中药有效部位和有效成分的组分配比、协同效应及药物新剂型研究进展

Research progress in composition ratios,synergistic effects and new drug formulations of active parts and active ingredients in traditional Chinese medicine

摘要

有效部位与有效成分是中药发挥治疗作用的物质基础,其合理配伍所形成的组合物能够达到增强药效、降低毒性、减少剂量、拓展新疗效、开发新剂型等目的,相关研究已成为中药配伍研究、药效物质基础阐释、精准药效成分筛选及新药研发的重要手段。中药配伍形式包括有效部位之间配伍、有效成分之间配伍及有效部位与有效成分配伍,最佳配伍方式的筛选主要采用正交设计法、均匀设计法、基线等比增减设计法等传统实验设计结合动物模型、细胞模型、酶活性抑制实验等。基于有效成分配比组分开发的中药新剂型主要有纳米颗粒、纳米胶束、共无定形系统、共晶体等。但目前研究也存在筛选方法传统、协同作用机制揭示不够深入、指导开发新剂型及新药不足等问题。未来,应结合人工智能技术筛选中药配比组分,结合多组学技术研究配比组分的协同效应及分子调节网络,积极拓展基于配比组分的新剂型研究,为高效、深入、全面揭示中药物质基础及新药研发提供参考。

Abstract

Active parts and active ingredients are the material basis for therapeutic effects of traditional Chinese medicines (TCMs), and the combinations formed by rational compatibility can achieve the purposes of enhancing efficacy, reducing toxicity, reducing dosage, expanding new therapeutic effects, and developing drug formulations, etc.The relevant research has become an important means for compatibility research, explanation of material basis of pharmacodynamics, screening of precise active ingredients, and research and development of new drugs of TCMs.The compatibility forms include combination of active parts, combination of active ingredients, and combination of active parts and active ingredients.The screening methods for the best combination mainly adopt traditional experimental design methods such as orthogonal design, uniform design, and baseline geometric design, combined with animal models, cell models, and enzyme activity inhibition tests.The new drug formulations of TCMs developed based on combinations formed by active ingredients mainly include nano-particles, nano-micelles, co-amorphous systems, and co-crystals.However, there are still problems in current research, such as lack of innovation in the screening methods, insufficient explanation of synergistic mechanisms, and insufficient guidance for the development of new drug formulations and new drugs.In the future, artificial intelligence (AI) should be used to screen the composition ratio of TCMs, multi-omics technologies should be used to investigate the synergistic effects and molecular regulatory networks of composition formed by compatibility, and the research of new drug formulations based on composition formed by compatibility should be actively expanded, so as to provide references for efficient, in-depth, and comprehensive revelation of the material basis and the research and development of new drugs of TCMs.

关键词

中药 / 有效部位 / 有效成分 / 组分配比 / 协同效应 / 中药新剂型 / 研究进展

Key words

traditional Chinese medicine / active parts / active ingredients / composition ratios / synergistic effects / new drug formulations / research progress

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基金资助

国家自然科学基金地区基金资助项目(82460867);甘肃省中医药管理局高水平重点课题资助项目(GZKZ-2024-16);甘肃省药品监督管理局药品监管科学研究项目(2023GSMPA046);甘肃省人民医院中西医结合优势病种科技专项(23GSSYE-7)