盐酸青藤碱醇质体水凝胶膏剂的制备及体外透皮效应

Preparation of sinomenine hydrochloride-loaded ethosome hydrogel patch and its in vitro transdermal effect

目的初探盐酸青藤碱醇质体水凝胶膏剂的最佳制备工艺,并探讨其体外透皮效应。方法以初黏力、胶强度作为考察指标,利用星点效应面法对水凝胶膏剂进行处方优化,加入一定量的盐酸青藤碱醇质体制备成盐酸青藤碱醇质体水凝胶膏剂,采用改良Franz扩散池对其体外透皮效应进行研究。结果水凝胶膏剂最佳处方组合为:0.30%EDTA-2Na,0.20%甘羟铝,6.00%聚丙烯酸钠,28.00%甘油,1.50%聚乙烯吡咯烷酮K-90,0.20%酒石酸,放置温度为30℃;并且制备含有1.00%盐酸青藤碱醇质体的水凝胶膏剂。结论盐酸青藤醇质体水凝胶膏剂的经皮透过量大于盐酸青藤碱水凝胶膏剂的透过量,具备良好的释药特性,有望为治疗类风湿关节炎创造了一种良好的制剂。

Objective To explore the optimal preparation of sinomenine hydrochloride-loaded ethosome hydrogel patch（SH-EHP）, and to investigate the in vitro transdermal absorption. Methods The optimal prescription of SH-EHP was investigated with response surface methodology with initial adhesion force and adhesive strength as the markers. SH-EHP was prepared by adding a certain amount of sinomenine hydrochloride-loaded ethosome, and transdermal absorption in vitro was studied with modified Franz diffusion cells. Results The optimal prescription formula of SH-EHP was EDTA-2Na（0.30%）, glycine aluminum（0.20%）, sodium polyacrylate（6.00%）, glycerin（28.00%）, polyvinylpyrrolidone K-90（1.50%）, tartaric acid（0.20%）, and sinomenine hydrochloride ethosome（1.00%） with the storage temperature at 30 ℃. Conclusion SH-EHP exhibits higher percutaneous permeability than sinomenine hydrochloride hydrogel patch, which is expected to be a better preparation for rheumatoid arthritis.