尼莫迪平与硫乙-β-环氧二烯的纳入复合物:制备,表征,体外和体外评估
Jiahui Liu1,2, Meichai Li1,2, Yongjie Huang1
1Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, 350108, China.
AAPS PharmSciTech
|January 8, 2025
概括
尼莫迪平 (NIMO) 的溶解性和安全性通过创建含有硫甲基乙烯-β-环极 (SBE-β-CD) 的包容复合物而得到改善. 这种新的NIMO-SBE-β-CD配方增强了神经恢复,与现有治疗方法相比降低了毒性.
科学领域:
- 药理学和药物输送 药理学和药物输送
- 纳米技术在医学中的应用
- 神经科学是一个神经科学.
背景情况:
- 尼莫迪平 (NIMO) 对于治疗缺血性神经损伤后亚脑下垂体出血 (SAH) 是至关重要的.
- 尼莫的临床使用受到水溶性差的限制,导致血管刺激,毒性和不稳定性.
- 如Nimotop®注射等现有配方在安全性和生物可用性方面存在挑战.
研究的目的:
- 通过与硫乙-β-环极 (SBE-β-CD) 进行包容复合,增强尼莫迪平 (NIMO) 的可溶性和稳定性.
- 与Nimotop®注射相比,评估新型NIMO-SBE-β-CD复合物的安全性,疗效和药理学特征.
- 评估NIMO-SBE-β-CD复合体在治疗缺血神经损伤和脑内出血方面的治疗潜力.
主要方法:
- 使用相溶性,DSC,FT-IR,XRD和SEM,制备和描述尼莫迪平-SBE-β-CD (NIMO-CD) 纳入复合物.
- 评估NIMO-CD的稀释稳定性,溶血活性,血管刺激和急性毒性 (LD50).
- 在脑内出血模型中的药理动力学,药理动力学,行为学 (mNSS,CT) 和组织病理学评估,使用Nimotop®作为对照.
主要成果:
- 在NIMO-CD复合体中,NIMO溶解度增加了1202倍.
- NIMO-CD表现出优异的24小时稀释稳定性,没有溶血活性,减少了血管刺激,LD50比Nimotop®高2.49倍.
- 尼莫-CD显著改善了神经恢复,减少了血瘤和水,显示了与Nimotop®具有增强安全概况的可比效果.
结论:
- 尼莫迪平-SBE-β-CD纳入复合体的形成显著提高了NIMO的溶解性和稳定性.
- 该NIMO-CD配方保持与Nimotop®的生物等价性,同时提供更好的安全性和降低毒性.
- 尼莫-CD为治疗缺血神经损伤和相关疾病提供了一个有希望的,潜在的优越替代方案.
相关概念视频
01:16Methods for Studying Drug Absorption: In vitro
199
In vitro experiments are crucial for understanding the transport and absorption of drugs through biological materials. These studies employ varied methods such as the diffusion cell method, the everted sac technique, and the everted ring technique.
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
199
01:09Methods for Studying Drug Absorption: In situ
201
In situ experiments, such as the Doluisio method and Single-Pass Perfusion technique, provide critical insights into drug uptake by simulating in vivo conditions for drug absorption.
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
201