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通过新型干粉吸入器和标准定量气雾剂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 via a novel dry powder inhaler and a standard metered dose inhaler.

作者信息

Hindle M, Peers E M, Parry-Billings M, Chrystyn H

机构信息

Pharmacy Practice, School of Pharmacy, University of Bradford, Bradford, UK.

出版信息

Br J Clin Pharmacol. 1997 Mar;43(3):336-8. doi: 10.1046/j.1365-2125.1997.00564.x.

DOI:10.1046/j.1365-2125.1997.00564.x
PMID:9088593
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2042743/
Abstract

AIMS

The number of dry powder inhaler (DPI) devices could increase because they are easier to use than a metered dose inhaler (MDI). Using urinary excretion, the relative bioavailability of salbutamol to the lungs and the body for a prototype DPI has been compared with an MDI.

METHODS

A randomized, double-blind, two way crossover study compared the amount of salbutamol in the urine 30 min following inhalation of 2 x 100 micrograms salbutamol from a prototype DPI (Innovata Biomed Ltd, UK) and a Ventolin (Allen and Hanburys Ltd, UK) MDI in 10 volunteers. The amount of salbutamol and its metabolite, the ester sulphate conjugate, renally excreted up to 24 h post inhalation was also determined to evaluate the relative bioavailability of salbutamol to the body.

RESULTS

The mean (s.d.) 30 min post-treatment urinary excretion for the prototype DPI and MDI was 8.4 (2.6) and 5.0 (1.9) micrograms, respectively (P < 0.001). The total amount of salbutamol and its ester metabolite excreted in the urine over the 24 h period after inhalation was 187.9 (77.6) and 137.6 (40.0) micrograms (P < 0.05).

CONCLUSIONS

The prototype DPI delivered more salbutamol to the body and the lungs than a conventional MDI. This finding supports further development of the prototype DPI. The urinary salbutamol method is able to discriminate between two different inhalation systems.

摘要

目的

干粉吸入器(DPI)装置的数量可能会增加,因为它们比定量吸入器(MDI)更易于使用。通过尿液排泄,已将一种原型DPI中沙丁胺醇相对于肺部和身体的相对生物利用度与MDI进行了比较。

方法

一项随机、双盲、双向交叉研究比较了10名志愿者从英国Innovata Biomed Ltd生产的原型DPI和英国Allen and Hanburys Ltd生产的万托林MDI吸入2×100微克沙丁胺醇后30分钟尿液中沙丁胺醇的含量。还测定了吸入后24小时内肾脏排泄的沙丁胺醇及其代谢产物硫酸酯共轭物的量,以评估沙丁胺醇相对于身体的相对生物利用度。

结果

原型DPI和MDI治疗后30分钟的平均(标准差)尿排泄量分别为8.4(2.6)和5.0(1.9)微克(P<0.001)。吸入后24小时内尿液中排泄的沙丁胺醇及其酯代谢产物的总量分别为187.9(77.6)和137.6(40.0)微克(P<0.05)。

结论

原型DPI比传统MDI向身体和肺部输送的沙丁胺醇更多。这一发现支持了原型DPI的进一步开发。尿沙丁胺醇方法能够区分两种不同的吸入系统。