开发一种创新的方法,以提高里瓦洛克萨班的溶解性能
Emma Adriana Ozon1, Erand Mati2, Oana Karampelas1
1Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, 6 Traian Vuia Street, 020945, Bucharest, Romania.
Heliyon
|July 18, 2024
概括
这项研究开发了一种新的方法,使用液态里瓦洛克萨班-环德林复合物创建固体剂型. 创新的喷涂技术提高了药物的溶解和生物可用性,从而改善了里瓦洛克萨班的输送.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 传统的固体剂量形式面临的挑战是,不完全的药物被纳入环氧德克斯特林复合物中.
- 像Rivaroxaban这样的疏水药物需要先进的配方策略来有效提供.
- 之前的研究重点是固态循环德克斯特林复合物,需要新的液态集成方法.
研究的目的:
- 开发一种创新的方法,将液态药物-环德林纳入复合物整合到固体剂型中.
- 为了配制和表征在纤维素颗粒上喷涂的里瓦罗克萨班-基基-β-环氧化液体复合物.
- 评估新型固体剂型的物理化学特性和体外溶解.
主要方法:
- 液态里瓦罗克萨班-基基-β-环氧德克斯纳入复合物的配方与基基纤维素.
- 使用Caleva迷你涂层器将液体复合分散剂喷涂到纤维素颗粒上 (CELLETS®780).
- 使用FTIR,XRD,SEM,DSC,HPLC-DAD和在各种介质中的体外溶解研究进行表征.
主要成果:
- 通过物理化学分析证实,里瓦罗克萨班成功被纳入氧-β-环氧中.
- 涂层细胞表现出优异的流动性,可压缩性和足够的硬度与10毫克里瓦洛克萨班负载.
- 在体外溶解的概况与Xarelto® 10mg囊相似,早期溶解率显著提高.
结论:
- 在颗粒上喷涂液态药物-环氧胺复合物的喷涂是一种可行的和有效的方法,用于固体剂型的开发.
- 这种创新方法提供了一个有前途的策略,以提高水性药物的生物可用性,如Rivaroxaban.
- 开发的配方代表了制药技术在改善药物输送方面取得的重大进步.
相关概念视频
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
787
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...
787
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
192
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...
192
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
127
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...
127
01:15Theories of Dissolution: Diffusion Layer Model
726
Dissolution, the process by which drug particles dissolve in a solvent, is explained by the diffusion layer model, a theoretical framework that simulates the absorption of oral drugs and allows us to analyze experimental data.
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
726
01:27Factors Influencing Drug Absorption: Drug Dissolution
458
The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
458
01:09Theories of Dissolution: The Danckwerts' Model and Interfacial Barrier Model
283
Various dissolution theories provide insight into the factors that influence the dissolution rate. Danckwerts' Model suggests that turbulence, rather than a stagnant layer, characterizes the dissolution medium at the solid-liquid interface. In this model, the agitated solvent contains macroscopic packets that move to the interface via eddy currents, facilitating the absorption and delivery of the drug to the bulk solution. The regular replenishment of solvent packets maintains the...
283