly soluble drug lopinavir (LPV) by preparing amorphous solid dispersions (ASDs) using solvent evaporation method. The ASD formulations were prepared with ternary mixtures of LPV, Eudragit® E100, and microcrystalline cellulose (MCC) at various weight ratios. The ASDs were subjected to solid-state characterization and in vitro drug dissolution testing. Chemometric models based on near infrared spectroscopy (NIR) and NIR-hyperspectroscopy (NIR-H) data were developed using the partial least squares (PLS) regression and externally validated to estimate the percent of the crystalline LPV in the ASD. Initially, the solid-state characterization data of ASDs showed transformation of the drug from crystalline to amorphous. Negligible fraction of crystalline LPV was present in the ASD (3%). Compared to pure LPV, ASDs showed faster and higher drug dissolution (<2% vs. 60.3–73.5%) in the first 15 min of testing. The ASD was stable against crystallization during stability testing at 40 °C/75% for a month. In conclusion, the prepared ASD was stable against devitrification and enhance the dissolution of LPV.
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