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制备局部给药的青藤碱喷雾剂,评价该制剂的特征.以体外经皮渗透试验筛选渗透促进剂;以稳定性试验考察抗氧剂的作用;以药代动力学试验和药效学试验研究该制剂的药理作用和副作用的趋势.氮酮是有效的渗透促进剂,抗氧剂硫脲以及乙醇作为喷雾剂的辅料.该制剂可以降低免疫佐剂引起的大鼠关节炎指数,其药代动力学参数均低于口服给药途径.青藤碱喷雾剂具有显著的抗炎功效、毒副作用较低.“,”We prepared and characterized the spray formulation of sinornenine for topical administration. The permeation enhan-cer was selected based on in vitro skin permeation studies. The antioxidant was optimized through stability studies. Pharmacoki-netic and pharmacological properties were determined in order to evaluate its side effect and pharmacodynamic action. It was found that azone was the most effective permeation enhancer, and sulfocarbamide was the optimal antioxidant. Alcohol was used as the additive of the sinomenine spray. Sinomenine spray decreased arthritis index of rats induced by Freund's complete adju-vant. The pharmacokinetic parameters of Cmax and AUC0-24 for spray were 1.17 μg/mL and 3.35 2g/h/mL, respectively, which were lower than those by oral administration. The relative bioavailability was 18.0%. Sinomenine spray was a promising topical delivery system with comparable anti-inflammatory efficacy, but possibly lower side effect.