Hayes M, Alam A F, Bruckner F E, Doherty S M, Myles A, English J, Marks V, Chakraborty J
Ann Rheum Dis. 1983 Apr;42(2):151-4. doi: 10.1136/ard.42.2.151.
Prednisolone concentration in plasma after a daily maintenance steroid dose was monitored in 83 patients with rheumatic diseases. Although no restrictions were imposed on the intake of food or drink, plasma drug levels tended to peak at 1 h after the ingestion of the standard tablets, whereas intestinal absorption of the enteric-coated preparation was found to be most unpredictable. A profound individual variation was observed in plasma prednisolone concentrations, and neither total nor unbound drug levels showed any consistent relationship with the size of the prednisolone dose or the control of the disease activity. The basal cortisol production was suppressed in one-third of the patients. There is no support from this study for the concept of an 'optimum therapeutic range' of plasma prednisolone for the treatment of rheumatic disease.
对83例风湿性疾病患者监测了每日维持剂量类固醇后的血浆泼尼松龙浓度。尽管对食物或饮料的摄入未作限制,但血浆药物水平往往在服用标准片剂后1小时达到峰值,而肠溶制剂的肠道吸收情况最不可预测。观察到血浆泼尼松龙浓度存在显著的个体差异,且总药物水平和游离药物水平均与泼尼松龙剂量大小或疾病活动控制无任何一致关系。三分之一的患者基础皮质醇分泌受到抑制。该研究不支持血浆泼尼松龙治疗风湿性疾病存在“最佳治疗范围”这一概念。