College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China.
Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China.
Int J Pharm. 2021 Jun 15;603:120703. doi: 10.1016/j.ijpharm.2021.120703. Epub 2021 May 12.
The study aims to markedly improve direct compaction (DC) properties of Zingiberis Rhizoma extracted powder (ZR) by modifying its texture and surface properties with nano-silica (NS). A wet coprocessing method was applied to evenly distribute up to 33.3% NS to ZR. To clarify uniqueness of NS, microcrystalline cellulose (MCC), a superior filler-binder in DC, was used as control. Coprocessed particles and physical mixtures (PMs) were comprehensively evaluated for surface features, micromeritic properties, and texture and compacting parameters. Compared to MCC, NS could more significantly modify the texture and surface features of ZR (e.g., hardness, cohesiveness, yield pressure, and nanoscaled surface roughness) via coprocessing, resulting in more striking improvements on multiple DC properties of ZR, including tabletability, flowability, lubricant sensitivity, hygroscopicity, etc. Especially, tensile strength (σ) of coprocessed ZR-NS (1:0.5) tablets was 4.62 and 3.22 times that of ZR and ZR-MCC counterparts pressed at 210 MPa, respectively. Moreover, percolation thresholds of σ enhancement were observed for ZR-NSs, but not for ZR-MCCs. Evaluation by the SeDeM expert system indicated that some ZR-NSs (but no ZR-MCCs) were qualified for DC. Collectively, coprocessing with NS by liquid dispersion appears to be a novel, effective, and pragmatic option for DC of drugs like ZR.
本研究旨在通过纳米二氧化硅（NS）来改善姜黄提取物粉末（ZR）的直接压缩（DC）性能，从而显著改变其质地和表面特性。采用湿共处理方法将高达 33.3%的 NS 均匀分布到 ZR 中。为了阐明 NS 的独特性，我们将微晶纤维素（MCC）作为对照，这是 DC 中一种优秀的填充剂-粘合剂。对共处理颗粒和物理混合物（PM）进行了全面评估，以评估其表面特征、微粉特性、质地和压缩参数。与 MCC 相比，NS 可以通过共处理更显著地改变 ZR 的质地和表面特性（例如，硬度、内聚性、屈服压力和纳米级表面粗糙度），从而显著改善 ZR 的多种 DC 性能，包括可压性、流动性、润滑剂敏感性、吸湿性等。特别是，共处理的 ZR-NS（1:0.5）片剂的拉伸强度（σ）是 ZR 和 ZR-MCC 压片（210 MPa）的 4.62 和 3.22 倍。此外，对于 ZR-NS 观察到了 σ 增强的渗流阈值，而对于 ZR-MCC 则没有。通过 SeDeM 专家系统评估表明，一些 ZR-NS（但不是 ZR-MCC）符合 DC 的要求。总之，通过液体分散进行 NS 共处理似乎是一种新颖、有效和实用的 DC 药物（如 ZR）的选择。
