基于微量喷射技术的奥曲肽长效生物可降解微球制备工艺研究

Study on Preparation and Quality of Sustained Release Biodegradable Octreotide Microsphere Based on Micro-injection

关键词:  微球  奥曲肽  复乳法  微量喷射技术

Key words:  microsphere  octreotide  W/O/W  micro-injection

摘要:

目的 将溶剂挥发法中的复乳法与微量喷射技术相结合，对奥曲肽长效生物可降解微球制备中微量喷射技术的应用进行了探索。方法 利用单因素法研究了驱动电压、喷射频率和搅拌器转速等因素对微球平均粒径和粒径分布的影响。结果 在实验中药物处方条件一定的情况下，驱动电压与粒径大小成正比，喷射频率和搅拌器转速与粒径大小反比。当驱动电压为60～100 V，喷射频率为3 000～7 000 Hz，搅拌器转速为150～450 r·min^-1时，粒径分布处于较为理想状态。结论 使用微量喷射技术制得微球外观圆整，形态良好，较传统复乳法制得的微球，其均一性及外观形态得到显著改善，提高了包封率(>30%)。

Abstract:

OBJECTIVE To combine the method of W/O/W with micro-injection and study the application of micro- injection on preparing sustained release biodegradable octreotide microspheres. METHODS It was studied by using a single factor analysis method on spray frequency, agitation speed and driving voltage as the factors. RESULTS In the constant prescription conditions, the driving voltage was proportional to the particle size, the spray frequency and mixer speed were inverse ratio to the particle size. When the driving voltage was 60-100 V, spray frequency was 3 000-7 000 Hz and agitation speed was 150-450 r·min^-1, the particle size distribution was in more ideal state. CONCLUSION The microsphere prepared by micro-injection are in rounded appearance and well formed. This method significantly improves uniformity and appearance compared with microsphere prepared simply by W/O/W, and there is a certain increase in encapsulation efficiency(>30%).