以药效为指标采用正交设计优化益气醒脑口服液的提取工艺

摘要

Objective To explore the optimization of the extraction process of Yi1i Xingnao oral liquid by orthogonal design with the pharmacological function as the index.Methods The orthogonal design method was used optimize the extraction process including the water content,extraction time,extraction times and alcohol concentration.The indexes including the area of cerebral infarction,water content of brain tissues,permeability of blood-brain barrier,superoxide dismutase (SOD),malondialdehyde (MDA),pathomorphology of brain tissues and content of calycosin-7-glucoside were taken as the evaluation criteria to assess the clinical efficacy of Yi1i Xingnao oral liquid on the rat model of ischemic reperfusion and screen the optimized extraction process.Results The results showed that the optimized extraction process involved A3B1C3D2,i.e.,the extraction should be made 3 times with 12 times of water by the ethanol precipitation with 60% ethanol alcohol and each time lasted for 1 hour.With this extraction process,the area of cerebral infarction was (18.68±1.15)%,the water content of brain tissues was (73.42±1.48)%,the Evans blue (EB)value of permeability of blood-brain barrier was (36.86±9.21)μg/g,the values of SOD and MDA were (81.06±10.97)nmol/mgprot and (13.58±4.96)nmol/mgprot respectively,the content of calycosin-7-glucoside was 158.32μg/ml,and the extracting solution had less precipitation with the best comprehensive evaluation result.Conclusion The optimized extraction process of Yiqi Xingnao oral liquid is A3B1C3D2 by the orthogonal design method in the pharmacodynamics experiment.The quality of the three batches of pilot-test production samples is stable,so A3B1C3D2 can be used as the optimized extraction process of Yiqi Xingnao oral liquid.%目的 探讨以药效为指标采用正交试验法优选益气醒脑口服液的提取工艺.方法 采用正交设计法优化益气醒脑口服液的加水量、提取时间、提取次数和醇沉浓度等提取工艺,并以脑梗死面积、脑组织含水量、血脑屏障通透性、脑组织超氧化物歧化酶(SOD)、丙二醛(MDA)、脑组织病理形态学及毛蕊异黄酮葡萄糖苷的含量为评判标准,考察益气醒脑口服液在缺血性再灌注大鼠模型上的疗效,筛选最佳制备工艺.结果 动物实验结果显示,加12倍量水提取3次,每次提取时间为1 h,以60%乙醇醇沉(即 A3B1C3D2)的工艺条件下,缺血性再灌注模型大鼠脑梗死面积为(18.68±1.15)%、脑组织含水量为(73.42±1.48)%、血脑屏障通透性 EB 为(36.86±9.21) μg/g、脑组织 SOD、MDA分别为(81.06±10.97)nmol/mgprot 和(13.58±4.96)nmol/mgprot,毛蕊异黄酮葡萄糖苷含量为158.32 μg/mL,沉淀较少,综合评定结果最佳.结论 通过药效学试验采用正交试验法筛选出益气醒脑口服液最佳的提取工艺为 A3B1C3D2,三批中试样品质量稳定,适合作为益气醒脑口服液的提取工艺.