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研究生:張佳惠
論文名稱:甲基培尼皮質醇錠劑之生體可用率研究
論文名稱(外文):Bioavailability studies of methylprednisolone tables
指導教授:劉正雄劉正雄引用關係
學位類別:碩士
校院名稱:中國醫藥學院
系所名稱:藥物化學研究所
學門:醫藥衛生學門
學類:藥學學類
論文種類:學術論文
論文出版年:2002
畢業學年度:90
語文別:中文
論文頁數:103
中文關鍵詞:生體可用率甲基培尼皮質醇錠劑之生體可用率研究
外文關鍵詞:methylprednisolonebioavailbility
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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.

目 錄
英文摘要…………………………………………..……………….. I
中文摘要…………………………………..………………………. II
內文目錄
第一章 緒 言 …………………………………………………... 1
第二章 總 論 …………………………………………………... 3
第一節 生體可用率研究介紹 …………………………… 3
第二節 在BA/BE生體可用率常用的定量法 …………… 5
第三節 Methylprednisolone簡介 ………………………… 8
第四節 Methylprednisolone理化特性 …………………… 9
第五節 Methylprednisolone藥理與臨床作用 …………… 11
第六節 Methylprednisolone藥物動力學研究 …………… 18
第七節 Methylprednisolone定量方法 …………………… 25
第八節 研究動機及目的 ………………………………... 27
第三章 實驗材料與方法 ………………..……………………… 28
第一節 實驗材料 ………………………………………….. 28
第二節 實驗方法 ………………………………………….. 32
第四章 結果與討論 ………………………………….………. 39
第五章 結 論 ……………………………..………………….. 46
附 表 ……………………………………………………………… 47
附 圖 ……………………………………………………………… 68
參考文獻…………………………………………………………… 92
附 錄…………………………………..……………………… 102

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