目的 优化三伏贴提取工艺和三伏贴凝胶膏剂（Sanfutie hydrogel patch，SHP）制剂成型工艺，并研究其透皮特性。方法 以芥子碱硫氰酸盐、延胡索乙素、去氢紫堇碱、十二碳四烯酰胺A/B、甘遂大戟萜酯C的含量以及浸膏得率的综合评分为考察指标，采用星点设计-响应面法（central composite design-response surface method，CCD-RSM）确定最佳提取工艺；以膏体的感官指标、初黏力、持黏力以及体外累积释放率的综合评分为考察指标，在单因素考察的基础上，采用正交试验设计法，对聚丙烯酸钠、甘羟铝、卡波姆940等辅料的用量进行优化，确定最佳处方；并采用Franz扩散池法进行体外透皮试验。结果 乙醇体积分数55%，料液比1∶15，回流时间100 min为最佳提取方式；聚丙烯酸钠4.1%，甘羟铝0.05%，卡波姆940 0.41%，酒石酸0.41%，聚乙二醇13.6%，三伏贴提取液用量22.7%为制备SHP的最优处方；凝胶膏剂中5个指标成分（芥子碱硫氰酸盐、延胡索乙素、去氢紫堇碱、十二碳四烯酰胺A/B、甘遂大戟萜酯C）的体外透皮行为均符合零级动力学过程。结论 采用最优提取工艺与制剂成型工艺制备的SHP外观色泽均一、黏性适中，且透皮特性良好。

Objective To systematically optimize the extraction process of Sanfutie (三伏贴) and the formulation molding processes of Sanfutie hydrogel patch (SHP), and to study its transdermal permeability characteristics. Methods The optimum extraction process was investigated using central composite design-response surface method based on the comprehensive score of the contents of sinapine thiocyanate, tetrahydropalmatine, dehydrocavidine, N-isobutyl-2E,4E,8Z,10Z/E dodecatetraenamide, kansuiphorin C and extraction yield. The combined scores of sensory indicators, initial adhesiveness, holding viscosity and in vitro cumulative release rate were used as indexes. Based on the results of single factor experiments, the best formula was selected by optimizing the dosage of sodium polyacrylate (NP 700), dihydroxyaluminum aminoacetate, carbomer 940 etc. using orthogonal test design. The transdermal permeability was investigated by the Franz diffusing method. Results The optimum extraction technology was as follows: ethanol concentration 55%, solid-liquid ratio 1:15 and extraction time of 100 min. The optimal prescription of SHP was as follows: NP700 4.1%, dihydroxyaluminum aminoacetate 0.05%, carbomer 940 0.41%, tartaric acid 0.41%, polyethylene glycol 400 13.6% and a dosage of 22.7% of Sanfutie extract solution. The in vitro transdermal dynamic behaviors of five index components (sinapine thiocyanate, tetrahydropalmatine, dehydrocavidine, dodecatetraene amide A/B, 5-kansuiphorin C) of SHP were conformed to zero-order kinetics. Conclusion The SHP was prepared by the optimal extraction and formulation molding with uniform color, moderate viscosity and good transdermal properties.

R283.6

国家自然科学基金青年基金项目（82003927）；上海中医药大学科技发展项目（24KFL030）