氨酸模仿并影响聚合物抑制剂在稳定药物超和的功能
Victus Kordorwu1, Steven Castleberry2, Steve Lustig1
1Department of Chemical Engineering, College of Engineering, Northeastern University, Boston, Massachusetts 02115, United States.
Molecular pharmaceutics
|February 20, 2025
概括
粘素是肠粘液的主要组成部分,对超和溶液中的药物沉有显著影响. 这一发现表明,粘蛋白在体内无形固体分散 (ASD) 的表现中起着至关重要的作用.
科学领域:
- 制药科学 制药科学
- 生物制药生物制药公司
- 药物运输 药物运输 药物运输
背景情况:
- 水溶性较差的药物往往需要先进的配方,如无形固体分散 (ASD),以提高生物可用性.
- 在模拟的肠液中进行生物相关溶解测试是评估ASD性能的标准.
- 肠道粘液,特别是粘膜在超和溶液中药物沉中的作用经常被忽视.
研究的目的:
- 研究粘蛋白对超和溶液中模型药物的沉的影响.
- 为了比较粘素的沉抑制效应与在ASD中使用的常见聚合物辅料.
- 了解粘蛋白对降水抑制剂疗效的潜在影响.
主要方法:
- 研究了在粘真菌的存在下从超和溶液中沉卡维迪醇和尼菲迪平.
- 与基甲基纤维素 (HPMC) 和Kollidon VA 64在0.2% (w/v) 的作用中比较木的作用.
- 评估了粘素和聚合物沉抑制剂之间的相互作用.
主要成果:
- 氨酸在体外显著改变了药物沉率.
- 氨酸在相同度下表现出与HPMC和Kollidon VA 64相似的沉抑制.
- 素的存在改变了HPMC和Kollidon VA 64的沉抑制作用.
结论:
- 氨酸在调节超和溶液中的药物沉中发挥着重要作用.
- 素可以作为有效的降水抑制剂,类似于常用的聚合物.
- 素与辅助剂的相互作用表明,素在无形固体分散的体内表现中起着复杂的作用.
相关概念视频
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
170
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...
170
Factors Affecting Dissolution: Particle Size and Effective Surface Area
672
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...
672
Drugs for Peptic Ulcer Disease: Sucralfate as Mucosal Protective Agents
362
In the intricate landscape of the gastric lumen, excessive acid secretion disrupts the natural defense mechanisms, weakening the mucus-bicarbonate barrier. This vulnerability allows pepsin to infiltrate epithelial cells, digesting mucosal proteins and triggering erosion, leading to ulcer formation.
In this scenario, mucosal protective agents like sucralfate play an essential role. Sucralfate, a complex of sulfated sucrose and aluminum hydroxide, demonstrates its usefulness in acidic conditions,...
In this scenario, mucosal protective agents like sucralfate play an essential role. Sucralfate, a complex of sulfated sucrose and aluminum hydroxide, demonstrates its usefulness in acidic conditions,...
362
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
277
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...
277
Factors Influencing Drug Absorption: Pharmaceutical Parameters
113
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...
113
Acid Suppressive Drugs for Peptic Ulcer Disease: Proton Pump Inhibitors
350
Peptic ulcers, often induced by H. pylori infections or NSAID usage, arise from disruptions in the delicate balance of gastric acid production. Peptic ulcers stem from heightened gastric acid levels due to H. pylori infections or NSAID use. The protective mucus layer diminishes in the presence of these factors, allowing gastric acid to erode the stomach lining and form ulcers.
Gastric acid, a potent cocktail of hydrogen and chloride ions, is produced in specialized parietal cells within the...
Gastric acid, a potent cocktail of hydrogen and chloride ions, is produced in specialized parietal cells within the...
350


