优化和评估基于盒子-Behnken设计的科尔奇辛补丁配方
Wenliang Dong1,2,3, Jiahao Feng1,2, Xiang Liu1,2
1College of Pharmaceutical Engineering of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, 301617, China.
研究人员使用BOX-Behnken设计 (BBD) 优化了胆固醇 (COL) 透皮贴片,以改善粘附和药物输送. 优化的贴片为口服COL提供了一个有希望的替代品,可能减少副作用.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 制定 发展 制定 发展
背景情况:
- 口服胆固醇 (COL) 的使用与胃肠道的副作用有关.
- 透皮药物递送系统提供了一种潜在的途径,可以绕过第一通代谢并减少全身毒性.
- 优化通过皮肤贴片的质量属性对于有效的药物输送至关重要.
研究的目的:
- 为了优化胆固醇 (COL) 通过皮肤贴片,以增强粘附性,药物释放和通过皮肤透.
- 使用BOX-Behnken设计 (BBD) 开发一种高性能的COL透皮配方.
- 为了评估优化COL透皮贴片的质量属性和稳定性.
主要方法:
- 使用BOX-Behnken设计 (BBD) 来优化COL含量,透增强剂 (亚,二醇) 度和溶剂蒸发时间.
- 为了评估这些变量的影响,进行了17次实验运行.
- 评估了包括粘附,体外释放 (IVRT) 和透皮透 (IVPT) 在内的质量属性. 还进行了富里埃变换红外光谱 (FT-IR) 和加速稳定性研究.
主要成果:
- 优化的配方含有9.8%的COL,5%的亚和5%的甘醇,在80°C蒸发23分钟.
- 优化的贴片表现出良好的粘附性质,并遵循48小时内药物释放和透的韦布尔方程.
- 获得的累积释放量为27.62mg,累积透量为256.34μg/cm2,没有显著的成分相互作用和良好的稳定性.
结论:
- BOX-Behnken设计有效优化了COL透皮贴片,产生了一种具有增强质量属性的配方.
- 开发的透皮系统显示了改善COL输送的潜力,为口服提供了替代品.
- 优化的COL透皮贴片有望减少与传统口服胆固醇治疗相关的副作用.
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