介孔二氧化硅负载奥曲肽制备吸入缓释微粉制剂  

Micropowder pharmacy for inhalation of slow-release produced by mesoporous silica loaded octreotide

作　　者：汪春江 黄永鹏 唐慧 李昇原 陈博 WANG Chunjiang;HUANG Yongpeng;TANG Hui;LI Shengyuan;CHEN Bo(State Key Laboratory of NBC Protectio for Civilian,Beijing 102205,China;School of Mechanical Engineering,Sichuan University of Scienoce and Engineering,Yibin 644000,China)

机构地区：[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

出　　处：《中国粉体技术》2023年第1期31-38,共8页China Powder Science and Technology

基　　金：青年科技英才自主基金项目,编号:2021F4401。

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。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.

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 

分 类 号：R944.9[医药卫生—药剂学]