基于多维检测和低场核磁共振技术探讨中药复方骨痹颗粒浸膏粉体吸湿性特征及其改性机制

目的研究中药复方骨痹颗粒浸膏粉体吸湿性特征及其改性机制,为中药固体制剂制备过程的关键工艺技术改进提供依据。方法以骨痹颗粒浸膏粉体为模型药物,将水提原液、水提醇沉中间体和含有不同表面活性剂的水提醇沉中间体经喷雾干燥得到浸膏粉体,采用粉末流动性测试和电镜扫描等多维检测技术分析表征上述浸膏粉体的微观制剂学性质;采用不同表面活性剂对水提醇沉中间体进行吸湿性改性研究,进而引入低场核磁共振技术分析改性后浸膏粉体吸收水分子的含量、相态、分布及结构信息;探索骨痹颗粒浸膏粉体的吸湿性改性机制。结果浸膏粉体喷雾干燥过程中,加入聚乙二醇1000、泊洛沙姆188和月桂醇硫酸镁等表面活性剂可改善粉体的吸湿性。经低场核磁分析可知,上述表面活性剂通过与亲水基结合或与空气中的自由水结合,使得粉体吸湿性降低。结论加入表面活性剂对于骨痹颗粒浸膏粉体的吸湿性具有较好的改善作用,改性机制与水的结合状态相关。

Hygroscopic characteristics and modification mechanism of Gubi Granules powder by multidimensional detection and low field nuclear magnetic resonance technology

Objective To study the hygroscopic characteristics and its modification mechanism of extract spray powders of traditional Chinese medicine (TCM) compound formula, and provide basis for the key technical improvement of TCM solid preparation.Methods Gubi extract powders were taken as a model drug. The spray-drying technology was applied to Gubi water extract stock solution, water extract alcohol precipitation intermediates, and water extract alcohol precipitation intermediates containing different surfactants to get different extract powders. The microscopic pharmaceutical properties of these aboved Gubi Granules powder were characterized by powder fluidity testing and scanning electronic microscope technology; Different surfactants were adopted to study the hygroscopicity modification of water extract of alcohol precipitation intermediates, and then low field nuclear magnetic resonance technology (LF-NMR) was introduced to analyse the content, phase, distribution, and structure information of the water molecules absorbed by the modified extract powders; The mechanism of hygroscopicity modification of TCM extract powders was explored.Results ln the spray drying process of extract powders, it can improve the powder hygroscopicity by adding with PEG1000, poloxamer 188, magnesium lauryl sulfate, etc. It was analysed by LF-NMR that the above-mentioned surfactant could decrease the moisture absorption of the extract spray powder by combining with hydrophilic groups or free water in the air.Conclusion The addition of surfactants has a good effect on the hygroscopicity of TCM extract powders, and the improvement mechanism is related to the state of water combination.