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相关概念视频

Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

691
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...
691
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

280
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...
280
Colloidal precipitates01:09

Colloidal precipitates

494
The high insolubility of some precipitates can result in an unfavorable relative supersaturation. This can lead to colloidal particles with a large surface-to-mass ratio, where adsorption is promoted. For instance, in the precipitation of silver chloride, silver ions are adsorbed on the surface of the colloidal particles, forming a primary layer. This layer attracts ions of opposite charge (such as nitrate ions), forming a diffuse secondary layer of adsorbed ions. This electric double layer...
494
Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

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
Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

402
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...
402
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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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...
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A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles
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开发基于Soluplus®的微粒无形固体分散剂,具有高药物负载,用于通过电子喷射增强切莱可西布溶解.

Fan Fan1,2, Feng Zhou1,2, Jiayu Zhang3

  • 1Laboratory of Advanced Theranostic Materials and Technology, Ningbo Institute of Materials Technology and Engineering, Chinese Academy of Sciences, Ningbo, 315201, China.

AAPS PharmSciTech
|January 29, 2025
PubMed
概括

电喷剂制造了稳定的无形固体分散 (ASD) 赛莱科西布 (CEL) 和Soluplus® (SOL) 具有高药物负载. 这些微粒子ASD显著增强了CEL溶解,为水溶性较差的药物提供了有希望的替代品.

关键词:
无形固体分散 (ASDs) 是一种无形固体分散.电气喷是一种电子喷.大量的毒品负载.可溶性增强 提高可溶性这是基于soluplus®的微粒.

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科学领域:

  • 制药科学 制药科学
  • 材料科学 材料科学 材料科学
  • 药物运输 药物运输 药物运输

背景情况:

  • 无形固体分散 (ASD) 改善药物溶解,但通常具有较低的药物负载.
  • 对于水溶性较差的药物,如赛莱科西布 (CEL),需要提高溶解度,以获得更好的治疗效果.
  • 发展具有高药含量的稳定ASD对于有效的口服药物配方至关重要.

研究的目的:

  • 开发基于Soluplus® (SOL) 的微粒子ASDs,具有高药物负载 (高达60%w/w) 的赛莱科西布 (CEL).
  • 为了实现CEL-SOL ASDs的长期物理稳定性 (≥16个月).
  • 使用电喷技术提高CEL的体外溶解率.

主要方法:

  • 电子喷雾被用来制造SOL-CEL微粒子ASDs.
  • 使用X射线衍射 (XRD) 和差分扫描热量计 (DSC) 来确认无形性质.
  • 福利埃变换红外光谱学 (FTIR) 分析了药物辅助剂相互作用 (键).

主要成果:

  • 电子喷雾的SOL-CEL微粒被证实是无形的.
  • FTIR分析显示,SOL和CEL之间存在键,这有助于ASD的稳定.
  • 在体外溶解研究显示,与晶体形式相比,CEL溶解率增加了8.2倍.

结论:

  • 电喷是一种生产高负载,稳定的CEL-SOLASD的可行方法.
  • 开发的ASD显著增强了水溶性较差的赛莱科西布的溶解.
  • 电子喷雾在ASD生产中比HME和SD等传统方法具有优势.