基于梅萨拉预混合物的延缓释放配方及其使用3D体内肠道模型对炎症性肠病的有效性评估
Sunil Kumar Sah1, Mamta Kumari1, Lohare Rahul Sanjay1
1Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Kolkata, West Bengal 700054, India.
这项研究使用预混合技术增强了梅萨拉 (一种治疗炎症性肠病的药物) 的特性,提高了其可溶性和透性,用于一种新型的延迟释放配方. 新配方有效地准结肠,而不需要涂层.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 生物制药生物制药公司
背景情况:
- 梅萨拉胺对于炎症性肠病 (IBD) 治疗至关重要.
- 现有的梅萨胺配方面临着溶解性,透性和向输送方面的挑战.
- 生物制药分类系统 (BCS) 属性修改是提高药物疗效的关键.
研究的目的:
- 使用预混合技术提高梅萨拉胺的溶解性和肠道透性.
- 开发一种新型的延迟释放梅萨胺配方,用于向结肠输送.
- 描述梅萨拉胺预混合物并评估其生物制药性质.
主要方法:
- 用喷雾干燥来制备梅萨拉预混合剂.
- 综合性表征包括颗粒大小分析,可溶性研究,FT-IR,PXRD,SEM,DSC和TGA.
- 进行了体外溶解和基于细胞的透性研究 (Caco-2,HUVEC,共同培养模型).
主要成果:
- 梅萨拉胺预混合物表现出较小的颗粒大小,增强的可溶性和降低的结晶性.
- 热分析表明稳定性有所改善,SEM显示球形粒子形态.
- 普雷米克斯配方显著增加了上皮和内皮的透性,并在炎症共同培养模型中证明了有效性.
结论:
- 普里米克斯技术成功地修改了梅沙胺的BCS特性,提高了其生物制药性质.
- 开发的延迟释放配方在没有功能性涂层的情况下,在肠道中实现了向药物释放.
- 这种方法为开发有效的针对结肠的梅萨胺口服配方用于IBD提供了一个有希望的策略.
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