星点设计-效应面法优化野扇花颗粒制备工艺及其药效学研究

Optimization of Preparation of Yeshanhua Granules by Central Composite Design-Response Surface Methodology and Its Pharmacodynamic Effects

目的:制备野扇花颗粒,并对其制备工艺进行优化,同时完成制剂初步药效学研究。方法:以料液比、提取次数、提取时间为主要考察因素,以总生物碱含量为评价指标,采用星点设计(CCD)-效应面法优选野扇花颗粒制备工艺,同时观察制剂对小鼠应激性胃溃疡、小鼠热板痛阈、醋酸引起小鼠扭体反应的影响。结果:野扇花颗粒的最优制备工艺料液比为1∶12,提取2次,每次120 min,制剂可显著降低应激性胃溃疡小鼠溃疡点数,可显著延长小鼠热刺激性疼痛的潜伏期,可显著降低醋酸引起的小鼠扭体次数。结论:通过CCD效应面法优选得到的野扇花颗粒制备工艺预测性好、合理可行,同时制剂具有抗胃溃疡、镇痛的药理作用。

Objective:To optimize the preparation of Yeshanhua Granules and to preliminarily investigate its pharmacodynamic effects.Methods:With the solid-to-liquid ratio,extraction times,and extraction time as the main influencing factors and the total alkaloid content as the evaluation index,the central composite design-response surface methodology(CCD-RSM)was used to optimize the preparation of Yeshanhua Granules.The effects of Yeshanhua Granules on stress gastric ulcer,the pain threshold in the hot plate test,and the writhing reaction induced by acetic acid in mice were observed.Results:The optimal preparation was achieved by extraction twice,120mineachtimeatasolid-to-liquidratioof1∶12.Under such conditions,Yeshanhua Granules could significantly reduce the number of ulcer points in mice with stress gastric ulcer,prolong the incubation period of pain caused by heat irritation,and decrease the number of writhing caused by acetic acid.Conclusion:The preparation processing of Yeshanhua Granules optimized by CCD-RSM was good in prediction,reliable,and feasible,by which Yeshanhua Granules displayed pharmacologic activities such as resisting gastric ulcer and relieving pain.