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    題名: The antinociceptive effect of buprenorphine and its long-acting ester buprenorphine benzoate in rats
    作者: (Yang C);(Lan KM);(Liu KS);陳郁文(Yu-Wen Chen);(Tzeng JI);(Ho ST);(Wang JJ)*
    貢獻者: 健康照護學院物理治療學系
    關鍵詞: 止痛藥,安息香酸鹽,Buprenorphine,酯,長效製劑;Analgesics,Benzoates,Buprenorphine,Esters,Long-acting preparations
    日期: 2004-09
    上傳時間: 2009-08-26 15:55:34 (UTC+8)
    摘要: "背景:當病人有長期的疼痛時,長效止痛劑是有需求的。為了延長一強效之止痛劑buprenorphine,我們合成了一個buprenorphine酯(buprenorphine benzoate)。本研究之目的在研究這個酯有無長效作用。方法:我們進行二項實驗,實驗一:我們測量buprenrophine HCl 0.05, 0.1及0.6 mol/kg之止痛效果。實驗二:我們測量buprenorphine benzoate 0.6 mol/kg之止痛效果。我們使用雄性Sprague-Dawley鼠(在同一藥物,同一劑量下,每組12隻鼠),並以紅外線熱源(plantar test)來偵測藥物之止痛效用。結果:大白鼠肌肉注射buprenorphine HCl 0.05, 0.1, 及0.6 mol/kg可產生3,4, 及4小時的止痛效果。大白鼠肌肉注射buprenorphine benzoate 0.6mol/kg可產生48小時的止痛效果。結論:在大白鼠以肌肉注射buprenorphine benzoate可產生一個非常長的止痛作用, 其效果為buprenorphine HCl的12倍。
    Background : A long-acting analgesic is particularly desirable in patients with long-lasting pain. In order to prolong the duration of action of a potent analgesic, buprenorphine, a buprenorphine ester (buprenorphine benzoate)was synthesized in our laboratory. The aim of the study was to evaluate whether the ester form could have along-lasting effect. Methods : Two studies were carried out. In study 1, we evaluated the antinociceptive effect of buprenorphine HCl at dosage of 0.05, 0.1, and 0.6 mol/kg. In study 2, we evaluated the antinociceptive effect of buprenorphine benzoate at dosage of 0.6 mol/kg. Male Sprague-Dawley rats (n = 12 in each group of different treatment) were used and the antinociceptive effects of the testing compounds were evaluated using the plantar test (a thermal test). Results : Intramuscular injection of buprenorphine HCl at dosage of 0.05, 0.1, and 0.6 mol/kg in rats produced dose-related antinociceptive effects with duration of action of 3, 4, and 4 h, respectively. Intramuscular injection of buprenorphine benzoate at 0.6 mol/kg produced a duration of action of 48 h. Conclusions : Intramuscular injection of buprenorphine benzoate in rats produced a longer duration of action, which is 12-fold longer than that of buprenorphine HCl.
    "
    關聯: 麻醉學雜誌 42(3 )135 ~139
    顯示於類別:[物理治療學系(停用)] 期刊論文

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