银杏叶片体外溶出度与空间分布均匀度评价及关联辨识研究  

Research on evaluation and correlation identification of in vitro dissolution and spatial distribution uniformity of Ginkgo Folium Tablets

作　　者：王静 吴志生[1,2] 李明爽 赵小军 王恺怡 何晗 林玲 王逸飞 WANG Jing;WU Zhisheng;LI Mingshuang;ZHAO Xiaojun;WANG Kaiyi;HE Han;LIN Ling;WANG Yifei(School of Chinese Materia Medica,Beijing University of Chinese Medicine,Beijing 102488,China;Engineering Research Center of Chinese Medicine Production and New Drug Development,Ministry of Education,Beijing 102488,China;Fangshan Hospital,Beijing University of Chinese Medicine,Beijing102499,China)

机构地区：[1]北京中医药大学中药学院,北京102488 [2]中药制药与新药开发教育部工程研究中心,北京102488 [3]北京中医药大学房山医院,北京102499

出　　处：《中草药》2024年第18期6144-6153,共10页Chinese Traditional and Herbal Drugs

基　　金：国家重点研发计划项目(2022YFC3501902);江西省重大科技研发专项(20203ABC28W018);国家自然科学基金项目(82274110);国家医学攻关产教融合创新平台——中药智能制造工程平台项目(90010062820031);中央高校基本科研业务费北京中医药大学揭榜挂帅项目(2022-JYB-JBZR-019);中央高校基本科研业务费北京中医药大学揭榜挂帅项目(2022-JYB-JBZR-018)。

摘　　要：目的建立银杏叶片体外溶出度与空间分布均匀度评价方法,探究体外溶出行为对空间分布均匀度的影响,实现银杏叶片质量控制。方法首先,采用《中国药典》2020年版方法完成银杏叶片溶出度测定,并基于模型依赖法对银杏叶片体外溶出特性进行评价;其次,通过对称参数图像分析法(symetry parameterimage analysis,SPIA)和均匀度百分比指数法(percentage of homogeneity,H%)对银杏叶片空间分布均匀度进行评价;最后,建立偏最小二乘(partial least square,PLS)和标准正则变换(standardized normal variate,SVR)模型对银杏叶片体外溶出度与活性药物成分(active pharmaceutical ingredient,API)空间分布均匀度进行关联辨识研究。结果银杏叶片在45 min内完全溶出且累积溶出率大于70%,且不同批次溶出行为存在差异;银杏叶片API空间分布均匀度范围为64.09%~76.54%,其中5个批次银杏叶片质量差异较大;银杏叶片体外溶出度与API空间分布均匀度PLS和SVR模型R^(2)值分别为0.1110和0.2540,两者没有相关性。结论所建方法可客观评价中药固体制剂的溶出度与空间分布均匀度,实现银杏叶片与空间分布均匀度的关联辨识研究,为银杏叶片制造过程质量控制及提升提供了方向。Objective To establish an evaluation method for the in vitro dissolution and spatial distribution uniformity of Ginkgo Folium Tablets(银杏叶片,GFT),explore the influence of in vitro dissolution behavior on spatial distribution uniformity,and achieve quality control of GFT.Methods Firstly,the dissolution rate of GFT was determined using the method specified in the 2020 edition of the Chinese Pharmacopoeia,and the in vitro dissolution characteristics of GFT were evaluated based on model-dependent methods.Secondly,the spatial distribution uniformity of GFT was evaluated using symmetry parameter image analysis(SPIA)and percentage of homogeneity(H%)methods.Finally,partial least square(PLS)and standardized normal variate(SVR)models were established to carry out correlation identification between the in vitro dissolution rate of GFT and the spatial distribution uniformity of active pharmaceutical ingredient(API).Results GFT completely dissolved within 45 min with a cumulative dissolution rate greater than 70%,and there were differences in dissolution behavior among different batches.The API spatial distribution uniformity in GFT ranged from 64.09%to 76.54%,and five batches showed significant differences in quality.The R^(2) values of PLS and SVR models for the in vitro dissolution rate and spatial distribution uniformity of API in GFT were 0.1110 and 0.2540,indicating a lack of correlation between the two parameters.Conclusion The established method can objectively evaluate the dissolution rate and spatial distribution uniformity of traditional Chinese medicine solid preparations and realize the correlation identification of GFT and spatial distribution uniformity,providing direction for quality control and improvement of GFT manufacturing process.

关 键 词：银杏叶片 体外溶出度 模型依赖法 空间分布均匀度 质量控制 对称参数图像分析法 均匀度百分比指数法 偏最小二乘 标准正则变换 

分 类 号：R283.6[医药卫生—中药学]