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协同形态与深层阳性溶剂的配方,用于通过皮肤给药
Yannick Guinet1, Laurent Paccou1, Alain Hédoux1
1UMR 8207-UMET-Unité Matériaux et Transformations, Université de Lille, CNRS, INRAE, Centrale Lille, F-59000 Lille, France.
Pharmaceutics
|June 28, 2023
概括
在局部配方中稳定无形布洛芬是有效药物输送的关键. 这项研究发现,特定的深溶解溶剂和共同形态混合物可以防止布洛芬再结晶,增强皮肤透.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 物理化学 物理化学
背景情况:
- 通过皮肤递送药物提供了口服药物的替代方案,最大限度地减少副作用.
- 优化局部配方需要增强药物透和物理稳定性.
- 像布洛芬这样的无形药物容易重新结晶,从而对疗效产生负面影响.
研究的目的:
- 在新型局部配方中研究无形布洛芬的物理稳定性.
- 探索使用深度环氧溶剂 (DES) 和共同形态混合物的稳定策略.
- 了解依据布洛芬再结晶抑制的机制.
主要方法:
- 使用低频拉曼光谱分析ibuprofen:L-menthol相图.
- 在甲基醇:薄荷醇DES中研究无形布洛芬的稳定性.
- 通过化和冷研磨来制备和表征氨酸-氨酸共形混合物.
- 确定玻璃过渡温度 (Tg) 和分析结相互作用 (拉曼光谱).
主要成果:
- 在不同度的ibuprofen:L-menthol混合物中观察到ibuprofen的再结晶.
- 无形布洛芬在提摩尔:孟托尔DES中配制时表现出增强的稳定性.
- 化处理的氨酸-氨酸混合物稳定了无形氨酸,而冷磨粉版本显示了再结晶.
- 重结晶抑制与异分子键的优先形成有关,防止了不论Tg的IBUPROFEN二分化.
结论:
- 甲醇:醇DES和化处理的氨酸 - 布洛芬混合物有效地稳定无形布洛芬.
- 异分子结合在防止局部配方中的布洛芬再结晶方面发挥着至关重要的作用.
- 结果为设计稳定的无形药物配方提供了洞察力,用于通过皮肤递送.
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