利西诺普里尔粘膜粘合剂持续释放矩阵颗粒的优化和评估:体外和体外研究
Modhi F Alagili1, Bushra T AlQuadeib1, Lubna Y Ashri1
1Department of Pharmaceutics, College of Pharmacy, King Saud University, Saudi Arabia, P.O. Box 84428, Riyadh 11671, Saudi Arabia.
概括
这项研究开发了持续释放的Lisinopril (LIS-SR) 基质颗粒,以改善药物的透性. 优化的颗粒显示出出色的粘膜粘附性和持续的LIS释放长达8小时,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
- 材料科学 材料科学 材料科学
背景情况:
- 利西诺普里尔 (LIS) 是一种抗高血压药物,具有较高的水溶性,但透性较差.
- 低透性限制了传统LIS配方的治疗疗效.
- 开发先进的药物输送系统对于克服LIS生物可用性挑战至关重要.
研究的目的:
- 通过挤出/球体化来制定和优化持续释放的利西诺普里尔 (LIS-SR) 基质颗粒.
- 研究藻酸盐 (SA) 和酸盐 (CS) 度对LIS-SR颗粒特性的影响.
- 为了评估优化LIS-SR配方的体外和体外性能.
主要方法:
- 使用3 ^ 2的因数设计来优化由Avicel®,SA和CS组成的LIS-SR矩阵颗粒.
- 评估颗粒的性能,包括平均线路扭矩,颗粒大小,溶解速率和粘合力.
- 雇佣了用于数据分析和优化的Statgraphics软件.
- 进行了ex vivo粘膜粘合和透研究.
主要成果:
- 优化的LIS-SR颗粒 (2.159%SA,0.357%CS) 的平均直线扭矩为1.055Nm,颗粒大小为1830.8μm.
- 优化的配方在6小时后持续释放了56.2%的LIS,并在1小时后保持了73%颗粒的粘膜粘合.
- 活体研究显示,与自由LIS相比,LIS透率增加了1.7倍,持续释放时间长达8小时.
结论:
- 挤出/球体化是一种有效的方法,用于制备具有理想特性的LIS-SR矩阵颗粒.
- 优化的LIS-SR配方显示了增强的粘膜粘合和持续的药物释放,改善了治疗潜力.
- 这些LIS-SR颗粒为改善Lisinopril的药理动力学概况和患者遵守提供了有希望的方法.
相关概念视频
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