挤出-滚圆法制备吗替麦考酚酯微丸

Preparation of Mycophenolate Mofetil Pellets by Extrusion-spheronization Process

采用挤出-滚圆法制备吗替麦考酚酯微丸,以单因素试验优化了挤出-滚圆工艺参数及黏合剂、崩解剂和微晶纤维素用量等处方因素。所得优化工艺为:吗替麦考酚酯75%,微晶纤维素15%,崩解剂羧甲淀粉钠10%,并以含1.5%羧甲纤维素钠的25%乙醇为黏合剂,挤出和滚圆速度为928 r/min,滚圆5 min。制品表面光滑,坚硬,圆整度良好,能用于后续的流化床包衣,并且在含0.5%十二烷基磺酸钠的p H 6.8磷酸钠缓冲液中2 h累积释放率达80%以上。

The mycophenolate mofetil（1） pellets were prepared by extrusion-spheronization method. The process parameters of extrusion-spheronization and formulation factors such as the amounts of adhesive, disintegrant and microcrystalline cellulose were optimized by single factor test. The optimal formulation contained 75% of 1, 15%of microcrystalline cellulose, 10% of carboxymethylstarch sodium as disintegrant with 25% ethanol containing 1.5% of carmellose sodium as adhesive. The rates of extrusion and spheronization were 928 r/min, the time of spheronization was 5 min. The pellets prepared under above conditions were smooth, hard and round enough to be coated in the following step. Furthermore, in p H 6.8 sodium phosphate buffer containing 0.5% sodium dodecyl sulfonate, the cumulative release at 2 h of the optimal pellets was above 80%.