Research Center Pharmaceutical Engineering GmbH, 8010, Graz, Austria.
Austrian Centre for Electron Microscopy and Nanoanalysis, Graz University of Technology, 8010, Graz, Austria.
Pharm Res. 2019 Apr 9;36(6):80. doi: 10.1007/s11095-019-2612-9.
The performance of carrier-based dry powder inhaler (DPI) formulations can be critically impacted by interfacial interactions driven by tribo-electrification. Therefore, the aim of the present work was to understand how distinct API particle characteristics affect the charging behaviour of blends intended for DPI delivery.
Salbutamol sulphate (SBS) particles engineered via spray-drying and jet milling were used as model APIs. D-mannitol was selected as a model carrier. The materials were characterized concerning their different particle properties and their charge was analysed alone and in blends before and after flow over a stainless-steel pipe.
The spray-dried SBS (amorphous and spherical) charged positively and to a higher extent than jet milled SBS (crystalline and acicular) that charged negatively and to a lower extent. D-mannitol charged positively and to a higher extent than the APIs. All drug-excipient blends charged negatively and differences were found between the spray-dried and jet milled SBS blends at 2% and 5% drug loads.
It was demonstrated how distinct solid-states, particle shape, size and morphology as well as different water contents of the different materials can affect tribo-charging. For their binary blends, the amount and nature of fines seem to govern inter-particle contacts critically impacting charge evolution.
载体制备的干粉吸入剂（DPI）配方的性能可能会受到摩擦电驱动的界面相互作用的严重影响。因此，本研究的目的是了解不同 API 颗粒特性如何影响用于 DPI 传递的混合物的充电行为。
采用喷雾干燥和射流磨工艺对硫酸沙丁胺醇（SBS）颗粒进行了工程化处理，将其用作模型 API。选择甘露醇作为模型载体。对材料进行了不同颗粒特性的表征，并在不锈钢管上流动前后单独分析了它们的电荷以及混合物的电荷。
喷雾干燥 SBS（无定形且呈球形）带正电，且充电程度比射流磨 SBS（结晶且呈针状）高，后者带负电，充电程度低。甘露醇带正电，充电程度比 API 高。所有药物-赋形剂混合物均带负电，并且在 2%和 5%药物负荷下，喷雾干燥和射流磨 SBS 混合物之间存在差异。
该研究证明了不同的固态、颗粒形状、大小和形态以及不同材料的含水量如何影响摩擦充电。对于它们的二元混合物，颗粒间接触的量和性质似乎对电荷演变有重要影响。
