摘要
处方前研究是对原料药理化性质和制剂性质的深入分析,是开发出有效、稳定的药物制剂前提和保证,已广泛应用于化学药物制剂领域。然而中药制剂研究仍存在经验性和盲目性,作为最基本的中药制剂原料,中药组分的整体性质研究仍然处于探索阶段。中药组分是一个多成分复杂体系,将成分构成完全阐明清楚难度大,笔者尝试提出以代表性成分表征组分整体性质的研究思路。遵循组分中各成分量与量的关系,构建不同成分组合,以生物活性为导向,通过体内外药效实验,辨识与组分整体药效无统计学差异的N个成分,作为代表性成分;测定平衡溶解度、油水分配系数、渗透性等性质,并通过相似性、离散度分析研究亚组分划分;以质量分散或药效贡献等为权重系数,将各代表性成分的个体性质进行拟合,表征组分/亚组分的整体性质。
Preformulation research, an in-depth research for pharmacological and pharmaceutical properties of raw materials, has been widely used in the field of chemical drugs. Although traditional Chinese medicine components(TCMCs) are the basic units in Chinese medicine preparation, the properties characterization of these components is still in an exploratory stage, because empiricism and blindness are still present in the development of the Chinese medicine preparations. TCMCs, a complex multi-component system, is very difficult to be analyzed in details. Herein, a research idea is put forward for the characterization of overall properties by using representative compositions. Firstly, various composition groups were set up for screening the representative components by in vitro and in vivo efficacy evaluation according to the original proportion. Then the equilibrium solubility, oil/water(O/W) partition coefficient and apparent permeability coefficient of the representative components were detected. Subsequently, the similarity assessment and discrete analysis were performed for the subdivision of TCMCs. The overall properties of TCMCs were fitted by mass fraction or efficacy contribution of each representative component, so as to characterize the overall properties of components/sub-components.
作者
柯仲成
林传燕
贾晓斌
KE Zhong-cheng;LIN Chuan-yan;JIA Xiao-bin(College of Chemistry and Chemical Engineering,Huangshan University,Huangshan 245041,China;College of Pharmacy,A nhui University of Tradhional Chinese Medicine,Hefei 230038,China;College of Pharmacy,Nanjing University of Chinese Medicine,Nanjing 210028,China;College of Traditional Chinese Medicine,China Pharmaceutical University,Nanjing 211198,China)
出处
《中国中药杂志》
CAS
CSCD
北大核心
2018年第23期4592-4598,共7页
China Journal of Chinese Materia Medica
基金
国家自然科学基金项目(81573620)
安徽省高校省级自然科学研究重点项目(KJ2017A394)
黄山学院人才启动项目(2018xkjq017)
黄山学院教学研究项目(2012JXYJ21)
关键词
中药组分
代表性成分
生物药剂学性质
traditional Chinese medicine components
representative component
biopharmaceutical properties
作者简介
柯仲成,副教授,研究方向为中药组分制荆,E-mail:xiaoke1020@126.com;通信作者:贾晓斌,教授,博士生导师,E-mail:jiaxiaobin2015@163.com.
