Improved blend and tablet properties of fine pharmaceutical powders via dry particle coating
Improved blend and tablet properties of fine pharmaceutical powders via dry particle coating
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DOI：
10.1016/j.ijpharm.2014.11.068
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发表时间：
2015-01-30
影响因子：
5.8
通讯作者：
Dave, Rajesh N.
中科院分区：
文献类型：
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作者：
Huang, Zhonghui;Scicolone, James V.;Dave, Rajesh N.
对流动性差的模型药物微粉对乙酰氨基酚（mAPAP，约为11 μ m）的干燥包衣对精细药物粉末混合物的流动和包装的改善进行了量化。精细辅料的流动性和包装密度差（类似于20 μ m）允许测试粘性原料药的干燥涂层可以抵消精细药物粉末混合物的流动性和包装差的假设。此外，精细赋形剂可以改善压实，减少偏析倾向。结果表明，在原料药负荷为10%、30%和60% （w/w）时，掺有干包覆原料药的共混物的流动函数系数（FFC）和堆积密度（bulk density）均显著高于未包覆二氧化硅的共混物。在最高的原料药负荷下（也使用较粗的辅料作为参考），无论辅料粒度如何，干包膜mAPAP共混物的流量和包装都显著增加，超过了致密性良好的辅料Avicel 102。此外，添加细辅料的片剂抗拉强度显著提高，表明其致密性得到改善。这些结果首次表明，干燥包衣精细、粘性的原料药粉末可以显著改善由精细赋形剂组成的高原料药负荷混合物的流动性和包装，同时改善片剂的压实性，表明直接压实的适用性。(C) 2014 Elsevier B.V.版权所有
The improvements in the flow and packing of fine pharmaceutical powder blends due to dry coating of micronized acetaminophen (mAPAP, similar to 11 mu m), a model poorly flowing drug, are quantified. Poor flow and packing density of fine excipients (similar to 20 mu m) allowed testing the hypothesis that dry coating of cohesive API may counteract poor flow and packing of fine pharmaceutical powder blends. Further, fine excipients could improve compaction and reduce segregation tendency. It was found that flow function coefficient (FFC) and bulk density enhancements for 10%, 30%, and 60% (w/w), API loading blends with dry coated API are significantly higher than those without coated silica. At the highest API loading, for which coarser excipients were also used as reference, the flow and packing of dry coated mAPAP blends were significantly increased regardless of the excipient particle size, exceeding those of a well compacting excipient, Avicel 102. In addition, tensile strength of tablets with fine excipients was significantly higher, indicating improved compactibility. These results show for the first time that dry coating of fine, cohesive API powder leads to significantly improved flow and packing of high API loading blends consisting of fine excipients, while achieving improved tablet compactibility, suggesting suitability for direct compaction. (C) 2014 Elsevier B.V. All rights reserved.