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聚合物片剂的细分行为。

The subdivision behavior of polymeric tablets.

机构信息

Laboratory of Food, Drugs and Cosmetics (LTMAC), University of Brasília (UnB), 70910-900 Brasília, DF, Brazil.

Laboratory of Food, Drugs and Cosmetics (LTMAC), University of Brasília (UnB), 70910-900 Brasília, DF, Brazil.

出版信息

Int J Pharm. 2019 Sep 10;568:118554. doi: 10.1016/j.ijpharm.2019.118554. Epub 2019 Jul 20.

Abstract

The subdivision behavior of polymeric tablets produced with the well-known polymers Soluplus® (SOL), polyvinyl pyrrolidone co-vinyl acetate (PVPVA) and hydroxypropyl methylcellulose (HPMC) was evaluated in this study. The polymeric tablets were submitted to different post-treatments (aging, thermal and exposure to compressed gaseous carbon dioxide) and its mechanical, spectroscopic and microstructure properties were assessed. SOL tablets showed the best results for tablet subdivision, particularly, the mean mass variation (3.9%) was significantly lower than the other two polymeric tablets (7.2% and 9.1% for PVPVA and HPMC, respectively), and showed better results than common tablets produced from powder matrices (7-14%). SOL tablets were also more sensitive to the different post-treatments applied, which reduced the mass loss and friability from 1.5% and 0.8%, respectively, to values close to zero and without altering their porosity. The thermal treatment of PVPVA tablets, in turn, also led to similar subdivision results, with mass loss of 0.3% and friability of 0.02%. In contrast, the granules of HPMC presented compaction difficulties making its tablets unsuitable for the subdivision process, even after additional post-treatment. Polymeric matrices with uniform internal structure and appropriate mechanical strength are the key to a better adaptation for the tablet subdivision.

摘要

本研究评估了知名聚合物 Soluplus®(SOL)、共聚维酮(PVPVA)和羟丙甲纤维素(HPMC)制备的聚合物片剂的细分行为。对聚合物片剂进行了不同的后处理(老化、热和暴露于压缩气态二氧化碳),并评估了其机械、光谱和微观结构性能。SOL 片剂在片剂细分方面表现出最佳效果,特别是平均质量变化(3.9%)明显低于另外两种聚合物片剂(PVPVA 和 HPMC 分别为 7.2%和 9.1%),并且优于由粉末基质生产的普通片剂(7-14%)。SOL 片剂对所施加的不同后处理也更敏感,这将质量损失和脆性从 1.5%和 0.8%分别降低至接近零的值,而不会改变其孔隙率。另一方面,PVPVA 片剂的热处理也导致类似的细分结果,质量损失为 0.3%,脆性为 0.02%。相比之下,HPMC 颗粒的压实困难使其片剂不适合细分过程,即使经过额外的后处理也是如此。具有均匀内部结构和适当机械强度的聚合物基质是改善片剂细分适应性的关键。

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