一种使用喷雾干燥固体分散技术的新型Posaconazole口服配方:体外和体外研究
Kaushika Patel1,2, Vijay Kevlani3, Shreeraj Shah4
1Department of Pharmaceutical Technology, L. J. Institute of Pharmacy, L J University, Ahmedabad, 382 210, India.
Drug delivery and translational research
|November 11, 2023
概括
这项研究开发了一种用于抗真菌药物Posaconazole的新型喷雾干燥分散配方,增强溶解性并实现胃保持性修饰释放以改善生物可用性.
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
- 配方 开发 发展
背景情况:
- 固体分散 (SD) 技术是为了提高溶解度而建立的.
- 无形固体分散 (ASD) 与可溶性改善一起提供了修改释放的潜力.
- 喷雾干燥是一种可扩展的技术,用于生产无形固体分散 (ASD).
研究的目的:
- 为Posaconazole开发一种新的三元喷雾干燥分散 (SDD) 胃保持性配方.
- 为了提高Posaconazole的溶解性,并实现改性释放以提高生物可用性.
- 为了评估配方的稳定性和in-vivo性能.
主要方法:
- 使用Soluplus®和Gelucire 43/01作为SD载体.
- 采用喷雾干燥技术和优化配方变量,使用3 ^ 2全工厂设计.
- 使用DSC,PXRD,SEM,GC-MS/HS对优化的批量进行了表征,并评估了体外药物释放,稳定性,体外停留时间和药理动力学.
主要成果:
- 优化的SDD配方证实了Posaconazole的无形状态.
- 描述揭示了微米大小的不规则颗粒与消除的残留溶剂.
- 与市场上销售的产品相比,这种配方表现出良好的稳定性,延长了胃内停留时间,并提高了大鼠的生物可用性.
结论:
- 成功开发了一种基于SDD的新型三元性胃阻塞配方,用于Posaconazole.
- 该配方显著改善了溶解性,修改了药物释放,并提高了生物可用性.
- 这种方法对开发有效的胃保持药物递送系统具有前景.
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