Nano- and Microstructured model carrier surfaces to alter dry powder inhaler performance

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• 作者：Niklas Renner^a ; Hartwig Steckel^b ; Nora Urbanetz^c ; Regina Scherließ ; ^a ; ^{rscherliess@pharmazie.uni-kiel.de}
• 关键词：Budesonide (PubChem CID ; 5281004) ; Formoterol fumarate (PubChem CID ; 53477580)
• 刊名：International Journal of Pharmaceutics
• 出版年：2017
• 出版时间：25 February 2017
• 年：2017
• 卷：518
• 期：1-2
• 页码：20-28
• 全文大小：1478 K
• 卷排序：518

文摘

The present study investigates the effect of different carrier surface modifications on the aerosolisation performance and on the effective carrier payload of interactive blends for inhalation. Two different active pharmaceutical ingredients (APIs) were used: Formoterol fumarate dihydrate (FF) and budesonide (BUD). Blends were prepared with glass beads as model carriers which have been subjected to mechanical surface modifications in order to introduce surface roughness via treatment with hydrofluoric acid (HF) and/or milling with tungsten carbide (TC).As far as effective carrier payload, in this study expressed as true surface coverage (TSC), is concerned, surface modification had varying effects on blends containing BUD or FF.Aerodynamic characterisation in vitro showed a significant decrease in respirable fraction for glass beads treated with HF (40.2–50.1%), due to the presence of clefts and cavities, where drug particles were sheltered during inhalation. In contrast, grinding with TC leads to surface roughness on a nano scale, ultimately increasing aerodynamic performance up to 20.0–38.1%. These findings are true for both APIs, regardless of their chemical properties.