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[摘要]
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EudragitEPO 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。
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[Abstract]
Objective To investigate the effect of prescription of Pressure Sensitive Adhesives on the percutaneous absorption of artesunate. Methods The effects of various additives on the crystallization of artesunate in polyacrylate adhesive matrix were investigated by the various of polyacrylate pressuresensitive adhesives formulation, and the effects of various additives and pressuresensitive adhesives on the permeation of artesunate across SD rat abdominal skin were studied by modified Franz mothern method. ResultsPolymethacrylates Eudragit EPO and Poly(vinyl pyrrolidone) PVP-K30 inhibited the crystallization of artesunate in polyacrylate adhesive matrix. The addition of Eudragit EPO and PVP-K30 increase the flux of artesunate with the polyacrylate adhesive matrix after a storage period of 6 weeks.Conclusion These observations indicate that improvement in thesolubility of artesunate is necessary to realize fully the clinically applicable transdermal delivery system for drug.
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