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

Ahmad Kantar
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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, in vivo 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.

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氟尼索内酯与用于雾化的吸入皮质类固醇的不同之处在于:水溶解度的作用。
儿童和成人支气管哮喘和喘息的循证管理建议使用吸入皮质类固醇(ICSs)。在使用一些用于ICS输送的吸入装置,例如加压计量吸入器和干粉吸入器,在幼儿和老年人中很常见,因此,它们被雾化器取代。我们回顾了比较研究,这些研究评估了福尼索利与目前市场上可用的其他ICSs,包括二丙酸倍氯米松、丙酸氟替卡松和布地奈德。此外,我们评估了这些ICSs的物理化学性质,以确定药物在肺部的命运。数据表明,任何类型的气动雾化器(传统的、开放呼吸的或呼吸增强的)在可吸入颗粒中的氟虫腈输出优于其他ics的输出。这主要是由于氟isolide具有较高的水溶性。此外,体内模拟研究表明,与氟尼索内相比,丙酸氟替卡松和二丙酸倍氯米松混悬液在哮喘儿童中吸入剂量的受试者间变异性要大得多。氟尼索内酯的理化性质和药动学特征有利于其雾化应用。
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来源期刊
Multidisciplinary Respiratory Medicine
Multidisciplinary Respiratory Medicine Medicine-Pulmonary and Respiratory Medicine
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0.00%
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期刊介绍: Multidisciplinary Respiratory Medicine is the official journal of the Italian Respiratory Society - Società Italiana di Pneumologia (IRS/SIP). The journal publishes on all aspects of respiratory medicine and related fields, with a particular focus on interdisciplinary and translational research. The interdisciplinary nature of the journal provides a unique opportunity for researchers, clinicians and healthcare professionals across specialties to collaborate and exchange information. The journal provides a high visibility platform for the publication and dissemination of top quality original scientific articles, reviews and important position papers documenting clinical and experimental advances.
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