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日用化学工业（中英文）

日用化学工业 ›› 2022, Vol. 52 ›› Issue (2): 134-139.doi: 10.3969/j.issn.1001-1803.2022.02.004

• 开发与应用 • 上一篇    下一篇

复合促渗剂对当归水溶性成分阿魏酸的体外透皮性能影响研究

冉鑫1,王继龙1,刘晓霞1,何红杰1,魏舒畅1,2,*(),冯晓莉1,李真真1   

  1. 1. 甘肃中医药大学,甘肃 兰州 730000
    2. 甘肃省中药制药工艺工程研究中心,甘肃 兰州 730000
  • 收稿日期:2021-05-12 修回日期:2021-12-08 出版日期:2022-02-25 发布日期:2022-02-22
  • 通讯作者: 魏舒畅
  • 基金资助:
    国家自然科学基金资助项目(82060721);甘肃中医药大学2019科创基金项目(2019KCYB-2)

Study on the effect of compound penetration enhancer on the permeability of Angelica’s water-soluble component ferulic acid in vitro

Ran Xin1,Wang Jilong1,Liu Xiaoxia1,He Hongjie1,Wei Shuchang1,2,*(),Feng Xiaoli1,Li Zhenzhen1   

  1. 1. Gansu University of Chinese Medicine, Lanzhou, Gansu 730000, China
    2. Gansu Engineering Research Center for Chinese Medicine Pharmaceutical Technology, Lanzhou, Gansu 730000, China
  • Received:2021-05-12 Revised:2021-12-08 Online:2022-02-25 Published:2022-02-22
  • Contact: Shuchang Wei

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摘要：

选用立式透皮扩散试验仪,以离体小鼠皮为透皮屏障进行体外透皮实验,研究了促渗剂氮酮、薄荷脑和冰片对当归水溶性成分阿魏酸的体外透皮性能影响,并优选出了较佳复合促渗剂。实验结果表明,三种促渗剂单用时,对阿魏酸透皮性能的影响大小顺序为：薄荷脑>冰片>氮酮,而联合使用时,顺序为：冰片>薄荷脑>氮酮。且优选出的较佳复合促渗剂为2%冰片+2%薄荷脑,结果显示二者联合使用优于氮酮、冰片、薄荷脑单独使用,其24 h单位面积累积透过量（Q24）可达34.32 µg/cm2,增渗倍数（ER）可达64.195,分别为单用薄荷脑和冰片的8倍和25倍,且滞后时间在2 h以内,协同作用明显,即优选出的复合促渗剂对当归水溶性成分阿魏酸的促渗效果很好,可为当归及以当归为主药方剂的经皮给药制剂开发提供促渗剂。

关键词: 当归, 阿魏酸, 促渗剂, 体外透皮

Abstract:

By using vertical transdermal diffusion tester and HPLC to determine the content of index components in the receiving solution, the in vitro transdermal absorption experiment was carried out by using isolated mouse skin as the transdermal barrier. The effects of classical penetration enhancers Azone, menthol and borneol on the in vitro transdermal penetration of ferulic acid, a water soluble component of Angelica sinensis, were studied, and the best compound penetration enhancer was selected. The experimental results show that the three penetration enhancers have a good effect on the penetration of ferulic acid in vitro, and the cumulative permeability of ferulic acid increases gradually within 24 hours. When used alone, the effect on the transdermal permeability of ferulic acid is menthol>borneol>azone., while used in combination, the effect on the transdermal permeability of ferulic acid is borneol>menthol>azone. And the best compound penetration enhancer is 2% borneol+2% menthol. The results show that the combination of them is better than azone, borneol and menthol alone. The cumulative permeability per unit area （Q24） in 24 hours is 34.32 μg/cm 2, and the multiple （ER） is 64.195, which is 8 times and 25 times higher than that of menthol and borneol alone, respectively, with the lag time less than 2 hours. The synergistic effect is obvious. In other words, the optimized compound penetration enhancer has a good effect on the penetration of ferulic acid, a water-soluble component of Angelica sinensis, and can provide a penetration enhancer for the development of Angelica sinensis and transdermal drug delivery preparations with Angelica sinensis as the main prescription. At the same time, by comparing the permeability of mouse skin and Strat-M TM membrane to ferulic acid, it is found that although the permeability of the two kinds of transdermal barrier is the same, the lag time of Strat-MTM membrane is much shorter than that of mouse skin, indicating that the barrier effect of Strat-MTM membrane on ferulic acid is less than that of mouse skin. Because the permeability of mouse skin is higher than that of human skin, if Strat-MTMmembrane is used in ferulic acid transdermal experiment in vitro, the transdermal lag time may be much different from the real situation.

Key words: Angelica sinensis （Oliv.） Diels, ferulic acid, penetration enhancer, skin penetration in vitro

中图分类号: 

  • TQ658