基于ACQ荧光探针研究纳米尺度的黄芩苷-小檗碱复合物微粒“整体转运均衡释放”的口服吸收特性

实现中药多组分/成分的高效口服递送，提高生物利用度发挥疗效，是现代中药制剂研究中的关键问题。药物纳米混悬（纳米晶体）技术是改善中药难溶性成分口服吸收的重要途径，但设计中药难溶性多成分同时递送的纳米混悬体系较为困难，且药物纳米微粒的吸收机制和体内命运研究仍然有待深入。本项目以常用药对黄芩黄连水煎产生的沉淀物——黄芩苷-小檗碱复合物为研究对象，基于“纳米尺度的中药多成分微粒（黄芩苷-小檗碱复合物）能够通过整体跨膜转运，体内均衡释放过程，促进口服吸收”这一假说，采用ACQ荧光探针示踪等新技术研究纳米尺度黄芩苷-小檗碱复合物微粒的口服吸收特性和跨膜转运机制，验证体内同步均衡释药过程，揭示其口服吸收的规律和特点，为深入研究和应用纳米混悬技术提高中药难溶性多成分口服吸收提供重要基础。同时，为进一步丰富中药“复方水煎自沉淀”配伍理论科学内涵，从中药制剂角度阐释中药药对的物质基础和药效作用特点提供新思路。

Effective oral delivery and bioavailability improvement of multi components of traditional Chinese medicine (TCM) have become the key issue in modern pharmaceutics of traditional Chinese medicine. Drug nanosuspensions (nanocrystals) technology is an important way to improve oral absorption of the traditional Chinese medicine insoluble components, but it finds difficult to design TCM of insoluble multi component nanosuspensions achieving simultaneous delivery. Besides the studies on absorption mechanism and in vivo fate of drug nanocrystals remain to be further. According to the precipitation from Scutellariae Radix-Coptidis Rhizoma formula decoction, based on the hypothesis that “nanosized TCM multi component particles (baicalin-berberine complex) could promote the oral absorption via the integral transportation and in vivo synchronous release”, this study is to evaluate oral absorption characteristics, transmembrane mechanism and in vivo release of nanosized baicalin-berberine complex particles employing some novel technologies such as ACQ fluorescent probe tracing. Revealing the rules and characteristics of oral absorption enhancement of nanosized baicalin-berberine complex particles, provides foundations for further research and application of nanosuspension technology to improve the TCM insoluble multi components as well as some new ideas for the interpretation of couplet TCM and precipitation from Chinese materia medica formula decoction.