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抗心律失常新药关附甲素(Guan-fu base A,GFA)为一种 C_(20)-二萜类生物碱,1966年由我国首次从黄花乌头(Aconitum coreanum(Levl.)Raipaics)的块根中分离得到。GFA与三氟醋酐(TFAA)反应,迅速定量地生成关附甲素双-三氟乙酸酯(GFA-TFAA),其结构经 GC-MSD 分析得到证实。GC-ECD 法对 GFA 的检测线性范围宽(10—20000ng/ml,r=0.9984),血浆中平均回收率为97.52%。日间及日内差的变异系数分别为9%及7%以下。该法用于 GFA 的临床前药理研究。GFA 三种剂量静脉给药6小时内的家兔血药浓度范围是:0.338±0.014至13.459±5.392μg/ml(10mg/kg),0.133±0.038至2.546±0.480μg/ml(2mg/kg)以及45.25±10.34至535.86±24.36 ng/ml(0.4 mg/kg)。
The new anti-arrhythmic drug Guanfu base A (GFA) is a C_(20)-diterpenoid alkaloid, which was first obtained in China in 1966 from Aconitum coreanum (Levl. Raipaics). Roots were separated. GFA reacts with trifluoroacetic anhydride (TFAA) to rapidly generate quantitatively Guanbutemol bis-trifluoroacetate (GFA-TFAA), whose structure was confirmed by GC-MSD analysis. The GC-ECD method has a broad detection range for GFA (10–20000 ng/ml, r=0.9984) and an average plasma recovery of 97.52%. The coefficient of variation of intraday and intraday intraday differences was 9% and 7%, respectively. This method is used for preclinical pharmacology studies of GFA. The plasma concentration of rabbits within three hours of intravenous administration of GFA was within the range of 0.338±0.014 to 13.459±5.392 μg/ml (10 mg/kg) and 0.133±0.038 to 2.546±0.480 μg/ml (2 mg/kg). And 45.25±10.34 to 535.86±24.36 ng/ml (0.4 mg/kg).