在肠道吸收部位指导下开发和评估Mirabegron口服可分解可控释放片的开发和评估
Mohammed I Ghanem1, Shimaa M Ashmawy2, Gamal M El Maghraby1
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt.
AAPS PharmSciTech
|July 23, 2024
概括
这项研究开发了一种口服分解控制释放片 (ODCRT) 用于mirabegron (MB) 输送,匹配过度活性膀 (OAB) 症状时间. ODCRT提供了即时的MB释放,以快速缓解症状,并持续释放长时间的效果.
科学领域:
- 制药技术 制药技术 制药技术
- 药物输送系统 药物输送系统
- 药理动力学 药理动力学
背景情况:
- 过度活性膀 (OAB) 综合征表现出时代生物学模式,需要定时释放药物.
- 米拉贝格伦 (MB) 的吸收在胃肠道上有所变化,影响最佳的输送策略.
- 目前的口服配方可能与OAB症状不一致,影响治疗疗效.
研究的目的:
- 设计一个口服分解控制释放片 (ODCRT) 的mirabegron (MB).
- 为了实现特定部位的药物释放,反映过度活性膀 (OAB) 的时代生物学.
- 为了将充满剂量的瞬间释放与剩余MB的持续释放相结合.
主要方法:
- 评估了子的肠道透性,以确定MB吸收部位.
- 通过与酸一起干燥共磨MB开发出一种快速溶解的分量.
- 使用乙醇辅助联合处理与Eudragit S100.配制一种延迟释放分离物.
- 使用DSC,X射线衍射和体外释放研究的特征化配方.
- 在持续的pH变化下制造和评估ODCRTs用于释放配置文件.
主要成果:
- 米拉贝格朗证明了在大肠和大肠中的偏好透.
- 与酸共同研磨产生了快速溶解的共同形态MB粉末.
- MB与Eudragit S100 (1:5) 的共同变形导致了pH依赖的释放,主要是在pH7.4.4时.
- 开发的ODCRT在口腔环境中释放了43.5%的MB,并延迟释放至pH7.4.
结论:
- 成功制造了一种ODCRT用于mirabegron的ODCRT,该ODCRT的指导是取决于位点的吸收原理.
- 在ODCRT提供了立即释放的负载分数的快速症状发作.
- 延迟释放分数确保了持续的治疗效果,与OAB时代生物学保持一致.
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