中文摘要
前期研究工作发现,共晶(CC)技术可成为药用新辅料(NPE)设计与构建的另一重要创新技术,由此提出CC新辅料(CC-NPE)设计理念。该理念的基本思想为:基于材料学、晶体学等理论筛选共晶配体(CCF),通过非共价键与现有辅料(PE)形成CC复合物,以改善PE功能性,或产生新的功能特色,从而更好地适于制剂需要。但目前该理念基础研究薄弱,科学内涵及设计与构建方法不明确,限制了其深入发展。据此,本项目通过:(1)研究原PE、CCF及CC三者的结构、功能性之间的内在规律,初步建立CC-NPE理论体系;(2)以蔗糖为模型建立系统、完善的CC-NPE设计与构建方法,夯实研究基础,并促进新技术的后续延伸与推广。本项目以CC技术优势契合NPE研发之所需,既是对CC技术向NPE领域应用范围的进一步拓展,又是对NPE创新技术的大胆探索与尝试,对推动我国NPE的创新发展和药物制剂水平的提高具有重要意义。
英文摘要
On the basis of our research, we realized that the cocrystallization technology has a potential to be an innovative strategy in developing novel pharmaceutical excipients (NPE), and so we are here to propose a design concept of cocrystal-NPE (CC-NPE). The basic idea of this concept is to screen suitable CC formers (CCF) based on the theories of material science and crystallography, and then to construct CC complexes by non-covalently connecting them with current pharmaceutical excipients (PE), in order to modify/generate novel functions of PE, which will contribute in the development of pharmaceutics. However, the unsolid basic research, confused scientific significance and unclear construction methods of CC-NPE limited its further and in-depth development. Therefore, the current project was designed (1) to initially establish the theoretical system of CC-NPE by investigating the internal relationship and principles of structures and functionalities among PE, CCF and generated CC, and (2) to develop a systemic and comprehensive design-construction method, solidify the research foundation of CC-NPE, as well as promote the extension and expansion of such innovative technology. By combining advantages of CC technology and development requisites of NPE, the present project is not only a further prolongation of CC technology into NPE field, but also a bold exploration of novel technology in NPE development. It is of great significance to facilitate the innovation and development of NPE and also improve the level of pharmaceutical preparations in our country.
