| 丙氨酸酯衍生物的合成及其对吲哚美辛的经皮促渗活性 |
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| 引用本文： | 李伟杰.丙氨酸酯衍生物的合成及其对吲哚美辛的经皮促渗活性[J].合成化学,2016,24(12):1043-1047. |
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| 作者姓名： | 李伟杰 |
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| 作者单位： | 韩山师范学院 化学与环境工程学院，广东 潮州 521041 |
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| 基金项目： | 广东省科技计划资助项目(2013B021800092) |
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| 摘 要： | 以N,N-二乙基-l-丙氨酸为原料，N,N′-二环己基碳二亚胺为缩合剂，4-甲氨基吡啶为催化剂，合成了7个新型的2-(N,N′-二乙基氨基)丙酸酯（1a~1g），其结构经1H NMR， MS（ESI）和元素分析表征。研究了其对药物吲哚美辛的体外经皮促渗活性。结果表明：1g对吲哚美辛的经皮促渗活性最好（94.2%）。
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| 关 键 词： | 丙氨酸酯衍生物 N N-二乙基-l-丙氨酸 催化合成 吲哚美辛 经皮促渗活性 |
| 收稿时间： | 2016-03-31 |
Synthesis of Alanine Ester Derivatives and Their Enhancing Effects on the Transdermal Drug Delivery of Indomethacin |
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| LI Wei-jie.Synthesis of Alanine Ester Derivatives and Their Enhancing Effects on the Transdermal Drug Delivery of Indomethacin[J].Chinese Journal of Synthetic Chemistry,2016,24(12):1043-1047. |
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| Authors: | LI Wei-jie |
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| Abstract: | Seven novel 2-(N,N-diethylamino)propanoates (1a~1g) were synthesized using N,N-di-ethyl-l-alanine as material, N,N-dicyclohexylcarbodiimide as condensation agent and 4-dimethylamin-opyridine as catalyst. The structures were characterized by 1 H NMR, MS( ESI) and elemental analy-sis. In vitro penetration enhancing activities of 1 were evaluated using rat skins as biomembrane and in-domethacin as model drug in TT-18-type diffusion cells. The results showed that 1 g exhibited good skin penetration enhancement of indomethacin(94. 2%). |
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| Keywords: | alanine ester N N-diethyl-l-alanine catalytic synthesis indomethacin skin penetration enhancing activity |
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