评估聚合物对通过微流化生产的印梅他辛悬浮物重新悬浮性的影响
Mathias Dam Mønster Sørensen1, Fanjin Wang2, Maryam Parhizkar2
1Department of Physics, Chemistry, and Pharmacy, University of Southern Denmark, Campusvej 55, 5230 Odense, Denmark.
概括
像PVP K30,PVP K17和P338这样的稳定剂增强了长效注射悬浮剂的稳定性. 稳定剂的选择极大地影响了复杂性,温度会对含有聚酸盐的配方产生负面影响.
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:
- 长效注射剂通过减少剂量频率来改善慢性疾病的治疗坚持.
- 长效注射剂中常见的纳米或微悬浮容易产生物理不稳定性,例如粒子生长和凝结.
- 确保这些配方的物理稳定性和再悬浮性对于有效的药物输送至关重要.
研究的目的:
- 评估各种稳定剂在防止印梅他辛悬浮液中颗粒生长和凝结方面的有效性.
- 评估不同稳定剂及其度对印梅他辛悬浮物的再悬浮性的影响.
- 调查储存温度和添加复悬浮剂对配方稳定性和复悬浮性的影响.
主要方法:
- 测试了八种稳定剂 (多酸盐20,多酸盐80,波洛克萨默188,波洛克萨默338,多维尼尔罗利K17,多维尼尔罗利K30,维生素E-TPGS,酸硫酸盐) 和聚乙烯糖醇4000).
- 准备和存储Indomethacin悬浮剂在三个不同的温度下四周.
- 评估了稳定性 (颗粒生长,凝结) 和复杂性,并使用统计和机器学习模型进行分析.
主要成果:
- 聚乙烯罗利 K30 (PVP K30),聚乙烯罗利 K17 (PVP K17) 和波洛克萨默 338 (P338) 在保持稳定的印美他辛悬浮液与最小的颗粒生长方面表现出有效性.
- 稳定器类型被确定为通过统计和机器学习建模影响重置可靠性的关键因素.
- 较高的储存温度对复杂性产生了负面影响,特别是在含有聚酸盐的配方中. 聚乙烯甘醇4000在某些配方中显示出有限的益处,甚至对某些配方的复杂性产生负面影响.
结论:
- PVP K30,PVP K17和P338是长期作用的注射性印梅他辛悬浮物的有效稳定剂,促进了物理稳定性.
- 配方设计必须考虑稳定剂的选择和储存条件,以确保有效的药物输送的最佳再悬浮性.
- 可能需要对再悬浮剂进行进一步的研究,以克服特定悬浮类型的温度诱导的不稳定性.
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