a Philadelphia College of Pharmacy, Department of Pharmaceutical Sciences , University of the Sciences , Philadelphia , PA , USA.
b Ascent Pharmaceuticals, Inc., Research & Development , Central Islip , NY , USA.
Drug Dev Ind Pharm. 2018 Apr;44(4):632-642. doi: 10.1080/03639045.2017.1405975. Epub 2017 Dec 7.
Fine particle ethylcellulose (FPEC) or poly(ethylene oxide) (PEO) addition to a Kollidon CL-SF was investigated to address low yield and poor sphericity in extruded-spheronized pellets.
The success of crospovidone as a diluent in extrusion-spheronization was dependent on a small particle size of the polymer. FPEC aided production of rugged and spherical pellets using a large particle size grade, Polyplasdone XL. PEO acted as an extrusion-spheronization aid when ethylcellulose was the diluent. These extrusion-spheronization aids could serve in this role when Kollidon CL-SF (K CL-SF) is the diluent.
The influence of formulation and process variables on pellet properties was investigated using design of experiments. A planetary mixer was used to prepare powder blends and the wetted mass after addition of water. An EXD 60 extruder produced extrudate that was spheronized in a Q230 marumerizer. Wet pellets were dried in a forced-air oven.
FPEC improved rounding up but reduced pellet yield. Poly(ethylene oxide) imparted desired characteristics to the wetted mass, the extrudate, and the spheronized pellets. Pellet average diameter, yield, sphericity, aspect ratio, friability, and dissolution profile were assessed. Equations for pellet characteristics facilitated discussion of the influences of factors and their interactions. Optimization was performed on pellets that included PEO.
PEO proved to be an exceptional extrusion-spheronization aid in the preparation of pellets using K CL-SF. It facilitated wetted mass extrusion with minimal mass loss to the extruder, and markedly improved the sphericity of the pellets produced by marumerization. Immediate release pellets were obtained.
研究将细颗粒乙基纤维素（FPEC）或聚（环氧乙烷）（PEO）添加到 Kollidon CL-SF 中，以解决挤出球形化颗粒中收率低和球形度差的问题。
作为挤出-球形化稀释剂的共聚维酮的成功取决于聚合物的小粒径。FPEC 有助于使用较大粒径等级的 Polyplasdone XL 生产坚固且球形的颗粒。PEO 作为挤出-球形化助剂，当乙基纤维素为稀释剂时。当 Kollidon CL-SF（K CL-SF）为稀释剂时，这些挤出-球形化助剂可以在这种作用。
使用实验设计研究制剂和工艺变量对颗粒特性的影响。行星式混合器用于制备粉末混合物和添加水后的湿质量。EXD 60 挤出机生产挤出物，在 Q230 丸化机中丸化。湿颗粒在强制空气烘箱中干燥。
FPEC 改善了圆整度，但降低了颗粒收率。PEO 赋予湿质量、挤出物和丸化颗粒所需的特性。评估了颗粒平均直径、收率、球形度、纵横比、脆性和溶出度。方程有助于讨论因素及其相互作用的影响。对包含 PEO 的颗粒进行了优化。
PEO 被证明是使用 K CL-SF 制备颗粒的出色挤出-球形化助剂。它促进了湿质量挤出，最大程度地减少了挤出机的质量损失，并显著改善了丸化生产的颗粒的球形度。获得了速释颗粒。
