基于表面修饰的中药粉体亲水性调控工艺设计与系统评价：以青黛为例

Powder modification technology can be targeted to change the physical or chemical properties of the powder to improve its application performance.significant changes have taken place in the ancient and modern TCM clinical usage of Indigo naturalis, Indigo naturalis decoction has become a mainstream. However, the actual intake and clinical efficacy of Indigo naturalis was seriously influenced because of the strong hydrophobicity.The research group intends to use modification technology to modify and change the wetting modification of indigo surface, improve the hydrophilicity, and prepare the new type of indigo powder for proper decoction.. Based on preliminary studies, the evaluation system of contact angel-wetting heat-surface free energy and its components surface elements -functional groups is adopted, three modification technologies of adsorption grafting, film forming and particles covering in Indigo naturalis are investigated, from three categories of macro phenomenon and micro mechanism, physical changes and chemical nature, thermodynamic and kinetic foundation, modification influence on wetting process and its principle are assessed systematically, the multidimensional evaluation system about surface properties is established;he procedure chain pertaining to “modifiers-modifying equipment-technological parameters” is used to optimize the modification process and summary the modified rules;And the task force also conducted a systematic evaluation of performance - effect - the use , to ensure that the modified indigo safe, effective, stable, compliant.This study has important clinical value and practical significance for promoting the development and upgrading of indigo slices and improving the traditional Chinese medicine processing skills.

粉体改性技术可针对性改变粉体的物理或化学性质，改善其应用性能。青黛在古今中医临床用法发生了重大变化，入汤剂成为主流，但青黛的强疏水性严重影响了汤剂中药物的分散性，制约了临床疗效。课题组拟采用改性技术，以青黛表面润湿性修饰转变为突破，提高亲水性，制备适宜汤剂给药的新型青黛粉体。.在前期青黛化学成分、产地加工原理及改性技术研究基础上，拟采用接触角-润湿热-表面自由能及其分量-表面元素与官能团的评价体系，对青黛进行吸附接枝、成膜及粒子包覆三条改性工艺研究，从宏观现象与微观机制、物理变化与化学本质、热力学与动力学基础三个方面系统评价改性对润湿过程的影响及其机理，建立表面性质的多维评价体系；从“改性剂-改性设备-工艺参数”过程链优化改性工艺、总结改性规律；并进行性-效-用系统评价，确保改性青黛安全、有效、稳定、顺应。本研究对于促进青黛饮片的发展升级，提升中药粉体加工技艺，具有重要临床价值与实践意义。

青黛是中医常用清热解毒药，疗效确切，使用广泛。但其古今临床用法发生了重大变化，青黛古代多做丸、散剂，而今入汤剂成为主流。但青黛的强疏水性严重影响了汤剂中药物的均匀分散，制约了临床疗效的发挥。课题借助现代粉体改性技术，以青黛表面特殊结构为切入点，以改善青黛润湿性与分散性为目标，进行了青黛表面润湿性的工艺调控、改性机制及评价方法的系统研究。.采用成分“敲出法”对青黛无机物与有机物进行梯度分离，对接触角、表面自由能及其分量、粒径、扫描电镜及表面元素、红外光谱等表面性质及结构性质进行表征，发现对青黛进行改性的关键对象在于青黛中的有机物部分，分析并确认了青黛亲水性与有机物含量相关联；探索了不同结构醇类改性剂与青黛共研磨吸附接枝改性的方法，醇类改性剂的羟基数目及空间构象与改性的关系；研究了PEG系列改性剂对青黛成膜改性、亲水性辅料乳糖对青黛包覆改性的工艺条件、过程、影响因素及其调控规律，考察了粒径、比表面积、堆密度等粉体学性质，接触角、有效成分溶出速率等亲水性质，SEM、表面元素及红外等微观性质，系统对比了改性前后青黛的表面性质和结构差异，并对其在高温、高湿、强光照射下的稳定性进行了研究；引入多重光散射技术，客观、准确评价青黛在水中分散状态，创建了接触角-表面自由能及其分量-表面元素与官能团的三维评价体系，从宏观现象与微观机制、物理变化与化学本质、热力学基础与动力学基础三个方面，系统评价粉体改性对润湿过程的影响及其机理，揭示了改性的基本原理；对改性前后青黛进行了不同模型解热作用研究，代谢组学分析，急性毒性评价，探讨改性青黛发挥解热活性的科学内涵及其安全性，完成了改性青黛粉体的“性-效-用”评价。.课题探明了易于分散、便于汤剂应用的新型亲水性青黛的成型机制及调控因素，拓展了青黛饮片的适应性；创建了疏水性中药饮片的粉体改性技术与评价方法，有利于提升中药粉体加工技艺，促进中药制剂技术的传承与创新。