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联苯乙酸-二乙胺经皮吸收贴剂的处方优化

Formulation optimization of feblinac-diethylamine transdermal patch
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摘要 目的制备联苯乙酸-二乙胺经皮吸收贴剂,以改善市售贴剂给药面积大的不足之处。方法采用有机溶媒挥散法制备联苯乙酸-二乙胺压敏胶分散型贴剂;通过体外经皮渗透实验进行处方优化,以水平双室扩散池为实验装置,以离体兔皮为通透屏障,采用单因素变量法对贴剂的促透剂种类和浓度进行筛选;对自制FEL-TEA贴剂的质量标准进行初步考察。结果确定优选处方为以联苯乙酸-二乙胺离子对复合物为主药,Duro-Tak~?87-4098型压敏胶为基质,质量分数10%氮酮为化学促透剂。结论处方优化后的联苯乙酸-二乙胺贴剂体外12 h累积经皮渗透量显著高于日本市售联苯乙酸贴剂,为开发联苯乙酸-二乙胺经皮吸收贴剂的后续研究提供了一定的实验依据。 Objective The aim of the present study was to prepare feblinac-diethylamine(FEL-DEA) patch to overcome the disadvantage of the large application area of SELTOUCH~?. Methods In this study, the drug-in-adhesive patch of feblinac-diethylamine was prepared using organic solvent evaporation method. Chemical enhancers were screened to enhance the permeation of the feblinac-diethylamine patch in vitro, which was carried out by using side-by-side horizontal diffusion cells through excised rabbit skin. And then the quality standard of FEL-DEA patch was preliminarily studied. Result The optimized patch contained FEL-DEA(equals to FEL 50 mg·m^(-2)), the adhesive Duro-Tak? 87-4098 and 10% Azone. Conclusion The optimized FEL-DEA patch had a significantly higher permeation than the commercial FEL patch. This study provided a basis for the follow-up research.
作者 刘楠楠 方亮
出处 《中国药剂学杂志(网络版)》 2016年第6期183-192,共10页 Chinese Journal of Pharmaceutics:Online Edition
关键词 药剂学 处方优化 体外经皮渗透实验 联苯乙酸-二乙胺 离子对 贴剂 pharmaceutics formulation optimization in-vitro skin permeation experiment feblinac-diethylamine ion-pair transdermal patch
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