Department of Pharmaceutics, Smt. R. B. Patel Mahila Pharmacy College, Atkot, Gujarat, India.
Pharm Dev Technol. 2011 Apr;16(2):146-51. doi: 10.3109/10837450903544559. Epub 2010 Jan 25.
The aim of the present study was to prepare and evaluate microspheres of Eudragit containing an antiviral drug stavudine. Microspheres were prepared by O/O solvent evaporation method using acetone/liquid paraffin system. The prepared microspheres were characterized for their micromeretic properties and entrapment efficiency; as well by Fourier transformed infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD) and scanning electron microscopy (SEM) which revealed the crystalline nature of drug in a final state. The in vitro studies revealed the controlled release of drug from microspheres up to 12 h and the best fit release kinetics was achieved with a Higuchi plot and found to be diffusion controlled. The yields of preparation and entrapment efficiencies were very high with a larger particle size for all the formulations. Mean particle size, entrapment efficiency and production yield were highly influenced by the type of polymer and polymer concentration.
本研究旨在制备并评价载抗病毒药物司他夫定的 Eudragit 微球。采用 O/O 溶剂蒸发法,以丙酮/液体石蜡为溶剂系统制备微球。对所制备的微球进行了粒径分布和包封率等微细化性质的评价;同时通过傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)、X 射线粉末衍射(XRPD)和扫描电子显微镜(SEM)进行了表征,结果表明药物在最终状态下为晶型。体外研究表明,药物能够从微球中持续释放长达 12 小时,且 Higuchi 图拟合的结果显示,药物释放动力学符合扩散控制。所有制剂的包封率和产率都非常高,粒径也较大。聚合物的类型和浓度对平均粒径、包封率和产率有很大影响。