桑枝总生物碱研发历程回顾(一):药学研究技术壁垒与规模化发展的挑战  

Review of the research and development of Ramulus Mori(Sangzhi) alkaloids(Ⅰ) : technical barriers and large-scale development challenges in pharmaceutical research

作　　者：刘玉玲[1] 汪仁芸[1] 夏学军[1] 申竹芳[1] 谢明智[1] 金笃嘉[1] 金毅群 朱向阳 刘志华 蒋玲敏 LIU Yuling;WANG Renyun;XIA Xuejun(Institute of Materia Medica,Chinese Academy of Medical Sciences&Peking Union Medical College,Beijing 100050,China)

机构地区：[1]中国医学科学院北京协和医学院药物研究所,100050 [2]北京五和博澳药业有限公司

出　　处：《中国糖尿病杂志》2020年第7期555-560,共6页Chinese Journal of Diabetes

基　　金：“十二五”国家科技重大专项课题资助项目(2013ZX09101005);“十三五”国家科技重大专项课题资助项目(2018ZX09711001);北京市科技计划“十病十药”研发资助项目(Z111100059011010)。

摘　　要：基于疗效与安全性的临床价值是评价药品的最终标准。只有做到物质基础明确、质量准确可控、产品稳定均一,才能确保临床疗效。药学研究的高技术壁垒和规模化发展的制约,是限制有效组分天然药物发展的关键环节。近期降血糖原创天然药物"桑枝总生物碱片"获批上市,成为10几年来我国首个获批的中药创新药,也是糖尿病治疗领域唯一有效组分天然药物。本文从有效组分的科学筛选、微量水溶性生物碱的提取分离与纯化、物质基础及其结构鉴定、复杂体系的质量控制、规模化放大的技术集成制约等环节,评述药学研究和规模化发展的应对策略及取得的突破,旨在为中医药发展理念"传承精华、守正创新"提供参考。The ultimate criterion for evaluating medicines is the clinical significance based on efficacy and safety.To ensure the clinical effect,stable and uniform products with clear material basis,accurate and controllable quality are necessary.For pharmaceutical research,the high technical barriers and large-scale development constraints are the key cogs that restrict the development of effective components derived from nature medicine.Recently,"Sangzhi alkaloids tablet",an original glucose-lowering natural medicine,has been approved,which is the first innovative traditional Chinese medicine approved in more than a decade,and also the only natural medicine with effective component in the field of diabetes treatment.Here,we discussed the strategies and breakthroughs of pharmaceutical research from the aspects of scientific screening of effective components,extraction,separation,and purification of trace water-soluble alkaloids,structural identification of the material basis,quality control of complex systems,and technical integration constraints of large-scale development etc,and provided an evidence for the"Inherit essence,keep upright innovation"in the development of traditional Chinese medicine.

关 键 词：桑枝总生物碱 糖尿病 2型 有效组分天然药物 药学研究 规模化发展 

分 类 号：R285[医药卫生—中药学]