Liew Celine V, Gu Li, Soh Josephine L P, Heng Paul W S
National University of Singapore, Singapore, Singapore.
Pharm Res. 2005 Aug;22(8):1387-98. doi: 10.1007/s11095-005-5279-3. Epub 2005 Aug 3.
This work seeks to explore and demonstrate the functionality of cross-linked polyvinylpyrrolidone (crospovidone) as a spheronization aid and a promising alternative to microcrystalline cellulose (MCC).
Pellets were prepared with various grades of crospovidone using both small- and large-scale extrusion-spheronization. A Box-Behnken experimental design was employed to elucidate the effects of operating variables on the quality of the pellets. Size and shape analyses of these pellets were conducted and compared to those prepared using MCC.
Crospovidone was believed to behave like a liquid repository in its interaction with water during extrusion-spheronization, although its binding ability was weaker than that of MCC. Spherical pellets of narrow size distribution could be made from the finer crospovidone grades with different lactose grades. However, crospovidone-based formulations required higher water levels than weight-equivalent MCC-based formulations. Crospovidone pellets were of equivalent quality to those prepared with MCC, especially in the shape, size, and yield.
Crospovidone can be successfully employed as a spheronization aid to produce good pellets without the need of a binder, unlike most of the previously proposed materials. This study exemplified the enormous potential of crospovidone to serve as a competent alternative to MCC in the production of pellets by extrusion-spheronization.
本研究旨在探索并证明交联聚乙烯吡咯烷酮（交联聚维酮）作为一种滚圆助剂的功能，以及它作为微晶纤维素（MCC）的一种有前景的替代品的潜力。
使用不同等级的交联聚维酮，通过小规模和大规模挤出滚圆法制备微丸。采用Box-Behnken实验设计来阐明操作变量对微丸质量的影响。对这些微丸进行尺寸和形状分析，并与使用微晶纤维素制备的微丸进行比较。
在挤出滚圆过程中，交联聚维酮与水相互作用时被认为起到了液体储存库的作用，尽管其结合能力比微晶纤维素弱。使用不同乳糖等级的更细等级的交联聚维酮可以制成尺寸分布窄的球形微丸。然而，基于交联聚维酮的制剂比重量相当的基于微晶纤维素的制剂需要更高的含水量。交联聚维酮微丸的质量与用微晶纤维素制备的微丸相当，特别是在形状、尺寸和收率方面。
与大多数先前提出的材料不同，交联聚维酮可以成功地用作滚圆助剂，无需粘合剂即可生产出优质微丸。本研究例证了交联聚维酮在通过挤出滚圆法生产微丸时作为微晶纤维素的有效替代品的巨大潜力。
