Qin Wei, He Yuanzhi, Guo Zhen, Zhang Liu, Wu Li, Yin Xianzhen, Shakya Shailendra, Maharjan Abi, Tang Yan, Zhu Weifeng, Zhang Jiwen
Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Asian J Pharm Sci. 2019 Mar;14(2):174-182. doi: 10.1016/j.ajps.2018.05.003. Epub 2018 Jun 9.
The microsphere was a primary particulate system for taste-masking with unique structural features defined by production process. In this article, ibuprofen lipid microspheres of octadecanol and glycerin monostearate were prepared to mask the undesirable taste of ibuprofen via three kinds of spray congealing processes, namely, air-cooling, water-cooling and citric acid solution-cooling. The stereoscopic and internal structures of ibuprofen microspheres were quantitatively analyzed by synchrotron radiation X-ray micro-computed tomography (SR-µCT) to establish the relationship between the preparation process and microsphere architectures. It was found that the microstructure and morphology of the microspheres were significantly influenced by preparation processes as the primary factors to determine the release profiles and taste-masking effects. The sphericity of ibuprofen microspheres congealed in citric acid solution was higher than that of other two and its morphology was more regular than that being congealed in air or distilled water, and the contact angles between congealing media and melted ibuprofen in octadecanol and glycerin monostearate well demonstrated the structure differences among microspheres of three processes which controlled the release characteristics of the microspheres. The structure parameters like porosity, sphericity, and radius ratio from quantitative analysis were correlated well with drug release behaviors. The results demonstrated that the exterior morphology and internal structure of microspheres had considerable influences on the drug release behaviors as well as taste-masking effects.
微球是一种用于掩味的初级微粒系统，具有由生产工艺定义的独特结构特征。在本文中，通过三种喷雾冷凝工艺，即空气冷却、水冷却和柠檬酸溶液冷却，制备了由十八醇和单硬脂酸甘油酯组成的布洛芬脂质微球，以掩盖布洛芬的不良味道。通过同步辐射X射线显微计算机断层扫描（SR-µCT）对布洛芬微球的立体和内部结构进行定量分析，以建立制备工艺与微球结构之间的关系。结果发现，微球的微观结构和形态受制备工艺的显著影响，而制备工艺是决定释放曲线和掩味效果的主要因素。在柠檬酸溶液中冷凝的布洛芬微球的球形度高于其他两种，其形态比在空气或蒸馏水中冷凝的更规则，并且冷凝介质与十八醇和单硬脂酸甘油酯中熔化的布洛芬之间的接触角很好地证明了三种工艺微球之间的结构差异，这些差异控制了微球的释放特性。定量分析得到的孔隙率、球形度和半径比等结构参数与药物释放行为具有良好的相关性。结果表明，微球的外部形态和内部结构对药物释放行为以及掩味效果有相当大的影响。
