Grdešič Peter, Vrečer Franc, Ilić Ilija
a Krka, tovarna zdravil, d.d., Novo mesto , Novo mesto , Slovenia ;
b Department of Pharmaceutical Technology, Faculty of Pharmacy , University of Ljubljana , Ljubljana , Slovenia.
Drug Dev Ind Pharm. 2016 Nov;42(11):1877-86. doi: 10.1080/03639045.2016.1181079. Epub 2016 May 13.
Information about flow and compaction properties of hypromellose (HPMC) polymers is essential for the technologists who are facing challenges regarding poor flow and compaction while developing new controlled release matrix tablets. There is a profound lack of studies in this field and none of the published ones deal with the compaction of the newly introduced HPMC grades specifically designed for direct compression (DC).
The objective behind this study was the evaluation of flow and compaction properties of six different grades of HPMC substitution type 2208 polymers, including two second generation directly compressible grades from Dow Chemical Company (K100LV, K15M, K4M CR, K4M DC, K100M CR and K100M DC).
Flow properties were determined using flow time and Carr index. Compaction properties were quantified using "out-of-die" Heckel and modified Walker models as well as tensile strength profile and elastic recovery. We used statistical approach to analyze the results.
Due to larger, rounder and smoother particles both DC grades showed distinctly better flow properties compared to their non-DC counterparts. Overall, K15M showed the best compaction properties, closely followed by K100LV. K100M grades showed superior compaction properties over K4M grades. The new, second generation DC grades had poorer compaction properties, however, they exhibited better flow properties on the other hand. Considering all compaction results, the Heckel model gave better description of compressibility compared to the Walker model, so it may be preferred in case of studying HPMC polymers and other similar materials.
对于在开发新型控释骨架片时面临流动性和压缩性差等挑战的技术人员而言，羟丙甲纤维素（HPMC）聚合物的流动性和压缩性信息至关重要。该领域的研究严重匮乏，且已发表的研究均未涉及专门为直接压片（DC）设计的新引入HPMC等级的压缩性。
本研究的目的是评估六种不同等级的2208型取代羟丙甲纤维素聚合物的流动性和压缩性，其中包括陶氏化学公司的两种第二代可直接压片等级（K100LV、K15M、K4M CR、K4M DC、K100M CR和K100M DC）。
使用流动时间和卡尔指数测定流动性。使用“模外”赫克尔模型和修正的沃克模型以及抗张强度曲线和弹性回复率来量化压缩性。我们采用统计方法分析结果。
由于颗粒更大、更圆且更光滑，两种直接压片等级的流动性明显优于其非直接压片对应等级。总体而言，K15M表现出最佳的压缩性，紧随其后的是K100LV。K100M等级的压缩性优于K4M等级。新型第二代直接压片等级的压缩性较差，然而，另一方面它们表现出更好的流动性。综合所有压缩结果，与沃克模型相比，赫克尔模型对可压缩性的描述更好，因此在研究HPMC聚合物和其他类似材料时可能更受青睐。
