摘要
研究了氯硝柳胺衍生物的透皮吸收 .和氯硝柳胺原药相比 ,氯硝柳胺的酯型前体药物对透皮速率并无显著影响 ,但前体药物的熔点越低 ,透皮速率越大 ;氯硝柳胺的醚型前体药物和复盐型药物增大了药物的水溶性 ,更有效地促进了药物的透皮吸收 .具有适宜正辛醇 /水分配系数的药物有大的透皮速率 .氯硝柳胺乙醇胺盐的透皮控释贴剂比氯硝柳胺的透皮控释贴剂有更显著的杀虫效果和更好的应用前景 .
The low melting point derivatives and the hydrophilic derivatives of niclosamide were designed and prepared to enhance the transdemal rate of niclosamide. Lowering the melting point of niclosamide by esterification with fatty acid did not have much effect on increasing the transdermal flux of niclosamide. However, the trend was evident that the lower the melting point, the greater the transdermal flux. Drugs with suitable octanol/water partition coefficient had great transdermal rate. The transdermal therapeutic system of complexing niclosamide with ethanolamine showed a more promising future than that of niclosamide for schistosomiasis control.
出处
《应用化学》
CAS
CSCD
北大核心
2001年第12期944-947,共4页
Chinese Journal of Applied Chemistry
基金
国家自然科学基金资助项目 ( 5 96 730 17)
