Department of Pharmaceutical Products, Federal University of Minas Gerais, Belo Horizonte, Minas Gerais, Brazil.
Drug Dev Ind Pharm. 2010 Nov;36(11):1348-55. doi: 10.3109/03639041003801901.
Simvastatin (SIM), a widely used drug for the treatment of hypercholesterolemia, is a crystalline substance and practically insoluble in water. Its low dissolution rate leads to a poor absorption, distribution, and target organ delivery because the bioavailability of drugs with low aqueous solubility is limited by their dissolution rates.
The aim of this study was to prepare solid dispersions (SD) of SIM with inert carriers in an attempt to improve the release profile.
In this work, SIM SD with polyethylene glycol (PEG 6000) or polyvinylpyrrolidone (PVP K15) in 1:1, 1:2, 1: 3, 1:4, and 1:5 ratios were prepared and their stability and dissolution properties were investigated. SD were characterized by differential scanning calorimetry and X-ray powder diffraction. Tablets containing SD SIM : PEG 6000 were developed and their dissolution profile evaluated.
Drug release from all SD was significantly improved when compared to their corresponding physical mixture or SIM alone. SD SIM:PVP showed drug degradation. The tablets gradually released SIM with a final quantity greater than 80% in 60 minutes.
The preparation of SIM SD with PEG or PVP is a promising strategy to improve the bioavailability of the drug. SIM SD with PEG are more advantageous over the dispersions prepared with PVP because they do not show drug degradation during preparation.
辛伐他汀（SIM）是一种广泛用于治疗高胆固醇血症的药物，它是一种结晶物质，几乎不溶于水。由于低水溶性药物的生物利用度受到其溶解速率的限制，因此其低溶解速率导致吸收、分布和靶器官传递不良。
本研究旨在制备 SIM 与惰性载体的固体分散体（SD），试图改善其释放特性。
在这项工作中，以 1:1、1:2、1:3、1:4 和 1:5 的比例制备了 SIM 与聚乙二醇（PEG 6000）或聚乙烯吡咯烷酮（PVP K15）的 SD，并研究了其稳定性和溶解性能。通过差示扫描量热法和 X 射线粉末衍射对 SD 进行了表征。制备了含有 SD SIM：PEG 6000 的片剂，并评估了其溶解特性。
与相应的物理混合物或单独的 SIM 相比，所有 SD 的药物释放均显著改善。SD SIM:PVP 显示出药物降解。片剂逐渐释放 SIM，60 分钟后最终释放量大于 80%。
用 PEG 或 PVP 制备 SIM SD 是提高药物生物利用度的一种很有前途的策略。与用 PVP 制备的分散体相比，用 PEG 制备的 SIM SD 更具优势，因为它们在制备过程中不会显示出药物降解。
