结合药效学优化儿童清肺止嗽糖浆提取工艺

Optimization of extraction process of Children′s Qingfei Zhisou Syrup based on pharmacodynamics

以青黛提取物中靛玉红含量为指标,考察乙醇回流提取法、水提法靛玉红的提取率,并结合氨水引咳小鼠模型、枸橼酸引咳豚鼠模型的止咳药效学实验研究进行君药青黛提取方法和全方提取工艺的优选。药学工艺部分所得醇提制剂中靛玉红提取率为51.89%,水提制剂中未检测到靛玉红。在药效学实验中,2种不同工艺制剂的儿童清肺止嗽糖浆均能有效延长咳嗽潜伏期,抑制咳嗽次数。在延长咳嗽潜伏期方面,2种工艺样品间比较无明显差异,在减少咳嗽次数方面,青黛等5味醇提、生石膏等3味水提样品高剂量在枸橼酸引咳豚鼠实验中止咳效果优于其他工艺制剂(P<0.05)。醇提工艺制备的儿童清肺止嗽糖浆中靛玉红的提取率高于水提工艺,止咳药效学研究中2种制剂均有较好的止咳效果,其中青黛等5味醇提、生石膏等3味水提制备的儿童清肺止嗽糖浆在枸橼酸引咳豚鼠模型实验中的止咳效果优于全方水提。综合以上2种方式所得结论,此工艺方药可利用度高,药效更佳,最终选择青黛等5味醇提、生石膏等3味水提为最佳提取工艺。

This study determined the extraction rates of indirubin in Indigo Naturalis by ethanol reflux extraction method and water extraction method.The pharmacodynamic study against cough induced by ammonia water in the mouse model and the cough induced by citric acid in the guinea pig model were performed to optimize the extraction process of the sovereign medicinal Indigo Naturalis and the whole prescription of Children′s Qingfei Zhisou Syrup.The extraction rate of indirubin by the ethanol reflux method was 51.89%,and indirubin was not detected in the product of water extraction.Two samples of Children′s Qingfei Zhisou Syrup prepared with different methods can prolong the incubation period of cough and suppress the frequency of coughs in pharmacodynamic experiments.In terms of prolonging the incubation period of cough,the two samples prepared with different methods had no significant difference.In terms of reducing the frequency of coughs,the high-dose Five kinds of ethanol extracts such as indigo naturalis and three kinds of water extracts such as gypsum had better effect against the citric acid-induced cough of guinea pigs than other samples(P<0.05).The extraction rate of indirubin in Children′s Qingfei Zhisou Syrup sample prepared with ethanol was higher than that with water.The two samples of Children′s Qingfei Zhisou Syrup prepared with the two methods showed good antitussive effects.The sample prepared with 5 ingredients(including Indigo Naturalis)extracted with ethanol and 3 ingredients(including Gypsum Fibrosum)extracted with water had better alleviation effect on the citric acid-induced cough of guinea pig than the whole water extract sample.In conclusion,the optimum extraction scheme is ethanol extraction for 5 ingredients including Indigo Naturalis in combination with water extraction for 3 ingredients including Gypsum Fibrosum,and the Children′s Qingfei Zhisou Syrup produced in this manner has better antitussive efficacy.