目的 采用正交試驗優(yōu)化祖師麻凝膠膏的組方，并研究其體外透皮吸收行為。方法 以初黏度、膏體強度和釋放度為考察指標(biāo)，綜合評分，采用L₁₈（3⁷）正交試驗對空白基質(zhì)輔料的用量進(jìn)行優(yōu)化，確定最佳處方組合并進(jìn)行驗證試驗。采用改良的Franz擴散池，通過體外透皮試驗，采用HPLC法同時測定最佳處方中瑞香苷、瑞香素-8-O-β-D-葡萄糖苷、祖師麻甲素的體外透皮滲透量。結(jié)果 優(yōu)選出祖師麻凝膠膏黏合劑最佳組方為卡波姆980、聚維酮K30、二氧化硅、阿拉伯膠、聚維酮K90、明膠、聚乙二醇400比例為8：3：4：12：8：10：8，體外透皮行為符合零級動力學(xué)過程。結(jié)論 采用優(yōu)選的黏合劑組方制備的凝膠膏劑的黏附性、膏體強度、釋藥性能等均良好，具有較好的使用舒適度，可作為祖師麻凝膠膏的基礎(chǔ)制劑組方使用，并可以為新型凝膠膏劑的開發(fā)提供技術(shù)參考。

Objective To optimize the formulation of Zushima Gel Paste by orthogonal test and study its trans-dermal absorption behavior in vitro. Methods The initial viscosity, paste strength, and release degree were used as indexes, and the dosage of blank matrix excipients was optimized by L₁₈(3⁷) orthogonal test to determine the optimal formulation combination and carry out validation test. The in vitro trans-dermal permeation of daphnetin, daphnetin-8-O-β-D-glucoside, and daphnetin in the optimal formulation was simultaneously determined by HPLC method using a modified Franz diffusion cell. Results The optimum formulation of Zushima Gel Paste was carbomer 980, polyvinyl K30, micronized silica gel, acacacia, polyvinyl K90, gelatin, and polyethylene glycol 400 with proportion of 8:3:4:12:8:10:8. The in vitro transdermal behavior conformed to the Zero-order kinetic process. Conclusion The gel paste prepared with the optimized adhesive formula has good adhesion, ointment strength, and drug release performance, and has good use comfort. It can be used as the basic preparation formula of Zushima Gel Paste, and can provide technical reference for the development of new gel ointment.

R944.2

廣州市科技計劃項目（201902010012）