Bioavailability of prednisolone in asthmatic patients with a poor response to steroid treatment.

O Mortimer, L Grettve, B Lindström, G Lönnerholm, O Zetterström
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Abstract

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.

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强的松龙在对类固醇治疗反应不佳的哮喘患者中的生物利用度。
强的松龙的绝对生物利用度在10例哮喘患者中进行了评估,这些患者对普通剂量的皮质类固醇反应不佳,即所谓的“类固醇抵抗性”支气管哮喘。采用高压液相色谱法测定口服(20 mg)和静脉注射(18.6 mg)单剂量泼尼松龙的血浆水平。测定血液中嗜酸性粒细胞的数量是用来估计药物的效果。从静脉注射数据确定的总血浆清除率、血浆半衰期和分布量与先前报道的健康志愿者和哮喘患者相似。口服强的松龙吸收迅速,具有完全的生物利用度。口服和静脉给药后,血液中嗜酸性粒细胞的数量都有类似的减少。因此,本研究不支持哮喘症状对口服皮质类固醇的抵抗在某些情况下是由于这些药物吸收不良或迅速消除的假设。
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