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The preparation of paeonol transdermal delivery systems based on the microemulsion-based gels and its pharmacokinetics characters
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- Author:
- No author available
- Journal Title:
- Acta Pharmaceutica Sinica
- Issue:
- 2
- DOI:
- No doi available
- Key Word:
- 丹皮酚;微乳凝胶;微透析;经皮给药;药代动力学
Abstract： 为构建基于微乳凝胶(microemulsion-based gels,MBGs)新载体的丹皮酚经皮给药系统,采用皮肤、血液双位点同步微透析结合LC/MS联用技术测定丹皮酚微乳、微乳凝胶及市售丹皮酚软膏在大鼠皮肤、血液中的药物浓度随时间的变化过程,并对其药代动力学参数进行比较分析.方法学研究表明,丹皮酚线性探针体内回收率(gin vivo)为(69.7±4.8)％,同心圆探针体内回收率为(51.6±7.2)％.大鼠腹部脱毛,分别给予丹皮酚微乳(1％丹皮酚)、微乳凝胶和市售丹皮酚软膏,以PBS (pH 7.4)溶液作为灌流液,灌流速度为5μL·mL-1,每隔20 min 收集1次微透析样品,共收集12 h,透析液采用LC/MS进行测定.皮肤药动学结果表明丹皮酚微乳、微乳凝胶与市售软膏相比,显著提高了药物在皮肤组织中的浓度;血液药动学结果表明微乳凝胶与市售软膏具有相近的生物利用度,但前者的血药浓度更平稳.本研究所构建的丹皮酚微乳凝胶有望为皮肤湿疹的治疗提供一种新的制剂；所建立的微透析/LC-MS联用技术能够在体、同步、实时监测大鼠皮肤、血液中的药物浓度,为经皮给药药代动力学研究提供了新的方法.
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