对于在各种溶剂中应用于人类表皮膜的化合物的定量结构透性关系
Michael S Roberts1, Qian Zhang2, Lorraine Mackenzie3
1Clinical and Health Sciences, University of South Australia, Adelaide, Australia; Therapeutics Research Centre, Frazer Institute, University of Queensland, Brisbane, Australia.
概括
溶剂的选择显著影响了化合物如何透到人体皮肤. 了解溶剂-皮肤-溶液相互作用对于优化局部药物输送和预测皮肤透至关重要.
科学领域:
- 皮肤药物递送和透增强.
- 溶剂和溶液的物理化学性质.
- 角层 (SC) 生物物理和脂质相互作用.
背景情况:
- 优化局部和透皮药物输送需要深入了解皮肤透.
- 溶剂特性极大地影响活性药物成分 (API) 在角层的溶解性和运输.
- 化合物作为模型溶液来研究基本的皮肤透机制.
研究的目的:
- 调查溶剂-皮肤-溶液相互作用对人类表皮透化合物的影响.
- 阐明溶剂性质 (分子大小,可溶性参数) 在调节皮肤透中的作用.
- 了解由于溶剂与角层相互作用而改变透的机械基础.
主要方法:
- 人类表皮透研究使用弗朗茨扩散细胞.
- 对三种化合物在各种溶剂中的透流量和滞后时间的评估.
- 测量化合物在溶剂和角层中的溶解度,溶剂吸收,皮肤水分和皮肤间的水分损失 (TEWL).
主要成果:
- 在不同的溶剂中观察到表皮流量和滞后时间的显著变化.
- 在使用特定溶剂时,观察到提高透性,延长延迟时间和减少扩散性.
- 溶剂进入角层的吸收增加了化合物的溶解性和热力学活性,影响了透动态.
结论:
- 溶剂吸收到角层中调节化合物的溶解性,透性和滞后时间.
- 溶剂诱导的储效应可以延长滞后时间,但不会改变稳定状态运输.
- 了解这些相互作用是设计有效的局部配方和预测药物透概况的关键.
关键词:
汉森溶解度参数 汉森溶解度参数补水 补水 水分 补水 补水时间滞后时间滞后.最大流量是最大的流量.可溶性 可溶性 溶性溶剂的吸收 溶剂的吸收角质层 (stratum corneum) 是一个层.更多相关视频
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