Derendorf H, Hochhaus G, Meibohm B, Möllmann H, Barth J
University of Florida, Gainesville 32610, USA.
J Allergy Clin Immunol. 1998 Apr;101(4 Pt 2):S440-6. doi: 10.1016/s0091-6749(98)70156-3.
There are significant differences in the pharmacokinetic properties of inhaled corticosteroids currently used in medical practice. All are rapidly cleared from the body but they show varying levels of oral bioavailability and more importantly variation in the rate of absorption after inhalation. Oral bioavailability is lowest for fluticasone propionate, indicating a low potential for unwanted systemic corticosteroid effects. Mathematical modeling has shown pulmonary residence times to be longest for fluticasone propionate and triamcinolone acetonide but shortest for budesonide and flunisolide. These properties appear to relate to pulmonary solubility, which appears to be the rate-limiting step in the absorption process.
目前医学实践中使用的吸入性糖皮质激素的药代动力学特性存在显著差异。所有药物都能迅速从体内清除，但它们的口服生物利用度水平各不相同，更重要的是吸入后的吸收速率存在差异。丙酸氟替卡松的口服生物利用度最低，这表明其产生不良全身糖皮质激素效应的可能性较低。数学模型显示，丙酸氟替卡松和曲安奈德的肺部停留时间最长，而布地奈德和氟尼缩松的最短。这些特性似乎与肺部溶解度有关，而肺部溶解度似乎是吸收过程中的限速步骤。
