青蒿琥酯贴剂压敏胶处方的研究

Studies on the prescription of pressure sensitive adhesives of Artesunate Patch

目的考察压敏胶基质处方对青蒿琥酯体外透皮吸收的影响。方法以聚丙烯酸酯压敏胶为基质设计不同的处方,考察了各种添加剂对青蒿琥酯在聚丙烯酸酯压敏胶基质中结晶的影响;通过改良的Franz透皮扩散池测定青蒿琥酯贴剂中青蒿琥酯透过SD大鼠腹部皮肤的渗透速率,以研究不同压敏胶和不同添加剂对经皮渗透速率的影响。结果聚丙烯酸树脂Eudragit EPO和聚乙烯吡咯烷酮(PVP-K30)对青蒿琥酯结晶均有较强的抑制作用,能提高青蒿琥酯在压敏胶中的载药量。体外透皮试验结果显示,储存6周后,添加Eudragit EPO、PVP-K30的青蒿琥酯贴剂中的青蒿琥酯的累计透过量比无添加剂贴剂的高。结论上述研究结果表明,提高青蒿琥酯在基质中的载药量有利于其开发成临床应用的贴剂。

Objective To investigate the effect of prescription of pressure sensitive adhesives on the percutaneous absorption of artesunate. Methods Various polyacrylate pressure sensitive adhesive formula- tions were designed. The effects of various additives on the crystallization of artesunate in polyaerylate adhesive matrix were investigated. Modified Franz mothern method was used to study the effects of various additives and pressure-sensitive adhesives on the permeation of artesunate across SD rat abdominal skin. Results Polymethacrylates Eudragit EPO and Polyvinyl pyrrolidone （PVP-K30） inhibited significantly the crystallization of artesunate in polyacrylate adhesive matrix, and increased the drug loading of artesu- nate in pressure sensitive adhesives. The addition of Eudragit EPO and PVP-K30 increased the flux of artesunate with the polyacrylate adhesive matrix after a storage period of 6 weeks. Conclusion These observations indicate that improvement of drug loading in the solubility of artesunate is necessary to fully realize the clinically applicable transdermal delivery system.