N,N-二甲基氨基乙酸酯的合成及其应用研究

Synthesis of N,N-Dimethyl Amino Acetates and Their Applications

应用改进方法合成了4个N,N＿二甲基氨基乙酸酯,其结构经IR谱、HNMR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:含w=2 5%的N,N＿二甲基氨基乙酸癸酯促进扑热息痛、消炎痛经皮渗透的效果比Azone(化学名:1＿正十二烷基氮杂环庚酮＿2)的强,且时滞缩短;N,N＿二甲基氨基乙酸辛酯的经皮促渗活性接近Azone;而N,N＿二甲基氨基乙酸己酯和N,N＿二甲基氨基乙酸月桂酯的经皮促渗活性不及Azone。

Four N,N-dimethylamino acetates were synthesized by an improved method, their chemical structures were determined by IR, ~1 H NMR and elemental analysis. Their penetration enhancing abilities were evaluated using naked mouse skins as bio-membrane, paracetamol or indomethacin as drug models in modified Franz-type diffusion cells. The results showed that 2.5% of decyl N,N-dimethylamino acetate exhibited excellent penetration enhancement of paracetamol and indomethacin, and exceeded those of Azone with a shorter lag time. The penetration enhancing activities of octyl N,N-dimethylamino acetate approached those of Azone.However, the enhancing effects of N,N-dimethylamino acetates with a dodecyl or n-hexyl chain were unsatifactory in comparision with those of Azone.