目的 优选芎汤加味方的处方工艺，通过药效学试验和急性毒性试验进行药效剂量筛选和初步安全性评价。方法 采用正交试验法对挥发油、核桃油提取工艺与非挥发性成分的乙醇回流提取工艺条件进行筛选，单因素试验法对提挥发油后水提液醇沉试验的乙醇浓度考察；采用大鼠局灶脑缺血模型筛选提取方法改良后药物的剂量，并采用小鼠急性毒性试验法对药物安全性进行初步考察。结果 芎汤加味方最佳提取工艺为：川芎、当归粉碎过10目筛，加10倍量水浸泡4 h，水蒸气蒸馏提取6 h，滤液浓缩备用，药渣保留；将150 ℃条件下加热1.5 h灭酶后的核桃仁粉碎至粗粉，加入4倍量石油醚，浸泡提取4次，每次40 min，药渣保留；对川芎、当归提油后药渣合并核桃仁药渣用10倍量70 %乙醇提取3次，每次1 h。药物对大鼠局灶性脑缺血的有效剂量为3.78 g·kg-1，折算成临床70 kg的成人每日用量为42 g。小鼠最大给药量（MLD）为120.96 g·kg-1，相当于临床70 kg的成人每公斤体质量日用量的201.6倍。结论 该优选提取工艺稳定可行，适用于芎汤加味方的提取。芎汤加味方对局灶脑缺血有保护作用，且安全、低毒。

Objective To optimize the extraction process of modified Xiongqiong decoction，and to evaluate the effective dosage and safety of the medicine by pharmacodynamic experiment and acute toxicity test. Methods Alcohol-reflus extraction process of volatile oil，walnut oil and non-volatile components was optimized with orthogonal test，while the concentration of alcohol in the test of water extraction and ethanol precipitation after volatile oil extraction was investigated with single factor experiments. Focal rat brain ischemia model was established to screen the effective dosage of the medicine extracted from modified Xiongqiong decoction，and mouse acute toxicity test was used to inspect its safety preliminarily. Results Optimal extraction process of modified Xiongqiong decoction was as follows：Rhizoma Chuanxiong and Radix Angelicae Sinensis were crushed and screened through mesh size of 10，the mixture was soaked in 10-fold water amount for 4 h，the filtrate was concentrated and the medicinal residue was in reserve after extracted with steam distillation for 6 h；walnuts were crushed into rough grains after heating at 150 ℃ for 1.5 h to remove the enzyme，the coarse powder was extracted by soaking with 4-fold amount petroleum ether for four times，40 minutes for each time，and the medicinal residue was in reserve. The dregs of the decoction were extracted with 10-fold amount of 70 % ethanol for 3 times，one hour per time. Effective dosage of the extract for protecting rat focal brain ischemia was 3.78 g·kg-1，which was equal to the daily dosage of 42 g of dried medicine for a person weighed 70 kg. Minimal lethal dose of the extract in mice was 120.96 g·kg-1，which was equal to 201.6 times of 70 kg person's daily dried medicine expenses. Conclusion The optimized extraction process for modified Xiongqiong decoction is stable and feasible，and the extract is safe and effective to protect focal brain ischemia.

R285.5；R284.2

国家科技重大新药创制专项——中药复方药理学研究及药效学评价关键技术（2009ZX09502-015）。