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 the use of independent and dependent variables. Preliminary studies were done to determine suitable range of the concentration of Eudragit polymer (10%–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. release studies showed that two formulations possess 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 study.

中文翻译：

---

含辛伐他汀的 Eudragit RS 纳米颗粒的变量优化及体内外降血脂活性评估

辛伐他汀是 BCS II 类药物，水溶性差、首过代谢和半衰期短。在目前的工作中，制备并评估了纳米颗粒。通过使用自变量和因变量来优化配方和工艺参数。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合适的 Eudragit 聚合物浓度范围（10%–30%）和药物与聚合物的比例（1:1 至 1:5）。结果表明，纳米颗粒的平均尺寸受到搅拌速度（5000 RPM、8000 RPM 和 12000 RPM）的影响。观察到在选定范围内随着药物量从100mg、150mg和200mg增加，结合效率和百分比产率增加的结果。释放研究表明，两种制剂具有最高的初始突释和缓慢的持续药物释放。研究期间，总胆固醇下降了 2.93 倍，甘油三酯水平增加了 3.27 倍。