目的 验证吸水性在中药分散片崩解过程中的关键作用,以期为中药分散片崩解迟缓的解决方法提供思路。方法 以油性物料姜黄清脂分散片为研究对象,对不同原料药(姜黄清脂分散片、乳糖片)、不同辅料组成的姜黄清脂分散片以及微粉硅胶改性前后的姜黄清脂分散片的吸水性、崩解过程进行测定,对比分析研究吸水性对片剂崩解过程的影响。结果 不同辅料处方[羧甲基淀粉钠(CMS-Na)、交联聚乙烯比咯烷酮(PVPP)、低取代羟丙基纤维素(L-HPC)、微晶纤维素(MCC)]的姜黄清脂片的吸水性均弱于乳糖片,其崩解过程也较慢;调整辅料比例后不同辅料处方姜黄清脂片的吸水性能排序为CMS-Na-PVPP(1:1) >PVPP >CMS-Na,崩解过程排序也相同;微粉硅胶对姜黄提取物进行改性后以上3种辅料处方的吸水能力均增强,崩解时间明显缩短。结论 研究证明了吸水性是影响中药分散片崩解的关键因素,采用微粉硅胶与原料药共研磨,是解决中药分散片崩解迟缓问题的重要工艺技巧。

Objective The purpose of this paper is to verify the key role of water absorption in the process of disintegration of Chinese materia medica(CMM) dispersible tablets, so as to provide the solution idea for slow disintegration of CMM dispersible tablets. Methods In this paper, the influence of water absorption of raw materials and auxiliary materials on disintegration process was verified using oily Jianghuang Qingzhi Tablets(JQT) as research object. The water absorption and disintegrating process of different drugs, JQT with different materials, and modified dispersible tablet were determined. Results The water absorption of JQT was lower than that of lactose tablets, and the disintegrating process was slower. The water absorption of different materials prescription of JQT was:CMS-Na-PVPP(1:1) >PVPP >CMS-Na, and disintegrating process is the same as the former order. The water absorption of JQT after modification enhanced, and disintegration time was significantly shortened. It indicated that the water absorption of raw materials and excipients was stronger, the disintegration was faster. Conclusion The study proves that water absorption is a key role in the disintegration of CMM dispersible tablets. And co-grinding of silica powder and raw materials is important technology to solve the problem of slow disintegration of CMM dispersible tablets.

国家自然科学基金资助项目(81274098,30973952);国家基础科学人才培养基金(J13100340-19)