在固态和水溶液中抗氧化剂二和衍生式环氧二之间的复合
Laura Catenacci1, Alexios I Vicatos2, Milena Sorrenti1
1Department of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy.
Pharmaceuticals (Basel, Switzerland)
|June 1, 2023
概括
这项研究使用各种环极素 (CD) 提高了丁 (PTB) 的溶解度. 修改后的CD有效地形成了包含综合体,显著增加了PTB.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 像甲 (PTB) 这样的生物活性化合物的水溶性差,限制了它们在药物中的应用.
- 开发提高溶解度的策略对于药物开发至关重要.
研究的目的:
- 准备和表征水溶性环极素 (CD) 含有利 (PTB) 的综合体.
- 评估不同修改后的CD和制备方法在提高PTB溶性的有效性.
主要方法:
- 使用固态 (联合研磨,,微波辐射) 和基于溶液的方法制备PTB-CD纳入复合物.
- 使用差分扫描热度计 (DSC) 和富里埃变换红外光谱法 (FTIR) 进行复合物的表征.
- 通过相位可溶性分析评估复杂化和可溶性增强.
主要成果:
- 通过DSC和FTIR证实了PTB-CD纳入复合物的成功形成.
- 阶段溶解性研究表明,在水溶液中存在显著的复杂性.
- 复杂关联常数 (K1:1) 在15,000到55,000M-1之间,以HPβCD < DIMEB < RAMEB < SBECD的顺序增加.
- 在100毫米的CD度下,可溶性增强因子达到700倍至1250倍.
结论:
- 修改后的环极素有效地与二一起形成包括综合体.
- 这些复合物显著提高了固醇的水溶性,为药物应用提供了潜在的潜力.
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