一种含氟经皮渗透剂的合成  

Synthesis of a Novel Fluoro-Penetration Enhancer

作　　者：周晋 吴琴 史鸿鑫[3] Zhou Jin;Wu Qin;Shi Hongxin(Zhejiang Hengfeng Packing Co.,Ltd.,Jiashan 314113,China;Hangzhou Children＇s Hospital,Hangzhou 310014,China;Zhejiang University of Technology,Chemical Engineering College,Hangzhou 310032,China)

机构地区：[1]浙江恒丰包装有限公司,浙江嘉善314113 [2]杭州市儿童医院药剂科,浙江杭州310014 [3]浙江工业大学化工学院,浙江杭州310032

出　　处：《有机氟工业》2017年第1期4-7,共4页Organo-Fluorine Industry

基　　金：浙江省科技厅资助项目(2011R09002-10)

摘　　要：研究了2-甲基-2-(全氟-2-三氟甲基-3-氧代己酰氧基)乙氧基羰基乙基甲基二聚氧乙烯基硅烷(V)及其经皮吸收性能。甲基丙烯酸-2-全氟-2'-甲基-3'-氧代己酰氧基乙基酯与甲基二氯硅烷,经硅氢化反应后,直接用聚乙二醇醇解反应得到V,产物经红外光谱(IR)和质谱(MS)表征确认。采用改良的Franz扩散装置,以离体鼠皮为屏障,研究2%薄荷醇、0.5%V、2%薄荷醇+0.5%V、2%氮酮对双氯芬酸钠经皮吸收的影响,增渗倍数分别为3.11、1.19、5.46和6.21。V经皮促渗透效果:单独使用时效果不佳,与薄荷醇混合使用时效果好。Preparation and percutaneous absorption of 2-methyl-2-perfluoro-2＇-methyl-3＇-oxoca-proyloxyl ethoxycarbonyl ethylmethyldipolyethoxylsilicane（ V） were investigated. V was synthesized from 2-perfluoro-2＇-methyl-3＇-oxocaproyloxylethyl methacrylate and methyldichlorosilicane by hydrosilication,then by alcoholysis with polyglycol,and was characterized by FT-IR and MS. The penetration percentage of diclofenac sodium in different solutions of 2% 1-menthol,0. 5% V,2% 1-menthol-0. 5% V and 2% azone were respectively determined with improved Franz equipment and using rate skin as transderma barrier. The enhancement ratio were3. 11,1. 19,5. 46 and 6. 21 respectively. V with 1-menthol could improve the trasdermal amount of diclofenac sodium,especially,but sole V express bad performance for it.

关 键 词：渗透促进剂 硅氢化反应 增渗倍数 透皮速率 薄荷醇 

分 类 号：TQ460.1[化学工程—制药化工]