扫描电子显微镜-能谱仪在吸入式干粉制剂表征中的应用进展

Application Progress of Scanning Electron Microscopy and Energy Dispersive Spectroscopy in the Characterization of Inhaled Dry Powder Inhaler Formulations

关键词:  扫描电子显微镜  能谱仪  吸入式干粉制剂  原料药  载体颗粒  宽高比

Key words:  scanning electron microscopy  energy dispersive spectroscopy  dry powder inhaler  API  carrier  aspect ratio

摘要:

目的 综述扫描电子显微镜-能谱仪在吸入式干粉制剂表征中的重要应用。方法 通过文献调研与归纳,扫描电子显微镜-能谱仪法表征吸入式干粉制剂,自动颗粒粒形粒径分析软件统计分析载体颗粒,对扫描电子显微镜在吸入式干粉制剂的研发过程中的4个广泛应用场景进行论证和总结。结果 吸入式干粉制剂学是高度依赖颗粒工程学的制剂类型,其性能和治疗功效很大程度上取决于原料药与辅料的微观特性。载体颗粒的尺寸、形状对高效肺部输送起决定性作用。而载体颗粒的表面粗糙度直接影响原料药与载体颗粒之间的黏附-脱附平衡,最终直接影响制剂雾化性能。扫描电子显微镜可以很直观地对颗粒的粒径、粒形以及表面粗糙情况进行快速评估。此外,也可通过扫描电子显微镜图像结合能谱分析判断原料药在载体颗粒上的负载情况,还可用来直接评估原料药颗粒的脱附能力。结论 扫描电子显微镜-能谱仪在吸入式干粉制剂的研发中具有广泛的应用意义,为该类型制剂的研发提供了先进的表征工具。

Abstract:

OBJECTIVE To review the main applications of scanning electron microscopy(SEM) and energy dispersive spectroscopy(EDS) in the characterization of dry powder inhaler formulations(DPI).METHODS Through literature research and induction, using SEM-EDS method to characterize the dry powder inhaler formulation, using SEM based automatic particle shape and size analysis software to perform statistical analysis of carrier particles, to summarize the key application scenarios of SEM-EDS in the scientific research or development of DPI formulations.RESULTS DPI was a preparation type highly dependent on particle engineering. Its performance and therapeutic efficacy largely depended on the micro characteristics of active pharmaceutical ingredient(API) and carrier. The size and shape of carrier particles played a decisive role in efficient lung transport. The surface roughness of carrier particles directly affected the adhesion-desorption balance between API and carrier particles, and finally directly affected the atomization performance of the preparation. SEM could quickly evaluate the particle size, particle shape and surface roughness. In addition, the loading of API on carrier particles and the desorption capacity of API-carrier system could also be judged by SEM-EDS analysis.CONCLUSION SEM-EDS has extensive application significance in the research and development of DPI preparations, it provides an advanced characterization method for the research and development of this type of preparations.