汪春江1，黄永鹏1，唐 慧1，李昇原1,2，陈 博1
（1. 国民核生化灾害防护国家重点实验室，北京 102205；2. 四川轻化工大学 机械工程学院，四川 宜宾 644000）
DOI:10.13732/j.issn.1008-5548.2023.01.004
收稿日期： 2022-05-06，修回日期：2022-11-01,在线出版时间：2022-12-01 20:15。
基金项目：青年科技英才自主基金项目，编号：2021F4401。
第一作者简介： 汪春江(1998—)，男，硕士研究生，研究方向为吸入及缓释药物微粉制剂的制备与应用。E-mail：wangcj327@163.com。
通信作者简介： 陈博(1983—)，男，副研究员，博士，硕士生导师，研究方向为药物粉体制备与应用。E-mail：NBC_BoChen@163.com。
摘要：采用溶胶-凝胶工艺制备4种不同的介孔二氧化硅载体材料，通过浸渍吸附-冷冻干燥工艺负载药物奥曲肽构建吸入缓释微粉制剂，并对载体与微粉制剂开展形貌结构、粒度分布、载药量、体外释放性能、体外吸入沉积性能的评价。结果表明：设计制备的4种介孔二氧化硅载体材料具有不同的形貌、粒径、比表面积、比孔容等，能够实现对奥曲肽的有效负载；构建的4种微粉制剂具有不同的形貌、载药量、体外释放性能以及体外吸入沉积性能；介孔二氧化硅微球-奥曲肽微粉制剂具有最优的综合性能，满足肺部吸入药物递送要求，排空率达到100%,有效部位沉积率大于60%,持续释药时间24 h;微粉制剂保持了载体原有的粒径均一的单分散球形的规则形貌，有利于提高药物转运递送剂量的准确性与重现性。
关键词：溶胶-凝胶工艺；介孔二氧化硅；奥曲肽；微粉制剂；吸入缓释剂
Abstract：Four different mesoporous silica carrier materials were prepared by sol-gel process. Octreotide was loaded by impregnation adsorption-freeze drying process so as to construct micropowder pharmacy for inhalation of slow-release. Properties of carriers and micropowder preparations including morphology, particle size distribution, drug loading, in vitro release property, in vitro inhalation deposition were evaluated. Research results show that the four mesoporous silica carriers have different morphology, particle size, specific surface area and specific pore volume.All of the carriers can load octreotide effectively. The four kinds of micropowder pharmachies have different performance such as morphology, drug loading, in vitro release performance and in vitro inhalation deposition.The micropowder pharmachies named as mesoporous silica microspheres-octreotide have the best comprehensive properties, which meet the drug delivery requirements for pulmonary. For mesoporous silica microspheres-octreotide, emptying rate reaches 100%, fine particle fraction is greater than 60% and sustained drug release time lasts 24 h. Micropowder pharmachies maintain the original uniform monodisperse spherical morphology of carrier particles, which are situated to increase the accuracy and reproducibility of drug deliveries.
Keywords：sol-gel process; mesoporous silica; octreotide; micropowder pharmacy; inhalation of slow-release
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