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苦杏仁甙药物动力学及其毒理初步研究

Pharmacokinetics and toxicity of amygdalin

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【作者】 李熙民; 陆婉琴; 秦芝玲; 金宝琴; 吴复跃;

【Author】 LI Xi-min, LU Wan-qin, QIN Zhi-ling (Shanghai Medical University, Shanghai 200032) JIN Bao-qin, WU Fu-yao (Shanghai Institute of Traditional Chinese Pharmacy, Shanghai 200010)

【机构】 上海医科大学; 上海中药研究所; 上海中药研究所 上海 200032; 上海 200032; 上海 200010; 上海 200010 上海医科大学肿瘤医院临床药理室;

【摘要】 本文应用GC-RIA(岛津)气相色谱仪,分析了8只健康家兔在接受苦杏仁甙(Ⅰ)后的血药浓度,绘制药-时曲线,求生物半减期((?)±SD),t1/(2α)(分布相)=38±4min,t1/(2β)(消除相)=77±18min。(Ⅰ)对正常小鼠毒性实验提示(Ⅰ)引起中毒的主要因素,除了与用药剂量大小有关外,与用药途径的关系更为重要。剂量相同条件下,非胃肠道给药(静注)较之胃肠道给药安全得多。1例食管癌病人用苦杏仁甙治疗,对用药后血、尿进行检测。

【Abstract】 Amygdalin (500mg/kg) was injected intravenously to 8 rabbits. The plasma concentration of the drug was measured by gas chromatography.From the concentration-time curve the phar-macokinetic parameters were calculated; t = 38 ± SD 4 min , and t, = 77 ± 18 min.Experiments on mice revealed that the cyanides toxicity was closely related to the dose and the route of administration.The same dose(500mg/kg)was given to mice. A comparison of the toxicity of drug given intravenously with that given orally in mice showed that the intravenous route of administration did indeed result in 100% survival without any toxicity, but oral route of administration were only 20% survival.The dosedecreased to 300 mg/kg, 40% survival.Amygdalin concentrations in blood and urine of a patient with esophageal carcinoma were also determined.Amygdalin was administered by intravenous infusion (6 g/3 h) then, the plasma and urine were measured by gas chromatography, respectively.Neither sample was responses, but when the amygdalinzyme was additional, respectively. Both sample were response. The amygdalin concentration was 0.0776 mg/kg in plasma and 3.4477 mg/kg in urine.

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