Taipei Medical University Institutional Repository:Item 987654321/6233
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    Title: Baclofen立體異構物於血液之液相色層分析研究
    Baclofen立體異構物於血液之液相色層分析研究
    Authors: 陳玉盆
    CHEN, YU-PEN
    Contributors: 藥學研究所
    Keywords: 骨骼肌鬆弛劑
    高效液相色層分析
    立體異構物
    多發性硬化症
    BACLOFEN
    GABA
    MULTIPLE-SCLEROSIS
    Date: 1987
    Issue Date: 2009-09-11 16:48:30 (UTC+8)
    Abstract: Baclofen是一種骨骼肌鬆弛劑,為GABA之衍生物,其作用機轉是促進內生之GABA緩慢
    釋出,並可抑制與奮性胺基酸傳導物質之釋放,主要作用於降低單胞突接合及多胞接
    合活化之反射以及中樞神經之抑制,臨床用於多發性硬化症(Multiple sclerosis)
    或脊髓受傷所引起肌肉痙攣、疼痛及冗肉僵化之舒解,據文獻報導,本品具有舒解痙
    攣作用之成分為R(-)-Baclofen,可見Baclofen具有藥理作用立體特異性存在,而
    臨床應用則以Racemic Baclofen投與。
    本實驗之目的是希望以高效液相層析法探討Baclofen光學異構物於體液分離方法,藉
    此研究該藥於體內動態上是否顯示立體特異現象;所採用之分離步驟:Baclofen is-
    omers與Chiral reagent作用,形成Diasteroisomers後,以傳統的逆相L.C.管柱加以
    分離。?D-gluco-pyranosyl isothiocyanate(GITC)與Baclofen之衍生物:以C 
    (3μm )之管柱分離,移動相為甲醇:磷酸鹽緩衝溶液(PH=2.8)(50:
    50),於紫外光檢測器波長為254nm下檢測,此方法純物之分離度良好(α val
    ue=1.08)但是由於血液檢體以此方法測試靈敏度不佳,故選用敏感度較佳,具
    有螢光之chiral reagent. ?(+)-1-(9-Fluorenyl)Baclofen 之血漿檢體
    經過陽離子交換樹脂(Dowex-50W-X4 )處理後,與(+)-FLEC反應,以逆相
    之固態萃取純化之,使用C (3μm )之管柱分離,移動相為氰甲烷:醋酸鹽緩
    衝溶液(PH=5.0)(47:53),vio 螢光檢測器,激發波長為260nm
    ,發散波長為315nm下檢測,經實驗結果以此方法可得良好之分離度(α Value=
    1.09),線性關係及再現性,測試之最小限量為(40ng/ml),應用本定量研
    究方法以動物投藥實驗,結果顯示此方法具有實用性。
    CH2NH2
    Structure of Baclofen:C1 C-H
    CH2COOH
    Data Type: thesis
    Appears in Collections:[School of Pharmacy] Dissertation/Thesis

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