甜味剂对PVP K30-A溶液具有塑化作用,用于固定剂量无形黄素-素固体分散的热挤出
Kamil Wdowiak1, Lidia Tajber2, Andrzej Miklaszewski3
1Department of Pharmacognosy and Biomaterials, Poznan University of Medical Sciences, 3 Rokietnicka St., 60-806 Poznan, Poland.
Pharmaceutics
|May 25, 2024
概括
这项研究开发了使用红醇作为可塑剂的黄素和hesperetin的无形固体分散. 这种配方显著改善了药物的溶解性和溶解性,提供了潜在的神经保护益处.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 药物运输 药物运输 药物运输
背景情况:
- 黄素和hesperetin显示出潜在的神经保护活性.
- 这些化合物的低溶解性限制了它们的治疗疗效.
- 开发先进配方对于提高生物可用性至关重要.
研究的目的:
- 为了开发固剂无形固体分散的黄素和hesperetin.
- 为了克服这些活性化合物的不良溶解性和溶解限制.
- 评估塑化剂对无形固体分散制剂的影响.
主要方法:
- 热挤出用于准备无形固体分散.
- 甜味剂 (乙醇,醇,醇) 被研究为PVP K30的增塑剂.
- 粉末X射线衍射,热分析和红外光谱学被用于表征.
- 进行了稳定性研究和药物参数 (溶解,可溶性,透性) 的评估.
主要成果:
- 红醇被确定为最佳的塑化剂,降低PVP K30.0的玻璃过渡温度.
- 库尔库和素的无形固体分散物已成功制备并通过表征技术得到证实.
- 无形状态保持稳定至少6个月.
- 优化的配方 (15%的活性化合物含有红醇) 在溶解率,溶解度和体外透性方面显著改善.
结论:
- 固定的剂量无形固体分散的黄素和hesperetin可以有效地准备使用热挤出与红醇作为可塑剂.
- 这种方法成功地提高了活性化合物的可溶性和溶解性.
- 开发的配方有望改善神经保护的治疗结果.
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