目的 制备艾叶油乳-水凝胶贴膏剂,并优化其处方和评价其体外透皮性能。方法 以初黏力、持黏力、180°剥离强度、内聚力和渗透度为评价指标,选择水凝胶贴膏剂骨架材料聚丙烯酸钠NP-700、交联剂甘羟铝、交联调节剂乙二胺四乙酸二钠(EDTA)和保湿剂甘油,开展正交优化试验。采用GC法测定样品液中桉油精、樟脑、龙脑的量,考察其体外透皮情况。结果 影响贴膏剂成型的因素顺序为甘油 >甘羟铝 >EDTA >聚丙烯酸钠NP-700,最佳组合为30%甘油、5%聚丙烯酸钠NP-700、0.3%甘羟铝、0.03% EDTA。3种成分的稳态渗透速率分别为85.216、4.442、3.941 μg/(cm²·h)。结论 艾叶油乳-水凝胶贴膏剂符合质量要求,透皮释药具有零级释放特点。

Objective To optimize formulations of emulsion-hydrogel transdermal patch of essential oil from Artemisia Argyi Folium, and to evaluate its transdermal characteristics in vitro. Methods The formulations were optimized by orthogonal experiment with four factors including hydrogel patch carrier (sodium polyacrylate NP-700), crosslinking agent (dihydroxyaluminium aminoacetate), crosslinking modifier (EDTA), and moisturizing agent (glycerol). Initial adhesive force, hold force, 180° peeling strength, cohesion, and permeability were measured. In addition, the contents of eucalyptol, camphor, and borneol in hydrogel transdermal patch were analyzed by GC. Results The impacting factors which affected the patch shaping were in the order of glycerol > dihydroxyaluminium aminoacetate > EDTA > sodium polyacrylate NP-700. The optimized formulation was as following: 30% glycerol, 5% NP-700, 0.3% dihydroxyaluminium aminoacetate, and 0.03% EDTA. The permeation rates of eucalyptol, camphor, and borneol were 85.216, 4.442, and 3.941 μg/(cm²·h), respectively. Conclusion Emulsion-hydrogel transdermal patch of essential oil from Artemisia Argyi Folium has a better quality and a transdermal property of zero-order release process.

国家自然科学基金面上项目(81470181);湖北省自然科学基金群体项目(2013CFA013)