体结构的表征及其可溶性潜力BCSII类药物在空腹状态模拟肠液中的BCSII类药物
Zoe McKinnon1, Ibrahim Khadra1, Gavin W Halbert1
1Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, 161 Cathedral Street, Glasgow, G4 0RE, United Kingdom.
International journal of pharmaceutics
|September 24, 2024
概括
药物在模拟肠液 (SIF) 中的溶解性随着两性度的增加而增加,而酸性药物是最容易溶解的. 体结构的大小因SIF成分而异,影响药物溶解度.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 物理化学 物理化学
背景情况:
- 模拟肠液 (SIF) 组成的变化影响药物的溶解性.
- 了解SIF中的体结构对于预测药物吸收至关重要.
- 研究了8种难溶的药物 (酸性,基本性,中性).
研究的目的:
- 在一系列空腹状态模拟肠液 (SIF) 中研究难溶性药物的溶性.
- 用动态光散射 (DLS) 和纳米粒子追踪分析 (NTA) 来描述SIF中形成的体结构.
- 探索SIF组成,体结构和药物溶解度之间的关系.
主要方法:
- 准备一套空腹状态模拟肠液 (SIF),反映人肠液 (HIF) 的变化.
- 对八种模范药物 (纳普罗森,印米他辛,丁,卡维迪洛尔,塔达拉菲尔,费洛迪平,费诺纤维酸盐,灰色富尔文) 的溶解度的确定.
- 使用动态光散射 (DLS) 和纳米粒子追踪分析 (NTA) 进行体结构的表征.
主要成果:
- 药物溶解性随着SIF中总两类度 (TAC) 的增加而增加.
- 酸性药物表现出比基本或中性药物更高的溶解度.
- 随着两类度的增加,体结构的大小下降;DLS和NTA显示出相似的趋势,在不同的两类度中有一些差异.
结论:
- SIF的成分显著影响着体结构的形成和药物的溶解性.
- 溶解度和体大小之间没有观察到直接的相关性.
- 需要进一步的研究来阐明体结构和SIF中的药物溶解度之间的确切关系.
更多相关视频
相关概念视频
Factors Influencing Drug Absorption: Drug Dissolution
425
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...
425
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
179
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...
179
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
1.2K
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...
1.2K
Factors Influencing Drug Absorption: Physicochemical Parameters
238
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...
238
Methods for Studying Drug Absorption: In vitro
210
In vitro experiments are crucial for understanding the transport and absorption of drugs through biological materials. These studies employ varied methods such as the diffusion cell method, the everted sac technique, and the everted ring technique.
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
210
Colloids and Suspensions
1.7K
Children at play often make suspensions such as mixtures of mud and water, flour and water, or a suspension of solid pigments in water known as tempera paint. These suspensions are heterogeneous mixtures composed of relatively large particles visible to the naked eye or seen with a magnifying glass. They are cloudy, and the suspended particles settle out after mixing. The suspended particles in a suspension settle out after some time of mixing. The separation of particles from a suspension is...
1.7K


