印度Pt拉维申格尔舒格拉大学Amber Vyas团队报道了含辛伐他汀的Eudragit RS纳米颗粒的变量优化，及体内外抗高血压活性评价。相关研究成果于2023年12月21日发表在《颗粒学报》。

BCS II类药物，辛伐他汀水溶性差、首次通过代谢和半衰期短有关。

该工作制备并评价了纳米颗粒。通过使用自变量和因变量对配方和工艺参数进行优化。研究人员进行了初步研究，以确定通过乳化和溶剂蒸发技术形成纳米颗粒的Eudragit聚合物的浓度（10%至30%）和药物与聚合物的比例（1:1至1:5）的合适范围。结果表明，纳米颗粒的平均尺寸受5000RPM、8000RPM和12000RPM的搅拌速度的影响。

观察到在选定范围内从100mg、150mg和200mg，随着药物量增加缔合效率和产率百分比增加。体外释放研究表明，两种制剂具有最高的初始爆发和缓慢的持续药物释放。在体内研究中，总胆固醇下降了2.93倍，甘油三酯水平上升了3.27倍。

附：英文原文

Title: Optimization of variables and assessment of in-vitro and in-vivo antihyperlipidemic activity of Eudragit RS nanoparticles containing simvastatin

Author: Bina Gidwani , Vishal Jain , Veenu Joshi , Ravindra Kumar Pandey , Shiv Shankar Shukla , Amber Vyas

Issue&Volume: 2023/12/21

Abstract: Simvastatin; a BCS class II drug is associated with poor aqueous solubility, first-pass metabolism and short half life. In the present work nanoparticles were prepared and evaluated. Optimization of formulation and process parameters was done through use of independent and dependent variables. Preliminary studies were done to determine suitable range of the concentration of Eudragit polymer (10% to 30%) and the ratio of drug to polymer (1:1 to 1:5) for the formation of nanoparticles by emulsification and a solvent evaporation technique. Results revealed that the mean size of nanoparticles was affected by stirring speed from 5000 RPM, 8000 RPM and 12000 RPM. The results of increase in association efficiency and percent yield with increase in amount of drug from 100 mg, 150 mg and 200 mg in selected range were observed. In-vitro release studies showed that two formulations posses highest initial burst and slow sustained drug release. There was 2.93-fold decrease in total cholesterol and 3.27-fold increases in triglyceride level during in-vivo study.

DOI: 10.1016/j.partic.2023.12.006

Source: https://www.sciencedirect.com/science/article/abs/pii/S1674200123003231