产业化生产中草乌不同炮制品的“减毒-存效”研究

研究产业化生产中草乌不同炮制品的毒性和药效的相关性,确定"减毒-存效"的最佳炮制方法。采用HPLC测定草乌及其不同炮制品中6种乌头碱类生物碱的含量;采用Bliss法分别测定草乌及其不同炮制品对小鼠半数致死量(LD50)或最大给药剂量;以二甲苯致耳肿胀法和醋酸扭体法试验考察不同炮制品的抗炎、镇痛作用。结果显示:①草乌生品中3种双酯型生物碱总量为0.358 8%;药典水煮法炮制品中3种双酯型生物碱总量为0.002 2%,3种单酯型生物碱总量为0.036 2%;常压蒸制法炮制品中3种双酯型生物碱总量为0.006 0%,3种单酯型生物碱总量为0.056 7%;②生草乌的LD50为5.4 g·kg^-1,药典水煮法和常压蒸制法炮制品的最大给药剂量为133.34 g·kg^-1;病理观察显示,与正常组比较,2种炮制品对于小鼠的心、肝、肾均有一定的损伤;③药典水煮法和常压蒸制法炮制品均具有抗炎、镇痛作用(P<0.01或P<0.05),其抗炎镇痛作用强弱为:常压蒸制法>药典水煮法。上述结果提示:生草乌毒性较大,采用常压蒸制法炮制后毒性明显降低,同时又保留了良好的的抗炎和镇痛作用;与药典水煮法相比,常压蒸制法具有工艺可操作性强、饮片质量稳定、抗炎镇痛作用更强等优势,适用于产业化生产。

"Attenuation-preservation effects" of different processed products of Aconiti Kusnezoffii Radix in industrialized production

To study the correlation between toxicity and efficacy of different processed Aconiti Kusnezoffii Radix productsin industrial production, in order to define the optimal processing method for "attenuation-preservation effects". The HPLC method was used to determine the content of six aconitine alkaloids in Aconiti Kusnezoffii Radix and its different processed products. The Bliss method was used to determine the half-lethal dose(LD50) or the maximum dose of Aconiti Kusnezoffii Radix and its different processed products in mice. The toluene-induced ear swelling method and the acetic acid twist method were used to investigate the anti-inflammatory and analgesic effects of different processed products. The results showed that: ① the total amount of diester alkaloids incrude Aconiti Kusnezoffii Radix was 0.358 8%;the total amount of diester alkaloids in Aconiti Kusnezoffii Radix prepared by pharmacopoeia-based boiling method was 0.002 2%, and the total amount of monoester alkaloids was 0.036 2%;the total amount of diester alkaloids in Aconiti Kusnezoffii Radix produced by atmospheric steaming method was 0.006 0%, and the total amount of monoester alkaloids was 0.056 7%;② the LD50 of Aconiti Kusnezoffii Radix was 5.4 g·kg^-1,and the maximum dose of processed products by two methods were 133.34 g·kg^-1;pathological observation showed that compared with the normal group, the two kinds of processed products of Aconiti Kusnezoffii Radix had certain damage to the heart, liver and kidney;③products processed by pharmacopoeia-based boiling method and atmospheric steaming method had anti-inflammatory and analgesic effects(P<0.01 or P<0.05). The anti-inflammatory and analgesic effects were as follows: the atmospheric steaming method was superior to the pharmacopoeia-based boiling method. The above results suggest that the crude Aconiti Kusnezoffii Radixis more toxic. The atmospheric steaming method can significantly reduce the toxicity, while retaining its good anti-inflammatory and analgesic effects, which is significantly better than the pharmacopoeia-based boiling method. The atmospheric steaming process is simple and easy to operate, and suitable for industrial production.