Zhao Xiao-Qing, Liao Dong-Ling, Qi Fei-Yu, Liang Zi-Chen, Tang Xue-Fang, Dai Sheng-Yun, Qiao Yan-Jiang, Xu Bing
Department of Chinese Medicine Informatics, Beijing University of Chinese Medicine Beijing 102400, China.
National Institutes for Food and Drug Control Beijing 102629, China.
Zhongguo Zhong Yao Za Zhi. 2023 Jun;48(12):3180-3189. doi: 10.19540/j.cnki.cjcmm.20230313.301.
In this paper, 50 batches of representative traditional Chinese medicine tablets were selected and the disintegration time was examined with the method in Chinese Pharmacopoeia. The disintegration time and disintegration phenomenon were recorded, and the dissolution behaviors of water-soluble and ultraviolet-absorbent components during the disintegration process of tablets were characterized by self-control method. The results revealed that coating type and raw material type influenced the disintegration time of tablets. It was found that only 4% of traditional Chinese medicine tablets had obvious fragmentation during the disintegration process, while 96% of traditional Chinese medicine tablets showed gradual dissolution or dispersion. Furthermore, according to the disintegration speed, disintegration phenomenon, and whether the cumulative dissolution of measured components was > 90% at complete disintegration, a disintegration behavior classification system(DBCS) was created for the regular-release traditional Chinese medicine tablets. As a result, the disintegration behaviors of 50 batches of traditional Chinese medicine tablets were classified into four categories, i.e. ⅠA_2, ⅠB_1, ⅡB_1, and ⅡB_2. traditional Chinese medicine tablets(Class I) with disintegration time ≤ 30 min were defined to be rapid in disintegration, which can be the objective of optimization or improvement of Chinese herbal extract(semi extract) tablets. Different drug release models were used to fit the dissolution curve of traditional Chinese medicine tablets with gradual dissolution or dispersion phenomenon(i.e. Type B tablets). The results showed that the dissolution curves of water-soluble components in the disintegration process conformed to the zero order kinetics and the Ritger-Peppas model. It could be inferred that the disintegration mechanisms of type B tablets were a combination of dissolution controlled and swelling controlled mechanisms. This study contributes to understanding the disintegration behavior of traditional Chinese medicine tablets, and provides a reference for the design and improvement of disintegration performance of traditional Chinese medicine tablets.
本文选取50批有代表性的中药片剂，按照《中国药典》方法考察其崩解时限，记录崩解时间及崩解现象，并采用自制方法表征片剂崩解过程中水溶性成分及紫外吸收成分的溶出行为。结果表明，包衣类型和原料类型对片剂崩解时间有影响。发现仅有4%的中药片剂在崩解过程中出现明显破碎，而96%的中药片剂表现为逐渐溶解或分散。此外，根据崩解速度、崩解现象以及崩解完全时测定成分的累积溶出量是否>90%，建立了普通释放型中药片剂的崩解行为分类系统（DBCS）。结果，50批中药片剂的崩解行为分为四类，即ⅠA_2、ⅠB_1、ⅡB_1和ⅡB_2。崩解时间≤30分钟的中药片剂（Ⅰ类）定义为崩解迅速，可作为优化或改进中药提取物（半浸膏）片的目标。采用不同的药物释放模型拟合具有逐渐溶解或分散现象的中药片剂（即B型片）的溶出曲线。结果表明，崩解过程中水溶性成分的溶出曲线符合零级动力学和Ritger-Peppas模型。由此推断，B型片的崩解机制为溶出控制和溶胀控制机制的组合。本研究有助于了解中药片剂的崩解行为，为中药片剂崩解性能的设计和改进提供参考。
