O'Connell Edward J
Department of Pediatrics, Allergy/Immunology, Mayo Clinic, Rochester, Minnesota 55905, USA.
Clin Ther. 2003;25 Suppl C:C42-60. doi: 10.1016/s0149-2918(03)80305-3.
The aim of inhaled corticosteroid (ICS) therapy for asthma is to attain high therapeutic activity in the airways while keeping the risk of systemic adverse effects relatively low. However, the physicochemical and pharmacokinetic properties of various ICSs affect this ratio, thereby influencing their ability to fulfill the requirements of an ideal agent.
This article reviews the physical and pharmacokinetic properties of budesonide, outlining how they, safety data, and use of different inhalation devices enable budesonide to meet many of the clinical requirements of an ideal ICS for the treatment of asthma.
ICS efficacy is influenced by lipophilicity, lung deposition, and retention in airway tissue, whereas the rate of elimination determines systemic activity. Budesonide is retained in the airways to a greater extent than other ICSs because of an esterification process that increases its lipophilicity. The prolonged retention of budesonide in the airways may contribute to its efficacy when administered QD. In addition to a pressurized metered-dose inhaler, budesonide is available as a dry-powder inhaler and in nebulized form, which can be used by asthma patients aged > or =6 months.
When combined with delivery devices suitable for a spectrum of patient groups, the physical and pharmacokinetic properties of budesonide lend it many of the characteristics of an ideal ICS, including favorable efficacy and tolerability profiles.
吸入性糖皮质激素（ICS）治疗哮喘的目的是在气道中获得高治疗活性，同时将全身不良反应的风险保持在相对较低水平。然而，各种ICS的物理化学和药代动力学特性会影响这一比例，从而影响它们满足理想药物要求的能力。
本文综述布地奈德的物理和药代动力学特性，概述这些特性、安全性数据以及不同吸入装置的使用如何使布地奈德满足治疗哮喘的理想ICS的许多临床要求。
ICS的疗效受亲脂性、肺部沉积和在气道组织中的滞留影响，而消除速率决定全身活性。由于酯化过程增加了其亲脂性，布地奈德在气道中的滞留程度比其他ICS更大。布地奈德在气道中的长时间滞留可能有助于其每日一次给药时的疗效。除了压力定量吸入器外，布地奈德还有干粉吸入器和雾化剂型，≥6个月的哮喘患者均可使用。
当与适用于一系列患者群体的给药装置相结合时，布地奈德的物理和药代动力学特性使其具有理想ICS的许多特征，包括良好的疗效和耐受性。
