随机甲基化β-循环德克斯特林含有复合物与可纳:制备,表征和改善药理特征
Yili Ding1,2, Shufeng Xu3, Charles Ding4
1College of Science, Mathematics and Technology, Wenzhou-Kean University, Wenzhou 325060, China.
Molecules (Basel, Switzerland)
|May 11, 2024
概括
研究人员改善了基托可纳.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 药用化学 医学化学
背景情况:
- 凯托可纳是一种强大的抗真菌药物,具有较差的水溶性 (0.017 mg/mL),限制了其临床使用.
- 臭味和皮肤刺激是传统可纳配方的额外缺点.
- 提高基托可纳的溶解性对于开发更有效的抗真菌疗法至关重要.
研究的目的:
- 开发基托可纳与随机甲基化β-环极素 (RMβCD) 的纳入复合物.
- 显著改善可纳的水溶性和药物动力学特征.
- 评估新型综合体作为一种改进的抗真菌药物的潜力.
主要方法:
- 通过相位溶解性研究选择循环德克斯.
- 使用水溶液方法复合,通过单因子和直角策略进行优化.
- 使用FTIR,DSC,TGA,SEM和NMR技术对包括复合物的表征.
主要成果:
- 与自由基托可纳相比,基托可纳-RMβCD复合体的水溶性增加了17000倍.
- 在体外研究表明,药物在75分钟内释放100%的药物.
- 在体内对狗的药理动力学研究显示,Cmax (7.56~13.58μg/mL) 和AUC0~72 (22.69~50.19μgh/mL) 的增加.
结论:
- 开发的基托可纳-RMβCD纳入复合物显著提高了基托可纳的溶解性和生物可用性.
- 该复合物表现出良好的体外释放和体外药物动力学特性.
- 这种新型复合物代表了一种改善的抗真菌药物的有希望的新配方.
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