Gambertoglio J G, Frey F J, Holford N H, Birnbaum J L, Lizak P S, Vincenti F, Feduska N J, Salvatierra O, Amend W J
Kidney Int. 1982 Apr;21(4):621-6. doi: 10.1038/ki.1982.69.
Prednisone and prednisolone are drugs with the potential for therapeutic inequivalence due to bioavailability problems. The objective of our study was to compare the systemic bioavailability of prednisolone from oral prednisone and prednisolone. Nine kidney transplant patients receiving prednisone (12.5 to 22.5 mg per day) were administered, in a randomized fashion, the same dose of oral prednisone (Deltasone), oral prednisolone (Delta-cortef) and intravenous prednisolone (Hydeltrasol). Prednisolone and prednisone levels were measured using a specific high-pressure liquid chromatographic assay. Since prednisolone exhibits dose-dependent pharmacokinetics because of nonlinear plasma protein binding, bioavailability from oral prednisone and oral prednisolone, compared to the intravenous dose, was 84.5 +/- 17.8% and 95.5 +/- 17.6% using unbound drug concentrations. These differences were not statistically significant. Furthermore, no significant differences were observed between the two oral formulations in peak prednisolone levels, time of peak levels or half-life using either total or unbound drug concentrations. The results from our study indicate that both of the oral preparations tested provide similar bioavailability of active prednisolone and the conversion of prednisone to prednisolone occurs rapidly.
由于生物利用度问题，泼尼松和泼尼松龙属于具有治疗等效性潜在差异的药物。我们研究的目的是比较口服泼尼松和泼尼松龙后泼尼松龙的全身生物利用度。9名接受泼尼松（每日12.5至22.5毫克）治疗的肾移植患者，以随机方式分别给予相同剂量的口服泼尼松（去氢可的松）、口服泼尼松龙（氢化可的松）和静脉注射泼尼松龙（氢羟皮质素）。使用特定的高压液相色谱分析法测定泼尼松龙和泼尼松的水平。由于泼尼松龙因血浆蛋白结合呈非线性而表现出剂量依赖性药代动力学，与静脉注射剂量相比，使用游离药物浓度时，口服泼尼松和口服泼尼松龙的生物利用度分别为84.5±17.8%和95.5±17.6%。这些差异无统计学意义。此外，无论是使用总药物浓度还是游离药物浓度，两种口服制剂在泼尼松龙峰值水平、峰值时间或半衰期方面均未观察到显著差异。我们的研究结果表明，所测试的两种口服制剂均能提供相似的活性泼尼松龙生物利用度，且泼尼松向泼尼松龙的转化迅速发生。
