阿替洛尔缓释微丸的制备和处方工艺研究

Preparation of Atenolol Sustained-release Pellets and the Research of Formulation and Process

目的 制备阿替洛尔缓释微丸,并对其体外释放行为进行研究。方法 采用挤出滚圆法制备载药丸芯,利用溶液层积法对载药丸芯进行缓释包衣。以圆整度和释放度为评价指标,对主要工艺参数：滚圆速度、滚圆时间和愈合时间;以及处方因素：微晶纤维素与主药的比例,丸芯粘合剂用量,以及缓释包衣增重进行考察。结果 所制得的缓释微丸在1、6、12、24 h的释放率分别为标示量的10%～15%,20%～45%,50%～75%,85%以上。释药行为符合零级动力学。结论 本研究处方工艺简便,重现性良好,适合工业化生产。

Objectives To prepare once - daily atenolol sustained release pellets with the research of the formulation and process. Methods Prepare the uncoated pellets with extrusion spheronization method and apply the sustained coating with solution layering scheme. Take the spherical shape and sustained release behavior of the pellets as responses, main process influencing factors： extrusion speed, spheronization speed and duration, as well as the main formulation influencing factors： the ratio between microcrystalline cellulose and atenolol, binder concentration and polymer weight gain were studied respectively. Results The accumulated release percent of the selfmade pellets at 2, 6, 12 and 24h intervals were 5% - 12% ,20 - 45% ,50% - 75%, above 85% respectively. The in vitro release behavior of the pellets met zero- order kinetics. Conclusions The formulation and process developed in the study were convenient and repeatable, which was suitable for mass production.