正交设计结合药效学实验优选四君子汤颗粒水提及精制工艺

目的优选四君子汤颗粒最佳水提及精制工艺。方法采取正交试验法,以人参皂苷Rg_1、Re、Rb_1及甘草酸、甘草苷的含量及出膏率为指标,考察浸泡时间、加水量、提取时间、提取次数4个因素,优选四君子汤颗粒最佳水提工艺;以药液质量浓度、药液含醇量、醇沉时间为考察因素,优选四君子汤颗粒最佳水提醇沉工艺;通过干预脾虚证药效学实验对醇沉前后提取物进行比较。结果四君子汤颗粒最佳水提工艺为加10倍量的水浸泡60 min,煎煮3次,每次30 min;最佳水提醇沉工艺为水提滤液浓缩至1 mL药液相当于原药材0.5 g,药液含醇量为80%,醇沉时间为12 h。与模型组比较,四君子汤颗粒水提物组、水提醇沉物组大鼠唾液淀粉酶活性和血清胃泌素含量均显著升高(P0.05),且能提高脾虚大鼠小肠木糖吸收功能(P0.05);与四君子汤颗粒的水提物组比较,四君子汤颗粒水提醇沉物组D-木糖排泄率有显著性差异(P0.05),但唾液淀粉酶活性和血清胃泌素含量无显著性差异(P0.05)。结论四君子汤颗粒不宜采用醇沉工艺进行精制,因此,选择水提工艺作为四君子汤颗粒的最佳提取工艺。

Optimization of water extracting and refining procession of Sijunzi Decoction Granules by orthogonal design and pharmacodynamics test

Objective To optimize the water extracting and refining procession of Sijunzi Decoction Granules (SDG). Methods The orthogonal test method was used to study the four factors including the soak time, amount of water added, extraction time and frequency by taking the dry extract yield of the medicinal materials and contents of ginsenoside Rg₁, Re, Rb₁, glycyrrhizic acid, and liquiritin as indicators to optimize the water extracting process of SDG. To optimize the alcohol precipitation process of SDG, the factors including the concentration of the medicinal materials, alcohol content, and time of alcohol precipitation were investigated. The extracts before and after alcohol precipitation were compared by intervening spleen deficiency syndrome pharmacodynamics experiment. Results The best water extracting procession of SDG was soaked for 60 min with 10 times of water, decocted three times, 30 min for each time. The optimal water extraction by alcohol sedimentation process was to concentrate the filtrate of water extraction to 1 mL, which was equivalent to 0.5 g of the original medicinal materials, with 80% alcohol content and 12 h alcohol precipitation time. Compared with the model group, the activity of salivary amylase and the conent of serum gastrin in the water extracting group and water extracting by alcohol sedimentation group of SDG were significantly increased and could improve the absorption function of xylose in small intestine of rats with spleen deficiency syndrome (P<0.05); Compared with the water extracting group of SDG, there was a significant difference in D-xylose excretion rate in the water extracting by alcohol sedimentation group of SDG (P<0.05), but there was no significant difference in activity of salivary amylase and content of serum gastrin (P>0.05). Conclusion The alcohol precipitation process is not suitable for refining of SDG. So the water extracting process is finally selected as the best extraction process of SDG.