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Comparative pharmacokinetics of salbutamol inhaled from a pressurized metered dose inhaler either alone or connected to a newly enhanced spacer design.
European Journal of Pharmaceutical Sciences ( IF 4.6 ) Pub Date : 2020-03-09 , DOI: 10.1016/j.ejps.2020.105304
Wesam G Ammari 1 , Ghaleb A Oriquat 2 , Mark Sanders 3
Affiliation  

BACKGROUND Coordination between actuation of a pressurized metered dose inhaler (pMDI) and inhalation is a critical manoeuvre that many patients fail to perform correctly. pMDIs connected to spacers do not require hand-lung coordination. This study evaluated the relative lung and systemic bioavailability and oropharyngeal deposition of salbutamol post-inhalation from Ventolin® Evohaler® (GlaxoSmithKline) either alone following verbal inhaler technique counselling (VC) or connected to a newly improved Able Spacer® (AS). METHODS In a two-period, randomized crossover study, 16 healthy adults inhaled 2 × 100 µg salbutamol puffs (1 min gap) from Ventolin using VC or AS. Immediately after each puff inhalation, each subject gargled with 20 mL water for oropharyngeal deposition (OD) determination. Urine samples were collected 0.5 h (pre-) and 0.5, 1.0 and 2.0 h post-inhalation. Urine was then pooled 2-24 h post-inhalation. The relative lung bioavailability (0-0.5 h urinary salbutamol excretion - USAL0.5) and systemic bioavailability (0-24 h urinary excretion of salbutamol and its metabolite - USALMET24) were determined. A one week washout separated VC and AS use. RESULTS The mean (SD) USAL0.5 of VC and AS was 5.36 (4.48) and 12.80 (10.83) µg, respectively. The mean (SD) OD was 11.35 (3.37) and 0.48 (0.30) µg, respectively. VC and AS were significantly different in USAL0.5 and OD (p<0.001). USALMET24 was comparable (p>0.05). CONCLUSIONS Compared with VC, AS doubled the inhaled salbutamol lung dose and minimised its precipitation in the oral cavity. The results suggest this inhalation aid can add therapeutic and safety benefits particularly in patients with continued pMDI technique issues despite repeated VC.

中文翻译:

从加压定量吸入器中吸入沙丁胺醇的比较药代动力学,可以单独使用,也可以与新增强的垫片设计相连。

背景技术加压计量吸入器(pMDI)的致动与吸入之间的协调是许多患者无法正确执行的关键操作。连接到垫片的pMDI不需要手肺协调。这项研究评估了Ventolin®Evohaler®(GlaxoSmithKline)吸入后沙丁胺醇的相对肺和全身生物利用度以及口咽沉积物的作用,方法是在口服吸入剂技术咨询(VC)后单独使用或与新改良的AbleSpacer®(AS)连接。方法在一项为期两阶段的随机交叉研究中,16名健康成年人使用VC或AS从Ventolin吸入2×100 µg沙丁胺醇粉扑(间隔1分钟)。每次吸入粉扑后,立即用20 mL水漱口以测定口咽部沉积(OD)。分别于0.5 h(pre-)和0.5,1收集尿液样本。吸入后0和2.0小时。然后在吸入后2-24小时合并尿液。确定了相对肺生物利用度(0-0.5小时尿沙丁胺醇排泄量-USAL0.5)和全身生物利用度(0-24小时尿沙丁胺醇及其代谢物排泄量-USALMET24)。一周的冲销将VC和AS的使用分开。结果VC和AS的平均(SD)USAL0.5分别为5.36(4.48)和12.80(10.83)µg。平均(SD)OD分别为11.35(3.37)和0.48(0.30)µg。VC和AS在USAL0.5和OD中有显着差异(p <0.001)。USALMET24具有可比性(p> 0.05)。结论与VC相比,AS将沙丁胺醇的肺部吸入剂量增加了一倍,并最大程度地减少了其在口腔中的沉淀。
更新日期:2020-03-09
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