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通过振动雾化喷雾干燥制备亚微米药物颗粒的创新方法:溶剂和表面活性剂类型的影响

Innovative approach to produce submicron drug particles by vibrational atomization spray drying: influence of the type of solvent and surfactant.

作者信息

Durli T L, Dimer F A, Fontana M C, Pohlmann A R, Beck R C R, Guterres S S

机构信息

Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre, RS , Brazil and.

出版信息

Drug Dev Ind Pharm. 2014 Aug;40(8):1011-20. doi: 10.3109/03639045.2013.798804. Epub 2013 May 15.

DOI:10.3109/03639045.2013.798804
PMID:23672183
Abstract

Spray drying is a technique used to produce solid particles from liquid solutions, emulsions or suspensions. Buchi Labortechnik developed the latest generation of spray dryers, Nano Spray Dryer B-90. This study aims to obtain, directly, submicron drug particles from an organic solution, employing this equipment and using dexamethasone as a model drug. In addition, we evaluated the influence of both the type of solvent and surfactant on the properties of the powders using a 3(2) full factorial analysis. The particles were obtained with high yields (above 60%), low water content (below 2%) and high drug content (above 80%). The surface tension and the viscosity were strongly influenced by the type of solvent. The highest powder yields were obtained for the highest surface tension and the lowest viscosity of the drug solutions. The use of ionic surfactants led to higher process yields. The laser diffraction technique revealed that the particles deagglomerate into small ones with submicrometric size, (around 1 µm) that was also observed by scanning electron microscopy. Interaction between the raw materials in the spray-dried powders was verified by calorimetric analysis. Thus, it was possible to obtain dexamethasone submicrometric particles by vibrational atomization from organic solution.

摘要

喷雾干燥是一种用于从液体溶液、乳液或悬浮液中制备固体颗粒的技术。Buchi Labortechnik公司开发了新一代喷雾干燥器——纳米喷雾干燥器B - 90。本研究旨在使用该设备并以地塞米松作为模型药物,直接从有机溶液中获得亚微米级药物颗粒。此外,我们使用3(2)全因子分析评估了溶剂类型和表面活性剂对粉末性质的影响。所获得的颗粒具有高产率(高于60%)、低含水量(低于2%)和高药物含量(高于80%)。表面张力和粘度受溶剂类型的强烈影响。对于药物溶液表面张力最高且粘度最低的情况,获得了最高的粉末产率。离子型表面活性剂的使用导致了更高的工艺产率。激光衍射技术表明颗粒解聚成亚微米尺寸的小颗粒(约1 µm),扫描电子显微镜也观察到了这一现象。通过量热分析验证了喷雾干燥粉末中原料之间的相互作用。因此,通过振动雾化从有机溶液中获得地塞米松亚微米颗粒是可能的。

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