用热激活的在位直肠凝制剂,用于使用eutectic混合物布洛芬
Fathima Firoz1, Tafika Yousef1, Yosra Asser1
1Bpharm graduate, Dubai Pharmacy College for Girls, Dubai, United Arab Emirates.
概括
这项研究开发了一种新型的Ibuprofen热敏 in situ凝用于直肠输送,为假药提供安全有效的替代品. 优化的配方显示药物释放速度快,没有粘膜刺激.
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:
- 肠直肠药物输送为系统性药物输送提供了一种替代途径.
- 传统的可以不方便,并具有可变的吸收.
- 在位形成凝提供局部和持续的药物释放.
研究的目的:
- 开发和描述一种热敏的in situ凝,用于直肠输送ibuprofen.
- 评估配方的物理化学性质,药物释放和安全性.
- 建立布洛芬in situ凝作为传统直肠剂型的可行替代品.
主要方法:
- 通过冷技术使用波洛克萨默188,波洛克萨默407和HPMC制备了热敏的in situ凝.
- 配方被评估为凝温度,时间,强度,可传播性,注射性,pH值,粘度和药物含量.
- 在实验室中进行了药物释放,粘结,体外建模,动力分析和组织病理学.
主要成果:
- 优化配方的凝温度在30-36°C之间,药物含量在93-110%之间.
- 选择的配方 (FS10,FS15) 在一小时内实现了完全的体外药物释放,具有可预测的动力学.
- 组织病理学证实在绵羊模型中没有粘膜刺激.
结论:
- 热敏性ibuprofen in situ凝是一种有前途的直肠载体.
- 这种配方提供了一个方便和有效的替代固体假药.
- 在现场开发的凝表现出良好的物理化学特性,快速释放药物,以及用于直肠注射的绝佳安全性.
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