Objective The influence of different alcohol extraction on the content of total alkaloid and acute toxicity of Rhizoma Pinelliae caused by different extracted crafts was compared, in order to provide a basis for safe and reasonable medication in clinic. Methods Using different alcohol extracted crafts to prepare the samples. UV method was used to determine the content of total alkaloid at 416nm wavelength. The classical acute toxicity methods were used in this study. The MTD value of acid-water extracted group and acid-alcohol extracted group were calculated by mg/kg basis; and the LD50 value of acid-water filtered group and acid-alcohol filtered group were tested by bliss method. Administration and observation the mice for 14 days, and the change of mice weight, the acute toxical symptoms, signs, death time and accumulated death rate were recorded. Results The content of total alkaloid is: acid-alcohol filtered group＞acid-alcohol extracted group＞acid-water filtered group＞acid-water extracted group.The MTD value of acid-water extracted group and acid-alcohol extracted group is 29.6 g·kg-1·d-1 and 27.2 g·kg-1·d-1 respectively,which are equal to 230.2 and 211.6 times of daily dosage in clinic;the LD50 value of acid-water filtered group and acid-alcohol filtered group is 14.15 g·kg-1·d-1 and 14.27 g·kg-1·d-1 respectively, 95％ confidence interval is respectively 12.981～15.563g·kg-1·d-1 and 13.167～15.204 g·kg-1·d-1 which are equal to 110.0 and 111.0 times of daily dosage in clinic. According to the observation of acute toxity tests, respiratory depression, hyperspasmia, diarrhea, dysphoria,vomit and tears running are the main acute toxical symptoms of different alcohol extractions. Conclusion Total alkaloid is one of toxic substances of Rhizoma Pinelliae which has obvious toxity. The temperature has great impact on the content of total alkaloid.which shows that some toxic ingredients could be destroyed by temperature easfiy.%目的 比较进行不同酸处理方式对半夏总生物碱含量的影响及急性毒性观察与评价,为临床用药的安全性提供依据.方法 分别用不同酸处理方式制备半夏不同样品,采用紫外分光光度法,取各供试品溶液与空白对照液,在波长416nm处测定吸光度,计算总生物碱含量,按照经典小鼠急毒试验方法,用bliss法计算半数致死量(LD50),公斤体重法计算最大耐受量(MTD),考察半夏酸水提取,酸醇提取(MTD)值、酸水渗漉、酸醇渗漉提取(LD50)值,连续给药观察14天,记录各组动物体重变化,毒性症状谱及死亡情况.结果 半夏不同酸处理提取(酸水提取、酸醇提取、酸水渗漉、酸醇渗漉)中总生物碱含量为酸醇渗漉液>酸醇提取液>酸水渗漉液>酸水提取液.急毒研究结果显示,半夏酸水提取MTD可达29.6 g·kg-1·d-1,相当于临床人用量的230.2倍;半夏酸醇提取MTD可达27.2g·kg-1·d-1,相当于临床人用量的211.6倍;半夏酸水渗漉提取LD50值为14.15 g·kg-1·d-1,95%的可信限为12.981～15.563 g·kg-1·d-1,相当于临床人用量的110.0倍.半夏酸醇渗漉提取LD50值为14.27g·kg-1·d-1,95%的可信限为13.167～15.204g·kg-1·d-1,相当于临床人用量的111.0倍.通过小鼠急毒实验观察:呼吸抑制、抽搐、腹泻、烦躁,呕吐和流泪是半夏不同酸处理提取样品主要的急性毒性症状,小鼠死亡多发生于4小时之内.结论 半夏总生物碱部位有明显毒性,是半夏产生毒性作用的物质基础之一,同时温度对半夏总生物碱富集物毒性影响较大,说明半夏产生毒性作用的部位中某些成分加热易被破坏.
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