College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, People's Republic of China.
Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang, Jiangxi, 330004, People's Republic of China.
AAPS PharmSciTech. 2020 Jul 16;21(5):201. doi: 10.1208/s12249-020-01739-4.
Core-shell composite particles (CPs) are the most preferred choice for direct compaction (DC), but their application in herbal tablets is limited. Hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (PVP) are usually employed as the shell materials, but there are few, if any, researches exploring the different effects of HPMC and PVP on the properties of herbal CPs. In this study, the CPs containing HPMC (CP X-H) and CPs containing PVP (CP X-P) were prepared based on herbal powders (X). Their physical properties were characterized comprehensively. The differences in properties between CP X-H and CP X-P were explored, and their mechanism analysis was also performed profoundly. The results demonstrated that (i) CP X-H and CP X-P exhibited similar flowability; (ii) CP X-H generally exhibited better compactibility, larger particle size, and more uniform particle size distribution, and lower bulk density, tap density, and hygroscopicity than CP X-P; (iii) compared with the tablets produced with CP X-P, ones with CP X-H exhibited similar weight variation (%), lower friability, and longer disintegration time. The mechanism analysis manifested that the differences in physical properties between HPMC and PVP were the important and fundamental factors, which led to the differences in structure and surface morphology of particles, and in fundamental properties of CPs. These findings are beneficial to the development of herbal core-shell CPs for DC.
核壳复合粒子(CPs)是直接压片(DC)最优选的选择,但它们在草药片剂中的应用受到限制。羟丙基甲基纤维素(HPMC)和聚乙烯吡咯烷酮(PVP)通常用作壳材料,但很少有研究探索 HPMC 和 PVP 对草药 CPs 性质的不同影响。在本研究中,基于草药粉末(X)制备了含有 HPMC 的 CPs(CP X-H)和含有 PVP 的 CPs(CP X-P)。全面表征了它们的物理性质。探索了 CP X-H 和 CP X-P 之间性质的差异,并进行了深入的机制分析。结果表明:(i)CP X-H 和 CP X-P 表现出相似的流动性;(ii)CP X-H 通常表现出更好的可压缩性、更大的粒径和更均匀的粒径分布,以及更低的堆密度、振实密度和吸湿性,而 CP X-P 则相反;(iii)与 CP X-P 制备的片剂相比,CP X-H 制备的片剂具有相似的重量变化(%)、更低的脆碎度和更长的崩解时间。机制分析表明,HPMC 和 PVP 之间的物理性质差异是导致颗粒结构和表面形态以及 CPs 基本性质差异的重要和基础因素。这些发现有助于开发用于 DC 的草药核壳 CPs。