Roche Nicolas, Usmani Omar, Franzini Laura, Labadini Lorenza, Mathews Kusum S, Panigone Sara, van Boven Job F M
Service de Pneumologie, Hôpital Cochin, APHP Centre et Université Paris Cité, Institut Cochin, INSERM UMR 1016, Paris, France.
Inserm, Équipe d'Épidémiologie Respiratoire Intégrative, CESP, Villejuif, France.
J Aerosol Med Pulm Drug Deliv. 2025 Feb;38(1):26-36. doi: 10.1089/jamp.2024.0023. Epub 2024 Nov 6.
The chlorofluorocarbons (CFCs) that were used as propellants in early pressurized metered-dose inhalers (pMDIs) had substantial ozone-depleting potential. Following the Montreal Protocol in 1987, the manufacture of a range of ozone-depleting substances, including CFCs, was gradually phased out, which required the propellants used in pMDIs to be replaced. Current pMDIs use hydrofluoroalkanes (HFAs) as propellants, such as 1,1,1,2-tetrafluoroethane (HFA-134a). Although these HFAs have no ozone-depleting potential, they have a high global warming potential (GWP), and consequently, their use is being phased down. One option for the discontinuation of HFA use in inhalers would be to discontinue all pMDIs, switching patients to dry powder inhalers (DPIs). However, a switch from pMDIs to DPIs may not be a clinically appropriate option for some patients; furthermore, the full lifecycle carbon footprint and the overall environmental impact of different inhalers should be considered. An alternative is therefore to reformulate the current HFA pMDIs to use low-GWP propellants, such as 1,1-difluoroethane (HFA-152a). This article summarizes the various steps and challenges associated with this change, illustrated using data from the inhaled triple combination of beclomethasone dipropionate, formoterol fumarate, and glycopyrronium bromide, a complex formulation of three molecules in a solution that contains liquid-phase propellant.
早期压力定量吸入器(pMDIs)中用作推进剂的氯氟烃(CFCs)具有很大的消耗臭氧层潜力。1987年《蒙特利尔议定书》签署后,包括CFCs在内的一系列消耗臭氧层物质的生产逐渐被淘汰,这就要求更换pMDIs中使用的推进剂。目前的pMDIs使用氢氟烷烃(HFAs)作为推进剂,如1,1,1,2-四氟乙烷(HFA-134a)。虽然这些HFAs没有消耗臭氧层的潜力,但它们具有很高的全球变暖潜能值(GWP),因此,它们的使用正在逐步减少。在吸入器中停止使用HFA的一个选择是停止所有pMDIs的使用,将患者转而使用干粉吸入器(DPIs)。然而,对于一些患者来说,从pMDIs转换为DPIs在临床上可能不是一个合适的选择;此外,还应考虑不同吸入器的全生命周期碳足迹和整体环境影响。因此,另一种选择是重新配制目前的HFA pMDIs,以使用低GWP的推进剂,如1,1-二氟乙烷(HFA-152a)。本文总结了与此变化相关的各个步骤和挑战,并以丙酸倍氯米松、富马酸福莫特罗和格隆溴铵的吸入三联复方制剂为例进行说明,这是一种在含有液相推进剂的溶液中包含三种分子的复杂制剂。