中药口服固体制剂制造分类系统(Ⅱ):片剂崩解行为分类  

Manufacturing classification system for oral solid dosage forms of traditional Chinese medicines(Ⅱ):classification of tablets disintegration behavior

作　　者：赵晓庆 廖冬灵 齐飞宇 梁子辰 唐雪芳 戴胜云 乔延江[1,3,4] 徐冰 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,Bejing University of Chinese Medicine,Beijing 102400,China;National Institutes for Food and Drug Control,Beijing 102629,China;Beijing Key Laboratory of Chinese Medicine Manufacturing Process Control and Quality Evaluation,Bejing Municipal Science&Technology Commission,Bejing 102400,China;Engineering Research Center of Chinese Medicine Production and New Drug Development,Ministry of Education,Beijing 102400,China)

机构地区：[1]北京中医药大学中药信息学系,北京102400 [2]中国食品药品检定研究院,北京102629 [3]北京市科学技术委员会中药生产过程控制与质量评价北京市重点实验室,北京102400 [4]中药制药与新药开发教育部工程研究中心,北京102400

出　　处：《中国中药杂志》2023年第12期3180-3189,共10页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(82074033);连云港市重大技术攻关“揭榜挂帅”项目(CGJBGS2101)。

摘　　要：该文以50批代表性中药片剂为研究对象,按照《中国药典》方法进行崩解时限检查,记录崩解时间和崩解现象,同时采用自身对照法对片剂崩解过程中水溶性且具有紫外吸收成分的溶出行为进行了表征。研究表明包衣类型和原料类型对片剂崩解时间存在影响。研究发现仅4%的中药片剂崩解过程发生了明显碎裂现象,而96%的中药片剂崩解过程以片心溶化或溶散为主。以片剂崩解快慢、崩解现象、完全崩解时测量成分的累积溶出度是否大于90%为判断依据,构建中药常释片剂崩解行为分类系统,50批中药片剂的崩解行为可分成ⅠA_(2)、ⅠB_(1)、ⅡB_(1)和ⅡB_(2)4类。将崩解时间小于或等于30 min的中药片剂(Ⅰ类)定义为具有快速崩解性能的中药片剂,可作为中药浸膏(半浸膏)片剂优化设计或改进的目标。采用药物释放模型拟合溶化或溶散崩解现象为主的中药片剂崩解过程的溶出曲线,结果崩解过程中水溶性成分的溶出符合零级动力学和Ritger-Peppas模型,推测该类中药片剂崩解机制主要为溶解和溶胀混合机制。该文研究结果有助于中药片剂崩解行为的理解,并为中药片剂崩解性能的设计和改进提供参考。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.Ⅰ A_(2),ⅠB_(1),Ⅱ B_(1),andⅡB_(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 tablet

关 键 词：中药片剂 崩解时间 崩解行为分类系统(DBCS) 溶出曲线 崩解机制 

分 类 号：R283.6[医药卫生—中药学]