目的 優(yōu)化三伏貼提取工藝和三伏貼凝膠膏劑（Sanfutie hydrogel patch，SHP）制劑成型工藝，并研究其透皮特性。方法 以芥子堿硫氰酸鹽、延胡索乙素、去氫紫堇堿、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綜合評分為考察指標(biāo)，采用星點設(shè)計-響應(yīng)面法（central composite design-response surface method，CCD-RSM）確定最佳提取工藝；以膏體的感官指標(biāo)、初黏力、持黏力以及體外累積釋放率的綜合評分為考察指標(biāo)，在單因素考察的基礎(chǔ)上，采用正交試驗設(shè)計法，對聚丙烯酸鈉、甘羥鋁、卡波姆940等輔料的用量進(jìn)行優(yōu)化，確定最佳處方；并采用Franz擴散池法進(jìn)行體外透皮試驗。結(jié)果 乙醇體積分?jǐn)?shù)55%，料液比1∶15，回流時間100 min為最佳提取方式；聚丙烯酸鈉4.1%，甘羥鋁0.05%，卡波姆940 0.41%，酒石酸0.41%，聚乙二醇13.6%，三伏貼提取液用量22.7%為制備SHP的最優(yōu)處方；凝膠膏劑中5個指標(biāo)成分（芥子堿硫氰酸鹽、延胡索乙素、去氫紫堇堿、十二碳四烯酰胺A/B、甘遂大戟萜酯C）的體外透皮行為均符合零級動力學(xué)過程。結(jié)論 采用最優(yōu)提取工藝與制劑成型工藝制備的SHP外觀色澤均一、黏性適中，且透皮特性良好。

Objective To systematically optimize the extraction process of Sanfutie (三伏貼) 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

國家自然科學(xué)基金青年基金項目（82003927）；上海中醫(yī)藥大學(xué)科技發(fā)展項目（24KFL030）