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題名 | A Novel Long-acting Analgesic: Buprenorphine Palmitate in Rats=一個新的長效止痛劑:Buprenorphine Palmitate在大白鼠之測試 |
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作者 | 郭珍妮; 林立青; 劉巡宇; 褚錦承; 劉國盛; 何善台; 王志中; | 書刊名 | 麻醉學雜誌 |
卷期 | 43:1 民94.03 |
頁次 | 頁11-16 |
分類號 | 416.5 |
關鍵詞 | 止痛劑; 酯; 長效製藥; 疼痛; Analgesics; Buprenorphine; Esters; Long-acting preparations; Pain; |
語文 | 英文(English) |
中文摘要 | 背景:當病人有長期的疼痛時,長效止痛劑是有需求的。為了長效止痛的目的,我們合成了一個新的buprenorphine酯類,buprenorphine棕櫚酸酯,本研究的目的在研究這個酯有無長效作用。方法:我們以plantar test在數種劑量下以大白鼠來偵測傳統止痛劑buprenorphine HCl及新化合物buprenorphine棕櫚酸酯之止痛作用。結果:我們發現在大白鼠肌肉注射buprenorphine HCl 0.05,0.1及1µmol/kg可產生和劑量相關之2,3及4小時之止痛療效。而在大白鼠肌肉注射buprenorphine棕櫚酸酯可產生和劑量相關之72,76及78小時之止痛效果。在相同的給藥劑量(同莫耳數,1µmol/kg)下,buprenorphine HCl及buprenorphine棕櫚酸酯之止痛效期為4及72小時。結論:在大白鼠肌肉注射buprenorphine棕櫚酸酯產生了一個長效的止痛作用,其效期是buprenorphine HCl的18倍。 |
英文摘要 | Background: A long-acting analgesic may be particularly desirable in patients with long-lasting pain. In order to provide a long-acting analgesic effect, a novel buprenorphine ester, buprenorphine palmitate, was synthesized in our laboratory. The aim of the study was to evaluate whether the ester had a long-lasting effect. Methods: The antinociceptive effects (dose-range studies) of buprenorphine HCl and buprenorphine palmitate were evaluated using the plantar test in Sprague-Dawley rats. Results: We found that intramuscular injection of buprenorphine HCl 0.05, 0.1 and 1 μmol/kg in rats produced dose-related antinociceptive effects of 2, 3, and 4h, respectively. Intramuscular injection of buprenorphine palmitate 1, 5, and 10μmol/kg also produced dose-related antinociceptive effects of 72, 76 and 78 h, respectively. On an equimolar basis of 1μmol/kg, the durations of action of intramuscular buprenorphine HCl and buprenorphine palmitate were 4 and 72 h, respectively. Conclusions: Intramuscular injection of buprenorphine palmitate in rats produced a long-lasting antinociceptive effect which was much longer (18-fold) than did intramuscular buprenorphine HCl. |
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