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开发和评估含有克洛皮多格雷尔二硫酸盐和阿司匹林的即时释放片-战略,以优化组合配方
Shahnaz Usman1, Muhammad Akram2, Anab Usman3
1Department of Pharmaceutics, RAK College of Pharmacy, RAK Medical and Health Sciences University, RAS, Al-Khaimah, UAE.
PloS one
|May 23, 2024
概括
这项研究开发了一种稳定,立即释放的固剂组合药片,即克洛皮多格雷尔二硫酸盐和阿司匹林. 新配方通过具有成本效益的直接压缩方法提高了阿司匹林的稳定性和患者的遵守性.
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:
- 阿司匹林对水分高度敏感,在固定剂量组合产品中构成稳定性挑战.
- 改善患者的遵从性和方便性对于管理需要双重抗血小板治疗的疾病至关重要.
研究的目的:
- 设计和开发一个稳定的立即释放的固剂组合药片克洛皮多格雷尔二硫酸盐和阿司匹林.
- 为了增强组合药片内对水分敏感的阿司匹林的稳定性.
- 通过简化剂量表单来提高患者的遵守性和便利性.
主要方法:
- 使用响应表面方法与32个因子设计 (使用设计专家软件) 来优化平板电脑的组成.
- 研究的独立变量 (微晶纤维素102,先化粉,酸纤维素) 以及它们对依赖变量的影响 (分解,易碎性).
- 进行了配方前后的质量控制测试,体外药物释放研究和应力稳定性测试.
主要成果:
- 优化的配方表现出可接受的脆性 (≤1.0%) 和分解时间.
- 实现药物快速释放,克洛皮多格雷尔和阿司匹林在20分钟内释放的80%以上.
- 压力研究证实了活性药物成分 (API) 与辅助剂在15天内的良好兼容性和稳定性.
结论:
- 直接压缩方法是生产这种固定剂量组合药片的成本高效方法.
- 开发的配方增强了阿司匹林的稳定性,并为患者提供了更好的方便和合规性.
- 设计专家软件有助于高效的配方优化,最大限度地减少试验和错误.
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