用边缘激活剂 (Tween20) 制备的Soluplus稳定型尼莫迪平因捕获的塑配方:比较物理化学评估
Hussein K Alkufi1, Hanan J Kassab2
1Department of Pharmacognosy, College of Pharmacy, University of Thi-Qar, 64001, Iraq.
Pharmaceutical nanotechnology
|November 6, 2024
概括
这项研究使用乙醇注射方法成功将尼莫迪平 (ND) 配制成塑性纳米微粒,显著提高了其用于治疗下关节出血的生物可用性. 优化的配方表现出增强的稳定性和药物释放特性.
科学领域:
- 纳米技术纳米技术
- 制药科学 制药科学
- 药物输送系统 药物输送系统
背景情况:
- 尼莫迪平 (ND) 是急性脑下关节出血的一个关键血管扩张剂.
- 它的疏水性质导致溶解性差,生物可用性低.
- 斯潘拉斯基纳米微粒为增强药物输送提供了一个潜在的解决方案.
研究的目的:
- 为了将尼莫迪平 (ND) 配制成塑料纳米纤维.
- 为了提高尼莫迪平的生物可用性.
- 评估纳米管状配方的物理化学特性和体外性能.
主要方法:
- 使用乙醇注射方法制备含有ND的Spanlastic纳米丝片.
- 配方使用Span60 (非离子表面活性剂) 和Tween 20 (边缘激活剂).
- 结合了像Soluplus这样的稳定剂,并与非稳定配方进行了比较;特征包括囊泡大小,PDI,%EE,zeta潜力和体外释放.
主要成果:
- 优化的配方 (F27) 呈现出有利的特征:囊泡大小 (VS) 为 125.7±0.29 nm,多分散指数 (PDI) 为 0.4744±0.002,捕获效率 (%EE) 为 85.43±0.17%,泽塔电位为 -20.01 ± 0.89 mV.
- 含有Soluplus的配方显示出更好的稳定性和更高的可变性指数 (DI).
- 扫描电子显微镜 (SEM) 揭示了均和球形的纳米,表明持续释放能力.
结论:
- 乙醇注射方法是有效的,以制订ND到spanlastic纳米丝片.
- 索鲁普卢斯作为稳定剂,防止晶体的发育和聚合,导致更稳定的配方.
- 开发的spanlastic nanovesicles显示了通过提高其生物可用性来改善尼莫迪平的治疗疗效的前景.
相关概念视频
Factors Influencing Drug Absorption: Pharmaceutical Parameters
121
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
121
Factors Affecting Dissolution: Particle Size and Effective Surface Area
735
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
735
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
178
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
178
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
287
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
287


