【摘要】 目的 优化短柄乌头砂炒工艺，并考察其急性毒性、抗心律失常活性。方法 以炒制温度、炒制时间、药砂比为影响因素，双酯型生物碱（乌头碱、滇乌碱）、单酯型生物碱（苯甲酰乌头原碱、 16-epi-pyroaconitine、 8-去乙酰滇乌碱和pyroyunaconitine）总含量的综合评分为评价指标，Box-Behnken响应面法优化砂炒工艺。采用急性毒性实验，计算生品、砂炒品LD50。建立大鼠心律失常模型，测定室性早搏潜伏期、室性心动过速发生率。结果 最优条件为炒制温度210℃，炒制时间15 min，药砂比1∶15，综合评分为93.932分。生品、砂炒品LD50分别为0.076、0.799 g/kg。与模型组比较，不同剂量（5、 8、 12、 16 mg/kg）砂炒品组室性早搏潜伏期延长（P<0.05）；与5 mg/kg剂量组比较，12～16 mg/kg剂量组室性心动过速发生率降低（P<0.05）。结论 砂炒后短柄乌头急性毒性降低，并且在高剂量下表现出较强的抗心律失常活性。更多还原

【Abstract】 AIM To optimize the stir-frying with sand process forAconitum brachypodumDiels., and to investigate its acute toxicity, anti-arrhythmic activity.METHODS With frying temperature, frying time and drug-sand ratio as influencing factors, comprehensive score for total contents of diester alkaloids( aconitine,yunaconitine) and monoester alkaloids( benzoylaconitine, 16-epi-pyroaconitine, 8-deacetylyunaconitine,pyroyunaconitine) as evaluation indices, the stir-frying with sand process was optimized by Box-Behnken response surface method. Acute toxicity test was adopted in the calculation of LD50of raw product and stir-frying with sandprocessed product. The model for rat arrhythmia was established, after which ventricular premature beat latency and incidence of ventricular tachycardia were determined.RESULTS The optimal conditions were determined to be210 ℃ for frying temperature, 15 min for frying time was, and 1 ∶ 15 for drug-sand ratio, the comprehensive score was 93. 932. The LD50of raw product, stir-frying with sand-processed product were 0. 076, 0. 799 g/kg,respectively. Compared with the model group, different doses(5, 8, 12, 16 mg/kg) of stir-frying with sandprocessed product groups demonstrated prolonged ventricular premature beat latencies(P<0. 05). Compared with the 5 mg/kg dose group, the 12-16 mg/kg dose group displayed decreased incidence of ventricular tachycardia(P<0. 05).CONCLUSION Reduced acute toxicity ofA. brachypodumis observable after stir-frying with sand,which exhibits strong anti-arrhythmic activity at high dose.更多还原