高极性基聚烯酸盐压力敏感粘合剂在瑞扎特里普坦通过皮肤递送药物贴片中的应用
Cong Li1, Donghui Hu2, Yafang Xu1
1School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning 110016, China.
International journal of pharmaceutics
|October 26, 2024
概括
这项研究开发了一种新型的瑞扎特里普坦透皮贴片,使用基压敏粘合剂 (PSA) 和离子对策略,用于持续的药物输送. 优化的贴片显示了提高药物的可混合性和有效性,而不会刺激皮肤.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 药物输送系统 药物输送系统
背景情况:
- 通过皮肤递送的药物在某些药物中比口服药物更有优势.
- 提高压力敏感粘合剂 (PSA) 中的药物混合性对于有效的透皮贴片配方至关重要.
- 利扎特里普坦 (Rizatriptan,简称RIZ) 是一种常用于治疗偏头痛的口服药物.
研究的目的:
- 设计一种使用高极性基PSA (AAOH-45) 和离子对策略的瑞萨特里普坦透皮贴片.
- 为了研究这种增强的药物-PSA混合性背后的分子机制.
- 优化药物持续释放的配方,并评估其药理动力学特征和安全性.
主要方法:
- 准备和表征无基,离子对复合物和含基的PSA.
- 优化配方因子,包括反离子,PSA和药物加载.
- 药理动力学研究和皮肤刺激测试,以评估性能和安全性.
- 分子模拟,FTIR,13C NMR,DSC,以及风湿学,以研究药物-PSA混合性和特性.
主要成果:
- 一种含有20% RIZ-Oleic 酸和80% AAOH-45 PSA 的优化配方实现了持续的药物输送 (MRT0-t = 20.21 ± 0.61 h).
- 透皮贴片没有显示皮肤刺激.
- 药物-PSA混合性与PSA中的基含量 (2-HEA) 有正相关,这归因于两极相似性,较低的流动性和更强的分子间相互作用.
结论:
- 高极性基PSA和离子对策略的组合有效地增强了瑞萨的混合性,并使持续的透皮输送成为可能.
- 这种方法提供了一个可行的替代口服瑞萨特里普坦的管理,改善了药理动力学特征和安全性.
- 这项研究为开发高药载荷透皮贴片提供了有价值的见解.
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