中南药学

目的 旨在优化自发热止痛消炎凝胶贴膏的制备工艺，并进行质量评价。方法 以聚丙烯酸钠、甘油和中药浸膏用量为自变量，以感官性状、含水量、膜残留量、初黏力和持黏力的综合评分为因变量，采用Box-Behnken响应面法优化止痛消炎凝胶贴膏制备工艺。以磷脂/胆固醇质量比、香兰基丁醚（VBE）体积分数及超声时间为自变量，以脂质体包封率为因变量，采用BoxBehnken响应面法设计优化VBE脂质体处方工艺。采用高效液相色谱测定贴膏中主要成分含量及脂质体包封率；并通过动态光散射法测定脂质体粒径及多分散性指数（PDI）。结果 最佳凝胶贴膏处方为中药浸膏1.858 g、聚丙烯酸钠1.785 g、甘油5.101 g。VBE脂质体最佳工艺为卵磷脂∶胆固醇∶VBE=3∶1∶1，超声处理11 min，所得脂质体平均粒径为（175.7±5.5）nm,PDI为（0.22±0.05），包封率为（76.3±2.5）%(n=3)。通过建立的质量评价方法，结合感官性状、膜残留量、含水量、初黏力和持黏力等指标，系统评估了自发热止痛消炎凝胶贴膏的质量。所得贴膏外观均匀、膜残留低、黏附性良好，符合2025年版《中国药典》贴膏剂的质量标准。结论 优化后的自发热止痛消炎凝胶贴膏工艺稳定、质量可控，具有载药量高、黏附性好及自发热起效快等优势，适用于医院规模化制备与质量管理。

Objective To optimize the preparation of a self-heating analgesic and anti-inflammation gel patch and establish corresponding quality evaluation method for the preparation. Methods A Box-Behnken response surface design was used to optimize the hydrogel patch formulation, with the amounts of sodium polyacrylate, glycerol and herbal extract as the independent variables, while the comprehensive score based on appearance, moisture content, residual membrane, tack, and holding adhesion as the dependent variable. Another Box-Behnken design was used to optimize the vanillyl butyl ether(VBE)-loaded liposome formulation, with the phospholipid/cholesterol ratio, VBE volume fraction, and ultrasonication time as the independent variables, while encapsulation efficiency as the dependent variable. The contents of major active constituents and liposome encapsulation efficiency were determined by high-performance liquid chromatography(HPLC). The particle size and polydispersity index(PDI) of the liposomes were measured by dynamic light scattering(DLS). Results The optimal formulation for the gel patch consists of 1.858 g Chinese medicine extract, 1.785 g sodium polyacrylate, and 5.101 g glycerol. The best lipid vesicle(VBE) preparation involved a ph osphatidylcholine∶cholesterol∶VBE ratio at 3∶1∶1, with 11 minutes of ultrasonic treatment. The obtained lipid vesicles had an average particle size of(175.7±5.5) nm, a PDI of(0.22±0.05), and an encapsulation efficiency of(76.3±2.5)%(n = 3). The quality of the self-heating analgesic and antiinflammation gel patch was assessed by established quality evaluation methods, with incorporation of sensory properties, membrane residue, moisture content, initial adhesion force, and holding adhesion as key indicators. The prepared gel patch presented a uniform appearance, minimal membrane residue and favorable adhesive properties, which conformed to the quality specifications for patches in the 2025 Edition of the China Pharmacopeia. Conclusion The optimized self-heating analgesic and anti-inflammation hydrogel patch has stable and controllable quality, with high drug loading capacity, strong adhesion, and rapid self-heating, making it suitable for small-scale or hospital-based preparation and quality control.