Li Jinzhi, Li Zhe, Ruan Hongsheng, Gao Yating, Hong Yanlong, Shen Lan, Lin Xiao
College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, PR China.
College of Chinese Materia Medica, Zhejiang Pharmaceutical College, Ningbo, PR China.
Pharm Dev Technol. 2022 Jul;27(6):725-739. doi: 10.1080/10837450.2022.2109671. Epub 2022 Aug 19.
Direct compression (DC) attracts increasing attention for tablet manufacturing; however, its application in medicinal plant tablets is still extremely limited. In this work, eight kinds of the water extract powder (GF)-based composite particles (CPs) were prepared with different cohesive surface engineering materials, including dextran, inulin, hypromellose, and povidone, alone or in combination with mannitol and colloidal silica. Their physical properties and compacting parameters were characterized comprehensively. All the CPs showed marked improvement in tabletability, which is about 2-4 times higher than that of GF and physical mixtures (PMs). Specifically, the CPs showed a 7.45-26.48 times higher hardness (Ha) value and a 1.26-2.74 times higher cohesiveness (Co) value than PMs. In addition, all the CPs (angle of repose being from 34.27° to 38.46°) showed better flowability than PMs (35.49° to 53.53°) and GF (51.86°). These results demonstrated that (i) fluid-bed coating was not a simple process of superposition and transmission of the physical properties of raw materials; and (ii) all the surface engineering materials studied could improve the DC properties of problematic GF to some degree. As a whole, through the design of fluid-bed coating CPs, qualified tablets with high GF loadings (up to 93%) were produced DC.
直接压片法(DC)在片剂制造中受到越来越多的关注;然而,其在药用植物片剂中的应用仍然极为有限。在本研究中,使用不同的粘性表面工程材料,包括单独或与甘露醇和胶体二氧化硅组合使用的葡聚糖、菊粉、羟丙甲纤维素和聚维酮,制备了八种基于水提取物粉末(GF)的复合颗粒(CPs)。对它们的物理性质和压片参数进行了全面表征。所有CPs的可压性均有显著提高,比GF和物理混合物(PMs)高出约2至4倍。具体而言,CPs的硬度(Ha)值比PMs高7.45至26.48倍,内聚性(Co)值比PMs高1.26至2.74倍。此外,所有CPs(休止角为34.27°至38.46°)的流动性均优于PMs(35.49°至53.53°)和GF(51.86°)。这些结果表明:(i)流化床包衣不是原材料物理性质简单叠加和传递的过程;(ii)所有研究的表面工程材料都能在一定程度上改善有问题的GF的直接压片性能。总体而言,通过流化床包衣CPs的设计,采用直接压片法制备出了高GF负载量(高达93%)的合格片剂。