中药口服固体制剂制造分类系统(Ⅳ):胶囊剂吸湿行为分类  

Manufacturing classification system for oral solid dosage forms of traditional Chinese medicines(Ⅳ):classification of hygroscopicity behaviors of capsules

作　　者：林雨 李焕正 梁子辰 徐芳芳[4,5,6] 张欣 王振中[2,3] 徐冰 肖伟 LIN Yu;LI Huan-zheng;LIANG Zichen;XU Fang-fang;ZHANG Xin;WANG Zhen-zhong;XU Bing;XIAO Wei(Nanjing University of Traditional Chinese Medicine,Nanjing 210023,China;Department of Chinese Medicine Informatics,Beijing University of Traditional Chinese Medicine,Beijing 102488,China;Bejing Key Laboratory of Chinese Medicine Production Process Control and Quality Evaluation,Bejing Municipal Science and Technology Commission,Beijing 102488,China;Jiangsu Kang Yuan Pharmaceutical Company Limited,Lianyungang 222001,China;National Key Laboratory on Technologies for Chinese Medicine Pharmaceutical Process Control and Intelligent Manufacture,Lianyungang 222001,China;National&Local Joint Engineering Research Center of TCM Intelligent Manufacturing Technology,Lianyungang 222001,China)

机构地区：[1]南京中医药大学,江苏南京210023 [2]北京中医药大学中药信息学系,北京102488 [3]北京市科委中药生产过程控制与质量评价北京市重点实验室,北京102488 [4]江苏康缘药业股份有限公司,江苏连云港222001 [5]中药制药过程控制与智能制造技术全国重点实验室,江苏连云港222001 [6]中成药智能制造国家地方联合工程研究中心,江苏连云港222001

出　　处：《中国中药杂志》2023年第15期3997-4006,共10页China Journal of Chinese Materia Medica

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

摘　　要：中药硬胶囊剂存在不同程度的吸湿性,影响药品稳定性和疗效。该文以市售30种中药胶囊剂为研究对象,分别测试了胶囊剂内容物、囊壳及胶囊剂整体的吸湿曲线,并采用一级动力学方程进行拟合,结果在24 h的吸湿过程中,囊壳可降低内容物0.80%~53.0%的吸湿增重,并降低胶囊剂内容物1.74%~91.3%的吸湿速率,表明囊壳对中药胶囊剂内容物的吸湿具有较强的延缓作用。测定了30种中药胶囊剂内容物的7个物性参数,以及整理14个处方工艺相关参数,建立了预测中药胶囊剂内容物(带壳)24 h吸湿率的偏最小二乘模型,发现囊壳的吸湿率与中药胶囊剂内容物(带壳)的吸湿性呈正相关,提示选择低吸湿率的囊壳有助于防潮;此外,制剂前处理工艺路线和成型原料类型影响吸湿性大小,胶囊内容物中的浸膏量占比越大、饮片细粉量占比越小,胶囊内容物的吸湿性越强。以24 h吸湿率15%为吸湿强弱的分类节点,以吸湿速率常数0.58为吸湿快慢的分类节点,建立中药胶囊剂吸湿行为分类系统:吸湿强且快的品种占约6.67%;吸湿强且慢的品种占约33.3%;吸湿弱且快的品种约占26.7%;吸湿弱且慢的品种约占33.3%。该分类系统有助于量化比较不同中药胶囊剂吸湿行为,为中药胶囊剂质量改进、防潮技术和材料研究提供参考。Hard capsules of traditional Chinese medicine(TCM)have different degrees of hygroscopicity,which affects the stability and efficacy of drugs.In this paper,30 kinds of commercially available TCM capsules were used as the research object.The hygroscopicity curves of capsule contents,capsule shells,and capsules were tested respectively,and the first-order kinetic equation was used for fitting.The results show that during the 24 h hygroscopicity process,the capsule shell can reduce the weight gain caused by the hygroscopicity of the contents by 0.80%-53.0%and the hygroscopicity rate of the capsule contents by 1.74%-91.3%,indicating that the capsule shell has a strong delay effect on the hygroscopicity of the contents of the TCM capsules.Seven physical parameters of the contents of 30 kinds of TCM capsules were determined,and 14 prescription process-related parameters were sorted out.A partial least squares model for predicting the hygroscopicity rate of the contents of TCM capsules(with shell)for 24 h was established.It is found that the hygroscopicity rate of the capsule shell is positively correlated with the hygroscopicity of the contents of TCM capsules(with shell),suggesting that the capsule shell with a low hygroscopicity rate is helpful for moisture prevention.In addition,the pre-treatment process route of the preparation and the type of molding raw materials affect the hygroscopicity.A larger proportion of the extract in the capsule content and a smaller proportion of the fine powder of the decoction pieces indicate stronger hygroscopicity of the capsule content.The 24 h hygroscopicity rate of 15%was used as the classification node of hygroscopicity strength,and the hygroscopicity rate constant of 0.58 was used as the classification node of hygroscopicity speed.The classification system of hygroscopicity behaviors of TCM capsules was established:the varieties with strong and fast hygroscopicity accounted for about 6.67%,while those with strong and slow hygroscopicity accounted for about 33.3%;the varieties wi

关 键 词：中药胶囊剂 吸湿行为分类 吸湿曲线 吸湿性影响因素 偏最小二乘法 

分 类 号：R283.6[医药卫生—中药学]