奥尔梅沙坦美多克索米尔的宿主-客人复杂化由Heptakis ((2,6-di-O-methyl) -β-cyclodextrin:与辅助剂的兼容性研究
Dana Emilia Man1, Ema-Teodora Nițu2,3, Claudia Temereancă4
1Faculty of Medicine, "Victor Babeş" University of Medicine and Pharmacy, 2 Eftimie Murgu Square, 300041 Timisoara, Romania.
Pharmaceutics
|January 8, 2025
概括
奥尔梅沙坦麦多克索米尔 (OLM) 含有肝素的综合体{2,6-di-O-methyl) -β-cyclodextrin (DMβCD) 提高了溶解度. OLM/DMβCD复合物与大多数辅助剂兼容,但在高温下与酸和α-乳糖单酸发生相互作用.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 物理化学 物理化学
背景情况:
- 奥尔梅沙坦美多克索米尔 (OLM) 是一种抗高血压剂,其水溶性差,生物可用性低.
- 宿主-客人包容综合体 (ICs) 是一种提高难溶性药物的物理化学性质的策略.
- 赫普塔基斯的2,6-di-O-methyl) -β-cyclodextrin (DMβCD) 被研究为OLM的宿主.
研究的目的:
- 开发和表征一个包含复合物 (IC) 的奥尔梅沙坦美多克索米尔 (OLM) 与heptakis(2,6-di-O-甲基) -β-环氧化 (DMβCD).
- 评估OLM/DMβCDIC与各种制药辅助剂的兼容性.
主要方法:
- 使用相溶性,热分析技术,FTIR,PXRD,UV光谱和分子建模,形成和描述OLM/DMβCDIC.
- 使用热和光谱方法评估药物辅助剂兼容性.
主要成果:
- 一个1:1的OLM:DMβCD纳入复合物成功形成,表现出改变的物理化学性质.
- 在环境条件下,OLM/DMβCDIC与大多数测试的辅助剂没有显著的相互作用.
- 在高于100°C的温度下,OLM/DMβCDIC与酸或α-乳糖单水酸之间观察到热不相容.
结论:
- OLM/DMβCD纳入复合体是开发改进的药物配方的有希望的候选者.
- 需要仔细选择辅助剂,特别是避免在高温制造过程中使用酸和α-乳糖单.
关键词:
兼容性兼容性兼容性的兼容性循环德克斯特林 (cyclodextrins) 是一个循环德克斯特林.辅助剂 辅助剂 辅助剂包容复杂的包容复杂的包容奥尔梅沙坦的美多克索米尔.提高可溶性 提高可溶性频谱学技术的使用.热方法 热方法 热方法更多相关视频
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