AI Article Synopsis
- - The study focused on enhancing the dissolution of the poorly soluble drug lopinavir (LPV) by creating amorphous solid dispersions (ASDs) using a solvent evaporation method with specific ratios of LPV, Eudragit® E100, and microcrystalline cellulose.
- - Solid-state characterization confirmed that the drug transitioned from crystalline to amorphous form, with only about 3% of crystalline LPV remaining in the ASDs.
- - The ASDs significantly improved drug dissolution rates (60.3-73.5% in 15 minutes compared to <2% for pure LPV) and proved stable against crystallization over a month at high temperatures and humidity.
Article Abstract
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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| http://dx.doi.org/10.1016/j.ijpharm.2021.120657 | DOI Listing |
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