| N,N-二取代甘氨酸酯的合成及其经皮促渗活性 |
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| 引用本文： | 李伟杰,许遵乐.N,N-二取代甘氨酸酯的合成及其经皮促渗活性[J].化学研究与应用,2005,17(6):762-765. |
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| 作者姓名： | 李伟杰 许遵乐 |
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| 作者单位： | 汕头大学多学科研究中心,广东,汕头,515063;中山大学化学与化学工程学院,广东,广州,510275 |
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| 基金项目： | 汕头大学自然科学基金博士启动基金（240-072009）资助项目 |
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| 摘 要： | 合成了4个新的N，N-二取代甘氨酸酯，其结构经^1HNMR谱、IR谱、MS-ESI谱和元素分析确证。在改良的Franz扩散池上，用离体裸鼠皮作生物膜，扑热息痛或消炎痛作药物模型进行经皮促渗活性对比试验。结果显示：N，N-二甲基甘氨酸-（E）-3，7-二甲基-2，6-辛二烯酯（2a）具有出色的促透活性，含2．5％的2a促进扑热息痛、消炎痛经皮渗透的效果分别是Azone的2．1和2．6倍，且时滞缩短，超过DDAA的经皮促渗活性；而N，N-二甲基甘氨酸-6-戊氧基-1-己酯（2b）的经皮促渗活性接近Azone，且时滞更短。
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| 关 键 词： | N N-二取代甘氨酸酯 合成 促渗活性 |
| 文章编号： | 1005-1656（2006）06-0762-04 |
| 收稿时间： | 2004-12-25 |
| 修稿时间： | 2005-05-16 |
Synthesis of N,N-disubstituted glycine esters and their penetration enhancing activities |
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| Li Wei-jie,Xu Zun-le.Synthesis of N,N-disubstituted glycine esters and their penetration enhancing activities[J].Chemical Research and Application,2005,17(6):762-765. |
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| Authors: | Li Wei-jie Xu Zun-le |
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| Institution: | 1. Muhidisciplinary Research Center, Shantou University, Shantou 515063, China; 2. School of Chemistry and Chemical Engineering, Zhongshan University, Guangzhou 510275, China |
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| Abstract: | Four novel N,N-disubstituted glycine esters were synthesized and their chemical structures were determined by ~1H NMR,IR,MS-ESI spectra and elemental analysis.Their penetration enhancing abilities were evaluated using naked mouse skins as bio-membrane and paracetamol or indomethacin as drug models in modified Franz-type diffusion cells.The results showed that 2.5% of N,N-dimethylglycine-(E)-3,7-dimethyl-2,6-octadienyl ester(2a) exhibited excellent penetration enhancement of paracetamol and indomethacin,as high as 2.1 and 2.6 times those of Azone with a shorter lag time respectively and exceeded those of DDAA.The penetration enhancing activities of N,N-dimethylglycine-6-pentoxyhexyl ester(2b) approached those of Azone with a shorter lag time. |
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| Keywords: | N N - disubstituted glycine ester synthesis penetration enhancing activity |
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