一种挥发性药物在皮肤上应用后的皮肤药理学
Andrea Pensado1,2, Panagiota Zarmpi1,3, Jane White4
1Department of Life Sciences, University of Bath, Claverton Down, Bath, BA2 7AY, UK.
这项研究验证了体外释放,皮肤透和角层 (SC) 采样,以量化挥发性药物输入率. 这些方法准确地评估含甲基酸盐 (MeSA) 的局部产品的皮肤吸收.
科学领域:
- 皮肤病学 皮肤病学
- 药理动力学 药理动力学
- 配方科学科学 配方科学
背景情况:
- 评估局部药物输送需要了解皮肤透率和输入速度.
- 由于潜在的蒸发,挥发性药物存在独特的挑战.
- 角层 (SC) 取样提供了一种测量药物吸收和清除的方法.
研究的目的:
- 评估体外释放,皮肤透和SC采样对量化挥发性药物输入的有用性.
- 为了比较体外和体外的SC药物吸收和清除动力学.
- 评估这些方法对局部挥发性药物产品的有效性.
主要方法:
- 使用膜进行体外药物释放研究.
- 在体外猪皮肤透测试.
- 在体外和体外 (人体) 角层 (SC) 取样,以测量不同时间点的甲基酸盐 (MeSA) 水平.
- 来自SC的药物清除的动态分析.
主要成果:
- 从配方中释放的药物是相似的 (在6小时内约65%).
- 在体外皮肤透显示在24小时内~50%的剂量交叉.
- 在体外SC药物吸收率>10倍高于体内;然而,体外和体内SC清除率相似.
- 质量平衡表明体外显著的蒸发 (在2小时内约33%).
结论:
- 在体外释放和皮肤透测试与SC采样相结合,是评估局部挥发性药物产品的有效工具.
- MeSA的皮肤药理动力学与配方中的药物负载成正比.
- 这些补充方法可以量化挥发性药物的输入速率到皮肤和通过皮肤.
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