关键词: 青藤碱, 喷雾剂, 稳定性, 药代动力学

Abstract:

We prepared and characterized the spray formulation of sinomenine for topical administration. The permeation enhancer was selected based on in vitro skin permeation studies. The antioxidant was optimized through stability studies. Pharmacokinetic 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 adjuvant. The pharmacokinetic parameters of Cmax and AUC0–24 for spray were 1.17 μg/mL and 3.35 μg/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.

Key words: Sinomenine, Sinomenine, Spray, Spray, Stability, Stability, Pharmacokinetics, Pharmacokinetics