二元和三元复合体的形成和特征的阿尔特米西宁与硫乙烯β-环氧和油酸的硫乙烯β-环氧和油酸
Muhammad Yousaf Shahzad1, Muhammad Abbas2, Muhammad Tayyab Ansari3
1Faculty of Pharmacy, Bahauddin Zakarya University, Multan, Pakistan.
Pakistan journal of pharmaceutical sciences
|May 14, 2024
概括
耐药疟疾需要更好的治疗方法. 这项研究使用循环德克斯特林复合物增强了明素 (ART) 的溶解性,改善了药物输送和抗疟疾的有效性.
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:
- 耐药疟疾构成了严重的全球健康威胁.
- 作为一种关键的抗疟疾药物,素 (ART) 具有较差的水溶性,这限制了它的有效性.
- 制定提高ART溶解性的策略对于对抗耐药疟疾菌株至关重要.
研究的目的:
- 为了提高甲美西宁 (ART) 的水溶性和溶解率.
- 开发和描述ART的二进制和三进制复合物,其中含有硫乙β-环极素 (SBE7β-CD) 和油酸.
- 评估复杂化对ART物理和化学性质的影响.
主要方法:
- 使用物理混合 (PM) 和溶剂蒸发 (SE) 方法制备二进制 (ART/SBE7β-CD) 和三进制 (ART/SBE7β-CD/油酸) 复合物.
- 使用粉末X射线衍射 (PXRD),扫描电子显微镜 (SEM) 和减弱总反射率里埃变换红外 (ATR-FTIR) 谱法对复合物的表征.
- 在模拟胃液 (pH1.6) 中评估水溶性和溶解概况.
主要成果:
- 与三元复合体相比,二元复合体在水溶性上显示出12倍的增强.
- 第三种SE复合物 (SECx) 在模拟的胃液中溶解率增加了35倍.
- 复杂化显著降低了ART结晶性,减少了颗粒大小,并表明了ART,SBE7β-CD和油酸之间的分子相互作用.
结论:
- 二元和三元复合有效地提高了素的水溶性和溶解.
- 溶剂蒸发方法为三元复合物产生了优异的结果,显著改善了药物释放.
- 这些发现为开发更有效的基于美素的抗疟疾配方以打击耐药性提供了有希望的方法.
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