洞察影响伊斯拉特拉维尔植入物中乙烯基乙烯酸共聚物晶度的因素
Xiaolong Zhu1, Ashish Punia1, Daniel Skomski1
1Analytical Research and Development, Merck & Co., Inc., Rahway, New Jersey 07065, United States.
Molecular pharmaceutics
|March 19, 2024
概括
这项研究分析了islatravir植入物中的乙烯-乙酸乙烯 (EVA) 结晶性. 药物加载增加了EVA结晶,而马辐射和表面层显著影响了植入物特性.
科学领域:
- * 制药科学 制药科学
- * 材料科学 材料科学
- * 聚合物化学 的研究.
背景情况:
- * 伊斯拉特拉维尔是一种强大的核酸逆转录酶转位抑制剂 (NRTTI),在艾滋病毒治疗中表现有前途.
- * 乙烯-乙酸 (EVA) 共聚合物植入物通过热挤出为伊斯拉特拉维尔提供了潜在的药物输送系统.
- *EVA结晶性是影响植入物的物理,质和药物释放性能的关键因素.
研究的目的:
- *系统地调查影响伊拉特拉维尔植入物中EVA结晶性的因素.
- * 了解药物加载,辅助剂和杀菌对EVA聚合物矩阵特性的影响.
- * 为了将EVA结晶性与植入物性能相关联,以优化药物输送.
主要方法:
- *差分扫描热量计 (DSC) 用于分析EVA结晶度.
- * 固态核磁共振 (NMR) 光谱学.
- * 用超微红切术来准备和分析薄切片的植入物.
- *对玛辐射灭菌效应的评估.
主要成果:
- *发现伊斯拉特拉维尔加载促进了EVA结晶.
- *硫酸 (BaSO4) 负载对EVA结晶度的影响很小.
- * 马辐射显著改变了EVA的结晶性和表面特征.
- * 与核心相比,植入物表面层表现出更高的结晶性.
结论:
- *药物加载对islatravir植入物中的EVA结晶产生积极影响.
- *绝育方法和植入物位置 (表面与核心) 极大地影响了EVA的结晶性.
- *了解这些因素对于设计强大而有效的islatravir-eluting EVA植入物至关重要.
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