米尔塔扎含有聚合物微粒的快速释放片:一种新的配方-体外和体内研究
Sara Nageeb El-Helaly1, Amira A Rashad2
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt. sara.elhelaly@pharma.cu.edu.eg.
Drug delivery and translational research
|February 14, 2024
概括
这项研究开发了使用聚合物微粒的米尔塔扎 (MTZ) 快速释放片剂配方. 新配方显著提高了子的MTZ溶解性和口服生物利用性.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 药理动力学 药理动力学
背景情况:
- 重度抑郁症是一种常见的疾病,用米尔塔扎 (MTZ) 治疗,这是一种BCSII类药物,由于广泛的第一通代谢,口服生物利用率低 (50%).
- 提高MTZ的可溶性和生物利用性对于有效治疗抑郁症至关重要.
研究的目的:
- 开发一种基于聚合物菌根的新型快速释放药片 (MTZ-PMs-RRT),以提高米尔扎 (MTZ) 的溶解性和口服生物利用性.
主要方法:
- 使用Solutol® HS 15,Brij 58和Transcutol® P.进行了Mirtazapine加载的聚合物 (MTZ-PMs) 的制备.
- 试验室表征包括颗粒大小,PDI,泽塔电位,溶解度和稳定性.
- MTZ-PMs被转化为干粉并压缩成快速释放片 (MTZ-PMs-RRT).
- 实验室药片评估和子体内药理动力学研究进行,将MTZ-PMs-RRT与Remeron®药片进行比较.
主要成果:
- 配方的MTZ-PM表现出增强的溶解性和稳定性.
- MTZ-PMs-RRT药片符合质量属性和溶解的药库标准.
- 在子中进行的药理动力学研究表明,MTZ生物可用性显著增加,与传统药片相比,MTZ的相对生物可用性达到153%.
结论:
- 开发的MTZ-PMs-RRT配方有效地提高了米尔塔扎的溶解性,稳定性和口服生物可用性.
- 这种简单而可扩展的制造工艺为改善米尔塔扎的治疗疗效提供了有希望的方法.
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