To differentiate traditional Chinese medicines(TCM) derived from congeneric species in TCM compound preparations is usually challenging. The roots of Panax ginseng(PG), Panax quinquefolium(PQ) and Panax notoginseng(PN...To differentiate traditional Chinese medicines(TCM) derived from congeneric species in TCM compound preparations is usually challenging. The roots of Panax ginseng(PG), Panax quinquefolium(PQ) and Panax notoginseng(PN) are used as popular TCM. They contain similar triterpenoid saponins(ginsenosides) as the major bioactive constituents. Thus far, only a few chemical markers have been discovered to differentiate these three species. Herein we present a multiple marker detection approach to effectively differentiate the three Panax species, and to identify them in compound preparations. Firstly, 85 batches of crude drug samples(including 32 PG, 30 PQ, and 23 PN) were analyzed by monitoring 40 major ginsenosides in the extracted ion chromatograms(EICs) using a validated LC–MS fingerprinting method. Secondly, the samples were clustered into different groups by pattern recognition chemometric approaches using PLS-DA and OPLS-DA models, and17 diagnostic chemical markers were discovered. Aside from the previously known Rf and p-F11, ginsenoside Rs1 could be a new marker to differentiate PG from PQ. Finally, the above multiple chemical markers were used to identify the Panax species in 60 batches of TCM compound preparations.展开更多
中药复方新药是中药新药研究和申报的主要类别。以2005—2020年申请临床试验(investigational new drug,IND)未获批准的中药复方新药为研究对象,对其适应症、处方来源、剂型、生产工艺等进行回顾分析;对涉及药理毒理、临床、药学及综合...中药复方新药是中药新药研究和申报的主要类别。以2005—2020年申请临床试验(investigational new drug,IND)未获批准的中药复方新药为研究对象,对其适应症、处方来源、剂型、生产工艺等进行回顾分析;对涉及药理毒理、临床、药学及综合方面的主要缺陷进行分类梳理。结果显示:(1)据不完全统计,2005—2020年申请IND的中药复方新药总数为895个,不批准369个,不批准率为41.23%。(2)不同适应症、处方来源、剂型、生产工艺的中药复方新药,在IND不批准率方面有一定差异。(3)从研究的主要缺陷分析,IND未获批准中药复方新药品种中,75.88%涉及药理毒理专业,34.08%涉及临床专业,22.19%涉及药学专业,32.80%涉及综合方面缺陷。(4)涉及药理毒理缺陷的品种,以药效实验项目及模型、毒理实验质量控制、毒理实验项目选择等方面的问题较多;涉及临床缺陷的,以临床定位、方药与病症不对应等问题较多;涉及药学缺陷的,以提取纯化工艺等方面的问题较多。对IND未获批准新药的回顾分析可为今后中药复方新药研究提供有益借鉴。展开更多
基金supported by National Natural Science Foundation of China(No.81222054)
文摘To differentiate traditional Chinese medicines(TCM) derived from congeneric species in TCM compound preparations is usually challenging. The roots of Panax ginseng(PG), Panax quinquefolium(PQ) and Panax notoginseng(PN) are used as popular TCM. They contain similar triterpenoid saponins(ginsenosides) as the major bioactive constituents. Thus far, only a few chemical markers have been discovered to differentiate these three species. Herein we present a multiple marker detection approach to effectively differentiate the three Panax species, and to identify them in compound preparations. Firstly, 85 batches of crude drug samples(including 32 PG, 30 PQ, and 23 PN) were analyzed by monitoring 40 major ginsenosides in the extracted ion chromatograms(EICs) using a validated LC–MS fingerprinting method. Secondly, the samples were clustered into different groups by pattern recognition chemometric approaches using PLS-DA and OPLS-DA models, and17 diagnostic chemical markers were discovered. Aside from the previously known Rf and p-F11, ginsenoside Rs1 could be a new marker to differentiate PG from PQ. Finally, the above multiple chemical markers were used to identify the Panax species in 60 batches of TCM compound preparations.
文摘中药复方新药是中药新药研究和申报的主要类别。以2005—2020年申请临床试验(investigational new drug,IND)未获批准的中药复方新药为研究对象,对其适应症、处方来源、剂型、生产工艺等进行回顾分析;对涉及药理毒理、临床、药学及综合方面的主要缺陷进行分类梳理。结果显示:(1)据不完全统计,2005—2020年申请IND的中药复方新药总数为895个,不批准369个,不批准率为41.23%。(2)不同适应症、处方来源、剂型、生产工艺的中药复方新药,在IND不批准率方面有一定差异。(3)从研究的主要缺陷分析,IND未获批准中药复方新药品种中,75.88%涉及药理毒理专业,34.08%涉及临床专业,22.19%涉及药学专业,32.80%涉及综合方面缺陷。(4)涉及药理毒理缺陷的品种,以药效实验项目及模型、毒理实验质量控制、毒理实验项目选择等方面的问题较多;涉及临床缺陷的,以临床定位、方药与病症不对应等问题较多;涉及药学缺陷的,以提取纯化工艺等方面的问题较多。对IND未获批准新药的回顾分析可为今后中药复方新药研究提供有益借鉴。
