栀黄消肿凝胶贴膏的制备工艺优化及药效学研究OA

Objective:To optimize the formulation of Zhihuang Xiaozhong gel plaster(ZGP)and evaluate its in vitro re-lease,transdermal properties,and preliminary pharmacodynamic effects.Methods:The matrix composition of ZGP was optimized using a D-optimal mixture design with sodium polyacrylate NP-700,dihydroxyaluminum aminoacetate,poly-vinylpyrrolidone(PVP K-30),tartaric acid,glycerol,and water as influencing factors.Evaluation indicators included sensory properties,initial adhesion,holding power,and peel strength.Using geniposide as the marker compound,the in vitro release and transdermal permeation of ZGP were investigated,and the optimal concentration of azone as a penetra-tion enhancer was screened from different mass fractions.A rat model of acute soft tissue injury was established.Mor-phological changes in muscle tissue were observed via hematoxylin-eosin(HE)staining,and the levels of interleukin-1β(IL-1β)and prostaglandin E2(PGE2)were detected by ELISA to preliminarily explore its therapeutic effect on soft tis-sue injury.Results:The optimal formulation of ZGP was:sodium polyacrylate NP-700 8.61%,dihydroxyaluminum aminoacetate 0.16%,PVP K-30 4.84%,tartaric acid 0.16%,glycerol 45.91%,water 24.19%,and extract 16.13%.The cumulative release rate of geniposide at 24 hours was(66.96±4.81)%,and 1%azone showed the best penetra-tion-enhancing effect.Pharmacodynamic experiments demonstrated that,compared with the model group,ZGP signifi-cantly improved muscle tissue damage and reduced the levels of PGE2 and IL-1β(P<0.001).Conclusion:The opti-mized ZGP exhibited a stable and feasible preparation process,favorable in vitro drug release and transdermal perme-ation properties,and significant anti-inflammatory effects,providing an experimental basis for developing a novel topical dosage form of the Zhihuang Xiaozhong formula.