用于肺部药物递送的纳米喷雾干燥粉雾剂

发布时间：2018-03-29 04:06

本文选题：纳米喷雾干燥　切入点：硫酸沙丁胺醇　出处：《中国新药杂志》2016年19期

【摘要】：目的:采用纳米喷雾干燥(NSD)技术制备粒径在理想肺吸入尺度范围内的纳微颗粒,并系统考察不同辅料对NSD颗粒的影响,以获得具有良好吸入效率的NSD粉雾剂。方法:以一水合乳糖(LAC)、可溶性淀粉(STA)、海藻糖(TRE)和-环糊精(-CD)为辅料,制备硫酸沙丁胺醇的NSD颗粒。采用扫描电镜观察NSD颗粒形貌;激光粒度仪表征NSD颗粒粒度分布情况;新一代药用撞击器测定NSD颗粒的排空率及有效部位沉积率。结果:LAC-1 NSD颗粒呈光滑圆球状、黏附力强,产率为77.7%,体积平均粒径12.184μm,用其制得的粉雾剂排空率(ED)和微颗粒(4.46μm)比例(FPF)为78.9%和11.2%;而采用STA-,TRE-和-CD修饰的NSD颗粒表面褶皱、分散性良好,体积平均粒径、产率、ED和FPF分别在2.2~2.4μm,80.1%~81.6%,90%~93%和40%~47%范围内。结论:采用NSD技术可显著提高粉雾剂的回收率,可获得具有更小空气动力学直径的药物颗粒,这展现了NSD技术在获得和优化纳微干粉颗粒以实现药物高效肺吸入方面的巨大潜力。
[Abstract]:Objective: using nano spray drying (NSD) preparation technology of particle size in the ideal aspiration scale range of nano particles, and the effects of different excipients on NSD particles, in order to obtain a good NSD powder spray inhalation efficiency. Methods: lactose monohydrate (LAC), soluble starch (STA), trehalose (TRE) and cyclodextrin (-CD) as adjuvant, NSD particles prepared salbutamol sulfate. To observe the morphology of NSD particles by scanning electron microscope; laser particle size instrument NSD particle size distribution; a new generation of pharmaceutical impactor determination of NSD particle emptying rate and the effective part of the deposition rate. Results: LAC-1 NSD is a smooth spherical particle, adhesion is strong, the yield is 77.7%, the volume average particle diameter of 12.184 mu m, made of the powder to the emptying rate (ED) and micro particles (4.46 m) ratio (FPF) were 78.9% and 11.2%; and the use of STA-, NSD TRE- and -CD particle surface fold modification, good dispersion Well, the volume average particle size, yield, ED and FPF respectively in 80.1%~81.6% 2.2~2.4, m, 90%~93% and 40%~47% range. Conclusion: using NSD technology can significantly improve the recovery rate of powder spray, can obtain the drug particles with smaller aerodynamic diameter, which shows the NSD technology in the acquisition and optimization of the enormous potential of Na micro powder particles to achieve high drug inhalation lung areas.

【作者单位】：中国医科大学法医学院;辽宁师范大学化学化工学院;苏州大学分析测试中心;中国医科大学公共基础学院;苏州惠仁生物科技有限公司;
【基金】：青年科学基金资助项目(21404120) 中国医科大学校内基金资助项目(XZR20160033)
【分类号】：R943

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