中文摘要 Methylprednisolone是一種合成的醣皮質類固醇，具有很強的抗發炎活性。口服後，可由腸胃道快速吸收，在肝臟代謝，經由腎臟排除。本實驗為比較兩種不同處方的Methylprednisolone錠劑，Medrol® (Upjohn)及Menisone®(培力)，在12位健康的志願受試者之生體可用率。 本實驗分析採高效液相層析法分析血漿檢品。以LiChroCART RP-18管柱及氰甲烷、醋酸水溶液(氰甲烷：醋酸水溶液=39：61(v/v))為移動相，在244nm的紫外光偵測波長下，以1ml/min的流速下進行分析。以Triamcinolone作為內部標準品。 健康受試者口服給藥20mg (5×4mg/tablet)後，大約1.67小時可達最高血中濃度0.144μg/ml；平均曲線下面積(AUC0-∞)約為0.582±0.096 μg·hr/ ml而排除半衰期則約為2.709±0.553 hrs。 本實驗結果以統計學方法two-way ANOVA比較此兩種不同處方產品的動力學參數，包括了Cmax、Tmax、AUC0-12及AUC0-∞。計算結果發現並無統計學上顯著的差異。因此可認為Medrol® tablets及Menisone®tablet(培力)此兩種不同產品是具有生體相等性的; Abstract Methylprednisolone is a memberane of synthetic glucocorticosteroid. It is well absorbed from the gastrointestinal tract; metabolism is primarily in the liver and excretion is via the kidney. In this study, two commercial methylprednisolone tablets, Medrol® and Menisone®, were compared in twelve normal, healthy Taiwanese male volunteers participated in a single-dose, two-period, two-sequence, two-treatment crossover study. Methylprednisolone plasma concentrations were analyzed with a validated high performance liquid chromatographic method. It was performed on a RP-18e column using a mobile phase of 61% water (pH4.28, by glacial acetic acid), 39% acetonitrile with ultraviolet dection (244nm). This method uses triamcinolone as the internal standard for the determination. After oral administration of Methylprednisolone 5×4 mg/tablet in the healthyl volunteers, the peak serum concetration of 0.144 μg/ml were achieved about 1.67hrs, the mean area under the serum concetration-time curve (AUC0-∞) was 0.582±0.096 μg·hr/ml, the mean terminatial half-life was 2.709±0.553 hrs。 There are no significant statistic different between pharmacokinetic parameter (p>0.05) of the two different products, including the peak serum concentration (Cmax), time to peak level (Tmax) and area under the curve (AUC). Base on the result obtained in this study, bioequivalence between these two different products was demonstrated.
