a Department of Pharmacy, School of Applied Sciences , University of Huddersfield , Queensgate , Huddersfield , UK.
b School of Chemical Engineering , University of Birmingham , Edgbaston , Birmingham , UK.
Pharm Dev Technol. 2018 Feb;23(2):183-197. doi: 10.1080/10837450.2017.1389958. Epub 2017 Oct 29.
Swelling, erosion, deformation, and consolidation properties can affect the performance of cellulose ethers, the most commonly used matrix former in hydrophilic sustained tablet formulations. The present study was designed to comparatively evaluate the swelling, erosion, compression, compaction, and relaxation properties of the cellulose ethers in a comprehensive study using standardised conditions. The interrelationship between various compressional models and the inherent deformation and consolidation properties of the polymers on the derived swelling and erosion parameters are consolidated. The impact of swelling (K) on erosion rates (K) and the inter-relationship between Heckel and Kawakita plasticity constants was also investigated. It is evident from the findings that the increases in both substitution and polymer chain length led to higher K, but a lower K; this was also true for all particle size fractions regardless of polymer grade. Smaller particle size and high substitution levels tend to increase the relative density of the matrix but reduce porosity, yield pressure (P), Kawakita plasticity parameter (b) and elastic relaxation. Both K versus K (R = 0.949-0.980) and P versus. b correlations (R = 0.820-0.934) were reasonably linear with regards to increasing hydroxypropyl substitution and molecular size. Hence, it can be concluded that the combined knowledge of swelling and erosion kinetics in tandem with the in- and out-of-die compression findings can be used to select a specific polymer grade and further to develop and optimize formulations for oral controlled drug delivery applications.
肿胀、侵蚀、变形和固结性能会影响纤维素醚的性能，纤维素醚是亲水持续释放片剂配方中最常用的基质形成剂。本研究旨在使用标准化条件对纤维素醚的膨胀、侵蚀、压缩、压实和松弛性能进行综合比较评估。在聚合物的固有变形和固结性能的基础上，整合了各种压缩模型与聚合物之间的相互关系，以及聚合物的固有变形和固结性能。还研究了溶胀（K）对侵蚀速率（K）的影响以及 Heckel 和 Kawakita 塑性常数之间的关系。研究结果表明，取代度和聚合物链长的增加都会导致 K 值增加，但 K 值降低；这对于所有粒径分数都是如此，无论聚合物等级如何。较小的粒径和较高的取代水平往往会增加基质的相对密度，但会降低孔隙率、屈服压力（P）、Kawakita 塑性参数（b）和弹性松弛。K 与 K（R=0.949-0.980）和 P 与 b 的相关性（R=0.820-0.934）均随羟丙基取代度和分子大小的增加呈合理线性关系。因此，可以得出结论，溶胀和侵蚀动力学的综合知识与压模内和压模外压缩结果相结合，可用于选择特定的聚合物等级，并进一步开发和优化用于口服控释药物递送应用的制剂。
