Production of spherical pellets by a hot-melt extrusion and spheronization process.
Production of spherical pellets by a hot-melt extrusion and spheronization process.
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DOI：
10.1016/s0378-5173(02)00152-7
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发表时间：
2002-08
影响因子：
5.8
通讯作者：
C. R. Young;J. J. Koleng-J.;J. Mcginity
中科院分区：
文献类型：
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作者：
C. R. Young;J. J. Koleng-J.;J. Mcginity
采用热熔挤出滚圆法成功制备了茶碱控释球形微丸。将无水茶碱、Eudragit® Preparation 4135 F、微晶纤维素和聚乙二醇8000粉末的粉末共混物过筛，共混，然后在Randcastle Microtruder®中熔融挤出。通过首先将薄的挤出复合材料棒切割成对称的粒料来制备热熔挤出粒料。然后将粒料在传统的滚圆机中在升高的温度下滚圆。研究了颗粒制剂组分和热熔挤出物的热性质，以确定制剂对HME的适用性。使用扫描电子显微镜检查小球以确定滚圆时间对表面形态的影响。茶碱从热熔挤出球形丸粒中的释放速率在初始丸粒生产后和在密封HDPE容器中在25°C/60%RH下储存1年后使用USP 24装置2溶解测试表征。
Controlled-release theophylline containing spherical pellets were successfully produced by a hot-melt extrusion (HME) and spheronization process. A powder blend of anhydrous theophylline, Eudragit® Preparation 4135 F, microcrystalline cellulose and polyethylene glycol 8000 powder was sieved, blended and then melt-extruded in a Randcastle Microtruder®. The hot-melt extruded pellets were prepared by first cutting a thin, extruded composite rod into symmetrical pellets. The pellets were then spheronized in a traditional spheronizer at an elevated temperature. Thermal properties of the pellet formulation components and the hot-melt extrudate were studied to determine suitability of the formulation for HME. Pellets were examined using scanning electron microscopy to determine the effect of spheronization time on surface morphology. The rate of release of theophylline from the hot-melt extruded spherical pellets was characterized using USP 24 Apparatus 2 dissolution testing after initial pellet production and after 1 year storage in sealed HDPE containers at 25°C/60% RH.