使用药物无形固体分散剂制备Dronedarone的每一个os配方
Afroditi Kapourani1, Alexandra-Eleftheria Manioudaki1, Konstantinos N Kontogiannopoulos1
1Laboratory of Pharmaceutical Technology, Division of Pharmaceutical Technology, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
Polymers
|November 14, 2023
概括
这项研究使用Soluplus®开发了无人机 (DRN) 的无形固体分散 (ASD),以克服其不良溶解性. 由此产生的DRN ASDs表现出增强的药物释放和物理稳定性,提供了一个有前途的配方策略.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 德罗纳达龙 (DRN) 是一种抗心律失常药物,对心律失常有显著的治疗潜力.
- 对于有效的药物配方和输送来说,DRN的低水溶性是一个重大挑战.
- 无形固体分散 (ASDs) 是一种可行的策略,可以提高难溶性药物的可溶性.
研究的目的:
- 研究基于无人机的无形固体分散 (ASD) 的发展和表征.
- 通过ASD配方提高无人机 (DRN) 的水溶性和溶解率.
- 评估优化的DRN ASDs的物理稳定性和药物释放性能.
主要方法:
- 评估了无人机的玻璃形成能力 (GFA) 和热稳定性.
- 通过薄膜造和溶剂转移方法选了各种聚合物 (HPMC,PVP,PVP/VA,SOL,EPO) 进行ASD形成.
- 使用融化灭方法准备了优化的DRN ASD,并使用pXRD和ATR-FTIR进行了它们的特征化.
- 在非沉条件下评估的体外药物释放.
主要成果:
- 德罗内达龙被确定为一种稳定的玻璃原体 (GFA III),在温度上稳定到~200°C.
- Soluplus® (SOL) 被确定为形成DRN ASDs的最有前途的载体.
- 物理化学表征证实了DRN在SOL中完全无形化,物理稳定性至少为3个月.
- 试验室研究显示,药物持续超和至少8小时,表明溶解的增强.
结论:
- 使用Soluplus® (SOL) 溶解制备的无形固体分散剂有效提高药物的溶解性和溶解性.
- 开发的DRN-SOL ASDs表现出良好的物理稳定性和持续的药物释放,解决了配方挑战.
- 这种配方方法有望改善无人机在治疗心律失常的治疗效果.
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