载体水性对固体自我纳米乳化药物输送系统和自我纳米乳化颗粒系统的影响
Jung Suk Kim1, Fakhar Ud Din2, Hyuk Jun Cho1
1College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea.
International journal of pharmaceutics
|November 6, 2023
概括
载体的水友性,比如半孔酸和基-β-环氧化,对固体纳米乳化系统的影响最小. 观察到外观和溶解度的差异,但药物的性能保持一致.
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:
- 固体自纳米乳化药物递送系统 (SNEDDS) 和自纳米乳化颗粒系统 (SEGS) 对难溶性药物具有优势.
- 载体选择对于优化这些固体剂型的性能至关重要.
- 研究载体水友性为配方开发提供了洞察力.
研究的目的:
- 评估载体水友性对固体SNEDDS和SEGS的影响.
- 为了比较介质酸盐 (疏水性) 和基-β-环氧 (疏水性) 作为固体载体.
- 评估对药物的溶解性,物理特性和口服生物利用性的影响.
主要方法:
- 液体SNEDDS的配方包括德克西布洛芬,Tween80,Kollipohr EL和玉米油.
- 使用Avicel和Ca-酸盐或HP-β-CD的SNEDDS喷雾干燥和流体床颗粒化.
- 粒子形态学,微粒学,结晶性,滴滴大小和溶解的表征.
- 在老鼠模型中评估口服生物利用率.
主要成果:
- 基于HP-β-CD的系统表现出球形颗粒 (SNEDDS) 或聚合颗粒 (SEGS),与Ca-系统不同.
- 在Ca-酸盐和德克西布洛芬之间观察到分子相互作用,但不是与HP-β-CD.
- 在载体类型之间的微米质特性,结晶性,滴滴特性,溶解或口服生物利用性方面没有发现显著差异.
- 与Ca-酸盐相比,HP-β-CD显著提高了德西布洛芬的溶解性.
结论:
- 载体水友性对固体SNEDDS和SEGS的整体性能和体内性能的影响最小.
- 在Ca-酸盐和HP-β-CD系统之间注意到粒子外观,分子相互作用和药物溶解度的差异.
- 这两种载体都适合开发固体纳米乳化系统,HP-β-CD提供了卓越的可溶性增强.
相关概念视频
Factors Affecting Dissolution: Particle Size and Effective Surface Area
860
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...
860
Factors Influencing Drug Absorption: Pharmaceutical Parameters
134
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...
134
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
209
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...
209
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
1.4K
Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
1.4K
Factors Influencing Drug Absorption: Physicochemical Parameters
302
The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
302
Factors Influencing Drug Absorption: Drug Dissolution
527
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...
527


