开发一种具有多重释放特征的胺持续释放颗粒
Sijun Wu1, Guoming Zhou1, Xi Wang1
1College of Pharmaceutical Engineering of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, 301617, China.
AAPS PharmSciTech
|September 25, 2024
概括
为了改善类风湿性关节炎的治疗,开发了新型胺 (SH) 持续释放颗粒. 这些颗粒可以最大限度地减少胃肠道副作用,并提供可控的药物释放,以改善患者的治疗结果.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 类风湿病学 类风湿病学
背景情况:
- 对于类风湿性关节炎的临床使用sinomenine化物 (SH) 受到胃肠道副作用的限制.
- 老年患者是类风湿性关节炎的主要人口,在胃排空方面表现出显著的变化.
- 胃空化的个体差异可能会影响药物的疗效,并导致胃肠道不良事件.
研究的目的:
- 开发具有多重释放特性的创新型胺 (SH) 持续释放颗粒.
- 为了减轻与SH管理相关的胃肠道副作用.
- 为了减少个体胃空化的变化对SH药物疗效的影响.
主要方法:
- 使用全因数设计,优化药物载荷层的配方.
- 制备SH持续释放颗粒,包括常规和肠膜涂层类型.
- 在体外溶解测试以评估酸性和肠道环境中的药物释放概况.
主要成果:
- 最佳配方产生了96.05%的颗粒产量,SH封装效率为83.36%.
- 颗粒呈现出高圆度 (0.971) 和受控的颗粒大小分布 (跨度为0.808).
- 在体外试验证实了4小时的SH在酸中的释放和双相释放 (4小时的抗酸性,然后8小时的肠道释放).
结论:
- 开发的SH持续释放颗粒表现出稳定且符合溶解的溶解行为.
- 该配方具有出色的物理稳定性和外观.
- 这项研究为创新的SH药物配方策略提供了宝贵的参考.
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