[健康志愿者中泼尼松和泼尼松龙的药代动力学参数]

[Pharmacokinetic parameters of prednisone and prednisolone in healthy volunteers].

作者信息

Etienne S D, Vandermeersch V, Chosidow O, Vu-Thi-My-Le C, Godeau P, Diquet B, Herson S

机构信息

Service de Médecine Interne de la Pitié, Groupe Hospitalier Pitié-Salpêtrière, Paris.

出版信息

Ann Med Interne (Paris). 1990;141(6):507-11.

PMID:2285202

Abstract

A cross-over, double-blind, randomized trial with 8 healthy volunteers was undertaken to compare prednisolone and prednisone pharmacokinetics after a single oral dose (1 mg/kg) of prednisone (Cortancyl) and prednisolone sodium metasulfobenzoate (Solupred). Maximum prednisolone concentrations measured after ingestion of prednisone are higher (535 +/- 32 ng/ml) and occur earlier than after taking prednisolone sodium metasulfobenzoate (198 +/- 114 ng/ml) (p less than 0.001). The areas under the curve are significantly larger after prednisone than after prednisolone sodium metasulfobenzoate (p less than 0.02). These findings suggest a decreased systemic availability of prednisolone after prednisolone sodium metasulfobenzoate (Solupred) administration and show, from a strictly pharmacokinetic point of view, that equimolar doses of prednisone and prednisolone sodium metasulfobenzoate are not equivalent therapies.

摘要

一项针对8名健康志愿者的交叉、双盲、随机试验开展，以比较单次口服剂量（1 mg/kg）泼尼松（Cortancyl）和甲磺苯甲酸钠泼尼松龙（Solupred）后泼尼松和泼尼松龙的药代动力学。摄入泼尼松后测得的最大泼尼松龙浓度更高（535±32 ng/ml），且比服用甲磺苯甲酸钠泼尼松龙后出现得更早（198±114 ng/ml）（p<0.001）。泼尼松后的曲线下面积显著大于甲磺苯甲酸钠泼尼松龙后的曲线下面积（p<0.02）。这些发现表明，服用甲磺苯甲酸钠泼尼松龙（Solupred）后泼尼松龙的全身可用性降低，并且从严格的药代动力学角度来看，等摩尔剂量的泼尼松和甲磺苯甲酸钠泼尼松龙并非等效疗法。