Szefler S J, Ebling W F, Georgitis J W, Jusko W J
Eur J Clin Pharmacol. 1986;30(3):323-9. doi: 10.1007/BF00541537.
The disposition and plasma binding of methylprednisolone were examined in seven normal volunteers following the administration of 5, 20 and 40 mg of intravenous methylprednisolone sodium succinate. Methylprednisolone exhibits linear plasma protein binding averaging 77%. The mean plasma methylprednisolone clearance of 337 ml X h-1 X kg-1 was independent of dose. The steroid appears to moderately distribute into tissue spaces with a mean volume of distribution of 1.41 X kg-1. Methylprednisolone disposition parameters were compared with the non-transcortin bound parameters for prednisolone. The prednisolone plasma clearance based on the transcortin free-drug is similar to methylprednisolone total plasma clearance. However, the corrected volume of distribution of prednisolone is only one-half that of methylprednisolone. The disposition rate of these two steroids is thus similar, in spite of their metabolic control by different enzymatic pathways and major influence of saturable transcortin binding on prednisolone elimination.
在7名正常志愿者静脉注射5毫克、20毫克和40毫克琥珀酸甲泼尼龙后，对甲泼尼龙的处置和血浆结合情况进行了研究。甲泼尼龙表现出平均77%的线性血浆蛋白结合率。甲泼尼龙的平均血浆清除率为337毫升×小时-1×千克-1，与剂量无关。该类固醇似乎适度分布于组织间隙，平均分布容积为1.41×千克-1。将甲泼尼龙的处置参数与泼尼松龙的非皮质素结合参数进行了比较。基于游离皮质素的泼尼松龙血浆清除率与甲泼尼龙的总血浆清除率相似。然而，泼尼松龙校正后的分布容积仅为甲泼尼龙的一半。因此，尽管这两种类固醇通过不同的酶途径进行代谢控制，且可饱和的皮质素结合对泼尼松龙消除有主要影响，但它们的处置速率相似。
