聚合对长效注射悬浮剂体外性能的影响
Nilesh Malavia1, Quanying Bao1, Daniela Amaral Silva2
1University of Connecticut, Department of Pharmaceutical Sciences, Storrs, CT 06269 USA.
International journal of pharmaceutics
|February 26, 2025
概括
颗粒聚合显著影响长效注射剂 (LAI) 悬浮药物释放. 了解粒子状态和剪切力效应对于优化LAI配方性能和可预测性至关重要.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 长效注射 (LAI) 悬浮剂对于持续的药物输送至关重要.
- 粒子聚合被认为是影响LAI性能的关键因素.
- 影响LAI悬浮中的颗粒聚合的因素需要进一步阐明.
研究的目的:
- 调查颗粒大小变化,剪切力和聚合状态对LAI悬浮体体内药物释放的影响.
- 探索不同的制备方法和配方差异如何影响粒子行为.
- 了解粒子特征和药物释放概况之间的关系.
主要方法:
- 制备五种同等的medroxyprogesterone acetate (MPA) LAI悬浮剂,配方和加工方式各不相同.
- 物理化学表征:颗粒大小,形态,沉积值,粘度.
- 评估剪切力对聚合物的影响 (震动,注射器使用,超声波,).
- 在体外溶解研究中,使用了一种新的内部适配器.
主要成果:
- MPA悬浮剂含有弱聚合物,强聚合物或初级颗粒.
- 弱聚合悬浮剂 (FA,FC) 显示了剪切灵敏度和可变释放.
- 强度聚合悬浮液 (FB) 抵抗了剪切,但在介质中脱聚,导致更快的释放.
- 初级颗粒悬浮物 (FD,FE) 在溶解过程中聚合,导致释放速度较慢.
结论:
- 颗粒聚合状态对MPA LAI悬浮体中的体外药物释放具有关键影响.
- 聚合物在剪切力下的行为影响药物释放动力学.
- 对粒子状态和剪切反应的彻底表征对于优化LAI配方以预测药物释放至关重要.
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