褪黑激素皮肤渗透性的研究

褪黑激素皮肤渗透性的研究

郝劲松, 祝贺, 郑俊民

沈阳药科大学药剂教研室, 沈阳 110015

收稿日期:1997-08-27 修回日期:1998-03-09 出版日期:1999-03-15 发布日期:1999-03-15

The Study on Skin Permeation of Melatonin

Hao Jinsong, Zhu He, Zheng Junmin

Department of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110015

Received:1997-08-27 Revised:1998-03-09 Online:1999-03-15 Published:1999-03-15

摘要/Abstract

摘要： 本文考察了渗透促进剂Azone(AZ)、油酸(OA)、丙二醇(PG)等和离子导入法(Ag/AgCl或Pt电极,电流密度0.19 mA/cm², 频率2000 Hz,占/空比1:1)对褪黑激素(MT)皮肤渗透性的影响。MT能透过小鼠全皮, 其稳态流量和渗透系数分别为1.622×10^-3μg/cm²·s和0.8888×10^-6 cm/s; 100%AZ、5%AZ/PG和10%OA/PG处理皮肤后, MT的稳态流量分别是未处理组的7.61、7.03和2.98倍; MT作为非离子性药物, 离子导入对其也有促渗作用, 离子导入处理组的稳态流量是未处理组的2.19倍。结果表明渗透促进剂(AZ、OA)、离子导入法均能增加MT的经皮渗透。

关键词: 褪黑激素, 渗透促进剂, 离子导入, 渗透性

Abstract: The permeation of melatonin (MT) through the full-thickness mouse skin treated with penetration enhancers such as laurocapram (AZ), oleic acid (OA) and propylene glycol (PG),and/or iontophoresis under the condition with Ag/AgCl or Pt electrode at a current density of 0. 19 mA/cm², frequency of 2000 Hz and on/off ratio of 1:1 was conducted. MT as an unionized lipophilic drug could permeate through full-thickness mouse skin, whose steady-state flux and permeation coefficient were 1.622×10^-3μg/cm²·s and 0.888×10^-6 cm/s, respectively. Penetration enhancers including 100% AZ, 5% AZ/PG and 10% OA/PG increased the steady-state flux of MT to 7.61, 7.03and 2.98 times compared with that through untreated skin, respectively. The flux of MT was enhanced by current application with Ag electrode with an enhancement factor of 2.19. These results showed that penetration enhancer AZ, OA and/or iontophoresis could enhance the skin permeation of MT.

Key words: Melatonin, Penetration enhancer, Iontophoresis, Permeation

Supporting:

郝劲松, 祝贺, 郑俊民. 褪黑激素皮肤渗透性的研究[J]. .

Hao Jinsong, Zhu He, Zheng Junmin. The Study on Skin Permeation of Melatonin[J]. .

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