白芥子涂方乳化型膏贴剂的制备工艺

Preparation Process of White Mustard Seed Varnish Emulsified Emplastrum

目的采用正交实验设计,优选白芥子涂方药材提取工艺和乳化型膏贴基质配比。方法分别以白芥子中芥子碱硫氰酸盐、甘遂中大戟二烯醇提取量,以及延胡素中延胡索乙素、细辛中细辛酯素提取量作为考察指标,选择L9(34)正交实验,考察各因素对乙醇回流提取工艺和超临界二氧化碳(CO2)萃取工艺的影响。选用石蜡、单甘酯、凡士林、甘油为乳化型膏贴基质配料,选择黏性、软硬度、熔化性、均匀度为考察指标进行综合评分,采用L9(34)正交实验优选基质配制比例。结果回流提取过程中,乙醇浓度对白芥子和甘遂提取均有显著影响(P<0.05),乙醇用量显著影响甘遂中大戟二烯醇浸出(P<0.05),二者合并提取优选工艺条件为加13倍量60%乙醇,回流提取1次,每次1h。超临界CO2萃取过程中,仅萃取釜压力对延胡索和细辛的提取效果产生显著影响(P<0.05)。确定优选工艺条件为:萃取压力25MPa,萃取温度40℃,95%乙醇为夹带剂,用量为药材用量3倍。基质成型过程,石蜡与凡士林用量是影响基质成型的关键因素(P<0.05),石蜡、单甘酯、凡士林和甘油的优选配比为2∶4∶2∶1。结论采用正交实验方法确定了白芥子涂方药材优选提取条件,以及乳化型膏贴基质配比。按优化处方制备的白芥子涂方乳化型膏贴剂具有载药量大、乳化性能好、促进药物透皮释放的特点。

Objective To optimize the extraction process of white mustard seed varnish and it ’ s matrix ratio by orthogonal design. Methods The extraction process was optimized by L9( 34) orthogonal design with the yield of extraction of sinapine thiocyanate,euphadienol,tetrahydropalmatine,and asarinin. The variance analysis method was used to find out the key factors on ethanol reflux extraction and supercritical CO2 extraction process. Paste substrate consists of paraffin,monoglyceride,vaseline,glycerin and so on.The research selected viscosity,hardness,melting property and evenness as indicators to evaluate the formulations.And the L9( 34) orthogonal experiment was used to select the optimal formulation. Results Ethanol concentration significantly affected the extraction of white mustard and Euphorbia kansui( P<0.05),and the amount of solvent only significantly affected the dissolution of euphadienol in Euphorbia kansui( P < 0. 05). The optimal extraction conditions for the combined extraction were as follows: adding 60% ethanol 13 times the amount of extractand reflux for 1 hour each time. During the supercritical CO2 extraction process extraction of axe pressure had a significant effect for the extraction efficiency of asarinin and corydalis only( P<0.05). The optimum extraction conditions are as follows: extraction pressure 25 MPa,extraction temperature40 ℃,95% ethanol as entrainer,which is 3 times the amount of medicinal materials.The key factors affecting the matrix molding paraffin and vaseline is the( P < 0.05),and the optimum ratio of paraffin,monoglyceride,vaseline and glycerin was 2∶4∶2∶1.Conclusion The optimum extraction conditions and the proportion of emulsion paste substrate are determined by orthogonal experiment in this study.The emulsified patch prepared according to the optimized formula has prominent characteristics of high drug loading,good emulsifying property and promoting the transdermal release of drugs.