目的 系统评估可溶性辅料对不同制备工艺中药浸膏片崩解行为的影响，为中药片剂处方设计提供依据。方法 选取11种代表性中药浸膏粉，比较了直接压片、干法制粒压片和湿法制粒压片3种工艺对片剂崩解时间和溶出度的影响。在此基础上，选择制粒后崩解性能较差的肉桂和拳参浸膏片作为对象，通过析因实验设计考察可溶性辅料种类（即糖醇类、乳糖类和淀粉及其衍生物类）、辅料添加量（即10%、20%和30%）以及制备工艺（即干法制粒压片和湿法制粒压片）对片剂崩解行为的调控作用。结果 除苦参纯浸膏片外，制粒工艺对崩解时间≤30 min的一元中药纯浸膏片（即槲寄生、当归、川芎、乌梅、麸炒苍术、制何首乌和薄荷）的崩解行为影响较小；而对于崩解时间＞30 min的一元中药纯浸膏片（即细辛、肉桂和拳参），制粒会延长其崩解时间并降低溶出度。在高载药量（≥70%）条件下，糖醇类和乳糖类辅料改善肉桂和拳参浸膏片崩解性能的效果最好；淀粉及其衍生物类辅料的促崩效果不明显，但在湿法制粒下能促进水溶性成分的溶出；肉桂浸膏片更适配湿法制粒压片工艺，而拳参浸膏片更适配干法制粒压片工艺。结论 在高载药量中药浸膏片的处方设计中，优选糖醇类或乳糖类辅料，并结合物料特性选择适宜的制粒工艺，是改善其崩解与溶出性能的有效策略。研究结果对中药片剂及相关固体制剂的研发提供了基础数据参考。

Objective To systematically evaluate the effects of soluble excipients on the disintegration behavior of Chinese medicine extract tablets prepared by different processes, thereby providing a scientific basis for the formulation design of Chinese medicine tablets. Methods A total of 11 representative Chinese medicine extract powders were selected, and the impacts of three processes (direct compression, dry granulation compression, and wet granulation compression) on tablet disintegration time and dissolution were compared. On this basis, Rougui (Cinnamomi Cortex) and Quɑnshen (Bistortae Rhizoma) extract tablets with poor disintegration performance were chosen for a factorial experimental design to investigate the modulating effects of soluble excipient type (sugar alcohols, lactose, and starch and its derivatives), proportion (10%, 20%, and 30%), and preparation process (dry granulation compression and wet granulation compression) on tablet disintegration. Results Except for Kushen (Sophorae Flavescentis Radix), the granulation process had minimal impact on the disintegration behavior of single Chinese medicine extract tablets, including Hujisheng (Visci Herba), Dɑnggui (Angelicae Sinensis Radix), Chuɑnxiong (Chuanxiong Rhizoma), Wumei (Mume Fructus), Fuchaocɑngzhu (Atractylodis Rhizoma stir-fried with bran), Zhiheshouwu (Polygoni Multiflori Radix Praeparata), Bohe (Menthae Haplocalycis Herba) with a disintegration time ≤ 30 min. However, for single extract tablets with slower disintegration (> 30 min), such as Xixin (Asari Radix et Rhizoma), Cinnamomi Cortex and Bistortae Rhizoma, granulation prolonged disintegration time and reduced dissolution rate. Under high drug-loading conditions (≥ 70%) sugar alcohols and lactose showed the most significant improvement in disintegration of Cinnamomi Cortex and Bistortae Rhizoma extract tablets, whereas starch and its derivatives exhibited limited effects but enhanced the dissolution of water-soluble components under wet granulation. Wet granulation was more suitable for Cinnamomi Cortex tablets, while dry granulation was preferable for Bistortae Rhizoma tablets. Conclusion In the formulation design of high drug-loading Chinese medicine extract tablets, selecting sugar alcohols or lactose as excipients and optimizing the granulation process based on material properties are effective strategies to enhance disintegration and dissolution. This study provides foundational data for the development of Chinese medicine tablets and related solid dosage forms.

R283.6

国家工信部重大任务专项“中药绿色智能制造技术”（2240STCZB2613）；北京中医药大学基本科研业务费（揭榜挂帅）项目（2023-JYB-JBZD-060）