Derendorf H, Möllmann H, Rohdewald P, Rehder J, Schmidt E W
Clin Pharmacol Ther. 1985 May;37(5):502-7. doi: 10.1038/clpt.1985.79.
Methylprednisolone in the form of its hemisuccinate ester was injected intravenously in doses of 10 mg/kg and 63.1 mg. Plasma levels of methylprednisolone and of the ester were measured and their kinetics were calculated. Results indicate dose dependency in the kinetics of both. About 10% of the dose was excreted unchanged as hemisuccinate in the urine, indicating incomplete conversion of the prodrug. When methylprednisolone (80 mg) was also taken by mouth, the relative bioavailability of the tablets was 99%. Saliva levels of methylprednisolone were low but paralleled plasma levels in the postdistribution phase. No methylprednisolone hemisuccinate was found in saliva.
以半琥珀酸酯形式存在的甲泼尼龙以10mg/kg的剂量和63.1mg静脉注射。测定了甲泼尼龙及其酯的血浆水平并计算了它们的动力学。结果表明两者的动力学均存在剂量依赖性。约10%的剂量以半琥珀酸形式原形经尿液排泄，表明前体药物转化不完全。当口服甲泼尼龙（80mg）时，片剂的相对生物利用度为99%。甲泼尼龙的唾液水平较低，但在分布后阶段与血浆水平平行。唾液中未发现半琥珀酸甲泼尼龙。
