设计和开发基于基托桑的二甲基烟酸-环氧二元系统的鼻粉,旨在用于鼻至脑的注射. 一个稳定性研究
Eleonora Sofia Cama1, Laura Catenacci1, Sara Perteghella1
1Department of Drug Sciences, University of Pavia, 27100 Pavia, Italy.
International journal of pharmaceutics
|May 11, 2024
概括
这项研究开发了一种稳定,可通过鼻子注射的二甲基烟酸 (DMF) 粉末,使用环氧德素复合和冷干燥. 这种方法增强了DMF的交付,用于多发性硬化症的潜在鼻至脑治疗.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 神经科学是一个神经科学.
背景情况:
- 通过鼻子给药提供了直接通往中枢神经系统 (CNS) 的途径.
- 丁甲基烟酸 (DMF) 是一种用于多发性硬化症的免疫调节剂和细胞保护剂,但在溶解性和稳定性方面面临挑战.
- 现有的DMF配方受到水溶性差和室温降解的限制.
研究的目的:
- 开发一种可通过鼻子注射的二甲基烟酸 (DMF) 粉末,用于鼻至脑的输送.
- 为了增强DMF的溶解性和稳定性,使用无形β-环素衍生物.
- 为了创建一种粘粘粉配方,以改善鼻腔药物输送.
主要方法:
- 复合DMF与基烯β-环氧化和甲基β-环氧化.
- 使用DSC,FTIR和PXRD进行DMF-环极素相互作用的表征.
- 阶段溶解性研究以评估复合效率.
- 使用各种制备方法 (包括冷干燥) 开发基托基粘粘粉.
主要成果:
- 通过成功地将DMF与环氧素衍生物复合,提高了溶解度和稳定性.
- 冷干燥产生了最佳的基托基粘粘粉,显示出优越的水解稳定性和DMF恢复.
- 鉴定证实了DMF和环氧素之间的二元产品的形成.
结论:
- 无形环素衍生物有效地提高了DMF的溶解性和稳定性,用于鼻腔注射.
- 结干燥的基托基粘膜粘合剂粉末代表了用于鼻至大脑输送DMF的有希望的配方.
- 这种策略克服了DMF的局限性,有可能改善多发性硬化症等神经疾病的治疗结果.
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