N,N-二取代甘氨酸酯的合成及其经皮促渗活性

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。

Synthesis of N,N-disubstituted glycine esters and their penetration enhancing activities

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.