School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23219, USA.
J Aerosol Med Pulm Drug Deliv. 2013 Jun;26(3):138-44. doi: 10.1089/jamp.2012.0975. Epub 2012 Sep 4.
A new in vitro test method for dry powder inhalers (DPIs) was recently found to be predictive of the published in vivo results for Budelin Novolizer. The present study was intended to assess the method's robustness by evaluating correlations between average drug deposition in vitro and in vivo from five different DPIs.
In vitro drug deposition from five marketed DPIs was assessed in a realistic physical airway model of a "medium" sized adult in an experimental setup that allowed deposition to be characterized regionally for carefully selected simulated air flow rate versus time profiles. The DPIs studied were Spiriva(®) HandiHaler(®), Relenza(®) Diskhaler(®), Salbutamol Easyhaler(®), Pulmicort(®) Turbuhaler(®), and Foradil(®) Aerolizer(®). In vitro regional deposition results were compared with those reported in the literature in order to create in vitro-in vivo correlations (IVIVCs) for each inhaler.
Mean percent total lung deposition (TLD ± SD) in vitro for Spiriva HandiHaler, Relenza Diskhaler, Salbutamol Easyhaler, Pulmicort Turbuhaler, and Foradil Aerolizer were 17.3 ± 1.2, 22.6 ± 1.1, 29.0 ± 1.1, 28.0 ± 3.0, and 21.7 ± 1.2, respectively. These results showed excellent agreement with reported in vivo values, with absolute prediction errors in TLD of ≤ 2% for all DPIs except Relenza Diskhaler. Similarly, in vitro mouth-throat and device deposition results were stoichiometrically comparable to those reported in vivo for all DPIs except Relenza Diskhaler and Turbuhaler. Inspection of the scintigraphy studies for Relenza Diskhaler and Turbohaler revealed possible problems with powder labeling and result interpretation in their in vivo clinical assessments.
A characteristic physical airway model representing a medium-sized adult, when coupled to carefully chosen characteristic inhalation maneuvers used in the clinic, produced results that correlated with regional drug deposition estimates from scintigraphy across a group of different DPIs.
最近发现一种新的干粉吸入器（DPI）体外测试方法可预测布地奈德 Novolizer 的已发表体内结果。本研究旨在通过评估五种不同 DPI 的体外和体内平均药物沉积之间的相关性来评估该方法的稳健性。
在一种“中等”成年人体的现实物理气道模型中，使用允许对精心选择的模拟气流速率与时间曲线进行区域性沉积特征描述的实验装置，评估五种市售 DPI 的体外药物沉积。研究的 DPI 为思力华® HandiHaler®、雷诺考特® Diskhaler®、信必可都保®、普米克® Turbuhaler®和奥克斯都保®。将体外区域性沉积结果与文献中报道的结果进行比较，为每个吸入器创建体外-体内相关性（IVIVC）。
思力华 HandiHaler、雷诺考特 Diskhaler、信必可都保、普米克 Turbuhaler 和奥克斯都保的体外总肺沉积（TLD±SD）的平均值分别为 17.3±1.2%、22.6±1.1%、29.0±1.1%、28.0±3.0%和 21.7±1.2%。这些结果与已报道的体内值非常吻合，除雷诺考特 Diskhaler 外，所有 DPI 的 TLD 绝对预测误差均≤2%。同样，除雷诺考特 Diskhaler 和 Turbuhaler 外，所有 DPI 的体外口咽和装置沉积结果与体内报道的结果在化学计量上是可比的。对雷诺考特 Diskhaler 和 Turbohaler 的闪烁扫描研究进行检查发现，其体内临床评估中可能存在粉末标记和结果解释方面的问题。
代表中等大小成人的特征性物理气道模型，与临床中精心选择的特征性吸入动作相结合，产生的结果与不同 DPI 的闪烁扫描区域性药物沉积估计值相关。
