结合离子对策略和皮肤透增强剂,开发持续释放的帕利皮里补丁
Yafang Xu1, Shuai Zhang1, Cong Li1
1Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning 110016, China.
International journal of pharmaceutics
|October 23, 2024
概括
使用离子配对和透增强剂开发了一种新的持续释放帕利皮里 (PAL) 补丁. 这种透皮贴片可以改善药物利用和控制释放,增强治疗潜力.
科学领域:
- * 制药科学 制药科学
- * 药物输送系统 药物输送系统
背景情况:
- *帕利佩里 (PAL) 是一种抗精神病药物,需要改进的输送方法.
- * 透皮贴片为口服提供了一个有希望的替代品,用于持续释放药物.
- * 通过皮肤递送药物的挑战包括药物溶解性差和穿透皮肤屏障.
研究的目的:
- * 开发一种持续释放的帕利佩里透皮贴片.
- * 通过离子对策略来增强药物粘合的可混合性和控制药物释放.
- * 通过皮肤透增强剂 (PPEs) 改善paliperidone的皮肤透.
主要方法:
- * 开发使用离子对策略和PPE的帕利佩里补丁.
- *通过Box-Behnken设计和体外透研究优化贴片配方 (55微米厚,7%PAL-LA,9.7%POCC).
- *药物动力学评估和机制研究,以评估持续释放和药物利用.
主要成果:
- *优化贴片显示持续释放,平均停留时间 (MRT0-t) 较长18.35±3.11小时,生物可用性 (BA) 较高63.14%.
- *开发的贴片显示了可比的Cmax与口服 gavage,但药物释放显著延长.
- * 离子对的形成有效地改善了药物的混合性和受控释放特性.
结论:
- *成功开发了一种持续释放的帕利佩里透皮贴片.
- * 离子配对和PPE的组合提供了一种有效的策略,可以增强通过皮肤递送药物的效果.
- * 开发出来的贴片具有有利的特性,可持续释放药物,具有良好的药物聚合物混合性和有效的药物利用.
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