使用定量吸入法和储雾罐装置吸入后沙丁胺醇对肺部的相对生物利用度。
Relative bioavailability of salbutamol to the lung following inhalation using metered dose inhalation methods and spacer devices.
作者信息
Hindle M, Chrystyn H
机构信息
School of Pharmacy, University of Bradford, West Yorkshire.
出版信息
Thorax. 1994 Jun;49(6):549-53. doi: 10.1136/thx.49.6.549.
BACKGROUND
Inhalation aids do not require coordination between actuation of a metered dose inhaler (MDI) with inspiration and reduce oropharyngeal impaction. The delivery of salbutamol to the lung and systemic availability following inhalation with three commonly used spacers and an open mouth technique have been evaluated using a simple noninvasive technique based on urinary excretion 30 minutes and 24 hours after the dose.
METHODS
Ten healthy subjects inhaled, on randomised study days, 4 x 100 micrograms from a Ventolin MDI and, subsequently, with the aid of a Volumatic, Bricanyl Spacer, and Nebuhaler spacer device. In addition, an open mouth inhaler technique was evaluated. Urine samples were collected 0-30 minutes and 0.5-24 hours after inhalation. From these samples the relative bioavailability to the lung (urinary salbutamol excretion 30 minutes after dosing) and the systemic bioavailability of the dose (24 hour urinary excretion of salbutamol and its metabolite) for each inhalation method was obtained.
RESULTS
The mean (SD) urinary excretion of salbutamol 30 minutes after inhalation using the MDI alone and with the Volumatic, Bricanyl Spacer, Nebuhaler, and open mouth technique was 2.83 (0.78)%, 3.37 (0.69)%, 4.09 (0.91)%, 4.34 (1.60)%, and 3.49 (0.98)%, respectively, expressed as a percentage of the nominal dose. The nebuhaler and Bricanyl Spacer spacer devices were found to increase the relative bioavailability of salbutamol to the lung compared with the MDI alone. Compared with the MDI the inhalation aid increases were much greater than the intra-individual variability of the urinary excretion method. In 11 individuals who each repeated the same inhalation procedure on four separate occasions, the mean (SD) coefficient of variation was 8.24 (2.36)%. The mean (SD) 24 hour urinary excretion of salbutamol and its metabolites was 26.6 (6.79), 27.0 (7.95), and 55.6 (9.74)% of the salbutamol dose for the Volumatic, Nebuhaler, and MDI, respectively. Similar values following the open mouth method and Bricanyl Spacer were 48.9 (10.97)% and 43.8 (11.57)%. These values, representing the systemic availability of the inhaled dose, were lower when inhaling with the aid of the Volumatic and Nebuhaler than inhalation from the MDI alone.
CONCLUSIONS
Spacer devices improve pulmonary bioavailability of salbutamol and reduce the systemically available dose.
背景
吸入辅助装置无需在定量吸入器（MDI）启动与吸气之间进行协调，可减少口咽沉积。采用一种基于给药后30分钟和24小时尿排泄的简单非侵入性技术，评估了使用三种常用储雾罐和一种张口技术吸入沙丁胺醇后药物在肺部的递送情况及全身可用性。
方法
10名健康受试者在随机研究日，从万托林MDI吸入4×100微克药物，随后分别借助Volumatic储雾罐、布地奈德储雾罐和Nebuhaler储雾罐装置吸入。此外，还评估了张口吸入技术。在吸入后0 - 30分钟和0.5 - 24小时收集尿液样本。从这些样本中得出每种吸入方法药物在肺部的相对生物利用度（给药后30分钟尿沙丁胺醇排泄量）和药物的全身生物利用度（沙丁胺醇及其代谢物24小时尿排泄量）。
结果
单独使用MDI以及借助Volumatic储雾罐、布地奈德储雾罐、Nebuhaler储雾罐和张口技术吸入后30分钟，沙丁胺醇的平均（标准差）尿排泄量分别为名义剂量的2.83（0.78）%、3.37（0.69）%、4.09（0.91）%、4.34（1.60）%和3.49（0.98）%。发现Nebuhaler储雾罐和布地奈德储雾罐装置与单独使用MDI相比，可提高沙丁胺醇在肺部的相对生物利用度。与MDI相比，吸入辅助装置带来的增加远大于尿排泄法的个体内变异性。在11名每人在四个不同场合重复相同吸入程序的受试者中，平均（标准差）变异系数为8.24（2.36）%。Volumatic储雾罐、Nebuhaler储雾罐和MDI吸入后，沙丁胺醇及其代谢物的平均（标准差）24小时尿排泄量分别为沙丁胺醇剂量的26.6（6.79）%、27.0（7.95）%和55.6（9.74）%。张口技术和布地奈德储雾罐吸入后的类似值分别为48.9（10.97）%和43.8（11.57）%。这些代表吸入剂量全身可用性的值，在借助Volumatic储雾罐和Nebuhaler储雾罐吸入时低于单独从MDI吸入。
结论
储雾罐装置可提高沙丁胺醇的肺部生物利用度并减少全身可用剂量。
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