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在用于雾化的吸入性糖皮质激素中,氟尼缩松的独特之处何在:深入探讨水溶性的作用。

What makes flunisolide different among inhaled corticosteroids used for nebulization: a close look at the role of aqueous solubility.

作者信息

Kantar Ahmad

机构信息

Pediatric Asthma and Cough Center, Istituti Ospedalieri Bergamaschi, Bergamo, Italy.

出版信息

Multidiscip Respir Med. 2021 Jan 15;16(1):719. doi: 10.4081/mrm.2021.719.

Abstract

Evidence-based management of bronchial asthma and wheezing in children and adults recommends the employment of inhaled corticosteroids (ICSs). Difficulty in using some inhalation devices for ICS delivery, such as pressurized metered-dose and dry-powder inhalers, is common among young children and in the elderly, and for that reason, they are replaced with nebulizers. We reviewed comparative studies that evaluated funisolide with other ICSs currently available on the market, including beclomethasone dipropionate, fluticasone propionate, and budesonide. Moreover, we assessed the physicochemical properties of these ICSs in determining drug fate in the lung. Data indicate that the flunisolide output in respirable particles by any type of pneumatic nebulizer (traditional, open breath or breathenhanced) is superior to the output of other ICSs. This is principally attributed to the higher water solubility of flunisolide. Furthermore, simulation studies demonstrate that the intersubject variability of the inhaled dose among asthmatic children was much greater for suspensions of fluticasone propionate and beclomethasone dipropionate than for those of flunisolide. The physicochemical properties and pharmacokinetic profile of flunisolide favor its employment in nebulization.

摘要

儿童和成人支气管哮喘与喘息的循证管理推荐使用吸入性糖皮质激素(ICS)。一些用于递送ICS的吸入装置,如压力定量吸入器和干粉吸入器,在幼儿和老年人中使用困难,因此,它们被雾化器所取代。我们回顾了评估氟尼缩松与目前市场上其他ICS(包括二丙酸倍氯米松、丙酸氟替卡松和布地奈德)的比较研究。此外,我们评估了这些ICS在确定肺部药物转归方面的理化性质。数据表明,任何类型的气动雾化器(传统型、开放式呼吸或呼吸增强型)产生的可吸入颗粒中的氟尼缩松输出量均优于其他ICS。这主要归因于氟尼缩松较高的水溶性。此外,模拟研究表明,丙酸氟替卡松和二丙酸倍氯米松悬浮液在哮喘儿童中的吸入剂量个体间变异性比氟尼缩松悬浮液大得多。氟尼缩松的理化性质和药代动力学特征有利于其用于雾化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/314c/7816085/fff5058e1279/mrm-16-1-719-g001.jpg

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