苏葶宣肺颗粒的制备工艺及初步药效研究

Preparation and efficacy of Suting Xuanfei granules

目的优选苏葶宣肺颗粒的最佳提取工艺和成型工艺,并探讨其对气管平滑肌的作用。方法采用L9(34)正交设计实验法,以迷迭香酸和黄芩苷的含量以及浸膏得率为指标,考察提取次数、提取时间和加水倍量对苏葶宣肺颗粒提取工艺的影响,优选苏葶宣肺颗粒的最佳提取工艺。以制粒情况、成型率、吸湿率、休止角及溶解度为评价指标,对辅料种类和药辅比例等因素进行考察,确定最佳制剂成型工艺。制备大鼠离体气管环后浸泡于K-H液,采用BL-420S生物机能系统测定其张力变化,分别观察苏葶宣肺颗粒对大鼠正常离体气管和磷酸组胺(His)、乙酰胆碱(ACh)致痉的大鼠离体气管张力的影响,计算解痉率。结果苏葶宣肺颗粒的最佳提取工艺为:加10倍量水,浸泡30 min,提取2次,每次提取60 min。3批正交验证实验综合评分均数为92.07,RSD为0.51%。最佳成型工艺为:浸膏、糊精、淀粉按3∶2.5∶4的比例制成软材,用10目筛网制成颗粒。苏葶宣肺颗粒对大鼠正常离体气管平滑肌具有舒张作用,对ACh和His致大鼠离体气管平滑肌收缩均有一定的解痉作用。结论本文建立了苏葶宣肺颗粒稳定可行的制备工艺,为后续的研发、质量控制奠定了基础。苏葶宣肺颗粒对离体气管平滑肌有舒张作用,其机制可能与抗组胺和抑制胆碱受体有关。

Objective To optimize the extraction and molding process of Suting Xuanfei granules,and determine its effect on the tracheal smooth muscle.Methods L9(34)orthogonal design experiment method was used,the content of rosmarinic acid and baicalin,and the extraction rate were used as indicators of the effect of extraction times,extraction time,and water volumn on the extraction of Suting Xuanfei granules,to optimize the optimal extraction process of Suting Xuanfei granules.The granulation condition,molding rate,moisture absorption rate,angle of repose,and solubility were used as the evaluation indicators,to determine the factors such as type of excipients and ratio of drugs to excipients in the optimal formulation molding process.The isolated rat trachea ring was prepared and soaked in K-H solution.The tension changes were measured with the BL-420S biological function system.The effects of Suting Xuanfei granules on the tension of the normal isolated rat trachea and the isolated rat trachea caused by histamine phosphate(His)and acetylcholine(ACh)were observed.The spasmolysis rate was calculated.Results The optimal extraction for Suting Xuanfei granules was as follows:adding 10 times of water,soaking for 30 min,and two extractions,each time 60 min.The average score of the three sets of orthogonal validation experiments was 92.07,and the RSD was 0.51%.The optimal molding process was as follows:the extract,dextrin,and starch were mixed at 3∶2.5∶4 to create a soft material.The mixture was then passed through a 10-mesh sieve to obtain granules.Suting Xuanfei granules showed a relaxing effect on the normally isolated tracheal smooth muscle in rats and also certain spasmolytic effect on ACh and His induced contraction of isolated tracheal smooth muscle in rats.Conclusion A stable and feasible preparation process route of Suting Xuanfei granules has been established,laying a foundation for subsequent research and development,production,and quality control.Suting Xuanfei granules has a relaxing effect on isolated tracheal smooth muscle,which may be related to antihistamine activity and the inhibition of cholinergic receptors.