Yang Ri-Zhao, Zhao Li-Jie, Huang Yan-Sheng, Feng Yi, Wang You-Jie, Chang Xin-Nan
Engineering Research Center of Modern Preparations of Traditional Chinese Medicine under Ministry of Education,Shanghai University of Traditional Chinese Medicine Shanghai 201203,China.
Infinitus (China) Company Limited Shenzhen 518000,China.
Zhongguo Zhong Yao Za Zhi. 2021 Jul;46(13):3356-3363. doi: 10.19540/j.cnki.cjcmm.20210205.307.
With Sangtang Yin granule as model drug,and based on the strategy of " unification of medicines and excipients",the feasibility of preparing high drug loading granules with traditional Chinese medicine( TCM) raw powder as carrier was explored. The powder yield,particle size and particle size distribution,fillibility,flowability,hygroscopicity,reconstituability and other key physical properties relating to preparations of 8 herbs( Dioscoreae Rhizoma,Euryales Semen,Atractylodis Macrocephalae Rhizoma,Coicis semen,Poria,Puerariae Lobatae Radix,Puerariae Thomsonii Radix and Coicis Semen by stir-frying with bran) were studied after being smashed,and the feasibility of taking them as excipients of TCM granules was evaluated by co-spray drying,dry granulation and other preparation techniques. According to the results of the physical properties of raw powders,raw powders of Dioscoreae Rhizoma,Euryales Semen and Puerariae Thomsonii Radix had a high powder yield,uniform particle size distribution,good fillibility,poor hygroscopicity and good reconstitutability,with the feature of assisting granule forming. Compared with the prescription of spray dry powder Sangtang Yin without any excipient,the co-sprayed powder had a high yield,good fillibility and compressibility. The yield of dry granules prepared by co-spraying dry powder was increased by more than 10%,and the particles had a uniform color,good fluidity and dissolubility with the drug-loading rate up to 100%. Based on the physical characteristics of TCM raw powder combined with the analysis of the preparation process,Dioscoreae Rhizoma and Puerariae Thomsonii Radix raw powder were selected as the carriers of granule preparations,and Sangtang Yin granule without any excipient was successfully prepared. The findings provide a feasible idea for the preparation of TCM granules with a high drug loading capacity.
以桑糖饮颗粒为模型药物，基于“药辅合一”策略，探讨以中药生粉为载体制备高载药量颗粒剂的可行性。对山药、芡实、白术、薏苡仁、茯苓、葛根、粉葛、麸炒薏苡仁8味粉碎后的药材进行制粉得率、粒度及粒度分布、填充性、流动性、吸湿性、可压性等与制剂相关的关键物理性质研究，并通过共喷雾干燥、干法制粒等制剂工艺对其作为中药颗粒剂辅料的可行性进行评价。根据生粉物理性质结果，山药、芡实、粉葛生粉制粉得率高，粒度分布均匀，填充性好，吸湿性差，可压性好，具有助流成粒特性。与无辅料喷雾干燥粉桑糖饮处方相比，共喷粉得率高，填充性和可压性好。共喷干粉制备干颗粒得率提高10%以上，颗粒色泽均匀，流动性好，溶散性好，载药率可达100%。基于中药生粉物理特性结合制剂过程分析，筛选山药、粉葛生粉作为颗粒剂制剂载体，成功制备了无辅料桑糖饮颗粒。研究结果为制备高载药量中药颗粒剂提供了可行思路。
