Physicochemical characterization and aerosol dispersion performance of organic solution advanced spray-dried microparticulate/nanoparticulate antibiotic dry powders of tobramycin and azithromycin for pulmonary inhalation aerosol delivery

Physicochemical characterization and aerosol dispersion performance of organic solution advanced spray-dried microparticulate/nanoparticulate antibiotic dry powders of tobramycin and azithromycin for pulmonary inhalation aerosol delivery
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DOI:
10.1016/j.ejps.2013.10.016
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发表时间:
2014-02-14
影响因子:
4.6
通讯作者:
Mansour, Heidi M.
Mansour, Heidi M.
中科院分区:
医学2区
文献类型:
--
作者:
Li, Xiaojian;Vogt, Frederick G.;Mansour, Heidi M.

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本研究的目的是系统地设计用于肺部感染靶向肺部给药的纯抗生素药物干粉吸入器(DPIs),并综合比较干粉吸入器(DPIs)的固体物化性质和喷雾干燥条件对气雾剂分散性能的影响。合理选择的两种模型抗菌药物妥布霉素(TOB)和阿奇霉素(AZI)代表了氨基糖苷类和大环内酯类两种不同的抗生素类药物。分别进行了分析。颗粒大小分布窄,呈单峰分布,在微粒子/纳米颗粒尺寸范围内。制得的SD粒子具有相对球形的粒子形态、光滑的表面形态、较低的残余水分含量、无长程分子有序性。排放剂量(ED%)、细颗粒物百分率(FFP%)和可吸入颗粒物百分率(Rf%)都很好。MMAD值在可吸入范围内(
The purpose of this study was to systematically design pure antibiotic drug dry powder inhalers (DPIs) for targeted antibiotic pulmonary delivery in the treatment of pulmonary infections and comprehensively correlate the physicochemical properties in the solid-state and spray-drying conditions effects on aerosol dispersion performance as dry powder inhalers (DPIs). The two rationally chosen model antibiotic drugs, tobramycin (TOB) and azithromycin (AZI), represent two different antibiotic drug classes of aminoglycosides and macrolides. respectively. The particle size distributions were narrow, unimodal, and in the microparticulate/nanoparticulate size range. The SD particles possessed relatively spherical particle morOhology, smooth surface morphology, low residual water content, and the absence of long-range molecular order. The emitted dose (ED%), fine particle fraction (FPF%) and respirable fraction (RF%) were all excellent. The MMAD values were in the inhalable range (