Kirby S M, Smith J, Ventresca G P
Clinical Pharmacology Division, Glaxo Research and Development Ltd, Greenford, Middlesex, UK.
Thorax. 1995 Jun;50(6):679-81. doi: 10.1136/thx.50.6.679.
Metered dose inhalers for the treatment of asthma use chlorofluorocarbons as propellants. These face an international ban due to their effect on the ozone layer. Salmeterol has been reformulated using the non-chlorinated propellant Glaxo inhalation grade HFA134a.
The safety, tolerability and systemic pharmacodynamic activity of the salmeterol/HFA134a inhaler, the current salmeterol inhaler, and placebo (HFA134a) were compared in 12 healthy volunteers in a double blind, randomised crossover study using a cumulative dosing design.
Safety and tolerability were similar and the response was related to the dose over the range used (50-400 micrograms) with both salmeterol inhalers. The salmeterol/HFA134a inhaler showed no differences from the current inhaler for pulse rate, blood pressure, tremor, QTc interval, and plasma glucose levels. The salmeterol/HFA134a inhaler had significantly less effect on plasma potassium levels.
In healthy volunteers the salmeterol/HFA134a inhaler is at least as safe and well tolerated as the current salmeterol inhaler, and has similar systemic pharmacodynamic activity.
用于治疗哮喘的定量吸入器使用氯氟烃作为推进剂。由于它们对臭氧层的影响,这些推进剂面临国际禁令。沙美特罗已重新配方,使用了非氯化推进剂葛兰素吸入级HFA134a。
在一项采用累积给药设计的双盲、随机交叉研究中,对12名健康志愿者比较了沙美特罗/HFA134a吸入器、当前的沙美特罗吸入器和安慰剂(HFA134a)的安全性、耐受性和全身药效学活性。
两种沙美特罗吸入器的安全性和耐受性相似,在所使用的剂量范围(50 - 400微克)内,反应与剂量相关。沙美特罗/HFA134a吸入器在脉搏率、血压、震颤、QTc间期和血浆葡萄糖水平方面与当前吸入器无差异。沙美特罗/HFA134a吸入器对血浆钾水平的影响明显较小。
在健康志愿者中,沙美特罗/HFA134a吸入器至少与当前的沙美特罗吸入器一样安全且耐受性良好,并且具有相似的全身药效学活性。