Advanced Drug Delivery Group, Faculty of Pharmacy, The University of Sydney, NSW, 2006, Australia.
Dekati Limited, Tykkitie 1, FIN-36240, Kangasala, Finland.
Pharm Res. 2017 Aug;34(8):1707-1715. doi: 10.1007/s11095-017-2178-3. Epub 2017 May 24.
This work investigated the effect of relative humidity (RH) on bipolar electrostatic charge profiles of dry powder inhaler aerosols using the Bipolar Charge Analyzer (BOLAR).
Two commercial products, Pulmicort® (400 μg, budesonide) and Bricanyl® (500 μg, terbutaline sulfate) Turbuhaler®, were used as model dry powder inhalers (DPIs) in this study. Three individual doses from each Turbuhaler® were sampled at 15, 40, 65 and 90% RH. Subsequently, charge and mass profiles were determined for each dispersion.
The aerosols from these two Turbuhaler® DPI were bipolarly charged, with larger particles carrying negative charge and smaller particles positive charge. Particles changed polarity around 2.60-4.17 μm and 0.95-2.60 μm for Pulmicort® and Bricanyl®, respectively. The effect of RH on particles differed between DPIs even though the mass output was not significantly affected. The net charge profiles of Pulmicort® were relatively independent of RH, whereas those of Bricanyl® showed a reduction in the charge magnitude with increasing RH. Both positive and negative charge profiles followed a similar trend with the change in RH and individually they had higher magnitudes than the measured net charge.
This study showed drug-specific bipolar charging of the Turbuhaler® DPI aerosols at varied RHs. Bricanyl® was more susceptible to RH and showed decreased bipolar and net charge levels with increasing RH, in comparison to Pulmicort®.
本研究使用双极电荷分析仪(BOLAR)考察相对湿度(RH)对干粉吸入器气溶胶的双极静电电荷分布的影响。
本研究使用两种市售产品,即 Pulmicort®(400μg,布地奈德)和 Bricanyl®(500μg,硫酸特布他林)Turbuhaler®,作为干粉吸入器(DPI)的模型。从每个 Turbuhaler®中采集三个单独剂量,在 15%、40%、65%和 90%RH 下进行采样。随后,对每个分散体进行电荷和质量分布的测定。
这两种 Turbuhaler®DPI 的气溶胶均带双极性电荷,较大的颗粒带负电荷,较小的颗粒带正电荷。颗粒在 2.60-4.17μm 和 0.95-2.60μm 左右发生极性反转,分别对应于 Pulmicort®和 Bricanyl®。尽管质量输出没有显著变化,但 RH 对颗粒的影响在两种 DPI 之间存在差异。Pulmicort®的净电荷分布相对独立于 RH,而 Bricanyl®的电荷分布则随着 RH 的增加而减小。正、负电荷分布都随 RH 的变化呈现出相似的趋势,且各自的电荷幅度都高于实测的净电荷。
本研究表明,在不同 RH 下,Turbuhaler®DPI 气溶胶具有特定药物的双极充电特性。与 Pulmicort®相比,Bricanyl®对 RH 更敏感,随着 RH 的增加,双极和净电荷水平下降。