甘草次酸醇质体水凝胶贴剂的制备与透皮给药研究
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陕西省教育厅产业化中试项目(2010jc20);国家重大新药创制科技重大专项(2009ZX09502-019)


Preparation and in vitro percutaneous permeation profile of glycyrrhetinic acid ethosome hydrogel patch
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    摘要:

    目的探讨甘草次酸醇质体水凝胶贴剂的制备方法,并考察其体外透皮给药的规律与特点。方法注入法制备甘草次酸醇质体,考察其包封率、粒径与表面电位,再制备成水凝胶贴剂;采用改良Franz立式扩散池,HPLC法测定甘草次酸含量,评价甘草次酸醇质体水凝胶贴剂的体外透皮给药规律与特点。 结果甘草次酸醇质体外观为圆球形或椭球形,具有层状结构;其对于甘草次酸的包封率为(75.63±1.86)%,粒径为(106.2±20.54) nm,表面电位为(-41.3±2.8) mV。与甘草次酸水凝胶贴剂比较,甘草次酸醇质体水凝胶贴剂的

    Abstract:

    Abstract : Objective:To study the preparation methods of glycyrrhetinic acid ethosomes hydrogel patch and evaluate the laws and characteristics of transdermal drug delivery in vitro. Method: Glycyrrhetinic acid ethosomes was prepared by ethanol infusion method. Its entrapment efficiency, size and surface potential were investigated, and it was then used to prepare the hydrogel patch. The amount of penetrated glycyrrhetinic acid was determined by HPLC on modified Franz diffusion cells, and then the laws and characteristics of glycyrrhetinic acid ethosomes hydrogel patch transdermal drug delivery in vitro were evaluated. Results: Glycyrrhetinic acid ethosome has an appearance of spherical or ellipsoidal, and with a layered structure; its encapsulation efficiency for glycyrrhetinic acid was 75.63 ± 1.86%, particle size was 106.2 ± 20.54nm, and the surface potential was - 41.3 ± 2.8mV. The percutaneous rate and accumulative infiltration quantity of glycyrrhetinic acid ethosomes hydro gel patch are significantly higher than glycyrrhetinic acid hydro gel patch. The accumulative infiltration quantity of glycyrrhetinic acid ethosomes hdrogel is 5.5 times larger than that of glycyrrhetinic acid hydrogel patch, which shows an extremely significant (t-test, P﹤0.05). Conclusion:Glycyrrhetinic acid ethosomes can significantly improve hydrogel patch transdermal delivery effects, and show that ethosomes hydrogel patch is a new ideal form of transdermal for glycyrrhetinic acid. Keyword: Glycyrrhetinic acid; Ethosome;Hydrogel patch; Transdermal drug delivery

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  • 收稿日期:2011-04-02
  • 最后修改日期:2011-06-22
  • 录用日期:2011-06-27
  • 在线发布日期: 2011-07-22
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