目的 优化虎力散凝胶贴膏（Hulisan gel plaster，HLS-GP）成型工艺，并进行初步药效学考察。方法 以初黏力、持黏力、黏着力和感官评分为指标，正交试验优化HLS-GP成型工艺；以党参炔苷、三七皂苷R₁（notoginsenoside R₁，NR₁）、8-去乙酰滇乌碱（8-deacetyl yunaconitine，8D-YNA）、滇乌碱和人参皂苷Rg₁（ginsenoside Rg₁，GRg₁）为指标，考察HLS-GP体外释药性及经皮渗透性，并从氮酮、丙二醇和薄荷脑中筛选最佳促渗剂；通过耳肿胀和醋酸扭体模型，初步探讨HLS-GP的抗炎镇痛作用。结果 HLS-GP的最佳处方为NP700 11 g，甘羟铝0.8 g，高岭土1.5 g，甘油40 g，酒石酸0.8 g，PVPK90 6 g，水20 g，验证实验结果符合要求。建立的党参炔苷、NR₁、8D-YNA、滇乌碱和GRg₁定量测定方法适用性好；5种成分24 h的累积释放率分别为（65.93±0.10）%、（77.42±0.13）%、（80.08±0.87）%、（69.86±0.17）%、（21.90±0.68）%，释放行为均符合一级动力学方程；筛选得到的最佳促渗剂为5%丙二醇，5种成分24 h的累积渗透量分别为（136.16±0.07）、（319.50±0.05）、（16.92±0.05）、（10.27±0.06）、（166.69±0.08）μg/cm²；抗炎镇痛结果表明，与对照组相比，模型组小鼠耳肿胀明显、潜伏期短、扭体次数多，而HLS-GP能够显著抑制小鼠耳肿胀、延长潜伏期，并减少扭体次数（P＜0.05、0.01）；同时，HLS-GP能够显著降低小鼠血清中炎症因子白细胞介素-6（interleukin-6，IL-6）、IL-1β、肿瘤坏死因子-α（tumor necrosis factor-α，TNF-α）和5-羟色胺（5-hydroxytryptamine，5-HT）、前列腺素E₂（prostaglandin E₂，PGE₂）的水平（P＜0.05、0.01）。结论 制得具有良好体外释药性和经皮渗透性的HLS-GP，且具有良好的抗炎镇痛作用，为虎力散经皮给药制剂的开发奠定基础。

Objective To optimise the forming process of Hulisan gel plaster (HLS-GP, 虎力散凝胶贴膏) and conduct preliminary pharmacodynamic investigation. Methods Orthogonal test was used to optimise the forming process of HLS-GP with initial tack, holding power, adhesion and sensory score as indicators. Lobetyolin, notoginsenoside R₁ (NR₁), 8-deacetyl-yunaconitine (8D-YNA), yunaconitine and ginsenoside Rg₁ (GRg₁) were used as indicators to investigate the in vitro release and transdermal permeability of HLS-GP and to screen for the optimal osmotic enhancer from azone, propylene glycol and menthol. A preliminary investigation of the anti-inflammatory and analgesic effects of HLS-GP through ear swelling and acetic acid writhing modelling. Results The optimum formulation of HLS-GP was 11 g NP700, 0.8 g aluminium glycinate, 1.5 g kaolin, 40 g glycerol, 0.8 g tartaric acid, 6 g PVP K90 and 20 g water, which confirmed that the results of the experiment met the requirements. The established methods for the determination of 8D-YNA, yunaconitine, lobetyolin, NR₁ and GRg₁ contents were applicable. And the 24 h cumulative release rates were (65.93 ±0.10)%, (77.42 ±0.13)%, (80.08 ±0.87)%, (69.86 ±0.17)% and (21.90 ±0.68)%, respectively, and the release behaviour followed the first-order kinetic equation. The optimal osmotic enhancer obtained from the screening was 5% propylene glycol, and the cumulative osmolality of the five components at 24 h were (136.16 ±0.07), (319.50 ±0.05), (16.92 ±0.05), (10.27 ±0.06) and (166.69 ±0.08) μg/cm², respectively. The anti-inflammatory and analgesic results showed that, compared with the control group, mice in the model group had obvious ear swelling, short latency, and a high number of writhing, whereas HLS-GP was able to significantly inhibit ear swelling, prolong latency, and reduce the number of writhing in the mice (P < 0.05). At the same time, HLS-GP was able to significantly reduce the serum levels of the inflammatory factors interleukin-6 (IL-6), IL-1β and tumor necrosis factor-α (TNF-α) in the mice with ear swelling and significantly reduce the serum levels of 5-hydroxytryptamine (5-HT), IL-1β and prostaglandin E₂ (PGE₂) in the acetate writhing mice (P < 0.05, 0.01). Conclusion HLS-GP with good in vitro drug release and transdermal permeability and good anti-inflammatory and analgesic effects were obtained, which can lay the foundation for the development of transdermal drug delivery formulations of Hulisan.

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云南省科技厅社会发展专项—重点研发计划项目（202303AC100025）；国家中医药管理局“十二五”重点学科—傣药学；国家自然科学基金资助项目（82174065）；云南省教育厅科学研究基金项目（2024Y379）；云南省中西医结合慢病防治重点实验室开放基金资助项目（YPKLG2024-016）；云南省傣医药与彝医药重点实验室资助项目（2024SS24074）