Mortimer O, Grettve L, Lindström B, Lönnerholm G, Zetterström O
Department of Clinical Pharmacology, University Hospital, Uppsala, Sweden.
Eur J Respir Dis. 1987 Nov;71(5):372-9.
The absolute bioavailability of prednisolone was assessed in ten asthmatic patients who responded poorly to ordinary doses of corticosteroids so-called "steroid-resistant" bronchial asthma. Plasma levels of prednisolone were measured by a high pressure liquid chromatographic method after oral (20 mg) and intravenous (18.6 mg) single-dose administration. Determination of the number of eosinophils in the blood was used as an estimate of the effect of the drug. The total plasma clearance, plasma half-life and volume of distribution determined from intravenous data were similar to those reported earlier for healthy volunteers and asthmatic patients. Orally administered prednisolone was rapidly absorbed and found to have complete bioavailability. There was a similar decrease in the number of eosinophils in the blood both after oral and after intravenous administration. Thus, the present study does not support the hypothesis that resistance of asthmatic symptoms to oral corticosteroids is due in some cases to poor absorption or rapid elimination of these drugs.
在10名对常规剂量皮质类固醇反应不佳(即所谓的“类固醇抵抗性”支气管哮喘)的哮喘患者中评估了泼尼松龙的绝对生物利用度。口服(20毫克)和静脉注射(18.6毫克)单剂量给药后,采用高压液相色谱法测量泼尼松龙的血浆水平。测定血液中嗜酸性粒细胞的数量作为药物疗效的评估指标。根据静脉给药数据确定的总血浆清除率、血浆半衰期和分布容积与先前报道的健康志愿者和哮喘患者相似。口服泼尼松龙吸收迅速,生物利用度完全。口服和静脉给药后血液中嗜酸性粒细胞数量均有类似减少。因此,本研究不支持以下假设:在某些情况下,哮喘症状对口服皮质类固醇的抵抗是由于这些药物吸收不良或消除过快所致。