基于粒子设计技术改善中药散剂口感与均一性问题--以珠黄吹喉散为例

Particle design for improving taste and homogeneity of traditional Chinese medicinal powder:taking Zhuhuang Chuihou Powder as an example

由于中药粉体来源复杂,理化性质迴异,因此在制备过程中常存在粒径差异大、混合均一性差与口服顺应性不佳等制剂学共性问题,直接影响固体制剂的质量、临床疗效及安全性。该研究以珠黄吹喉散为研究对象,通过考察粉体学性质提取其制剂学缺陷,复方中雄黄与煅硼砂质重有毒,易离析,存在安全隐患,同时,黄连、黄柏为复方中苦味主要来源。基于"药辅合一"制剂思想,采用粒子设计技术制备以苦味药为核、矿物药为壳的"壳-核"包覆结构的复合粒子;红外光谱和扫描电镜结果均提示复合粒子的形成,复合粒子口感得到改善;相较于物理混合物,复合粒子中盐酸小檗碱、二硫化二砷及四硼酸钠的含量均匀性与其外观均一性的RSD均显著下降。中药粒子设计技术的导入解决了传统散剂——珠黄吹喉散因混乱、无序而导致的分散不均等问题,实现了该制剂均匀分散、稳定可控的目的,从而改善原制剂品质,为中药散剂的质量控制提供了科学依据。

Due to the complex source and different physical and chemical properties of traditional Chinese medicines(TCM)powder,there are many common pharmaceutical problems in its preparation,such as large particle size difference,poor mixing uniformity,and poor compliance with oral intake,which has directly affected the quality of solid preparations as well as their clinical efficacy and safety.This study observed the property of Zhuhuang Chuihou Powder and extract its pharmaceutical defects.It was found that realgar and calcined Borax in Zhuhuang Chuihou Powder were heavy in texture and toxic,and they were easy to be isolated,indicating the potential safety hazard.At the same time,Coptidis Rhizoma and Phellodendri Chinensis Cortex were the main sources of its bitterness.Therefore,based on the idea of"drug-excipients unity",the particle design technology was used to prepare core/shell-type composite particles with bitter medicines as the core and mineral medicines as shell.Both infrared spectroscopy and scanning electron microscopy results indicated the formation of composite particles,and the taste of these composite particles were improved.Compared with the physical mixtures,the composite particles exhibited significantly decreased RSD values in the content uniformity of berberine hydrochloride,arsenic disulfide,and sodium tetraborate and appearance uniformity.The introduction of particle design technology solved the problem of uneven dispersion of Zhuhuang Chuihou Powder,thus ensuring its uniform dispersion,stability,and control and improving the quality of the original preparation.This has provided a scientific basis for the quality control of TCM powder.