Rottendorf Pharma GmbH, Ennigerloh, Germany.
Drug Dev Ind Pharm. 2009 Nov;35(11):1325-32. doi: 10.3109/03639040902902401.
Microcrystalline cellulose (MCC) is the most important pelletization aid in extrusion/spheronization. Because of known disadvantages, the search for substitutes is ongoing. In this context, crospovidone has proven to offer substantial advantages as pelletization aid because of its ability to turn low-soluble active ingredients into fast-dissolving stable pellets.
Pellets from crospovidone with different amounts of paracetamol, hydrochlorothiazide, and spironolactone as model drugs were prepared by extrusion/spheronization. For comparison, pellets with MCC as extrusion aid were also produced. The pellets of different formulations were evaluated in terms of yield, aspect ratio, mean Feret diameter, 10% interval fraction, tensile strength, disintegration, and drug release profile.
Only crospovidone types exhibiting small particle sizes are suitable as pelletization aid. While maintaining the pharmaceutical quality aspects, it was possible to incorporate up to 60% (w/w) active pharmaceutical ingredients (API) into pellets with crospovidone. The most distinguished differences between pellets based on crospovidone and MCC are the disintegration and drug release behavior. The pellets containing binary mixtures of the low-soluble APIs and crospovidone resulted in fast release in contrast to the pellets with MCC as pelletization aid, which exhibited a slow release.
Crospovidone shows an excellent behavior as pelletization aid and produces fast-releasing pellets even with low-soluble APIs.
微晶纤维素（MCC）是挤出/滚圆中最重要的制粒助剂。由于已知的缺点，人们一直在寻找替代品。在这种情况下，交联聚维酮已被证明作为制粒助剂具有很大的优势，因为它能够将低溶性的活性成分转化为快速溶解的稳定颗粒。
用不同量的对乙酰氨基酚、氢氯噻嗪和螺内酯作为模型药物的交联聚维酮颗粒通过挤出/滚圆法制备。为了进行比较，也制备了以 MCC 作为挤出助剂的颗粒。通过收率、长径比、平均 Feret 直径、10%间隔分数、拉伸强度、崩解和药物释放曲线对不同配方的颗粒进行了评估。
只有表现出小粒径的交联聚维酮类型才适合作为制粒助剂。在保持药物质量方面的同时，有可能将高达 60%（w/w）的活性药物成分（API）掺入到交联聚维酮颗粒中。基于交联聚维酮和 MCC 的颗粒之间最显著的区别是崩解和药物释放行为。含有低溶性 API 和交联聚维酮的二元混合物的颗粒与 MCC 作为制粒助剂的颗粒相比，表现出快速释放，而 MCC 作为制粒助剂的颗粒则表现出缓慢释放。
交联聚维酮作为制粒助剂表现出优异的性能，即使使用低溶性 API 也能产生快速释放的颗粒。
